A drug is a chemical substance that has a phyisological effect on an organism. Medicinal, herbal, and illegal drugs can be included in this type.
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Colchicine is a medication used for gout. It is a toxic natural product and secondary metabolite, originally extracted from plants of the genus Colchicum (autumn crocus, Colchicum autumnale, also known as "meadow saffron"). It was used originally to treat rheumatic complaints, especially gout, and still finds use for these purposes today despite dosing issues concerning its toxicity. It was also prescribed for its cathartic and emetic effects.
In addition to gout, colchicine's present medicinal use is in the treatment of familial Mediterranean fever, pericarditis and Behçet's disease. It is also being investigated for its use as an anticancer drug.
The plant source of colchicine, the autumn crocus (Colchicum autumnale), was described for treatment of rheumatism and swelling in the Ebers Papyrus (ca. 1500 B.C.), an Egyptian medical papyrus. The use of the bulb-like corms of Colchicum for gout probably traces back to ca. 550 A.D., as the "hermodactyl" recommended by Alexander of Tralles. Colchicum extract was first described as a treatment for gout in De Materia Medica by Pedanius Dioscorides in the first century CE. Colchicum corms were used by the Persian physician ibn Sina
Nonoxynol-9, sometimes abbreviated as N-9, is an organic compound that is used as a surfactant. It is a member of the nonoxynol family of nonionic surfactants. N-9 and related compounds are ingredients in various cleaning and cosmetic products. It is widely used in contraceptives for its spermicidal properties. However, its use in STD prevention is controversial.
As a spermicide, it attacks the acrosomal membranes of the sperm, causing the sperm to be immobilized. Nonoxynol-9 is the active ingredient in most spermicidal creams, jellies, foams, gel, film, and suppositories.
A 2004 study found that over a six-month period, the typical-use failure rates for five nonoxynol-9 vaginal contraceptives (film, suppository, and gels at three different concentrations) ranged from 10% to 20%.
Many models of condoms are lubricated with solutions containing nonoxynol-9. In this role, it has been promoted as a backup method for avoiding pregnancy and a microbicide for sexually transmitted diseases in the event of condom failure. However, the 2001 WHO / CONRAD Technical Consultation on Nonoxynol-9 concluded that
Compared to regular lubricated condoms, condoms containing nonoxynol-9 present another
Rosuvastatin (marketed by AstraZeneca as Crestor) is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. It was developed by Shionogi.
The primary uses of rosuvastatin is for the treatment of dyslipidemia. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.
Rosuvastatin has structural similarities with most other synthetic statins, e.g., atorvastatin, cerivastatin, pitavastatin, but rosuvastatin unusually also contains sulfur.
Crestor is actually rosuvastatin calcium, in which calcium replaces the hydrogen in the carboxylic acid group on the right of the two structure diagrams.
Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins. Its approximate elimination half life is 19 h and its time to peak plasma concentration is reached in 3–5 h following oral administration.
Putative beneficial effects of rosuvastatin therapy on chronic heart failure may be negated by increases in collagen turnover markers as well as a reduction in plasma
Marketed formulations:Rosiglitazone maleate 4 film coated tablet
Rosiglitazone is an antidiabetic drug in the thiazolidinedione class of drugs. It works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin. It is marketed by the pharmaceutical company GlaxoSmithKline (GSK) as a stand-alone drug (Avandia) and in combination with metformin (Avandamet) or with glimepiride (Avandaryl). Annual sales peaked at approximately $2.5bn in 2006, but declined after reports of adverse effects. The drug's patent expires in 2012.
Some reports have found rosiglitazone is associated with an increased risk of heart attacks, but other reports have not found a statistically significant increase. Concern about adverse effects has reduced the use of rosiglitazone despite its sustained effects on glycemic control. The drug is currently the subject of over 13,000 lawsuits against GSK. As of July 2010, GSK has agreed to settlements on more than 11,500 of these suits.
The drug is controversial in the U.S. Some reviewers have concluded rosiglitazone caused more deaths than pioglitazone (Actos), and have recommended rosiglitazone be taken off the market, but an Food and Drug Administration panel disagreed,
Marketed formulations:Loratadine 10 film coated tablet
Loratadine (INN) is a second-generation H1 histamine antagonist drug used to treat allergies. Structurally, it is closely related to tricyclic antidepressants, such as imipramine, and is distantly related to the atypical antipsychotic quetiapine.
Loratadine is marketed by Schering-Plough under several trade names (e.g., Claritin) and also by Shionogi in Japan. It is available as a generic drug and is marketed for its non-sedating properties. In a version named Claritin-D or Clarinase, it is combined with pseudoephedrine, a decongestant; this makes it useful for colds as well as allergies but adds potential side-effects of insomnia, anxiety, and nervousness.
Schering-Plough developed loratadine as part of a quest for a potential blockbuster drug: a nonsedating antihistamine. However, by the time Schering submitted the drug to the U.S. Food and Drug Administration (FDA) for approval, the agency had already approved a competitor's non-sedating antihistamine, terfenadine (trade name Seldane), and, therefore, put loratadine on a lower priority.
Loratadine was approved by the FDA in 1993. It accounted for 28% of Schering's total sales. The drug continued to be available only by
Aciclovir (INN) ( /eɪˈsaɪklɵvɪər/) or acyclovir (USAN, former BAN), chemical name acycloguanosine, abbreviated as ACV, is a guanosine analogue antiviral drug, marketed under trade names such as Cyclovir, Herpex, Acivir, Acivirax, Zovirax, and Xovir. One of the most commonly used antiviral drugs, it is primarily used for the treatment of herpes simplex virus infections, as well as in the treatment of varicella zoster (chickenpox) and herpes zoster (shingles).
Aciclovir was seen as the start of a new era in antiviral therapy, as it is extremely selective and low in cytotoxicity. Nucleosides isolated from a Caribbean sponge, Cryptotethya crypta, were the basis for the synthesis of aciclovir. It was codiscovered by Howard Schaffer following his work with Robert Vince, S. Bittner and S. Gurwara on the adenosine analog acycloadenosine which showed promising antiviral activity. Later, Schaffer joined Burroghs-Wellcome and continued the development of aciclovir with Pharmacologist Gertrude B. Elion. Vince later went on to invent abacavir, the NNRTI drug for HIV patients. Elion was awarded the 1988 Nobel Prize in Medicine, partly for the development of aciclovir. Dr. Richard Whitley, a
Atenolol is a selective β1 receptor antagonist, a drug belonging to the group of beta blockers (sometimes written β-blockers), a class of drugs used primarily in cardiovascular diseases. Introduced in 1976, atenolol was developed as a replacement for propranolol in the treatment of hypertension. The chemical works by slowing down the heart and reducing its workload. Unlike propranolol, atenolol does not pass through the blood–brain barrier thus avoiding various central nervous system side effects.
Atenolol is one of the most widely used β-blockers in the United Kingdom and was once the first-line treatment for hypertension. The role for β-blockers in hypertension was downgraded in June 2006 in the United Kingdom to fourth-line, as they perform less appropriately or effectively than newer drugs, particularly in the elderly.
Atenolol is used for a number of conditions including: hypertension, angina, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.
It is also used to treat the symptoms of Graves' disease until antithyroid medication can take effect.
Due to its hydrophilic properties, the drug is less suitable
Diethylstilbestrol (DES, former BAN stilboestrol) is a synthetic nonsteroidal estrogen that was first synthesized in 1938. It is also classified as an endocrine disruptor. Human exposure to DES occurred through diverse sources, such as dietary ingestion from supplemented cattle feed and medical treatment for certain conditions, including breast and prostate cancers. From about 1940 to 1970, DES was given to pregnant women in the mistaken belief it would reduce the risk of pregnancy complications and losses. In 1971, DES was shown to cause a rare vaginal tumor in girls and women who had been exposed to this drug in utero. The United States Food and Drug Administration subsequently withdrew DES from use in pregnant women. Follow-up studies have indicated DES also has the potential to cause a variety of significant adverse medical complications during the lifetimes of those exposed. The United States National Cancer Institute recommends women born to mothers who took DES undergo special medical exams on a regular basis to screen for complications as a result of the drug. Individuals who were exposed to DES during their mothers' pregnancies are commonly referred to as "DES daughters"
Marketed formulations:Azithromycin monohydrate 20 powder for suspension
Azithromycin (Zithromax, Azithrocin, Zmax) is an azalide, a subclass of macrolide antibiotics. Azithromycin is one of the world's best-selling antibiotics. It is derived from erythromycin, with a methyl-substituted nitrogen atom incorporated into the lactone ring, thus making the lactone ring 15-membered.
Azithromycin is used to treat or prevent certain bacterial infections, most often those causing middle ear infections, strep throat, pneumonia, typhoid, and sinusitis. In recent years, it has been used primarily to prevent bacterial infections in infants and those with weaker immune systems. It is also effective against certain sexually transmitted infections, such as nongonococcal urethritis, chlamydia, and cervicitis. Recent studies have indicated it also to be effective against late-onset asthma, but these findings are controversial and not widely accepted.
Azithromycin is used to treat many different infections, including acute otitis media, nonstreptococcal bacterial pharyngitis, gastrointestinal infections such as traveler's diarrhea, respiratory tract infections such as pneumonia, cellulitis, babesiosis, Bartonella infection, chancroid cholera, donovanosis, leptospirosis,
Marketed formulations:Fluvoxamine maleate 50 film coated tablet
Fluvoxamine (brand name Luvox) is an antidepressant which functions as a selective serotonin reuptake inhibitor (SSRI). Fluvoxamine was first approved by the U.S. Food and Drug Administration (FDA) in 1993 for the treatment of obsessive compulsive disorder (OCD). Fluvoxamine CR (controlled release) is approved to treat social anxiety disorder. Fluvoxamine is also prescribed to treat major depressive disorder (MDD) and anxiety disorders, such as panic disorder and post-traumatic stress disorder (PTSD).
The FDA has added a Black box warning for this drug in reference to increased risks of suicidal thinking and behavior in young adults and children. A study from the Institute for Safe Medication Practices identified Luvox as being 8.4 times more likely than other medications to be associated with violence.
Fluvoxamine was developed by Solvay Pharmaceuticals (Belgium) and was the first SSRI, a non-TCA drug approved by the U.S. Food and Drug Administration (FDA) specifically for the treatment of OCD. It was one of the first SSRI antidepressants to be launched (1984 in Belgium and Switzerland), and following its FDA approval in 1993, it was launched in the U.S. in December 1994,
Enalapril (marketed as Vasotec in the USA, Enaladex in some other countries, and Enacard for veterinary use) is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. ACE converts the peptide hormone angiotensin I to angiotensin II. One of the actions of angiotensin II is the vasoconstriction of blood vessels resulting in an increase in blood pressure. ACE inhibitors such as enalapril prevent this effect. Enalapril has been shown to lower the death rate in systolic heart failure. Enalapril was the first member of the group known as the dicarboxylate-containing ACE inhibitors.
Enalapril as a treatment for high blood pressure works by modulating the renin-angiotensin-aldosterone system (RAAS).
Squibb developed the first inhibitor, captopril, but it had adverse effects such as a metallic taste (which, as it turned out, was due to the sulfhydryl group). Merck & Co. developed enalapril as a competing prodrug.
Enalaprilat, the first dicarboxylate-containing ACE inhibitor, was developed partly to overcome these limitations of captopril. The sulfhydryl moiety was replaced by a carboxylate moiety, but additional
Ethchlorvynol is a sedative and hypnotic medication developed by Pfizer in the 1950s. In the United States Abbott Laboratories used to sell it under the tradename Placidyl. During their heyday, they were known on the street as "jelly-bellies" or "pickles". Since Abbott and Banner Pharmacaps, which manufactured the generic version, discontinued production in 1999, ethchlorvynol has no longer been available in the United States.
Ethchlorvynol has been used to treat insomnia, but has been largely superseded and is only offered where an intolerance or allergy to other drugs exists.
Along with expected sedative effects of relaxation and drowsiness, ethchlorvynol can cause skin rashes, faintness, restlessness and euphoria. Early adjustment side effects can include nausea and vomiting, numbness, blurred vision, stomach pains and temporary dizziness. An overdose is marked by confusion, fever, peripheral numbness and weakness, reduced coordination and muscle control, slurred speech, reduced heartbeat.
It is addictive and after prolonged use can cause withdrawal symptoms including convulsions, hallucinations, and memory loss. Due to these problems, it is unusual for ethchlorvynol to be
Marketed formulations:Doxycycline 100 film coated tablet
Doxycycline is a member of the tetracycline antibiotics group, and is commonly used to treat a variety of infections. Doxycycline is a semisynthetic tetracycline invented and clinically developed in the early 1960s by Pfizer Inc. and marketed under the brand name Vibramycin. Vibramycin received US Food and Drug Administration approval in 1967, becoming Pfizer's first once-a-day, broad-spectrum antibiotic. Other brand names include Monodox, Microdox, Periostat, Vibra-Tabs, Oracea, Doryx, Vibrox, Adoxa, Doxyhexal, Doxylin, Doxoral, Doxy-1 and Atridox (topical doxycycline hyclate for periodontitis).
In addition to the general indications for all members of the tetracycline antibiotics group, doxycycline is frequently used to treat Lyme disease, chronic prostatitis, sinusitis, syphilis, chlamydia infection, pelvic inflammatory disease, acne, rosacea, and rickettsial infections.
It is used in prophylaxis against malaria. It should not be used alone for initial treatment of malaria, even when the parasite is doxycycline-sensitive, because the antimalarial effect of doxycycline is delayed. This delay is related to its mechanism of action, which is to specifically impair the progeny of the
Pioglitazone is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action to treat diabetes. Pioglitazone is marketed as trademarks Actos in the USA, Canada, the UK and Germany, Glustin in Europe,Glizone and Pioz in India by Zydus Cadila and USV Limited, respectively and Zactos in Mexico by Takeda Pharmaceuticals. Actos was the tenth-best selling drug in the U.S. in 2008, with sales exceeding $2.4 billion. Its cardiovascular safety profile compares favorably with rosiglitazone (Avandia), which was withdrawn after concerns about an increased risk of cardiac events. However, pioglitazone has subsequently been found to be associated with bladder tumors and has been withdrawn in some countries.
Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α. It modulates the transcription of the insulin-sensitive genes involved in the control of glucose and lipid metabolism in the muscle, adipose tissue, and the liver. As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent
Pethidine (INN) or meperidine hydrochloride (USAN) (commonly referred to as Demerol in the US but also referred to as: isonipecaine; lidol; pethanol; piridosal; Algil; Alodan; Centralgin; Dispadol; Dolantin; Mialgin (in Indonesia); Petidin Dolargan (in Poland); Dolestine; Dolosal; Dolsin; Mefedina) is a fast-acting opioid analgesic drug.
Pethidine was the first synthetic opioid synthesized in 1932 as a potential anti-spasmodic agent by the chemist Otto Eislib. Its analgesic properties were first recognized by Otto Schaumann working for IG Farben, Germany.
Pethidine is indicated for the treatment of moderate to severe pain, and is delivered as a hydrochloride salt in tablets, as a syrup, or by intramuscular, subcutaneous or intravenous injection. For much of the 20th century, pethidine was the opioid of choice for many physicians; in 1975 60% of doctors prescribed it for acute pain and 22% for chronic severe pain.
Compared to morphine, pethidine was supposed to be safer and carry less risk of addiction, and to be superior in treating the pain associated with biliary spasm or renal colic due to its putative antispasmodic effects. In fact, pethidine is no more effective than morphine
Misoprostol is a drug that is used for the prevention of nonsteroidal anti-inflammatory drug (NSAID) induced gastric ulcers, to treat missed miscarriage, to induce labor, and as an abortifacient. The latter use is controversial in the United States. Misoprostol was invented and marketed by G.D. Searle & Company (now Pfizer) under the trade name Cytotec (often misspelled Cyotec), but other brand-name and generic formulations are now available as well.
Pharmacologically, misoprostol is a synthetic prostaglandin E1 (PGE1) analogue.
Misoprostol is approved for use in the prevention of NSAID induced gastric ulcers. It acts upon gastric parietal cells, inhibiting the secretion of gastric acid via G-protein coupled receptor mediated inhibition of adenylate cyclase, which leads to decreased intracellular cyclic AMP levels and decreased proton pump activity at the apical surface of the parietal cell. Because other classes of drugs, especially H2-receptor antagonists and proton pump inhibitors, are more effective for the treatment of acute peptic ulcers, Misoprostol is only indicated for use by people who are both taking NSAIDs and are at high risk for NSAID induced ulcers, including the
Cytarabine, or cytosine arabinoside, is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma. It is also known as Ara-C (Arabinofuranosyl Cytidine). It kills cancer cells by interfering with DNA synthesis.
It is called cytosine arabinoside because it combines a cytosine base with an arabinose sugar. Cytosine normally combines with a different sugar, deoxyribose, to form deoxycytidine, a component of DNA. Certain sponges, where it was originally found, use arabinoside sugars to form a different compound (not part of DNA). Cytosine arabinoside is similar enough to human cytosine deoxyribose (deoxycytidine) to be incorporated into human DNA, but different enough that it kills the cell. This mechanism is used to kill cancer cells. Cytarabine is the first of a series of cancer drugs that altered the sugar component of nucleosides. Other cancer drugs modify the base.
Cytarabine was first synthesized in 1959 by Richard Walwick, Walden Roberts, and Charles Dekker at the University of California, Berkeley.
It was approved by the United States Food and Drug Administration in June 1969, and was
Flecainide acetate ( /flɛˈkeɪnaɪd/ US dict: fle·kā′·nīd) is a class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormal fast rhythms of the heart). It is used to treat a variety of cardiac arrhythmias including paroxysmal atrial fibrillation (episodic irregular heartbeat originating in the upper chamber of the heart), paroxysmal supraventricular tachycardia (episodic rapid but regular heartbeat originating in the atrium), and ventricular tachycardia (rapid rhythms of the lower chambers of the heart). Flecainide works by regulating the flow of sodium in the heart, causing prolongation of the cardiac action potential.
Flecainide was originally sold under the trade name Tambocor (manufactured by 3M pharmaceuticals). Flecainide went off-patent on February 10, 2004, and is now available in generic version and under the trade names Almarytm, Apocard, Ecrinal, and Flécaine.
Flecainide is used in the treatment of many types of supraventricular tachycardias, including AV nodal re-entrant tachycardia (AVNRT) and Wolff-Parkinson-White syndrome (WPW). This is because of the action of flecainide on the His-Purkinje system.
It also has limited use in the treatment of
Hydrochlorothiazide, abbreviated HCTZ, HCT, or HZT, is a first-line diuretic drug of the thiazide class that acts by inhibiting the kidneys' ability to retain water. This reduces the volume of the blood, decreasing blood return to the heart and thus cardiac output and, by other mechanisms, is believed to lower peripheral vascular resistance. Hydrochlorothiazide is a calcium-sparing diuretic, meaning it can help the body get rid of excess water while still keeping calcium.
Hydrochlorothiazide is frequently used for the treatment of hypertension, congestive heart failure, symptomatic edema, diabetes insipidus, renal tubular acidosis, and the prevention of kidney stones.
It is also sometimes used for hypercalciuria, Dent's disease and Ménière's disease. For diabetes insipidus, the effect of thiazide diuretics is presumably mediated by a hypovolemia-induced increase in proximal sodium and water reabsorption, thereby diminishing water delivery to the ADH-sensitive sites in the collecting tubules and reducing the urine output.
Thiazides are also used in the treatment of osteoporosis. Thiazides decrease mineral bone loss by promoting calcium retention in the kidney, and by directly
Sodium valproate (INN) or valproate sodium (USAN) is the sodium salt of valproic acid and is an anticonvulsant used in the treatment of epilepsy, anorexia nervosa, panic attack, anxiety disorder, posttraumatic stress disorder, migraine and bipolar disorder, as well as other psychiatric conditions requiring the administration of a mood stabilizer. Sodium valproate can be used to control acute episodes of mania and acute stress reaction. Side effects can include tiredness, tremors, nausea, vomiting and sedation. The intravenous formulations are used when oral administration is not possible.
In pregnancy, valproate has the highest risk of birth defects of any of the commonly used antiepilepsy drugs. However, some epilepsy can only be controlled by valproate, and seizures also pose grave risk to mother and child.
Some of the common adverse effects include tiredness, tremor, sedation and gastrointestinal disturbances. In addition, about 10% of the users experience reversible hair loss.
Trade names are in bold, followed by the manufacturer.
In much of Europe, Depakine and Depakine Chrono (tablets) are equivalent to Epilim and Epilim Chrono above.
Sodium valproate is a weak blocker of
Isoflurane (2-chloro-2-(difluoromethoxy)-1,1,1-trifluoro-ethane) is a halogenated ether used for inhalational anesthesia. Together with enflurane and halothane, it replaced the flammable ethers used in the pioneer days of surgery. Its name comes from being a structural isomer of enflurane, hence they have the same empirical formula. It is a racemic mixture of (R) and (S) optical isomers. Its use in human medicine is now starting to decline, being replaced with sevoflurane, desflurane and the intravenous anaesthetic propofol. Isoflurane is still frequently used for veterinary anaesthesia.
Isoflurane is always administered in conjunction with air and/or pure oxygen. Often nitrous oxide is also used. Although its physical properties imply that anaesthesia can be induced more rapidly than with halothane, its pungency can irritate the respiratory system, negating this theoretical advantage conferred by its physical properties. It is usually used to maintain a state of general anesthesia that has been induced with another drug, such as thiopentone or propofol. It vaporizes readily, but is a liquid at room temperature. It is completely nonflammable.
Similar to many general anesthetics,
Minoxidil is an antihypertensive vasodilator medication which also slows or stops hair loss and promotes hair regrowth. Now off-patent, it is available over-the-counter for the treatment of androgenic alopecia. Minoxidil must be used indefinitely for continued support of existing hair follicles and the maintenance of any experienced hair regrowth. It is marketed under many trade names, including Avacor Physician's Formulation, Loniten (oral), Mintop, Amexidil, Rogaine, Spectral.DNC, and Vanarex. Kopexil is a derivative of minoxidil missing the piperidine substituent.
Minoxidil was first used exclusively as an oral drug (with the trade name 'Loniten') to treat high blood pressure. However, it was discovered to have an interesting side effect: hair growth. Minoxidil may cause increased growth or darkening of fine body hairs, or in some cases, significant hair growth. When the medication is discontinued, the hair loss will return to normal rate within 30 to 60 days. Upjohn Corporation produced a topical solution that contained 2% minoxidil to be used to treat baldness and hair loss, under the brand name Rogaine in the United States and Canada, and Regaine in Europe and the
Digitoxin is a cardiac glycoside. It has similar structure and effects to digoxin (though the effects are longer-lasting). Unlike digoxin (which is eliminated from the body via the kidneys), it is eliminated via the liver, so could be used in patients with poor or erratic kidney function. However, it is now rarely used in current Western medical practice. While several controlled trials have shown digoxin to be effective in a proportion of patients treated for heart failure, the evidence base for digitoxin is not as strong, although it is presumed to be similarly effective.
Digitoxin exhibits similar toxic effects to the more commonly used digoxin, namely: anorexia, nausea, vomiting, diarrhea, confusion, visual disturbances, and cardiac arrhythmias. Antidigoxin antibody fragments, the specific treatment for digoxin poisoning, are also effective in serious digitoxin toxicity.
The first description of the use of foxglove dates back to 1775. For quite some time, the active compound was not isolated. Oswald Schmiedeberg was able to obtain a pure sample in 1875. The modern therapeutic use of this molecule was made possible by the works of the pharmacist and the French chemist
Vitamin B12, vitamin B12 or vitamin B-12, also called cobalamin, is a water-soluble vitamin with a key role in the normal functioning of the brain and nervous system, and for the formation of blood. It is one of the eight B vitamins. It is normally involved in the metabolism of every cell of the human body, especially affecting DNA synthesis and regulation, but also fatty acid synthesis and energy production. Neither fungi, plants or animals are capable of producing vitamin B12. Only bacteria and archaea have the enzymes required for its synthesis, and they therefore form its only sources in nature. The vitamin is the largest and most structurally complicated vitamin and can be produced industrially only through bacterial fermentation-synthesis.
Vitamin B12 consists of a class of chemically related compounds (vitamers), all of which have vitamin activity. It contains the biochemically rare element cobalt. Biosynthesis of the basic structure of the vitamin is accomplished only by bacteria (which usually produce hydroxocobalamin), but conversion between different forms of the vitamin can be accomplished in the human body. A common semi-synthetic form of the vitamin, cyanocobalamin,
Donepezil, marketed under the trade name Aricept by its developer Eisai and partner Pfizer, is a centrally acting reversible acetylcholinesterase inhibitor. Its main therapeutic use is in the palliative treatment of mild to moderate Alzheimer's disease. Common side effects include gastrointestinal upset. It has an oral bioavailability of 100% and easily crosses the blood–brain barrier. Because it has a half-life of about 70 hours, it can be taken once a day.
Currently, no definitive proof shows the use of donepezil or other similar agents alters the course or progression of Alzheimer's disease (AD). However, six- to 12-month controlled studies have shown modest benefits in cognition and/or behavior. Pilot studies have reported donepezil therapy may potentially have effects on markers of disease progression, such as hippocampal volume. Therefore, many neurologists, psychiatrists, and primary-care physicians use donepezil in patients with Alzheimer's disease. In 2005, the UK National Institute for Clinical Excellence (NICE) withdrew its recommendation for use of the drug for mild-to-moderate AD, on the basis of no significant improvement in functional outcome, quality of life, or
Oxycodone is an analgesic medication synthesized from poppy-derived thebaine. It was developed in 1916 in Germany, as one of several new semi-synthetic opioids in an attempt to improve on the existing opioids: morphine, diacetylmorphine (heroin), and codeine.
Oxycodone oral medications are generally prescribed for the relief of moderate to severe pain. Currently it is formulated as single ingredient products or compounded products. Some common examples of compounding are oxycodone with acetaminophen/paracetamol or non-steroidal anti-inflammatory drugs such as ibuprofen. The formulations are available as generics but are also made under various brand names. OxyContin is Purdue Pharma's brand for time-release oral oxycodone. The manufacturing rights to time-released generic oxycodone are under dispute.
Oxycodone is effective for managing moderate to moderately severe acute or chronic pain. It has been found to improve quality of life for those with many types of pain.
Oxycodone can also be used as an alternative to other opiates to treat severe diarrhea and diarrhea predominant irritable bowel syndrome when drugs such as loperamide and diphenoxylate are ineffective.
In 2001, the
Propranolol (INN) is a sympatholytic non-selective beta blocker. Sympatholytics are used to treat hypertension, anxiety and panic. It was the first successful beta blocker developed. Propranolol is available in generic form as propranolol hydrochloride, as well as an AstraZeneca and Wyeth product under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR (Sandoz).
Propranolol is indicated for the management of various conditions including:
While once first-line treatment for hypertension, the role for beta-blockers was downgraded in June 2006 in the United Kingdom to fourth-line as they perform less well than other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta-blockers at usual doses carry an unacceptable risk of provoking type 2 diabetes.
Propranolol is also used to lower portal vein pressure in portal hypertension and prevent esophageal variceal bleeding.
Propranolol is often used by musicians and other performers to prevent stage fright. It has been taken by surgeons to reduce their own innate hand tremors during surgery.
Propranolol 80 mg daily can be used
Marketed formulations:Ziprasidone mesylate 20 lyophilized powder for injectable solution
Ziprasidone (marketed as Geodon, Zeldox by Pfizer) was the fifth atypical antipsychotic to gain approval (February 2001) in the United States. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia, and acute mania and mixed states associated with bipolar disorder. Its intramuscular injection form is approved for acute agitation in schizophrenic patients for whom treatment with just ziprasidone is appropriate.
Ziprasidone is also used off-label for depression, bipolar maintenance, mood disorders, anxiety, aggression, dementia, attention deficit hyperactivity disorder, obsessive compulsive disorder, autism, and post-traumatic stress disorder, though Pfizer was penalized for promoting such uses in US. The brand name Geodon has been suggested to bring to mind the phrase 'down (don) to earth (geo)' referring to the goals of the medication.
The oral form of ziprasidone is the hydrochloride salt, ziprasidone hydrochloride. The intramuscular form, on the other hand, is the mesylate salt, ziprasidone mesylate trihydrate, and is provided as a lyophilized powder.
Geodon was one of four drugs which Pfizer pleaded guilty to misbranding "with the intent
Cyclopentolate is a mydriatic and cycloplegic agent commonly used during pediatric eye examinations. It works as a muscarinic antagonist. Cyclopentolate is also administered as an atropine substitute to reverse muscarinic and CNS effects of indirect cholinomimetic (anti-AChase) administration.
When used in eye drops in pediatric eye examinations, Cyclopentolate 0.5% and 1.0% is used to stop the eye focusing at near distance, enabling the optometrist, ophthalmologist or orthoptist to obtain a more accurate reading of the focusing power of the eyes. Brand names include Cyclogyl, Cylate, & Pentolair.
The drops take around 30 minutes to work and around 24 hours to wear off (with patients advised not to drive a vehicle or operate machinery for the first 12 hours). The pupils become wider when Cyclopentolate is administered, making the eyes more sensitive to light. Close objects (and possibly distant objects) will also appear blurred.
Side effects to Cyclopentolate are rare, but can include effects such as disorientation, incoherent speech or visual disturbances during the 24-hour period that the drug has an effect.
Etanercept (trade name Enbrel) is a biopharmaceutical that treats autoimmune diseases by interfering with tumor necrosis factor (TNF; a soluble inflammatory cytokine) by acting as a TNF inhibitor. Pfizer describes in a SEC filing that the drug is used to treat rheumatoid, juvenile rheumatoid and psoriatic arthritis, plaque psoriasis and ankylosing spondylitis. Sales reached record $3.3 billion in 2010.
Etanercept is a fusion protein produced through expression of recombinant DNA. That is, it is a product of a DNA "construct" engineered to link the human gene for soluble TNF receptor 2 to the gene for the Fc component of human immunoglobulin G1 (IgG1). Expression of the construct produces a continuous protein "fusing" TNF receptor 2 to IgG1. Production of Etanercept is accomplished by the large-scale culturing of cells that have been "cloned" to express this recombinant DNA construct.
The prototypic fusion protein was first synthesized and shown to be highly active and unusually stable as a modality for blockade of TNF in vivo in the early 1990s by Bruce A. Beutler, an academic researcher then at the University of Texas Southwestern Medical Center at Dallas, and his colleagues.
Lidocaine (INN) ( /ˈlaɪdɵkeɪn/), Xylocaine, or lignocaine (former BAN) ( /ˈlɪɡnɵkeɪn/) is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery.
Lidocaine, the first amino amide–type local anesthetic, was first synthesized under the name Xylocaine by Swedish chemist Nils Löfgren in 1943. His colleague Bengt Lundqvist performed the first injection anesthesia experiments on himself. It was first marketed in 1949.
The efficacy profile of lidocaine as a local anesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. Therefore, lidocaine is suitable for infiltration, block and surface anesthesia. Longer-acting substances such as bupivacaine are sometimes given preference for spinal and peridural anesthesias; lidocaine, on the other hand, has the advantage of a rapid onset of action. Epinephrine vasoconstricts arteries reducing bleeding and also delays the resorption of Lidocaine, almost doubling the duration of anaesthesia. For surface anesthesia several formulations are available that can be
Sodium thiopental, better known as Sodium Pentothal (a trademark of Abbott Laboratories), thiopental, thiopentone sodium, or Trapanal (also a trademark), is a rapid-onset short-acting barbiturate general anaesthetic. Thiopental is a core medicine in the World Health Organization's "Essential Drugs List", which is a list of minimum medical needs for a basic healthcare system. It is also usually the first of three drugs administered during most lethal injections in the United States.
Barbiturates are a class of drugs that act on the GABAA receptor in the brain and spinal cord. The GABAA receptor is an inhibitory channel that decreases neuronal activity, and barbiturates enhance the inhibitory action of the GABAA receptor. Barbiturates, benzodiazepines, and alcohol all bind to the GABAA receptor. Barbiturates that act on the barbiturate binding site of the GABAA receptor directly gate the chloride ion channel of the GABAA receptor, whereas benzodiazepines acting on the benzodiazepine site on the GABAA receptor increase the opening frequency of the chloride ion channel. This explains why overdoses of barbiturates may be lethal whereas overdoses of benzodiazepines alone are typically
Acetylcholine (often abbreviated ACh) is an organic, polyatomic ion that acts as a neurotransmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans. Acetylcholine is one of many neurotransmitters in the autonomic nervous system (ANS) and the only neurotransmitter used in the motor division of the somatic nervous system (sensory neurons use glutamate and various peptides at their synapses). Acetylcholine is also the principal neurotransmitter in all autonomic ganglia.
In cardiac tissue acetylcholine neurotransmission has an inhibitory effect, which lowers heart rate. However, acetylcholine also behaves as an excitatory neurotransmitter at neuromuscular junctions in skeletal muscle.
Acetylcholine (ACh) was first identified in 1914 by Henry Hallett Dale for its actions on heart tissue. It was confirmed as a neurotransmitter by Otto Loewi, who initially gave it the name Vagusstoff because it was released from the vagus nerve. Both received the 1936 Nobel Prize in Physiology or Medicine for their work. Acetylcholine was also the first neurotransmitter to be identified.
Acetylcholine is an ester of acetic acid and choline
Interferon beta-1a (also interferon beta-1-alpha) is a drug in the interferon family used to treat multiple sclerosis (MS). It is produced by mammalian cells, while Interferon beta-1b is produced in modified E. coli. Interferons have been shown to produce about a 18–38% reduction in the rate of MS relapses, and to slow the progression of disability in MS patients. There is currently no cure for MS, though starting a course of interferons early may slow its progress.
Interferon beta-1a is sold under the trade names Avonex (Biogen Idec) and Rebif (Merck Serono); CinnoVex (CinnaGen) is biosimilar.
It is believed that Interferon beta based drugs achieve their beneficial effect on MS progression via their anti-inflammatory properties. Studies have also determined that Interferon beta improves the integrity of the blood–brain barrier (BBB), which generally breaks down in MS patients, allowing increasing amounts of undesirable substances to reach the brain. This strengthening of the BBB may be a contributing factor to Interferon-Beta's beneficial effects. These studies were carried out in vitro and thus may not necessarily work the same way in people.
The most commonly reported side
Carisoprodol is a centrally acting skeletal muscle relaxant. It is slightly soluble in water and freely soluble in alcohol, chloroform and acetone. The drug's solubility is practically independent of pH. Carisoprodol is manufactured and marketed in the United States by Meda Pharmaceuticals. under the brand name Soma, and in the United Kingdom and other countries under the brand names Sanoma and Carisoma. The drug is available by itself or mixed with aspirin, and in one preparation with codeine and caffeine, as well.
On June 1, 1959 several American pharmacologists convened at Wayne State University in Detroit, Michigan to discuss a new drug. The drug, originally thought to have antiseptic properties, was found to have central muscle-relaxing properties. It had been developed by Frank M. Berger at Wallace Laboratories and was named carisoprodol.
Carisoprodol was a modification of meprobamate, intended to have better muscle relaxing properties, less potential for abuse, and less risk of overdose. The substitution of one hydrogen atom with an isopropyl group on one of the carbamyl nitrogens was intended to yield a molecule with new pharmacological properties.
Reports from Norway have
Marketed formulations:Phenelzine sulfate 15 film coated tablet
Phenelzine (Nardil, Nardelzine) is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class which is used as an antidepressant and anxiolytic. Along with tranylcypromine and isocarboxazid, phenelzine is one of the few non-selective MAOIs still in widespread clinical use.
Phenelzine is used primarily in the treatment of major depressive disorder (MDD). Patients with depressive symptomology characterized as "atypical", "nonendogenous", and/or "neurotic", have been reported to respond particularly well to phenelzine. The medication has also been found to be useful in patients who do not respond favorably to first and second-line treatments for depression, or are said to be "treatment-resistant". In addition to being a recognized treatment for major depressive disorder, phenelzine has been found in studies to be effective in treating dysthymia, bipolar depression (BD), panic disorder (PD), social anxiety disorder (SAD), bulimia, and post-traumatic stress disorder (PTSD).
Phenelzine is a non-selective and irreversible inhibitor of the enzyme monoamine oxidase (MAO). It inhibits both of the respective isoforms of MAO, MAO-A and MAO-B, and does so almost
Tadalafil is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. On 10.2011 FDA approved Cialis for treatment the signs and symptoms of benign prostatic hyperplasia (BPH) as well as a combination of BPH and erectile dysfunction (ED) when the conditions coincide. It initially was developed by the biotechnology company ICOS, and then again developed and marketed world-wide by Lilly ICOS, LLC, the joint venture of ICOS Corporation and Eli Lilly and Company. Cialis tablets, in 5 mg, 10 mg, and 20 mg doses, are yellow, film-coated, and almond-shaped. The approved dose for pulmonary arterial hypertension is 40 mg (two 20-mg tablets) once daily.
Tadalafil is also manufactured and sold under the name of Tadacip by the Indian pharmaceutical company Cipla in doses of 10 mg and 20 mg.
On November 21, 2003 the Food and Drug Administration approved tadalafil (as Cialis) for sale in the United States as the third ED prescription drug pill (after sildenafil citrate (Viagra) and vardenafil (Levitra)). Cialis's 36-hour effectiveness earned it the nickname,
Loxapine (Loxapac, Loxitane) is a typical antipsychotic medication, used primarily in the treatment of schizophrenia. It is a member of the ( benzodiazepine ) dibenzoxazepine class and as a dibenzazepine derivative, it is structurally related to clozapine (which belongs to the chemically closely akin class of dibenzodiazepines). Several researchers have argued that Loxapine may behave as an atypical antipsychotic.
Loxapine may be metabolized by N-demethylation to amoxapine, a tetracyclic antidepressant.
Care should be taken with consumption. At least 3 cases were reported of loxapine succinate abuse.
The most significant side-effects of loxapine are excessive salivation (hypersalivation) and indifference to surroundings. Loxapine, if administered to individuals without schizophrenia, causes emotional quieting and insensitivity. In persons with psychosis, it may control aggressive behaviour and restlessness, and reduce the severity of hallucinations and delusions. Other Side effects include tardive dyskinesia, neuroleptic malignant syndrome, extrapyramidal side effects, tremor, gynecomastia and sedation.
The typical starting dosage is 10 mg twice daily; usual dose range 30–50 mg
Methyltestosterone (brand names: Android, Testred, Virilon) is a 17-alpha-alkylated anabolic steroid used to treat men with a testosterone deficiency. It bears close structural similarity to testosterone, but has a methyl group at C17 in order to increase oral bioavailability.
Gentamicin is an aminoglycoside antibiotic, used to treat many types of bacterial infections, particularly those caused by Gram-negative organisms. However, gentamicin is not used for Neisseria gonorrhoeae, Neisseria meningitidis or Legionella pneumophila. Gentamicin is also ototoxic and nephrotoxic, with this toxicity remaining a major problem in clinical use.
It is synthesized by Micromonospora, a genus of Gram-positive bacteria widely present in the environment (water and soil). To highlight their specific biological origins, gentamicin and other related antibiotics produced by this genus (verdamicin, mutamicin, sisomicin, netilmicin, retymicin) generally have their spellings ending in ~micin and not in ~mycin. Gentamicin is a bactericidal antibiotic that works by binding the 30S subunit of the bacterial ribosome, interrupting protein synthesis.
Like all aminoglycosides, when gentamicin is given orally, it is not systemically active. This is because it is not absorbed to any appreciable extent from the small intestine. It is administered intravenously, intramuscularly or topically to treat infections. It appears to be completely eliminated unchanged in the urine. Urine must be
Glutethimide is a hypnotic sedative that was introduced in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms. Doriden is the brand-name version of the drug; both the generic and brand-name forms are rarely prescribed today.
In long term use rebound effects, which resembled those seen in withdrawal, have anecdotally been described in patients, who were still taking a stable dose of the drug. The symptoms included delirium, hallucinosis, convulsions and fever.
Glutethimide is a CYP2D6 enzyme inducer. When taken with codeine, it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) to morphine. The general sedative effect also adds to the effect of the combination.
Glutethimide is a Schedule II drug under the Convention on Psychotropic Substances. It was originally a Schedule III drug in the United States under the Controlled Substances Act, but in 1991 it was upgraded to Schedule II, after it was discovered that misuse combined with codeine increased the effect of the codeine and deaths had
Lamotrigine, marketed in the US and most of Europe as Lamictal ( /ləˈmɪktəl/) by GlaxoSmithKline, is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. It is also used off-label as an adjunct in treating depression. For epilepsy, it is used to treat focal seizures, primary and secondary tonic-clonic seizures, and seizures associated with Lennox-Gastaut syndrome. Like many other anticonvulsant medications, Lamotrigine also seems to act as an effective mood stabilizer, and has been the first U.S. Food and Drug Administration (FDA)-approved drug for this purpose since lithium, a drug approved almost 30 years earlier. It is approved for the maintenance treatment of bipolar type I. Chemically unrelated to other anticonvulsants (due to lamotrigine's being a phenyltriazine), lamotrigine has many possible side-effects. Lamotrigine is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs, but it could have additional actions inasmuch as it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and carbamazepine and is effective in the treatment of the depressed phase of bipolar
Marketed formulations:Levofloxacin 750 film coated tablet
Levofloxacin (Levaquin (U.S.), Tavanic (E.U.), and others) is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class and is used to treat severe or life-threatening bacterial infections or bacterial infections that have failed to respond to other antibiotic classes.
Levofloxacin is a chiral fluorinated carboxyquinolone. Investigation of ofloxacin, an older drug that is the racemic mixture, found that the l form [the (–)-(S) enantiomer] is more active. This specific component is levofloxacin.
Levofloxacin interacts with other drugs, as well as herbal and natural supplements. Such interactions increase the risk of cardiotoxicity and arrhythmias, anticoagulation, the formation of non-absorbable complexes, as well as increasing the risk of toxicity.
Levofloxacin is associated with serious and life-threatening adverse reactions as well as spontaneous tendon ruptures and irreversible peripheral neuropathy. Such reactions may manifest long after therapy had been completed and in severe cases may result in life-long disabilities. Hepatoxicity has also been reported with the use of levofloxacin.
As of 2011, the U.S. Food and Drug Administration (FDA) has added two Black
Lindane, also known as gamma-hexachlorocyclohexane, (γ-HCH), gammaxene, Gammallin and erroneously known as benzene hexachloride (BHC), is an organochlorine chemical variant of hexachlorocyclohexane that has been used both as an agricultural insecticide and as a pharmaceutical treatment for lice and scabies.
Lindane is a neurotoxin that interferes with GABA neurotransmitter function by interacting with the GABAA receptor-chloride channel complex at the picrotoxin binding site. In humans, lindane affects the nervous system, liver and kidneys, and may be a carcinogen. It is unclear whether lindane is an endocrine disruptor.
The World Health Organization classifies lindane as "Moderately Hazardous," and its international trade is restricted and regulated under the Rotterdam Convention on Prior Informed Consent. In 2009 the production and agricultural use of lindane was banned under the Stockholm Convention on persistent organic pollutants. A specific exemption to that ban allows it to continue to be used as a second-line pharmaceutical treatment for lice and scabies.
The chemical was originally synthesised in 1825 by Faraday, but its pesticidal action was discovered only in 1942,
Clozapine (sold as Clozaril, Gen-Clozapine in Canada, Azaleptin, Leponex, Fazaclo, Froidir; Denzapine, Zaponex in the UK; Klozapol in Poland, Clopine in Australia and New Zealand) is an atypical antipsychotic medication used in the treatment of schizophrenia, and is also used off-label in the treatment of bipolar disorder. In 2005 three pharmaceutical companies marketed this drug: Novartis Pharmaceuticals (manufacturer), Mylan Laboratories and Ivax Pharmaceuticals (market generic clozapine). The first of the atypical antipsychotics to be developed, it was first introduced in Europe in 1971, but was voluntarily withdrawn by the manufacturer in 1975 after it was shown to cause agranulocytosis, a condition involving a dangerous decrease in the number of white blood cells, that led to death in some patients. In 1989 after studies demonstrated that it was effective in treating treatment-resistant schizophrenia the United States Food and Drug Administration (FDA) approved the use of clozapine's solely for that use, requiring regular white blood cell and absolute neutrophil counts. The FDA also requires clozapine to carry five black box warnings for agranulocytosis, seizures, myocarditis,
Mifepristone is a synthetic steroid compound used as a pharmaceutical. It is a progesterone receptor antagonist used as an abortifacient in the first months of pregnancy, and in smaller doses as an emergency contraceptive. Mifepristone is also a powerful glucocorticoid receptor antagonist, and has occasionally been used in refractory Cushing's Syndrome (due to ectopic/neoplastic ACTH/Cortisol secretion). During early trials, it was known as RU-38486 or simply RU-486, its designation at the Roussel Uclaf company, which designed the drug. The drug was initially made available in France, and other countries then followed—often amid controversy. It is marketed under tradenames Mifegyne and Mifeprex.
In April 1980, as part of a formal research project at Roussel-Uclaf for the development of glucocorticoid receptor antagonists, chemist Georges Teutsch synthesized mifepristone (RU-38486, the 38,486th compound synthesized by Roussel-Uclaf from 1949 to 1980; shortened to RU-486); which was discovered to also be a progesterone receptor antagonist. In October 1981, endocrinologist Étienne-Émile Baulieu, a consultant to Roussel-Uclaf, arranged tests of its use for medical abortion in eleven
Marketed formulations:Quetiapine fumarate 200 film coated tablet
Quetiapine ( /kwɨˈtaɪ.əpiːn/ kwi-TY-ə-peen) (branded as Seroquel, Xeroquel, Ketipinor), is an atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and at a lower dose an add-on to treat depression.
Annual sales are approximately $5.7 billion worldwide, with $2.9 billion in the United States. The U.S. patent, which was set to expire in 2011, received a pediatric exclusivity extension which pushed its expiration to March 26, 2012. The patent has already expired in Canada. There are now several generic versions of quetiapine, such as Quepin, Syquel' and Ketipinor.
Quetiapine fumarate is used to treat either schizophrenia or bipolar disorder.
In the United States, the FDA has approved quetiapine for the short term treatment of schizophrenia and of acute manic episodes associated with bipolar disorder (bipolar mania) and for treatment of bipolar depression.
Quetiapine is also used off-label for aggression, Alzheimer’s disease, anger management, anxiety, attention deficit hyperactivity disorder, bipolar maintenance, dementia, depression, mood disorder, post-traumatic stress disorder, and sleeplessness, though AstraZeneca was penalized for promoting such
Spironolactone (INN, BAN, USAN) (pronounced "SPY-row-no-LACK-tone"), commonly referred to simply as "spiro", and marketed primarily under the brand name Aldactone in most countries, is a synthetic, steroidal antimineralocorticoid agent with additional antiandrogen and weak progestogen properties, as well as some indirect estrogen and glucocorticoid effects, which is used primarily as a diuretic and antihypertensive, but also for the purpose of reducing elevated or unwanted androgen activity in the body. It acts predominantly as a competitive antagonist of the aldosterone (or mineralocorticoid) receptor, and belongs to a class of pharmaceutical drugs known as potassium-sparing diuretics.
Spironolactone is a relatively old drug, having been introduced clinically in 1959. It has been mostly superseded in cardiovascular conditions (e.g., heart failure and hypertension) by the newer agents such as the structurally related compound eplerenone, which is also an aldosterone antagonist but is selective and lacks many of the actions and side effects of spironolactone, and as such is much more tolerable in comparison. However, spironolactone nonetheless still finds frequent use as an
Alpha 1-Antitrypsin or α1-antitrypsin (A1AT) is a protease inhibitor belonging to the serpin superfamily. It is generally known as serum trypsin inhibitor. Alpha 1-antitrypsin is also referred to as alpha-1 proteinase inhibitor (A1PI) because it inhibits a wide variety of proteases. It protects tissues from enzymes of inflammatory cells, especially neutrophil elastase, and has a reference range in blood of 1.5 - 3.5 gram/liter (in US the reference range is generally expressed as mg/dL or micromoles), but the concentration can rise manyfold upon acute inflammation. In its absence, neutrophil elastase is free to break down elastin, which contributes to the elasticity of the lungs, resulting in respiratory complications such as emphysema, or COPD (chronic obstructive pulmonary disease) in adults and cirrhosis in adults or children.
A1AT is a 52-kDa serpin and, in medicine, it is considered the most prominent serpin; the terms α1-antitrypsin and protease inhibitor (Pi) are often used interchangeably.
Most serpins inactivate enzymes by binding to them covalently, requiring very high levels to perform their function. In the acute phase reaction, a further elevation is required to "limit"
Neostigmine (Prostigmin, Vagostigmin) is a parasympathomimetic that acts as a reversible acetylcholinesterase inhibitor.
Neostigmine was first synthesized by Aeschlimann and Reinert in 1931.
Neostigmine is made by first reacting 3-dimethylaminophenol with N-dimethylcarbamoyl chloride, which forms a dimethylcarbamate. Next, that product is alkylated using dimethylsulfate, which forms neostigmine.
By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. Unlike physostigmine, neostigmine has a quaternary nitrogen; hence, it is more polar and does not enter the CNS. Its effect on skeletal muscle is greater than that of physostigmine, and it can stimulate contractility before it paralyzes. Neostigmine has moderate duration of action, usually two to four hours. Neostigmine binds to the anionic site of cholinesterase. The drug blocks the active site of acetylcholinesterase so the enzyme can no longer break down the acetylcholine molecules before they reach the postsynaptic membrane receptors. This allows for the threshold to be reached so a new impulse can be triggered in the next neuron. In myasthenia gravis there are
Thalidomide ( /θəˈlɪdəmaɪd/) is a sedative drug introduced in the late 1950s that was used to treat morning sickness and to aid sleep. It was sold from 1957 until 1961, when it was withdrawn after being found to be a teratogen - a cause of birth defects. Modern uses of thalidomide (trademarked as Thalomid, according to FDA Orange Book) include treating multiple myeloma in combination with dexamethasone, and erythema nodosum leprosum, with strict controls on its use to prevent birth defects. Research is ongoing in its use to treat other cancers and autoimmune conditions, although its use is controversial; the thalidomide tragedy led to much stricter testing being introduced for drug and pesticide licensing.
Thalidomide was developed by German pharmaceutical company Grünenthal in Stolberg near Aachen. Heinrich Mückter, a former Nazi Party member and army physician, had headed Grünenthal's research department since the foundation of the company and was responsible for inventing thalidomide. During World War II he had been responsible at the German Supreme High Command institute for virus and typhus research in Kraków to produce Rudolf Weigl's vaccine against epidemic
Marketed formulations:Aztreonam 2 lyophilized powder for injectable solution
Aztreonam (trade names Azactam injection, Cayston inhalation) is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration (FDA) in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases.
Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them. Aztreonam is bactericidal but less so than some of the cephalosporins.
Acinetobacter anitratus, Escherichia coli and Proteus mirabilis species are generally susceptible to Aztreonam, while some Pseudomonas aeruginosa, Staphylococci, Staphylococcus aureus, Staphylococcus hemolyticus and Xanthomonas maltophilia are resistant to Aztreonam. Furthermore, Aeromonas hydrophila, Citrobacter diversus, Enterobacter agglomerans,
Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction. It is sold under the trade names Tensilon and Enlon (according to FDA Orange Book).
Indication: edrophonium (by the so-called Tensilon test) is used to differentiate myasthenia gravis from cholinergic crisis. In myasthenia gravis, where a person is not able to produce enough neuromuscular stimulation, edrophonium will reduce the muscle weakness by effectively supplying more acetylcholine. In a cholinergic crisis, where a person has too much neuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block.
Edrophonium, ethyl-(3-hydroxyphenyl)dimethylammonium chloride, is made by reacting 3-dimethylaminophenol with ethyl bromide, which forms ethyl(3-hydroxyphenyl)dimethylammonium bromide, the bromine atom of which is replaced with a chlorine atom by reacting it with silver chloride, giving edrophonium.
Fluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia, manic phases of bipolar disorder, agitation, and dementia. It belongs to the piperazine class of phenothiazines. The medication may help control symptoms by blocking or lessening the effects of dopamine in the brain. It is not entirely known how the medication works. However, it is known to block or lessen the effects of dopamine, a chemical in the brain. Dopamine may be elevated in people with schizophrenia or other psychoses. It also can be used as a calming drug in horses, though such use is illegal.
The medication was originally manufactured by Bristol-Myers Squibb. Although brand-name fluphenazine is no longer manufactured, a generic version is still available. It is made by several different companies. The medication comes in oral liquid, tablets (1mg, 2.5mg, 5mg, 10mg), and injectable forms (including a short-acting and long-acting form).
Fluphenazine has an incomplete oral bioavailability of 40% to 50% (due to extensive first pass metabolization in the liver). Its half life is 15 to 30 hours.
In children over age 16 and in adults, fluphenazine is usually given in
Paracetamol INN ( /ˌpærəˈsiːtəmɒl/ or /ˌpærəˈsɛtəmɒl/), or acetaminophen USAN /əˌsiːtəˈmɪnəfɨn/, is a widely used over-the-counter analgesic (pain reliever) and antipyretic (fever reducer). It is commonly used for the relief of headaches and other minor aches and pains and is a major ingredient in numerous cold and flu remedies. In combination with opioid analgesics, paracetamol can also be used in the management of more severe pain such as post-surgical pain and providing palliative care in advanced cancer patients. The onset of analgesia is approximately 11 minutes after oral administration of paracetamol, and its half-life is 1–4 hours. Though acetaminophen is used to treat inflammatory pain, it is not generally classified as an NSAID because it exhibits only weak anti-inflammatory activity.
While generally safe for use at recommended doses (1,000 mg per single dose and up to 4,000 mg per day for adults), acute overdoses of paracetamol can cause potentially fatal liver damage and, in rare individuals, a normal dose can do the same; the risk is heightened by alcohol consumption. Paracetamol toxicity is the foremost cause of acute liver failure in the Western world, and accounts
Pentazocine is a synthetically prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat moderate to moderately severe pain. Pentazocine is sold under several brand names, such as Fortral, Talwin NX (with the μ-antagonist naloxone, will cause withdrawal in opioid dependent persons on injection), Talwin, Talwin PX (without naloxone), Fortwin (Lactate injectable form) and Talacen (with acetaminophen). This compound may exist as one of two enantiomers, named (+)-pentazocine and (-)-pentazocine. (-)-pentazocine is a κ-opioid receptor agonist, while (+)-pentazocine is not, instead displaying a ten-fold greater affinity for the σ receptor. Talwin PX is the main pentazocine pharmaceutical in Canada, where laws and regulations prohibit the addition of naloxone to the formulation for non-therapeutic purposes. Related drugs include phenazocine, dezocine, cyclazocine and several chemicals used in research on the central nervous system.
Pentazocine is used to treat moderate to severe pain
Pentazocine is administered by subcutaneous (rarely), intramuscular, and intravenous injection as the lactate. It is also available in
Methylphenidate (MPH; MPD) is a psychostimulant drug approved for treatment of ADHD or attention-deficit hyperactivity disorder, postural orthostatic tachycardia syndrome and narcolepsy. It is better known by its 1948 trademarked name of Ritalin (original owner CIBA, now Novartis Corporation), was first licensed by the FDA in 1955 for treating ADHD, prescribed from 1960, and became heavily prescribed in the 1990s, when ADHD itself became more widely accepted.
ADHD and some other conditions are believed to be linked to sub-performance of the dopamine, norepinephrine, serotonin and glutamate processes in the brain responsible for self-regulation functions, leading to self-regulation disorders compromising the sufferer's attention, self-control, behaviour, motivation, and executive function; methylphenidate primarily works by reducing the reuptake (removal) of dopamine and norepinephrine (and to a lesser extent serotonin) which improves the levels and utility of these neurotransmitters in the brain.
Methylphenidate may also be prescribed for off-label use in treatment-resistant cases of lethargy, depression, and obesity. Methylphenidate incorporates a phenethylamine skeleton within
Marketed formulations:Quinidine sulfate 300 extended release film coated tablet
Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent (Ia) in the heart. It is a stereoisomer of quinine, originally derived from the bark of the cinchona tree. The drug causes increased action potential duration, as well as a prolonged QT interval.
Like all other class I antiarrhythmic agents, quinidine primarily works by blocking the fast inward sodium current (INa). Quinidine's effect on INa is known as a 'use dependent block'. This means at higher heart rates, the block increases, while at lower heart rates, the block decreases. The effect of blocking the fast inward sodium current causes the phase 0 depolarization of the cardiac action potential to decrease (decreased Vmax).
Quinidine also blocks the slowly inactivating, tetrodotoxin-sensitive Na current, the slow inward calcium current (ICa), the rapid (IKr) and slow (IKs) components of the delayed potassium rectifier current, the inward potassium rectifier current (IKI), the ATP-sensitive potassium channel (IKATP) and Ito.
At micromolar concentrations, quinidine inhibits Na⁺/K⁺-ATPase by binding to the same receptor sites as the digitalis glycosides such as ouabain.
The effect of quinidine on the
Marketed formulations:Aspirin 325 film coated tablet
Aspirin (USAN), also known as acetylsalicylic acid (/əˌsɛtəlˌsælɨˈsɪlɨk/ ə-SET-əl-SAL-i-SIL-ik; abbreviated ASA), is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin was first isolated by Felix Hoffmann, a chemist with the German company Bayer in 1897.
Salicylic acid, the main metabolite of aspirin, is an integral part of human and animal metabolism. While in humans much of it is attributable to diet, a substantial part is synthesized endogenously.
Aspirin also has an antiplatelet effect by inhibiting the production of thromboxane, which under normal circumstances binds platelet molecules together to create a patch over damaged walls of blood vessels. Because the platelet patch can become too large and also block blood flow, locally and downstream, aspirin is also used long-term, at low doses, to help prevent heart attacks, strokes, and blood clot formation in people at high risk of developing blood clots. It has also been established that low doses of aspirin may be given immediately after a heart attack to reduce the risk of another heart attack or of the death of
Ciclosporin (INN/BAN) (pronounced /ˌsaɪkləˈspɔrɪn/), cyclosporine (USAN), cyclosporin (former BAN), or cyclosporin A (often shortened to CsA) is an immunosuppressant drug widely used in organ transplantation to prevent rejection. It reduces the activity of the immune system by interfering with the activity and growth of T cells. It was initially isolated from the fungus Tolypocladium inflatum (Beauveria nivea), found in a soil sample obtained in 1969 from Hardangervidda, Norway by Dr. Hans Peter Frey, a Sandoz biologist. Most peptides are synthesized by ribosomes, but ciclosporin is a cyclic nonribosomal peptide of 11 amino acids and contains a single D-amino acid, which are rarely encountered in nature.
The immunosuppressive effect of ciclosporin was discovered on 31 January 1972 by employees of Sandoz (now Novartis) in Basel, Switzerland, in a screening test on immune suppression designed and implemented by Hartmann F. Stähelin, M.D. The success of ciclosporin in preventing organ rejection was shown in kidney transplants by Calne and colleagues at the University of Cambridge, and in liver transplants performed by Dr. Thomas Starzl at the University of Pittsburgh Hospital. The
Melatonin /ˌmɛləˈtoʊnɪn/, also known chemically as N-acetyl-5-methoxytryptamine, is a naturally occurring compound found in animals, plants, and microbes. In animals, circulating levels of the hormone melatonin vary in a daily cycle, thereby allowing the entrainment of the circadian rhythms of several biological functions.
Many biological effects of melatonin are produced through activation of melatonin receptors, while others are due to its role as a pervasive and powerful antioxidant, with a particular role in the protection of nuclear and mitochondrial DNA.
Products containing melatonin have been available over-the-counter in the United States since the mid-1990s. In many other countries, the sale of this neurohormone is not permitted or requires a prescription.
Melatonin has been identified in many plants including Feverfew (Tanacetum parthenium), and St John's wort (Hypericum perforatum). The physiological roles of melatonin in plants involve regulation of their response to photoperiod, defense against harsh environments, and the function of an antioxidant. The latter may be the original function of melatonin in organisms with the others being added during evolution. Melatonin
Nystatin (originally named Fungicidin) is a polyene antifungal medication to which many molds and yeast infections are sensitive, including Candida. Due to its toxicity profile, there are currently no injectable formulations of this drug on the US market. However, nystatin may be safely given orally as well as applied topically due to its minimal absorption through mucocutaneous membranes such as the gut and the skin.
Cutaneous, vaginal, mucosal and esophageal Candida infections usually respond well to treatment with nystatin. Cryptococcus is also sensitive to nystatin. In the UK its licence for treating neonatal oral thrush is restricted to those over the age of one month (miconazole is an appropriate alternative for younger babies).
Nystatin is often used as prophylaxis in patients who are at risk for fungal infections, such as AIDS patients with a low CD4 count and patients receiving chemotherapy.
It is prescribed in units, with doses varying from 100,000 (for oral infections) to 1 million (for intestinal ones). As it is not absorbed from the gut, it is safe for oral use and does not have problems of drug interactions.
It is also used in cellular biology as an inhibitor of the
Troglitazone (Rezulin, Resulin or Romozin) is an antidiabetic and anti-inflammatory drug, and a member of the drug class of the thiazolidinediones. It was developed by Daiichi Sankyo Co.(Japan). In the United States, it was introduced and manufactured by Parke-Davis in the late 1990s, but turned out to be associated with an idiosyncratic reaction leading to drug-induced hepatitis. One FDA medical officer evaluating troglitazone, John Gueriguian, did not recommend its approval due to potential high liver toxicity, but a full panel of experts approved it in January 1997. Once the prevalence of adverse liver effects became known, troglitazone was withdrawn from the British market in December 1997, from the United States market in 2000, and from the Japanese market soon afterwards.
Troglitazone, like the other thiazolidinediones (pioglitazone and rosiglitazone), works by activating peroxisome proliferator-activated receptors (PPARs).
Troglitazone is a ligand to both PPARα and – more strongly – PPARγ. Troglitazone also contains an α-tocopheroyl moiety, potentially giving it vitamin E-like activity in addition to its PPAR activation. It has been shown to reduce inflammation: troglitazone
Cocaine (benzoylmethylecgonine) (INN) is a crystalline tropane alkaloid that is obtained from the leaves of the coca plant. The name comes from "coca" and the alkaloid suffix -ine, forming cocaine. It is a stimulant, an appetite suppressant, and a topical anesthetic. Biologically, cocaine acts as a serotonin–norepinephrine–dopamine reuptake inhibitor, also known as a triple reuptake inhibitor (TRI). It is addictive because of its effect on the mesolimbic reward pathway.
Unlike most molecules, cocaine has pockets with both high hydrophilic and lipophilic efficiency, violating the rule of hydrophilic-lipophilic balance. This causes it to cross the blood–brain barrier far better than other psychoactive chemicals.
It is illegal to possess, grow, or distribute cocaine for non-medicinal and non-government-sanctioned purposes in almost every country. Still it is consumed extensively throughout the world.
Cocaine is a powerful nervous system stimulant. Its effects can last from 15–30 minutes to an hour, depending on the route of administration.
Cocaine increases alertness, feelings of well-being and euphoria, energy and motor activity, feelings of competence and sexuality. Athletic
Methotrexate (rINN) ( /mɛθɵˈtrɛkseɪt/), abbreviated MTX and formerly known as amethopterin, is an antimetabolite and antifolate drug. It is used in treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions. It acts by inhibiting the metabolism of folic acid. Methotrexate began to replace the more toxic antifolate aminopterin starting in the 1950s. The drug was developed by Yellapragada Subbarao.
Methotrexate was originally developed and continues to be used for chemotherapy either alone or in combination with other agents. It is effective for the treatment of a number of cancers including: breast, head and neck, leukemia, lymphoma, lung, osteosarcoma, bladder, and trophoblastic neoplasms.
It is used as a treatment for some autoimmune diseases, including rheumatoid arthritis, psoriasis, psoriatic arthritis, lupus and Crohn's disease, to name a few. Although methotrexate was originally designed as a chemotherapy drug (in high doses), in low doses methotrexate is a generally safe and well tolerated drug in the treatment of certain autoimmune diseases. Because of its effectiveness, low-dose methotrexate is now first-line therapy for the
Triazolam (marketed in English-speaking countries under the brand names Apo-Triazo, Halcion, Hypam, and Trilam) is a benzodiazepine drug. It possesses pharmacological properties similar to that of other benzodiazepines, but it is generally only used as a sedative to treat severe insomnia. In addition to the hypnotic properties triazolam possesses, amnesic, anxiolytic, sedative, anticonvulsant and muscle relaxant properties are also present. Due to its short half-life, triazolam is not effective for patients that suffer from frequent awakenings or early wakening.
Its use at low doses has been deemed acceptable by the American Food and Drug Administration (FDA) and several other countries.
Studies have found a much higher incidence of psychiatric disturbances (sometimes severe) with triazolam, even when using the lower doses of 0.125 mg. Clinical trials which Upjohn had withheld from publishing showed a very unfavourable risk benefit ratio with 9.9% of patients dropping out of one triazolam study versus 1.9% of trial subjects taking a comparison benzodiazepine, flurazepam. Another study not published by Upjohn found 12.2% of triazolam patients dropped out, again due to psychiatric
Benzatropine (INN), also known as benztropine (USAN, BAN), is an anticholinergic marketed under the trade name Cogentin which is used in the treatment of Parkinson's disease, Parkinsonism, and dystonia.
Benzatropine is an anticholinergic drug used in patients to reduce the side effects of antipsychotic treatment, such as pseudoparkinsonism and dystonia. Benzatropine is also a second-line drug for the treatment of Parkinson's disease. It improves tremor, but not rigidity and bradykinesia. Benzatropine is also sometimes used for the treatment of dystonia, a rare disorder that causes abnormal muscle contraction, resulting in twisting postures of limbs, trunk, or face.
These are principally anticholinergic:
While some studies suggest that use of anticholinergics increases the risk of tardive dyskinesia (a long-term side effect of antipsychotics), other studies have found no association between anticholinergic exposure and risk of developing tardive dyskinesia, although symptoms may be worsened.
Benzatropine is a centrally acting anticholinergic/antihistamine agent resulting from the combination of the tropine portion of the atropine molecule and the benzohydryl portion of
Disulfiram is a drug discovered in the 1920s and used to support the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. It blocks the processing of alcohol in the body, thus causing an unpleasant reaction when alcohol is consumed. Disulfiram should be used in conjunction with counseling and support. Trade names for disulfiram in different countries are Antabuse and Antabus manufactured by Odyssey Pharmaceuticals. Disulfiram is also being studied as a treatment for cocaine dependence, as it prevents the breakdown of dopamine (a neurotransmitter whose release is stimulated by cocaine); the excess dopamine results in increased anxiety, higher blood pressure, restlessness and other unpleasant symptoms. Several studies have reported that it has anti-protozoal activity as well. Research for possible disulfiram use in cancer therapy has been announced.
The drug's action was discovered by accident in 1948 by the researchers Erik Jacobsen, Jens Hald, and Keneth Ferguson at the Danish drug company Medicinalco. The substance was intended to provide a remedy for parasitic infestations; however, workers testing the substance on themselves reported severe symptoms
Imatinib (originally STI571) is a drug used to treat certain cancers. It is marketed by Novartis as Gleevec (USA) or Glivec (Europe/Australia/Latin America) as its mesylate salt, imatinib mesilate (INN).
Imatinib is the first of a new class of drugs that act by specifically inhibiting a certain enzyme – a receptor tyrosine kinase – that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all rapidly dividing cells. Imatinib was a model for other targeted therapies that inhibited this class of enzymes.
It is used in treating chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and some other diseases. By 2011, Gleevec has been FDA approved to treat ten different cancers.
In CML, the tyrosine kinase enzyme ABL in white blood cells is locked in its activated form. This causes the excessive proliferation and high white blood cell count which is characteristic of CML. Imatinib binds to the site of tyrosine kinase activity, and prevents its activity, causing tumor cell death (apoptosis).
In January 2012, three of the developers of imatinib were awarded the Japan Prize for their work.
Imatinib was developed in the late
Amiodarone is an antiarrhythmic agent used for various types of cardiac dysrhythmias, both ventricular and atrial. It was discovered in 1961. Despite relatively common side-effects, it is used in arrhythmias that are otherwise difficult to treat with medication.
The original observation that amiodarone's progenitor molecule, khellin, had cardioactive properties, was made by the Lebanese physiologist Gleb von Anrep while working in Cairo. Khellin is a plant extract of Khella or Ammi visnaga, a common plant in north Africa. Anrep noticed that one of his technicians had been cured of anginal symptoms after taking khellin, then used for various, non-cardiac ailments. This led to efforts by European pharmaceutical industries to isolate an active compound. Amiodarone was initially developed in 1961 at the Labaz company, Belgium, by chemists Tondeur and Binon, who were working on preparations derived from khellin. It became popular in Europe as a treatment for angina pectoris.
As a doctoral candidate at Oxford University, Dr. Bramah Singh determined that amiodarone and sotalol had antiarrhythmic properties and belonged to a new class of antiarrhythmic agents (what would become the class
Marketed formulations:Clarithromycin 50 granule for suspension
Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. In addition, it is sometimes used to treat legionellosis, Helicobacter pylori, and lyme disease.
Clarithromycin is available under several brand names, for example Crixan, Claritt, Clarac, Biaxin, Klaricid, Klacid, Klaram, Klabax, Claripen, Clarem, Claridar, Fromilid, Clacid, Clacee, Vikrol, Infex, Clariwin, Resclar, Ranbaxy and Clarihexal.
Clarithromycin was invented by researchers at the Japanese drug company Taisho Pharmaceutical in the 1970s. The product emerged through efforts to develop a version of the antibiotic erythromycin that did not experience acid instability in the digestive tract, causing side effects, such as nausea and stomach ache. Taisho filed for patent protection for the drug around 1980 and subsequently introduced a branded version of its drug, called Clarith, to the Japanese market in 1991. In 1985, Taisho partnered with the American company Abbott Laboratories for the international
Digoxin INN (/dɨˈdʒɒksɨn/) is a purified cardiac glycoside extracted from the foxglove plant, Digitalis lanata. Its corresponding aglycone is digoxigenin, and its acetyl derivative is acetyldigoxin. Digoxin is widely used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication. Digoxin preparations are commonly marketed under the trade names Lanoxin, Digitek, and Lanoxicaps. It is also available as a 0.05 mg/ml oral solution and 0.25 mg/ml or 0.5 mg/ml injectable solution. It is marketed by GlaxoSmithKline and many other pharmaceutic manufacturers.
Today, the most common indications for digoxin are atrial fibrillation and atrial flutter with rapid ventricular response. Beta blockers and/or calcium channel blockers should be the first choice. High ventricular rate leads to insufficient diastolic filling time. By slowing down the conduction in the AV node and increasing its refractory period, digoxin can reduce the ventricular rate. The arrhythmia itself is not affected, but the pumping function of the heart improves owing to improved filling.
The use of digoxin in heart
Linezolid (INN, /lɪˈnɛzəlɪd/ li-NEZ-ə-lid) is a synthetic antibiotic developed by a team at Pharmacia and Upjohn Company. It is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.
A member of the oxazolidinone class of drugs, linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA). The main indications of linezolid are infections of the skin and soft tissues and pneumonia (particularly hospital-acquired pneumonia), although off-label use for a variety of other infections is becoming popular. Linezolid is marketed by Pfizer under the trade names Zyvox (in the United States, United Kingdom, Australia, and several other countries), Zyvoxid (in Europe), and Zyvoxam (in Canada and Mexico). Generics are also available, such as Linospan (in India, by Cipla) and Arlin (in Bangladesh, by Beximco).
Discovered in the 1990s and first approved for use in 2000, linezolid was the first commercially available 1,3-oxazolidinone antibiotic. As of 2009, it is the only marketed
Lovastatin (Merck's Mevacor) is a member of the drug class of statins, used for lowering cholesterol (hypolipidemic agent) in those with hypercholesterolemia and so preventing cardiovascular disease. Lovastatin is a naturally occurring drug found in food such as oyster mushrooms and red yeast rice.
The primary uses of lovastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.
Compactin and lovastatin, natural products with a powerful inhibitory effect on HMG-CoA reductase, were discovered in the 1970s, and taken into clinical development as potential drugs for lowering LDL cholesterol.
In 1982, some small-scale clinical investigations of lovastatin, a polyketide-derived natural product isolated from Aspergillus terreus, in very high-risk patients were undertaken, in which dramatic reductions in LDL cholesterol were observed, with very few adverse effects. After the additional animal safety studies with lovastatin revealed no toxicity of the type thought to be associated with compactin, clinical studies
Rofecoxib ( /ˌrɒfɨˈkɒksɪb/) is a nonsteroidal anti-inflammatory drug (NSAID) that has now been withdrawn over safety concerns. It was marketed by Merck & Co. to treat osteoarthritis, acute pain conditions, and dysmenorrhoea. Rofecoxib was approved by the Food and Drug Administration (FDA) on May 20, 1999, and was marketed under the brand names Vioxx, Ceoxx, and Ceeoxx.
Rofecoxib gained widespread acceptance among physicians treating patients with arthritis and other conditions causing chronic or acute pain. Worldwide, over 80 million people were prescribed rofecoxib at some time.
On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use. Merck withdrew the drug after disclosures that it withheld information about rofecoxib's risks from doctors and patients for over five years, resulting in between 88,000 and 140,000 cases of serious heart disease. Rofecoxib was one of the most widely used drugs ever to be withdrawn from the market. In the year before withdrawal, Merck had sales revenue of US$2.5 billion from Vioxx. By the time it was discontinued in 2004,
Sulfonamide or sulphonamide is the basis of several groups of drugs. The original antibacterial sulfonamides (sometimes called sulfa drugs or sulpha drugs) are synthetic antimicrobial agents that contain the sulfonamide group. Some sulfonamides are also devoid of antibacterial activity, e.g., the anticonvulsant sultiame. The sulfonylureas and thiazide diuretics are newer drug groups based on the antibacterial sulfonamides.
Sulfa allergies are common, hence medications containing sulfonamides are prescribed carefully. It is important to make a distinction between sulfa drugs and other sulfur-containing drugs and additives, such as sulfates and sulfites, which are chemically unrelated to the sulfonamide group, and do not cause the same hypersensitivity reactions seen in the sulfonamides.
In bacteria, antibacterial sulfonamides act as competitive inhibitors of the enzyme dihydropteroate synthetase (DHPS), an enzyme involved in folate synthesis. As such, the microorganism will be "starved" of folate and die.
Humans, in contrast to bacteria, acquire folate (vitamin B9) through the diet.
The sulfonamide chemical moiety is also present in other medications that are not antimicrobials,
Marketed formulations:Chlorpromazine hydrochloride 25 film coated tablet
Chlorpromazine (as chlorpromazine hydrochloride, abbreviated CPZ; marketed in the United States as Thorazine and elsewhere as Largactil) is a dopamine antagonist of the typical antipsychotic class of medications possessing additional antiadrenergic, antiserotonergic, anticholinergic and antihistaminergic properties used to treat schizophrenia. First synthesized on December 11, 1950, chlorpromazine was the first drug developed with specific antipsychotic action, and would serve as the prototype for the phenothiazine class of drugs, which later grew to comprise several other agents. The introduction of chlorpromazine into clinical use has been described as the single greatest advance in psychiatric care, dramatically improving the prognosis of patients in psychiatric hospitals worldwide; the availability of antipsychotic drugs curtailed indiscriminate use of electroconvulsive therapy and psychosurgery, and was one of the driving forces behind the deinstitutionalization movement.
Chlorpromazine works on a variety of receptors in the central nervous system, producing anticholinergic, antidopaminergic, antihistaminic, and weak antiadrenergic effects. Both the clinical indications and
Clonazepam is a benzodiazepine drug having anxiolytic, anticonvulsant, muscle relaxant, and hypnotic properties. It is marketed by Roche under the trade name Klonopin (or Klonapin) in the United States and Rivotril in Argentina, Australia, Brazil, Canada, Costa Rica, Mexico and Europe. Other names such as Ravotril, Rivatril, Rivotril, Clonex, Paxam, Petril or Kriadex are known throughout the rest of the world. Clonazepam has an unusually long elimination half-life of 18–50 hours, making it generally considered to be among the long-acting benzodiazepines. Clonazepam is a chlorinated derivative of nitrazepam and therefore a chloro-nitrobenzodiazepine.
Clonazepam has a slow onset with a peak four hours after ingestion. It has high effectiveness rate and low toxicity in overdose but, as most medications, it may have drawbacks due to adverse reactions including paradoxical effects and drowsiness. Other long-term effects of benzodiazepines include tolerance, benzodiazepine dependence, and benzodiazepine withdrawal syndrome, which occurs in a third of people treated with clonazepam for longer than four weeks. Clonazepam is classified as a high potency benzodiazepine.
The use of clonazepam
Fluoxetine (also known by the tradenames Prozac, Sarafem, Fontex, among others) is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Fluoxetine was first documented in 1974 by scientists from Eli Lilly and Company. It was presented to the U.S. Food and Drug Administration in February 1977, with Eli Lilly receiving final approval to market the drug in December 1987. Fluoxetine went off-patent in August 2001.
Fluoxetine is approved for the treatment of major depression (including pediatric depression), obsessive-compulsive disorder (in both adult and pediatric populations), bulimia nervosa, panic disorder and premenstrual dysphoric disorder. In addition, fluoxetine is used to treat trichotillomania if cognitive behaviour therapy is unsuccessful. In combination with olanzapine it is known as Symbyax.
Despite the availability of newer agents, fluoxetine remains extremely popular. In 2010, over 24.4 million prescriptions for generic formulations of fluoxetine were filled in the United States alone, making it the third most prescribed antidepressant after sertraline (SSRI; became generic in 2006) and citalopram (SSRI; became generic in 2003). In 2011, 6
Haloperidol is a dopamine antagonist of the typical antipsychotic class of medications. It is a butyrophenone derivative and has pharmacological effects similar to the phenothiazines.
Haloperidol is an older antipsychotic used in the treatment of schizophrenia and acute psychotic states and delirium. A long-acting decanoate ester is used as an injection given every four weeks to people with schizophrenia or related illnesses who have poor adherence to medication regimens and suffer frequent relapses of illness, or to overcome the drawbacks inherent to its orally administered counterpart that burst dosage increases risk or intensity of side effects. In some countries, such as the United States of America, injections of antipsychotics such as haloperidol can be ordered by a court at the request of a psychiatrist.
Haloperidol is sold under the tradenames Aloperidin, Bioperidolo, Brotopon, Dozic, Duraperidol (Germany), Einalon S, Eukystol, Haldol (common tradename in the US and UK), Halosten, Keselan, Linton, Peluces, Serenace, Serenase, and Sigaperidol.
Haloperidol was discovered by Paul Janssen. It was developed in 1958 at the Belgian company Janssen Pharmaceutica and submitted to
Streptomycin is an antibiotic drug, the first of a class of drugs called aminoglycosides to be discovered, and was the first antibiotic remedy for tuberculosis. It is derived from the actinobacterium Streptomyces griseus. Streptomycin is a bactericidal antibiotic. Streptomycin cannot be given orally, but must be administered by regular intramuscular injections. An adverse effect of this medicine is ototoxicity, nephrotoxicity, fetal auditory toxicity and neuromuscular paralysis.
Streptomycin is a protein synthesis inhibitor. It binds to the small 16S rRNA of the 30S subunit of the bacterial ribosome, interfering with the binding of formyl-methionyl-tRNA to the 30S subunit. This leads to codon misreading, eventual inhibition of protein synthesis and ultimately death of microbial cells through mechanisms that are still not understood. Speculation on this mechanism indicates that the binding of the molecule to the 30S subunit interferes with 50S subunit association with the mRNA strand. This results in an unstable ribosomal-mRNA complex, leading to a frameshift mutation and defective protein synthesis; leading to cell death. Humans have structurally different ribosomes from bacteria,
Azathioprine (INN, /ˌæzəˈθaɪɵpriːn/, abbreviated AZA) is an immunosuppressive drug used in organ transplantation and autoimmune diseases and belongs to the chemical class of purine analogues. Synthesized originally as a chemotherapy drug and a pro-drug for mercaptopurine in 1957, it has been widely used as a immunosuppressant for more than 50 years.
It is believed that azathioprine acts as a pro-drug for mercaptopurine, inhibiting an enzyme that is required for the synthesis of DNA. Thus it most strongly affects proliferating cells, such as the T cells and B cells of the immune system. Despite more than 50 years of widespread clinical use of azathioprine, the understanding of its mechanism of action is still incomplete.
The main adverse effect of azathioprine is bone marrow suppression, and people with a genetic deficiency of the enzyme thiopurine S-methyltransferase this can be serious. It is also listed by the International Agency for Research on Cancer as a Group 1 carcinogen (carcinogenic to humans).
Azathioprine is produced by a number of manufacturers under different brand names (Azasan by Salix in the U.S., Imuran by GlaxoSmithKline in Canada, the U.S., Australia, Ireland
Duloxetine (sold under the brand names Cymbalta, Ariclaim, Xeristar, Yentreve, Duzela) is a serotonin-norepinephrine reuptake inhibitor (SNRI) manufactured and marketed by Eli Lilly. It is effective for major depressive disorder and generalized anxiety disorder (GAD). Duloxetine failed the US approval for stress urinary incontinence amidst concerns over liver toxicity and suicidal events; however, it was approved for this indication in Europe, where it is recommended as an add-on medication in stress urinary incontinence instead of surgery. It can also relieve the symptoms of painful peripheral neuropathy, particularly diabetic neuropathy, and it is used to control the symptoms of fibromyalgia.
The main uses of duloxetine are in major depressive disorder, general anxiety disorder, stress urinary incontinence, painful peripheral neuropathy, fibromyalgia, and chronic musculoskeletal pain associated with osteoarthritis and chronic lower back pain. It is being studied for various other indications.
Duloxetine has demonstrated efficacy for the treatment of major depressive disorder. Recently, duloxetine was shown to be effective in elderly with recurrent major depressive disorder where
Marketed formulations:Oxcarbazepine 300 film coated tablet
Oxcarbazepine (ox-kar-BAY-zih-peen) is an anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. It is also used to treat anxiety and mood disorders, and benign motor tics. Oxcarbazepine is marketed as Trileptal by Novartis and available in some countries as a generic drug.
In treatment of epilepsy, oxcarbazepine has recently been found to be associated with a greater enhancement in mood and reduction in anxiety symptoms than other drugs employed to treat epilepsy.
It also appears to be effective in approximately half of patients with bipolar disorder and is well tolerated.
Oxcarbazepine is a structural derivative of carbamazepine, with a ketone in place of the carbon-carbon double bond on the dibenzazepine ring. This difference helps reduce the impact on the liver of metabolizing the drug, and also prevents the serious forms of anemia or agranulocytosis occasionally associated with carbamazepine. Aside from this reduction in side effects, it is thought to have the same mechanism as carbamazepine - sodium channel inhibition (presumed to be the main mechanism of action) - and is generally used to treat the same conditions.
Oxcarbazepine is a prodrug
Physostigmine (also known as eserine from éséré, West African name for the Calabar bean) is a parasympathomimetic alkaloid, specifically, a reversible cholinesterase inhibitor. It occurs naturally in the Calabar bean.
The chemical was synthesized for the first time in 1935 by the chemists Percy Lavon Julian and Josef Pikl. It is available in the U.S. under the trade names Antilirium, Eserine Salicylate, Isopto Eserine, and Eserine Sulfate.
Physostigmine acts by interfering with the metabolism of acetylcholine. It is a covalent (reversible - bond hydrolyzed and released) inhibitor of acetylcholinesterase, the enzyme responsible for the breakdown of acetylcholine in the synaptic cleft of the neuromuscular junction. It indirectly stimulates both nicotinic and muscarinic receptors.
Physostigmine has two chiral carbon atoms. Therefore, attention needs to be paid to the synthesis of the correct diastereomers. There are 71 syntheses of physostigmine; 33 yield racemic mixtures, 38 yield a pure chiral product. The first total synthesis of physostigmine was achieved by Julian and Piki in 1935. It is summarized in Figure 3. The main goal of Julian’s physostigmine synthesis was to get the
Marketed formulations:Ribavirin 200 film coated tablet
Ribavirin (brand names: Copegus, Rebetol, Ribasphere, Vilona, and Virazole) is an anti-viral drug indicated for severe RSV infection (individually), hepatitis C infection (used in conjunction with peginterferon alfa-2b or peginterferon alfa-2a), and other viral infections. Ribavirin is a prodrug, which when metabolized resembles purine RNA nucleotides. In this form it interferes with RNA metabolism required for viral replication. How it exactly affects viral replication is unknown; many mechanisms have been proposed for this (see Mechanisms of Action, below) but none of these has been proven to date. Multiple mechanisms may be responsible for its actions.
The primary observed serious adverse side effect of ribavirin is hemolytic anemia, which may worsen preexisting cardiac disease. The mechanism for this effect is due to ribavarin's buildup inside erythrocytes. Oxidative damage to erythrocyte cell membrane is usually inhibited by glutathione; however, with reduced ATP levels caused by ribavirin, glutathione levels are impaired, permitting oxidative erythrocyte cell lysis. The gradual loss of erythrocytes leads to anemia. The anemia is dose-dependent and may sometimes be compensated
Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine and thebaine. It is an orally active narcotic analgesic and antitussive. It is available in tablet, capsule, and syrup form.
Hydrocodone is often compounded with other generally less effective non-opioid compounds such as paracetamol (also known as acetaminophen) or ibuprofen, both often added to discourage recreational use (as paracetamol can cause potentially fatal liver toxicity at high doses), and to provide a possible synergy of analgesic effects between hydrocodone and the non-opioid compounds present. The particular niche in which hydrocodone is most commonly used is as an intermediate centrally acting analgesic. Abrupt discontinuation of hydrocodone may result in withdrawal symptoms.
Because of concerns about liver damage from protracted use of paracetamol at high doses, four pharmaceutical companies (Purdue Pharma, Cephalon, Zogenix, and Egalet) are developing extended-release capsules and other forms of hydrocodone by itself.
Hydrocodone was first synthesized in Germany in 1920 by Carl Mannich and Helene Löwenheim. It was approved by the Food and Drug
Marketed formulations:Telithromycin 300 film coated tablet
Telithromycin is the first ketolide antibiotic to enter clinical use and is sold under the brand name of Ketek. It is used to treat community acquired pneumonia of mild to moderate severity. After significant controversy regarding safety and research fraud, the US Food and Drug Administration sharply curtailed the approved uses of the drug in 2007.
Telithromycin is a semi-synthetic erythromycin derivative. It is created by substituting a ketogroup for the cladinose sugar and adding a carbamate ring in the lactone ring. An alkyl-aryl moiety is attached to this carbamate ring. Furthermore, the carbon at position 6 has been methylated, as is the case in clarithromycin, to achieve better acid-stability.
French pharmaceutical company Hoechst Marion Roussel (later Sanofi-Aventis) began phase II/III clinical trials of telithromycin (HMR-3647) in 1998. Telithromycin was approved by the European Commission in July 2001 and subsequently went on sale in October 2001. In the US, telithromycin received U.S. Food and Drug Administration (FDA) approval on April 1, 2004 .
FDA staffers publicly complained that safety problems and data integrity issues were ignored prior to approval, and the House
Theobromine (theobromide), also known as xantheose, is a bitter alkaloid of the cacao plant, with the chemical formula C7H8N4O2. It is found in chocolate, as well as in a number of other foods, including the leaves of the tea plant, and the kola (or cola) nut. It is in the methylxanthine class of chemical compounds, which also includes the similar compounds theophylline and caffeine. (In caffeine, the only difference is that the NH group of theobromine is an N-CH3 group.) Despite its name, the compound contains no bromine—theobromine is derived from Theobroma, the name of the genus of the cacao tree, (which itself is made up of the Greek roots theo ("God") and brosi ("food"), meaning "food of the gods") with the suffix -ine given to alkaloids and other basic nitrogen-containing compounds.
Theobromine is a slightly water-soluble (330 mg/L), crystalline, bitter powder; the colour has been listed as either white or colourless. It has a similar, but lesser, effect than caffeine in the human nervous system, making it a lesser homologue. Theobromine is an isomer of theophylline, as well as paraxanthine. Theobromine is categorized as a dimethyl xanthine.
Theobromine was first discovered
Zinc pyrithione is a coordination complex of zinc. This colourless solid is used as an antifungal and antibacterial agent.
The pyrithione ligands, which are formally monoanions, are chelated to Zn via oxygen and sulfur centers. In the crystalline state, zinc pyrithione exists as a centrosymmetric dimer (see figure), where each zinc is bonded to two sulfur and three oxygen centers. In solution, however, the dimers dissociate via scission of one Zn-O bond.
This compound was first described in the 1930s.
Pyrithione is the conjugate base derived from 2-mercaptopyridine-N-oxide (CAS# 1121-31-9), a derivative of pyridine-N-oxide.
Zinc pyrithione is best known for its use in treating dandruff and seborrhoeic dermatitis. It also has antibacterial properties and is effective against many pathogens from the Streptococcus and Staphylococcus genera. Its other medical applications include treatments of psoriasis, eczema, ringworm, fungus, athletes foot, dry skin, atopic dermatitis, tinea, and vitiligo.
Due to its low solubility in water (8 ppm at neutral pH), zinc pyrithione is suitable for use in outdoor paints and other products that provide protection against mildew and algae. It is an
Marketed formulations:Basiliximab 4 powder for injectable solution
Basiliximab (trade name Simulect) is a chimeric mouse-human monoclonal antibody to the α chain (CD25) of the IL-2 receptor of T cells. It is used to prevent rejection in organ transplantation, especially in kidney transplants. It is a Novartis Pharmaceuticals product and was approved by the Food and Drug Administration (FDA) in 1998.
It is a chimeric CD25 monoclonal antibody of the IgG1 isotype. It acts as an antagonist at the interleukin-2(IL-2) binding site of the p55 subunit (Tac antigen) of the high affinity IL-2 receptor (CD25) on the surface of the activated T lymphocytes.
Minimum serum level should be 0.2 ug/ml(ELISA) Dose is 20 mg two times 4 days apart generally in an adult. It is given in two doses, the first within 2 hours of the start of the transplant operation and the second 4 days after the transplant. These saturate the receptors and prevent T cells from replication and also from activating the B cells, which are responsible for the production of antibodies, which would bind to the transplanted organ and stimulate an immune response against the transplant.
Like the similar drug daclizumab, basiliximab reduces the incidence and severity of acute rejection in kidney
Mycophenolic acid INN ( /ˌmaɪkoʊfɨˈnɒlɪk/) or mycophenolate is an immunosuppressant drug used to prevent rejection in organ transplantation. It inhibits an enzyme needed for the growth of T cells and B cells. It was initially marketed as the prodrug mycophenolate mofetil (MMF) to improve oral bioavailability. More recently, the salt mycophenolate sodium has also been introduced. Mycophenolic acid is commonly marketed under the trade names CellCept (mycophenolate mofetil; Roche) and Myfortic (mycophenolate sodium; Novartis).
In general, mycophenolate is used for the prevention of organ transplant rejection. Mycophenolate mofetil is indicated for the prevention of organ transplant rejection in adults and renal transplant rejection in children over 2 years; whereas mycophenolate sodium is indicated for the prevention of renal transplant rejection in adults. Mycophenolate sodium has also been used for the prevention of rejection in liver, heart, and/or lung transplants in children older than two years.
An immunosuppressant that has drastically decreased the incidence of acute rejection in solid transplant recipients, mycophenolate is increasingly utilized as a steroid sparing treatment
Tacrine is a centrally acting anticholinesterase and indirect cholinergic agonist (parasympathomimetic). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Tacrine was first synthesised by Adrien Albert at the University of Sydney. It also acts as a histamine N-methyltransferase inhibitor.
Tacrine was the prototypical cholinesterase inhibitor for the treatment of Alzheimer's disease. Studies found that it may have a small beneficial effect on cognition and other clinical measures, though study data was limited and the clinical relevance of these findings was unclear.
Newer cholinesterase inhibitors, such as donepezil, are now preferred over tacrine.
As stated above, overdosage of tacrine may give rise to severe side effects such as nausea, vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Tertiary anticholinergics, such as atropine, may be antidotes for overdose.
Major form of metabolism is in the liver via hydroxylation of benzylic carbon by Cytochrome P450 (CYP450). This forms the major metabolite 1-hydroxy-tacrine (velnacrine) which is still
Marketed formulations:Amitriptyline hydrochloride 150 film coated tablet
Amitriptyline (Tryptomer, Elavil, Tryptizol, Laroxyl, Saroten, Sarotex, Lentizol, Endep) is a tricyclic antidepressant (TCA). It is the most widely used TCA and has at least equal efficacy against depression as the newer class of SSRIs according to a study from early 2001. As well as reducing depressive symptoms, these types of tricyclics also ease migraines, tension headaches, anxiety attacks and some schizophrenic symptoms. It is also known to reduce aggression and violent behaviour.
Amitriptyline is used for a number of medical conditions including: depressive disorders, anxiety disorders, attention deficit hyperactivity disorder, migraine prophylaxis, eating disorders, bipolar disorder, post-herpetic neuralgia, and insomnia.
Amitriptyline is used in ankylosing spondylitis for pain relief. It is also used as a preventive for patients with recurring biliary dyskinesia (sphincter of Oddi dysfunction).
Amitriptyline is also used in the treatment of nocturnal enuresis (bedwetting) in children.
Amitriptyline may be prescribed for other conditions such as cyclic vomiting syndrome post-traumatic stress disorder (PTSD), chronic pain, tinnitus, chronic cough, carpal tunnel syndrome
Marketed formulations:Topiramate 25 film coated tablet
Topiramate (brand name Topamax) is an anticonvulsant (antiepilepsy) drug. It was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceutical. Topiramate was first approved by the US FDA in 1996. Generic versions are available in Canada and these were approved by the Food and Drug Administration (FDA) in September 2006. Mylan Pharmaceuticals was recently granted final approval for generic topiramate 25, 100, and 200 mg tablets and sprinkle capsules by the FDA for sale in the United States. 50 mg tablets were granted tentative approval. The last patent for topiramate in the U.S. was for pediatric use; this patent expired on February 28, 2009.
Topiramate is used to treat epilepsy in children and adults, and it was originally used as an anticonvulsant. In children, it is indicated for the treatment of Lennox-Gastaut syndrome, a disorder that causes seizures and developmental delay. It is also Food and Drug Administration (FDA) approved for, and most frequently prescribed for, the prevention of
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testicles of males and the ovaries of females, although small amounts are also secreted by the adrenal glands. It is the principal male sex hormone and an anabolic steroid.
In men, testosterone plays a key role in the development of male reproductive tissues such as the testis and prostate as well as promoting secondary sexual characteristics such as increased muscle, bone mass, and the growth of body hair. In addition, testosterone is essential for health and well-being as well as the prevention of osteoporosis.
On average, in adult human males, the plasma concentration of testosterone is about 7-8 times as great as the concentration in adult human females' plasma, but as the metabolic consumption of testosterone in males is greater, the daily production is about 20 times greater in men. Females also are more sensitive to the hormone. Testosterone is observed in most vertebrates. Fish make a slightly different form called 11-ketotestosterone. Its counterpart in insects is ecdysone. These ubiquitous steroids
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. When taken orally, it is 26.6 times more potent than the naturally occurring hormone cortisol and 6.6 times more potent than prednisone.
Dexamethasone is used to treat many inflammatory and autoimmune conditions, such as rheumatoid arthritis and bronchospasm. Idiopathic thrombocytopenic purpura, decreased numbers of platelets due to an immune problem, responds to 40 mg daily for four days; it may be administered in 14-day cycles. It is unclear whether dexamethasone in this condition is significantly better than other glucocorticoids.
It is also given in small amounts (usually five or six tablets) before and/or after some forms of dental surgery, such as the extraction of the wisdom teeth, an operation which often leaves the patient with puffy, swollen cheeks.
It is injected into the heel when treating plantar fasciitis, sometimes in conjunction with triamcinolone acetonide.
It is useful to counteract allergic anaphylactic shock, if given in high doses.
It is present in certain eye drops – particularly after eye surgery– and as a nasal spray
Marketed formulations:Frovatriptan succinate 2.5 film coated tablet
Frovatriptan (trade name Frova) is a triptan drug developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual migraine. The product is licensed to Endo Pharmaceuticals in North America and Menarini in Europe.
Frovatriptan inhibits excessive dilation of arteries that supply blood to the head. It is available as 2.5 mg tablets.
Frovatriptan has mean terminal elimination half-life of approximately 26 hours, which is substantially longer than other triptans.
Frovatriptan is a 5HT receptor agonist, with high affinity for the 5-HT1B/1D receptors. It has no significant effects on the GABAA mediated channel activity and benzodiazepine binding sites.
Serious but rare cardiac events have been reported in patients with risk factors predictive of CAD. These include: coronary artery vasospasm, transient myocardial ischemia, myocardial infarction, ventricular tachycardia and ventricular fibrillation.
Frovatriptan should not be given to patients with:
Frovatriptan is available only by prescription in the United States, and Canada where a secondary New Drug Approval (sNDA) was filed in July 2006, and which is currently pending. The FDA anticipates
Ibuprofen (INN) ( /ˈaɪbjuːproʊfɛn/ or /aɪbjuːˈproʊfən/ EYE-bew-PROH-fən; from the nomenclature iso-butyl-propanoic-phenolic acid) is a nonsteroidal anti-inflammatory drug (NSAID) used for relief of symptoms of arthritis, fever, as an analgesic (pain reliever), especially where there is an inflammatory component, and dysmenorrhea.
Ibuprofen is known to have an antiplatelet effect, though it is relatively mild and somewhat short-lived when compared with aspirin or other better-known antiplatelet drugs. In general, ibuprofen also acts as a vasoconstrictor, having been shown to constrict coronary arteries and some other blood vessels mainly because it inhibits the vasodilating prostacyclin produced by cyclooxygenase 2 enzymes. Ibuprofen is a 'core' medicine in the World Health Organization's WHO Model List of Essential Medicines, which is a list of minimum medical needs for a basic healthcare system.
Ibuprofen was derived from propanoic acid by the research arm of Boots Group during the 1960s. It was discovered by Andrew RM Dunlop, with colleagues Stewart Adams, John Nicholson, Vonleigh Simmons, Jeff Wilson and Colin Burrows, and was patented in 1961. Originally marketed as Brufen,
Lysergic acid diethylamide, abbreviated LSD or LSD-25, also known as lysergide (INN) and colloquially as acid, is a semisynthetic psychedelic drug of the ergoline family, well known for its psychological effects which can include altered thinking processes, closed and open eye visuals, synesthesia, an altered sense of time and spiritual experiences, as well as for its key role in 1960s counterculture. It is used mainly as an entheogen, recreational drug, and as an agent in psychedelic therapy. LSD is non-addictive, is not known to cause brain damage, and has extremely low toxicity relative to dose, although in rare cases adverse psychiatric reactions such as anxiety or delusions are possible.
LSD was first synthesized by Albert Hofmann in 1938 from ergotamine, a chemical derived by Arthur Stoll from ergot, a grain fungus that typically grows on rye. The short form "LSD" comes from its early code name LSD-25, which is an abbreviation for the German "Lysergsäure-diethylamid" followed by a sequential number. LSD is sensitive to oxygen, ultraviolet light, and chlorine, especially in solution, though its potency may last for years if it is stored away from light and moisture at low
Methadone (also known as Symoron, Dolophine, Amidone, Methadose, Physeptone, Heptadon and many other names) is a synthetic opioid, used medically as an analgesic and a maintenance anti-addictive and reductive preparation for use by patients with opioid dependency. It was developed in Germany in 1937, mainly because Germany required a reliable source of opiates. Because it is an acyclic analog of morphine or heroin, methadone acts on the same opioid receptors as these drugs, and thus has many of the same effects. Methadone is also used in managing severe chronic pain, owing to its long duration of action, extremely powerful effects, and very low cost. Methadone was introduced into the United States in 1947 by Eli Lilly and Company.
Methadone is mainly used in the treatment of opioid dependence. It has cross-tolerance with other opioids including heroin and morphine, offering very similar effects and a long duration of effect. Oral doses of methadone can stabilise patients by mitigating opioid withdrawal syndrome. Higher doses of methadone can block the euphoric effects of heroin, morphine, and similar drugs. As a result, properly dosed methadone patients can reduce or stop
Methamphetamine (USAN) ( /ˌmɛθæmˈfɛtəmiːn/), also known as metamfetamine (INN), meth, ice, speed, crystal, glass, Pro, tik, N-methylamphetamine, methylamphetamine, and desoxyephedrine, is a psychostimulant of the phenethylamine and amphetamine class of psychoactive drugs.
Methamphetamine occurs in two enantiomers, dextrorotary and levorotary; dextromethamphetamine possesses the well-known psychostimulant effects of the drug, while levomethamphetamine is CNS-inactive. Although rarely prescribed, dextromethamphetamine is FDA approved for the treatment of ADHD and obesity under the trade name Desoxyn, while levomethamphetamine is a non-prescription over-the-counter nasal decongestant.
Illicitly, methamphetamine may be sold either as pure dextromethamphetamine or in a racemic mixture. Both dextromethamphetamine and racemic methamphetamine are Schedule II controlled substances in the United States and similarly the production, distribution, sale, and possession of methamphetamine is restricted or illegal in many jurisdictions. Internationally, methamphetamine has been placed in Schedule II of the United Nations Convention on Psychotropic Substances treaty.
Orlistat (marketed as a prescription under the trade name Xenical by Roche in most countries, or over-the-counter as Alli by GlaxoSmithKline in the United Kingdom and the United States), also known as tetrahydrolipstatin, is a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. It is intended for use in conjunction with a physician-supervised reduced-calorie diet. Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. However, due to simplicity and stability, orlistat rather than lipstatin was developed into an anti-obesity drug.
The effectiveness of orlistat in promoting weight loss is definite, though modest. Pooled data from clinical trials suggest that people given orlistat in addition to lifestyle modifications, such as diet and exercise, lose about 2–3 kilograms (4.4–6.6 lb) more than those not taking the drug over the course of a year. Orlistat also modestly reduces blood pressure, and appears to prevent the onset of type 2 diabetes, whether due to weight loss itself or to other effects;
Phenytoin sodium (/fəˈnɪtoʊɨn/) is a commonly used antiepileptic. Phenytoin acts to suppress the abnormal brain activity seen in seizure by reducing electrical conductance among brain cells by stabilizing the inactive state of voltage-gated sodium channels. Aside from seizures, it is an option in the treatment of trigeminal neuralgia in the event that carbamazepine or other first-line treatment seems inappropriate.
It is sometimes considered a class 1b antiarrhythmic.
Phenytoin sodium has been marketed as Phenytek by Mylan Laboratories, previously Bertek Pharmaceuticals, and Dilantin; Australia also Dilantin Kapseals and Dilantin Infatabs in the USA, Eptoin by Abbott Group in India and as Epanutin in the UK and Israel, by Parke-Davis, now part of Pfizer. In the USSR and post-USSR countries, it was/is marketed as Дифенин (Diphenin, Dipheninum).
Phenytoin (diphenylhydantoin) was first synthesized by German chemist Heinrich Biltz in 1908. Biltz sold his discovery to Parke-Davis, which did not find an immediate use for it. In 1938, outside scientists including H. Houston Merritt and Tracy Putnam discovered phenytoin's usefulness for controlling seizures, without the sedative effects
This article is about the antibiotic Roxithromycin. For the Norwegian company see Roxar AS.
Roxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin, containing the same 14-membered lactone ring. However, an N-oxime side chain is attached to the lactone ring. It is also currently undergoing clinical trials for the treatment of male-pattern hair loss.
Roxithromycin is available under several brandnames, for example, Xthrocin, Roxl-150, Roxo, Surlid, Rulide, Biaxsig, Roxar, Roximycin, Roxomycin, Rulid, Tirabicin and Coroxin. Roxithromycin is not available in the United States. Roxithromycin has also been tested to possess antimalarial activity.
German pharmaceutical company Hoechst Uclaf brought out roxithromycin in 1987.
Roxithromycin is commonly available as tablets or oral suspension.
Roxithromycin prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum as erythromycin, but is more
Marketed formulations:Infliximab 10 lyophilized powder for injectable solution
Infliximab (INN; trade name Remicade) is a monoclonal antibody against tumour necrosis factor alpha (TNF-α) used to treat autoimmune diseases. Remicade is marketed by Janssen Biotech, Inc. (formerly Centocor Biotech, Inc.) in the USA, Mitsubishi Tanabe Pharma in Japan, Xian Janssen in China, and Schering-Plough (now part of Merck & Co) elsewhere.
Infliximab was approved by the U.S. Food and Drug Administration (FDA) for the treatment of psoriasis, Crohn's disease, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis, and ulcerative colitis. Infliximab won its initial approval by the FDA for the treatment of Crohn's disease in August 1998.
Infliximab works by binding to tumour necrosis factor alpha. TNF-α is a chemical messenger (cytokine) and a key part of the autoimmune reaction. Originally, the action of infliximab (in rheumatoid arthritis) was assumed to work by blocking the action of TNF-α by preventing it from binding to its receptor in the cell. This still seems to be true. However, another TNF-α-neutralizing medication, etanercept (Enbrel), is worse than a placebo in Crohn's disease, so TNF-α-neutralisation is not responsible for its powerful action in the
Atropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects. It is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5. It is classified as an anticholinergic drug (parasympatholytic). The species name "belladonna" ("beautiful woman" in Italian) comes from the original use of deadly nightshade as a way of dilating women's pupils to make them beautiful. Both atropine and the genus name for deadly nightshade derive from Atropos, one of the three Fates who, according to Greek mythology, chose how a person was to die. Atropine is a core medicine in the World Health Organization's "Essential Drugs List", which is a list of minimum medical needs for a basic health care system.
Working as a nonselective muscarinic acetylcholinergic antagonist, atropine increases firing of the sinoatrial node (SA) and conduction through the atrioventricular node (AV) of the heart, opposes the actions of the vagus
Carbachol (Carbastat, Carboptic, Isopto Carbachol, Miostat), also known as carbamylcholine, is a cholinomimetic drug that binds and activates the acetylcholine receptor. Thus it is classified as a cholinergic agonist. It is primarily used for various ophthalmic purposes, such as for treating glaucoma, or for use during ophthalmic surgery. It is generally administered as an ophthalmic solution (i.e. eyedrops).
Carbachol is a choline carbamate and a positively charged quaternary ammonium compound. It is not well absorbed in the gastro-intestinal tract and does not cross the blood–brain barrier. It is usually administered topical ocular or through intraocular injection. Carbachol is not easily metabolized by cholinesterase, it has a two to 5 minute onset of action and its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration. Since carbachol is poorly absorbed through topical administration, benzalkonium chloride is mixed in to promote absorption.
Carbachol is a parasympathomimetic that stimulates both muscarinic and nicotinic receptors. In topical ocular and intraocular administration its principal effects are miosis and increased
Marketed formulations:Naproxen sodium 220 extended release film coated tablet
Naproxen sodium (INN) ( /nəˈprɒksən/) is a nonsteroidal anti-inflammatory drug (NSAID). Naproxen and naproxen sodium are marketed under various trade names, including: Aleve, Anaprox, Antalgin, Feminax Ultra, Flanax, Inza, Midol Extended Relief, Nalgesin, Naposin, Naprelan, Naprogesic, Naprosyn, Narocin, Proxen, Synflex and Xenobid.
Naproxen was originally marketed as the prescription drug Naprosyn by Syntex in 1976, and naproxen sodium was first marketed under the trade name Anaprox in 1980. It remains a prescription-only drug in much of the world. In the United States, the Food and Drug Administration (FDA) approved its use as an over-the-counter (OTC) drug in 1994; OTC preparations in the U.S. are mainly marketed by Bayer HealthCare under the trade name Aleve and generic store brand formulations. In Australia, packets of 275-mg tablets of naproxen sodium are Schedule 2 pharmacy medicines, with a maximum daily dose of five tablets or 1375 mg. In the United Kingdom, 250-mg tablets of naproxen were approved for OTC sale under the brand name Feminax Ultra in 2008, for the treatment of primary dysmenorrhoea in women aged 15 to 50. Aleve became available over-the-counter in most
Omeprazole (INN) ( /oʊˈmɛprəzoʊl/) (Prilosec and generics) is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux (LPR) and Zollinger–Ellison syndrome. Omeprazole is one of the most widely prescribed drugs internationally and is available over the counter in some countries.
Used to treat GERD (gastroesophageal reflux disease), gastric and duodenum ulceration and gastritis.
Omeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole in penicillin-hypersensitive patients) in the 7–14 day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is the causative factor in the majority of peptic ulcers.
Omeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, omeprazole blocks the final step in acid production, thus reducing gastric acidity.
Some of the most frequent side effects of omeprazole (experienced by over 1% of those taking the drug) are headache, diarrhea, abdominal pain, nausea,
Tretinoin is the acid form of vitamin A and is also known as all-trans retinoic acid or ATRA. It is a drug commonly used to treat acne vulgaris and keratosis pilaris. It is available as a cream or gel (brand names Aberela, Airol, Renova, Atralin, Retin-A, Avita, Retacnyl, Refissa, or Stieva-A). It is also used to treat acute promyelocytic leukemia (APL), and is sold for this indication by Roche under the brand name Vesanoid. It is also available as a generic.
Tretinoin is most commonly used as a form of acne treatment. It was the first retinoid developed for this type of topical use. Tretinoin is the best studied retinoid in the treatment of photoaging. It is used by some as a hair loss treatment and also a component of many commercial products that are advertised as being able to slow skin aging or remove wrinkles. Topical tretinoin is also used to treat and reduce the appearance of stretch marks by increasing collagen production in the dermis.
Tretinoin, marketed as Vesanoid, is used to treat at least one form of cancer (acute promyelocytic leukemia (APL), also called acute myeloid leukemia subtype M3), usually together with other drugs, by causing the immature blood cells to
Itraconazole (R51211), invented in 1984, is a triazole antifungal agent prescribed to patients with fungal infections. The drug may be given orally or intravenously.
Itraconazole has a broader spectrum of activity than fluconazole (but not as broad as voriconazole or posaconazole). In particular, it is active against Aspergillus, which fluconazole is not. It is also licensed for use in blastomycosis, histoplasmosis, and onychomycosis. Itraconazole is over 99% protein-bound and has virtually no penetration into cerebrospinal fluid. Therefore, it should never be used to treat meningitis or other central nervous system infections. According to the Johns Hopkins Abx Guide, it has "negligible CSF penetration, however treatment has been successful for cryptococcal and coccidioidal meningitis".
It is also prescribed for systemic infections, such as aspergillosis, candidiasis, and cryptococcosis, where other antifungal drugs are inappropriate or ineffective. Itraconazole is currently being explored as an anticancer agent for patients with basal cell carcinoma, non-small cell lung cancer, and prostate cancer.
The mechanism of action of itraconazole is the same as the other azole
Ketamine is a drug used in human and veterinary medicine. Ketamine is primarily used for the induction and maintenance of general anesthesia, usually in combination with a sedative. Other uses include sedation in intensive care, analgesia (particularly in emergency medicine), and treatment of bronchospasm. Ketamine has a wide range of effects in humans, including analgesia, anesthesia, hallucinations, elevated blood pressure, and bronchodilation.
It has been shown to be effective in treating depression in patients with bipolar disorder who have not responded to anti-depressants. In persons with major depressive disorder, it produces a rapid antidepressant effect, acting within two hours as opposed to the several weeks taken by typical antidepressants to work. It is also a popular anesthetic in veterinary medicine.
Its hydrochloride salt is sold as Ketanest, Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist. At high, fully anesthetic level doses, ketamine has also been found to bind to opioid μ receptors type 2 in cultured human neuroblastoma cells – however, without agonist activity – and to sigma receptors in rats. Also, ketamine
Oxytocin (Oxt) ( /ˌɒksɨˈtoʊsɪn/) is a mammalian hormone that acts primarily as a neuromodulator in the brain.
Oxytocin is best known for its roles in sexual reproduction, in particular during and after childbirth. It is released in large amounts after distension of the cervix and uterus during labor, facilitating birth, and after stimulation of the nipples, facilitating breastfeeding.
Recent studies have begun to investigate oxytocin's role in various behaviors, including orgasm, social recognition, pair bonding, anxiety, and maternal behaviors. For this reason, it is sometimes referred to as the "love hormone". The inability to secrete oxytocin and feel empathy is linked to sociopathy, psychopathy, narcissism, and general manipulativeness. However, there is some evidence that oxytocin promotes 'tribal' behaviour, combining trust and empathy with the in-group with suspicion and rejection of outsiders.
The word oxytocin was derived from the Greek ὼκυτοκίνη, ōkytokínē, meaning “quick birth”, after its uterine-contracting properties were discovered by British pharmacologist Sir Henry Hallett Dale in 1906. The milk ejection property of oxytocin was described by Ott and Scott in 1910
Marketed formulations:Paroxetine hydrochloride hemihydrate 40 film coated tablet
Paroxetine (also known by the trade names Aropax, Paxil, Pexeva, Seroxat, Sereupin) is an antidepressant drug of the SSRI type. Paroxetine is used to treat major depression, obsessive-compulsive disorder, panic disorder, social anxiety, posttraumatic stress disorder and generalized anxiety disorder in adult outpatients.
Marketing of the drug began in 1992 by the pharmaceutical company SmithKline Beecham, now GlaxoSmithKline. Generic formulations have been available since 2003 when the patent expired.
In adults, the efficacy of paroxetine for depression is comparable to that of older tricyclic antidepressants, with fewer side effects and lower toxicity. Differences with newer antidepressants are subtler and mostly confined to side effects. It shares the common side effects and contraindications of other SSRIs, with high rates of nausea, somnolence, and sexual side effects. Paroxetine is associated with clinically significant weight gain. Pediatric trials of paroxetine for depression did not demonstrate statistical efficacy better than placebo.
Discontinuing paroxetine is associated with a high risk of withdrawal syndrome. Due to the increased risk of birth defects, pregnant women or
Marketed formulations:Chloramphenicol sodium succinate 1 lyophilized powder for injectable solution
Chloramphenicol (INN) is a bacteriostatic antimicrobial that became available in 1949. It is considered a prototypical broad-spectrum antibiotic, alongside the tetracyclines, and as it is both cheap and easy to manufacture it is frequently an antibiotic of choice in the Third World.
Chloramphenicol, also known as chlornitromycin, is effective against a wide variety of Gram-positive and Gram-negative bacteria, including most anaerobic organisms. Due to resistance and safety concerns, it is no longer a first-line agent for any infection in developed nations, although it is sometimes used topically for eye infections. Nevertheless, the global problem of advancing bacterial resistance to newer drugs has led to renewed interest in its use. In low-income countries, chloramphenicol is still widely used because it is inexpensive and readily available.
The most serious adverse effect associated with chloramphenicol treatment is bone marrow toxicity, which may occur in two distinct forms: bone marrow suppression, which is a direct toxic effect of the drug and is usually reversible, and aplastic anemia, which is idiosyncratic (rare, unpredictable, and unrelated to dose) and in general fatal.
Diazepam ( /daɪˈæzɨpæm/), first marketed as Valium ( /ˈvæliəm/) by Hoffmann-La Roche, is a benzodiazepine drug. Diazepam is also marketed in Australia as Antenex. It is commonly used for treating anxiety, insomnia, seizures including status epilepticus, muscle spasms (such as in cases of tetanus), restless legs syndrome, alcohol withdrawal, benzodiazepine withdrawal and Ménière's disease. It may also be used before certain medical procedures (such as endoscopies) to reduce tension and anxiety, and in some surgical procedures to induce amnesia. It possesses anxiolytic, anticonvulsant, hypnotic, sedative, skeletal muscle relaxant, and amnestic properties. The pharmacological action of diazepam enhances the effect of the neurotransmitter GABA by binding to the benzodiazepine site on the GABAA receptor (via the constituent chlorine atom) leading to central nervous system depression.
Adverse effects of diazepam include anterograde amnesia (especially at higher doses) and sedation, as well as paradoxical effects such as excitement, rage or worsening of seizures in epileptics. Benzodiazepines also can cause or worsen depression. Long-term effects of benzodiazepines such as diazepam
Methcathinone (α-methylamino-propiophenone or ephedrone) is a psychoactive stimulant, sometimes used as a recreational drug and considered addictive. It is usually snorted, but can be smoked, injected, or taken orally. Methcathinone is currently a DEA Schedule I controlled substance in the United States.
The C=O bond at the Rβ-position (directly right of the benzene ring) is slightly polar, and as a result the drug does not cross the lipid blood–brain barrier quite as well as amphetamine. Nevertheless, it is a potent CNS stimulant and dopamine reuptake inhibitor. Chronic high dosage use may result in acute mental confusion ranging from mild paranoia to psychosis. These symptoms typically disappear quickly if use is stopped.
Unlike methamphetamine, methcathinone is not legal under any circumstances in the US due to its classification as a Schedule I substance. Conversely, methamphetamine has certain approved medical uses such as treatment of morbid obesity, narcolepsy and ADHD.
Methcathinone was first synthesized in 1928 in the United States and finally patented by Parke Davis in 1957. It was used in the Soviet Union during the 1930s and 1940s as an anti-depressant (under the name
Perphenazine is a typical antipsychotic drug. Chemically, it is classified as a piperazinyl phenothiazine. It has been in clinical use for decades.
Perphenazine is roughly five times as potent as chlorpromazine; thus perphenazine is considered a medium-potency antipsychotic.
It has an oral bioavailability of approximately 40% and a half-life of 8 to 12 hours (up to 20 hours), and is usually given in 2 or 3 divided doses each day. It is possible to give two-thirds of the daily dose at bedtime and one-third during breakfast to maximize hypnotic activity during the night and to minimize daytime sedation and hypotension without loss of therapeutic activity.
Perphenazine is used to treat psychosis (e.g. in schizophrenics) and the manic phases of bipolar disorder. Perphenazine effectively treats the positive symptoms of schizophrenia, such as hallucinations and delusions, but its effectiveness in treating the negative symptoms of schizophrenia, such as flattened affect and poverty of speech, is unclear. Earlier studies found the typical antipsychotics to be ineffective or poorly effective in the treatment of negative symptoms, but two recent, large-scale studies found no difference
Amoxicillin (INN), formerly amoxycillin (BAN), and abbreviated amox, is a moderate-spectrum, bacteriolytic, β-lactam antibiotic used to treat bacterial infections caused by susceptible microorganisms. It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other β-lactam antibiotics. Amoxicillin is one of the most common antibiotics prescribed for children.
Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, which are resistant to a broad spectrum of β-lactam antibiotics, such as penicillin. For this reason, it is often combined with clavulanic acid, a β-lactamase inhibitor. This increases effectiveness by reducing its susceptibility to β-lactamase resistance.
Amoxicillin is used in the treatment of a number of infections including: acute otitis media, streptococcal pharyngitis, pneumonia, skin infections, urinary tract infections, salmonella, lyme disease, and chlamydia infections. It is also used to prevent bacterial endocarditis in high risk people who are having dental work done, to prevent strep pneumococus infections in those without a spleen, and for both the prevention and the treatment of
Cathinone, or benzoylethanamine (marketed as hagigat in Israel), is a monoamine alkaloid found in the shrub Catha edulis (khat) and is chemically similar to ephedrine, cathine and other amphetamines. Cathinone induces the release of dopamine from striatal preparations that are prelabelled either with dopamine or its precursors. It is probably the main contributor to the stimulant effect of Catha edulis. Cathinone differs from many other amphetamines in that it has a ketone functional group. Other amphetamines that share this structure include the antidepressant bupropion and the stimulant methcathinone, among others.
Internationally, cathinone is a Schedule I drug under the Convention on Psychotropic Substances. Circa 1993, the DEA added cathinone to the Controlled Substances Act's Schedule I.
The sale of khat is legal in some jurisdictions, but illegal in others — see Khat (Regulation). Cathinone is also often used as the key ingredient of recreational drug mixes commonly known as 'bath salts' in the United States.
Cathinone is structurally related to methcathinone, in much the same way as amphetamine is related to methamphetamine. Cathinone differs from amphetamine by possessing
Enfuvirtide (INN) is an HIV fusion inhibitor, the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It is marketed under the trade name Fuzeon (Roche).
Enfuvirtide therapy costs an estimated US$25,000 per year in the United States. Its cost and inconvenient dosing regimen are factors behind its use as a reserve, for "salvage" therapy in patients with multi-drug resistant HIV.
Enfuvirtide originated at Duke University, where researchers formed a pharmaceutical company known as Trimeris. Trimeris began development on enfuvirtide in 1996 and initially designated it T-20. In 1999, Trimeris entered into partnership with Hoffmann-La Roche to complete the development of the drug. It was approved by the U.S. Food and Drug Administration (FDA) on March 13, 2003 as the first HIV fusion inhibitor, a new class of antiretroviral drugs. It was approved on the basis of two studies (TORO 1 and TORO 2) which compared the effect of optimized regimens of antiretroviral medication with and
Sumatriptan is a synthetic drug belonging to the triptan class, used for the treatment of migraine headaches. Structurally, it is an analog of the naturally occurring neuro-active alkaloids dimethyltryptamine (DMT), bufotenine, and 5-methoxy-dimethyltryptamine, with an N-methyl sulfonamidomethyl- group at position C-5 on the indole ring.
Sumatriptan is produced and marketed by various drug manufacturers with many different trade names such as Sumatriptan, Imitrex, Treximet, Imigran, Imigran recovery.
Sumatriptan was the first clinically available triptan (in 1991). In the United States and most developed countries, it is available only by medical prescription. However, it can be bought over the counter in the UK in 50mg dosage if already prescribed for the patient. Several dosage forms for sumatriptan have been approved, including tablets, solution for injection, and nasal inhalers.
On April 15, 2008, the US FDA approved Treximet, a combination of sumatriptan and naproxen, an NSAID. This combination has shown a benefit over either medicine used separately.
In July 2009, the US FDA approved a single-use jet injector formulation of sumatriptan. The device delivers a subcutaneous
Marketed formulations:Vardenafil hydrochloride 2.5 film coated tablet
Vardenafil (INN) is a PDE5 inhibitor used for treating erectile dysfunction that is sold under the trade names Levitra (Bayer AG, GSK, and SP) and Staxyn.
Vardenafil was co-marketed by Bayer Pharmaceuticals, GlaxoSmithKline, and Schering-Plough under the trade name Levitra. As of 2005, the co-promotion rights of GSK on Levitra have been returned to Bayer in many markets outside the U.S. In Italy, Bayer sells vardenafil as Levitra and GSK sells it as Vivanza. Thus, because of European Union trade rules, parallel imports might result in Vivanza sold next to Levitra in the EU.
An orally disintegrating form, marketed as Staxyn, has been gaining approvals in countries such as the United States and Canada.
Vardenafil's indications and contra-indications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. Vardenafil's relatively short effective time is
Procaine is a local anesthetic drug of the amino ester group. It was used primarily to reduce the pain of intramuscular injection of penicillin, and it was also used in dentistry. Owing to the ubiquity of the trade name Novocain, in some regions procaine is referred to generically as novocaine. It acts mainly by being a sodium channel blocker.
Procaine was first synthesized in 1905, shortly after amylocaine. It was created by the German chemist Alfred Einhorn who gave the chemical the trade name Novocaine, from the Latin nov- (meaning new) and -caine, a common ending for alkaloids used as anesthetics. It was introduced into medical use by surgeon Heinrich Braun. Prior to the discovery of Stovaine and Novocaine, cocaine was the most commonly used local anesthetic.
The primary use for procaine is as a topical anaesthetic.
Procaine is used less frequently today since more effective (and hypoallergenic) alternatives such as lidocaine (Xylocaine) exist. It has been discontinued from US markets. Like other local anesthetics (such as mepivacaine, and prilocaine), procaine is a vasodilator, and is often coadministered with epinephrine for the purpose of vasoconstriction. Vasoconstriction
Dextroamphetamine is a psychostimulant drug approved for the treatment of attention deficit-hyperactivity disorder (ADHD) and narcolepsy.
Dextroamphetamine is the dextrorotatory, or "right-handed", stereoisomer of the amphetamine molecule. The amphetamine molecule has two stereoisomers; levoamphetamine and dextroamphetamine. Names for dextroamphetamine include d-amphetamine, dexamphetamine, dexamfetamine, and (S)-(+)-amphetamine. Dextroamphetamine is available as a generic drug or under several brand names, including Dexedrine and Dextrostat.
The dextroamphetamine salts constitute around 75% of the ADHD drug Adderall. Dextroamphetamine is also an active metabolite of the prodrug lisdexamfetamine (Vyvanse), as well as of several older N-substituted amphetamine prodrugs used as anorectics, such as clobenzorex (Asenlix), benzphetamine (Didrex), and amphetaminil (Aponeuron).
Important side effects of therapeutic dextroamphetamine include stunted growth in young people and occasionally a psychosis can occur at therapeutic doses during chronic therapy as a treatment emergent side effect. When abused at high doses the risk of experiencing side effects and their severity
2C-I or 2,5-dimethoxy-4-iodophenethylamine is a psychedelic phenethylamine of the 2C family. It was first synthesized by Alexander Shulgin. It was described in Shulgin’s 1991 book PiHKAL: A Chemical Love Story. The drug is used recreationally for its psychedelic and entactogenic effects and is sometimes called "smiles.". 2C-I is commonly sold in its hydrochloride salt form, which is a fluffy, sparkling-white powder, which can sometimes be pressed into a tablet form.
In the early 2000s (decade), 2C-I, was sold in Dutch smart shops, after 2C-B, which was previously sold, was banned. In April 2008, 2C-I was also banned in the Netherlands, along with three other 2C-x phenethylamines previously sold in Dutch smartshops for short periods of time. During the same period, 2C-I also became available in powder form from several online vendors of research chemicals in the United States, Asia, and Western Europe.
It is often misrepresented as mescaline in US street sale of singular dosages, as it shares some level of similarity in psychological effect. Both chemicals are members of the psychedelic phenethylamine class of drugs, except 2C-I is an analog of mescaline in the 2C-x series. A major
Marketed formulations:Allopurinol sodium 20 lyophilized powder for injectable solution
Allopurinol (Zyloprim, and generics) is a drug used primarily to treat hyperuricemia (excess uric acid in blood plasma) and its complications, including chronic gout.
Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. Xanthine oxidase is responsible for the successive oxidation of hypoxanthine and xanthine, resulting in the production of uric acid, the product of human purine metabolism. In addition to blocking uric acid production, inhibition of xanthine oxidase causes an increase in hypoxanthine and xanthine. While xanthine cannot be not converted to purine ribotides, hypoxanthine can be salvaged to the purine ribotides adenosine and guanosine monophosphates. Increased levels of these ribotides may cause feedback inhibition of amidophosphoribosyl transferase, the first and rate-limiting enzyme of purine biosynthesis. Allopurinol, therefore, decreases uric acid formation and may also inhibit purine synthesis.
Allopurinol inhibits the breakdown (catabolism) of the thiopurine drug mercaptopurine, and it was specifically invented by Gertrude Elion to enhance the
Amphetamine (USAN, abbreviated from alpha-methylphenethylamine), α-methylphenethylamine, or amfetamine (INN) is a psychostimulant drug of the phenethylamine class that produces increased wakefulness and focus in association with decreased fatigue and appetite.
Brand names of medications that contain, or metabolize into, amphetamine, include Adderall, Dexedrine, Dextrostat, Desoxyn, Didrex, ProCentra, and Vyvanse, as well as Benzedrine or Psychedrine in the past.
The drug is also used recreationally and as a performance enhancer.
Important side effects of therapeutic amphetamine include stunted growth in young people and occasionally a psychosis can occur at therapeutic doses during chronic therapy as a treatment emergent side effect. When abused at high doses the risk of experiencing side effects and their severity increases.
Physical effects of amphetamine can include hyperactivity, dilated pupils, vasoconstriction, blood shot eyes, flushing, restlessness, dry mouth, bruxism, headache, tachycardia, bradycardia, tachypnea, hypertension, hypotension, fever, diaphoresis, diarrhea, constipation, blurred vision, aphasia, dizziness, twitching, insomnia, numbness, palpitations,
Androstenedione (also known as 4-androstenedione and 17-ketoestosterone) is a 19-carbon steroid hormone produced in the adrenal glands and the gonads as an intermediate step in the biochemical pathway that produces the androgen testosterone and the estrogens estrone and estradiol.
Androstenedione is the common precursor of male and female sex hormones. Some androstenedione is also secreted into the plasma, and may be converted in peripheral tissues to testosterone and estrogens.
Androstenedione can be synthesized in one of two ways. The primary pathway involves conversion of 17-hydroxypregnenolone to dehydroepiandrosterone by way of 17,20-lyase, with subsequent conversion of dehydroepiandrosterone to androstenedione via the enzyme 3-β-hydroxysteroid dehydrogenase. The secondary pathway involves conversion of 17-hydroxyprogesterone, most often a precursor to cortisol, to androstenedione directly by way of 17,20-lyase. Thus, 17,20-lyase is required for the synthesis of androstenedione, whether immediately or one step removed.
Androstenedione is further converted to either testosterone or estrogen. Conversion of androstenedione to testosterone requires the enzyme 17β-hydroxysteroid
Marketed formulations:Citalopram 40 film coated tablet
Citalopram (/saɪˈtælɵpræm/; brand names: Celexa, Cipramil) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has U.S. Food and Drug Administration (FDA) approval to treat major depression, and is prescribed off-label for a number of anxiety conditions, despite new studies alleging placebos (sugar pills) to be similarly effective to SSRI's."People get better when they take the drug, but it's not the chemical ingredients of the drugs that are making them better," Harvard's Irving Kirsch said. "It's largely the placebo effect."
Citalopram is approved to treat the symptoms of major depression.
Adult dosing: discontinue with gradual dose reduction and monitoring for withdrawal symptoms doses above 40 mg/day are not recommended due to the risk for QT prolongation
Depression: initial, 20 mg/day ORALLY as a single dose in the morning or evening; dose increases should usually occur in increments of 20 mg at intervals of no less than one week; MAX, 40 mg/day
A test of the GRIK4 gene can be made in order to know if a depressed patient will respond to the citalopram
Citalopram is frequently used off-label to treat anxiety, panic disorder, PMDD, body
Codeine or 3-methylmorphine (a natural isomer of methylated morphine, the other being the semi-synthetic 6-methylmorphine) is an opiate used for its analgesic, antitussive, antidiarrheal, antihypertensive, antianxiety, sedative and hypnotic properties, to suppress premature labor contractions, myocardial infarction, relief of skin irritation from itching, as well as many other uses. Codeine is the second-most predominant alkaloid in opium, at up to three percent; it is much more prevalent in the Iranian poppy (Papaver bracteatum), and codeine is extracted from this species in some places although the below-mentioned morphine methylation process is still much more common. It is considered the prototype of the weak to midrange opioids (tramadol, dextropropoxyphene, dihydrocodeine, hydrocodone, oxycodone).
Codeine is used to treat mild to moderate pain and to relieve cough. Codeine is also used to treat diarrhea and diarrhea predominant irritable bowel syndrome, although loperamide (which is available OTC for milder diarrhea), diphenoxylate, paregoric or even laudanum (also known as Tincture of Opium) are more frequently used to treat severe diarrhea.
Codeine is marketed as both a
Legal status:Schedule 4 Prescription Only Medicine
Marketed formulations:Erythromycin lactobionate 500 lyophilized powder for injectable solution
Erythromycin is a macrolide antibiotic that has an antimicrobial spectrum similar to or slightly wider than that of penicillin, and is often used for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including Mycoplasma and legionellosis. It was first marketed by Eli Lilly and Company, and it is today commonly known as EES (erythromycin ethylsuccinate, an ester prodrug that is commonly administered).
In structure, this macrocyclic compound contains a 14-membered lactone ring with ten asymmetric centers and two sugars (L-cladinose and D-desosamine), making it a compound very difficult to produce via synthetic methods.
Erythromycin is produced from a strain of the actinomycete Saccharopolyspora erythraea.
Abelardo Aguilar, a Filipino scientist, sent some soil samples to his employer Eli Lilly in 1949. Eli Lilly’s research team, led by J. M. McGuire, managed to isolate erythromycin from the metabolic products of a strain of Streptomyces erythreus (designation changed to "Saccharopolyspora erythraea") found in the samples.
Lilly filed for patent protection of the compound and U.S. patent 2,653,899 was granted in
Marketed formulations:Fentanyl citrate 600 soluable film
Fentanyl (also known as fentanil, brand names Sublimaze, Actiq, Durogesic, Duragesic, Fentora, Matrifen, Haldid, Onsolis, Instanyl, Abstral, Lazanda and others) is a potent, synthetic narcotic analgesic with a rapid onset and short duration of action. It is a strong agonist at the μ-opioid receptors. Historically it has been used to treat breakthrough pain and is commonly used in pre-procedures as a pain reliever as well as an anesthetic in combination with a benzodiazepine.
Fentanyl is approximately 100 times more potent than morphine, with 100 micrograms of fentanyl approximately equivalent to 10 mg of morphine and 75 mg of pethidine (meperidine) in analgesic activity. It has an LD50 of 3.1 milligrams per kilogram in rats, and an LD50 of 0.03 milligrams per kilogram in monkeys.
Fentanyl was first synthesized by Paul Janssen in 1960 following the medical inception of pethidine several years earlier. Janssen developed fentanyl by assaying analogues of the structurally related drug pethidine for opioid activity. The widespread use of fentanyl triggered the production of fentanyl citrate (the salt formed by combining fentanyl and citric acid in a 1:1 stoichiometry), which entered the
Furosemide (INN) or frusemide (former BAN) is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi-Aventis under the brand name Lasix, and also under the brand name Frumex. It has also been used to prevent Thoroughbred and Standardbred race horses from bleeding through the nose during races.
Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs.
Furosemide is primarily used for the treatment of hypertension and edema. It is the first-line agent in most people with edema due to congestive heart failure. It is also used for hepatic cirrhosis, renal impairment, nephrotic syndrome, in adjunct therapy for cerebral/pulmonary edema where rapid diuresis is required (IV injection), and in the management of severe hypercalcemia in combination with adequate rehydration.
Although disputed, it is considered ototoxic: "usually with large parenteral doses and rapid administration and in renal impairment". Furosemide also can lead to gout due to hyperuricemia. Hyperglycemia is also a common side effect.
The tendency, as
Marketed formulations:Indapamide 1.25 film coated tablet
Indapamide is a thiazide diuretic drug marketed by Servier, generally used in the treatment of hypertension, as well as decompensated cardiac failure. The US trade name for indapamide is Lozol. Indapamide is marketed as Natrilix outside the US, and as Insig in Australia. Combination preparations with perindopril (an ACE inhibitor antihypertensive) are also available.
It is described as a thiazide-like diuretic.
Indapamide is available generically as 1.25 mg and 2.5 mg non-scored tablets.
Hypertension and edema due to congestive heart failure. Indapamide has been proven in the HYVET trial to reduce stroke and all cause mortality when given with or without perindopril to people over the age of 80 for the treatment of hypertension.
The adult dosage is 1.25 to 5 mg, orally and once daily, usually in the morning.
Indapamide is contraindicated in known hypersensitivity to sulfonamides, severe renal failure, hepatic encephalopathy or severe hepatic failure and hypokalemia (low blood potassium levels).
There is insufficient safety data to recommend indapamide use in pregnancy or breastfeeding.
Caution is advised in the combination of indapamide with lithium and nonantiarrhythmic drugs
Nandrolone (19-nortestosterone) is an anabolic steroid that may be present naturally in the human body, albeit in minute quantities of less than 0.4 ng/ml. Nandrolone is most commonly sold commercially as its decanoate ester (Deca-Durabolin) and less commonly as a phenylpropionate ester (Durabolin). Nandrolone decanoate is used in the treatment of osteoporosis in postmenopausal women (though now not recommended) at a dose of 50 mg every three weeks. It is also used for some aplastic anaemias.
The positive effects of the drug include muscle growth, appetite stimulation and increased red blood cell production and bone density. Clinical studies have shown it to be effective in treating anaemia, osteoporosis and some forms of neoplasia including breast cancer, and also acts as a progestin-based contraceptive. For these reasons, in the United States nandrolone received FDA approval in 1983.
Because nandrolone is not broken down into DHT, the deleterious effects common to most anabolic steroids on the scalp, skin, and prostate are lessened to a degree; but is rather broken down to the much weaker androgen dihydronandrolone. The lack of alkylation on the 17α-carbon drastically reduces the
Pilocarpine is a parasympathomimetic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist in the parasympathetic nervous system, which acts therapeutically at the muscarinic acetylcholine receptor M3 due to its topical application, e.g., in glaucoma and xerostomia.
Pilocarpine has been used in the treatment of chronic open-angle glaucoma and acute angle-closure glaucoma for over 100 years. It acts on a subtype of muscarinic receptor (M3) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis. Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humor leaves the eye to decrease intraocular pressure.
Pilocarpine is often used as an antidote for scopolamine, atropine, and hyoscyamine poisoning.
In ophthalmology pilocarpine is also used to reduce the possibility of glare at night from lights if the patient underwent implantation of phakic intraocular lenses; the use of pilocarpine would reduce
Pyridostigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. Since it is a quaternary amine, it is poorly absorbed in the gut and does not cross the blood–brain barrier, except possibly in stressful conditions.
In a synapse, action potentials are conducted along motor nerves to their terminals where they initiate a Ca2+ influx and the release of acetylcholine (ACh). The ACh diffuses across the synaptic cleft and binds to receptors on the post synaptic membrane, causing an influx of Na+ and K+ ions, resulting in depolarization. If large enough, this depolarization results in an action potential. To prevent constant stimulation once the ACh is released, an enzyme called acetylcholinesterase is present in the endplate membrane close to the receptors on the post synaptic membrane, and quickly hydrolizes ACh.
Pyridostigmine inhibits acetylcholinesterase in the synaptic cleft, thus slowing down the hydrolysis of acetylcholine. It is a quaternary carbamate inhibitor of cholinesterase that does not cross the blood–brain barrier which carbamylates about 30% of peripheral cholinesterase enzyme. The carbamylated enzyme eventually regenerates by natural hydrolysis and
Sevoflurane (1,1,1,3,3,3-hexafluoro-2-(fluoromethoxy)propane), also called fluoromethyl hexafluoroisopropyl ether, is a sweet-smelling, nonflammable, highly fluorinated methyl isopropyl ether used for induction and maintenance of general anesthesia. Together with desflurane, it is replacing isoflurane and halothane in modern anesthesiology. It is often administered in a mixture of nitrous oxide and oxygen. After desflurane, it is the volatile anesthetic with the fastest onset and offset. Though desflurane has the lowest blood/gas coefficient of the currently used volatile anesthetics, sevoflurane is the preferred agent for mask induction due to its lesser irritation to mucous membranes.
First reports of sevoflurane appeared in the literature in 1971. The agent was developed by Ross Terrell, PhD. It was introduced into clinical practice initially in Japan in 1990. Its name comes from having seven fluorine atoms. The rights for sevoflurane in the US and other countries were held by Abbott Laboratories. It is now available as a generic drug.
Sevoflurane forms at least two degradation products, compound A [fluoromethyl-2,2-difluoro-1-(trifluoromethyl)vinyl ether] also called PIFE
Speedball (alternatively known as powerballing) is a term commonly referring to the hazardous intravenous use of cocaine with heroin or morphine in the same syringe. The speedball can also be taken by insufflation. The original speedball used cocaine hydrochloride mixed with morphine sulfate, as opposed to heroin. The term can also be applied to use of pharmaceutical opioids, benzodiazepines or barbiturates along with amphetamines derivates. This cocktail of drugs can cause a strong physical dependence and withdrawal symptoms. Cocaine acts as a stimulant, whereas heroin/morphine acts as a depressant. Coadministration is meant to provide an intense rush of euphoria with a high that is supposed to combine the effects of both drugs, while hoping to reduce the negative effects, such as anxiety, hypertension, palpitations and other common side effects of stimulants and sedation/drowsiness from the depressant. While this is somewhat effective as one drug (the CNS stimulant) triggers the sympathetic nervous system and the other (the CNS depressant) triggers the parasympathetic nervous system, the two systems that regulate the fight-or-flight & rest-and-digest responses, respectively, and
Temazepam (brand names Restoril - 15 mg/30 mg and Normison, among others) is an intermediate-acting 3-hydroxy hypnotic of the benzodiazepine class of psychoactive drugs. Temazepam is approved for the short-term treatment of insomnia. In addition, temazepam has anxiolytic (anti-anxiety), anticonvulsant, and skeletal muscle relaxant properties.
Temazepam was first synthesized in 1964, but it first came into use in 1969 when its ability to counter insomnia was realized. By the late 1980s, temazepam was one of the most popular and widely prescribed hypnotics on the market and it became one of the most widely prescribed drugs.
Temazepam is a hypnotic agent. In sleep laboratory studies, temazepam significantly decreased the number of nightly awakenings but has the drawback of distorting the normal sleep pattern.
Temazepam is officially indicated for severe insomnia and other severe or disabling sleep disorders. The prescribing guidelines in the UK limit the prescribing of hypnotics to two-to-four weeks due to concerns of tolerance and dependence.
The United States Air Force uses temazepam as one of the hypnotics approved as "no-go pills" to help aviators and special duty personnel sleep
Tranylcypromine (Parnate, Jatrosom) is a drug of the substituted phenethylamine and amphetamine classes which acts as a monoamine oxidase inhibitor (MAOI)—it is a nonselective and irreversible inhibitor of the enzyme monoamine oxidase (MAO). It is used as an antidepressant and anxiolytic agent in the clinical treatment of mood and anxiety disorders, respectively.
Tranylcypromine was originally developed as an analog of amphetamine. Although it was first synthesized in 1948, its MAOI action was not discovered until 1959. Precisely because tranylcypromine was not, like isoniazid and iproniazid, a hydrazine derivative, its clinical interest increased enormously, as it was thought it might have a more acceptable therapeutic index than previous MAOIs.
The drug was introduced by Smith, Kline and French in the United Kingdom in 1960, and approved in the United States in 1961. It was withdrawn from the market in February 1964 due to a number of patient deaths involving hypertensive crises with intracranial bleeding. However, it was reintroduced later that year with more limited indications and specific warnings of the risks.
Despite their well-established efficacy, indications for
Methaqualone, (brand name Quaaludes /ˈkweɪluːdz/ KWAY-lewdz) is a sedative-hypnotic drug that is similar in effect to barbiturates, a general central nervous system depressant. The sedative-hypnotic activity was first noted by Indian researchers in the 1950s and in 1962 methaqualone itself was patented in the US by Wallace and Tiernan. Its use peaked in the early 1970s as a hypnotic, for the treatment of insomnia, and as a sedative and muscle relaxant. It has also been used illegally as a recreational drug. Since at least 2001, it has been widely used in South Africa, where it is commonly referred to as "smarties" or "geluk-tablette" (meaning happy tablets). Clandestinely produced methaqualone is still seized by government agencies and police forces around the world.
Methaqualone was first synthesized in India in 1951 by Indra Kishore Kacker and Syed Hussain Zaheer, and was soon introduced to Japanese and European consumers as a safe barbiturate substitute. By 1965 it was the most commonly prescribed sedative in Britain, where it has been sold legally under the names Malsed, Malsedin, and Renoval. In 1965 a Methaqualone/antihistamine combination was sold as the sedative drug
Marketed formulations:Clopidogrel bisulfate 300 film coated tablet
Clopidogrel (INN) is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi under the trade name Plavix. The drug works by irreversibly inhibiting a receptor called P2Y12, an adenosine diphosphate (ADP) chemoreceptor on platelet cell membranes. Adverse effects include hemorrhage, severe neutropenia, and thrombotic thrombocytopenic purpura (TTP).
Clopidogrel is a prodrug, the action of which may be related to an ADP receptor on platelet cell membranes. The drug specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in activation of platelets and eventual cross-linking by the protein fibrin. The blockade of this receptor inhibits platelet aggregation by blocking activation of the glycoprotein IIb/IIIa pathway. The IIb/IIIa complex functions as a receptor mainly for fibrinogen and vitronectin but also for fibronectin and von Willebrand factor. Activation of this receptor complex is the "final common pathway" for platelet aggregation and is important in the cross-linking of platelets by
Echothiophate (Phospholine) is a parasympathomimetic and a phosphorothioate. It is an acetylcholinesterase inhibitor.
It is used as an ocular antihypertensive in the treatment of chronic glaucoma and, in some cases, accommodative esotropia. It is available under several trade names such as Phospholine Iodide (Wyeth-Ayerst).
Echothiophate binds irreversibly to cholinesterase. Because of the very slow rate at which echothiophate is hydrolyzed by cholinesterase, its effects can last a week or more. Adverse effects include muscle spasm and other systemic effects.
It covalently binds by its phosphate group to serine group at the active site of the cholinesterase. Once bound, the enzyme is permanently inactive and the cell has to make new enzymes.
Wyeth Pharmaceuticals stopped manufacturing echothiophate iodide in the US in 2003. After contacting the American Academy of Ophthalmology (AAO), Wyeth rescinded their decision and, according to AAO public relations representative Michelle Stephens, the AAO and Wyeth were in talks for about a year about manufacturing it.
In the meantime, a worldwide shortage of the drug has occurred.
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.
Granisetron was developed by chemists working at the British drug company Beecham around 1988 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA.
A granisetron transdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008. Sancuso is manufactured by ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland.
Granisetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.
Granisetron is a well-tolerated
Metoclopramide (INN) ( /ˌmɛtəˈklɒprəmaɪd/) is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.
Metoclopramide is commonly used to treat nausea including that which is due to chemotherapy and that occurring post operatively. Evidence also supports its use for gastroparesis (poor stomach emptying) and gastroesophageal reflux disease.
Metoclopramide is used to treat nausea and vomiting associated with conditions such as uremia, radiation sickness, malignancy, labor, infection, migraine headaches, and emetogenic drugs. In the setting of painful conditions such as migraine headaches, metoclopramide may be used in combination with paracetamol (acetaminophen) (available in the UK as Paramax, and in Australia as Metomax), or in combination with aspirin (MigraMax).
Metoclopramide increases peristalsis of the jejunum and duodenum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb. These gastroprokinetic effects make metoclopramide useful in the
Progesterone also known as P4 (pregn-4-ene-3,20-dione) is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy (supports gestation) and embryogenesis of humans and other species. Progesterone belongs to a class of hormones called progestogens, and is the major naturally occurring human progestogen.
Progesterone was independently discovered by four research groups.
Willard Myron Allen co-discovered progesterone with his anatomy professor George Washington Corner at the University of Rochester Medical School in 1933. Allen first determined its melting point, molecular weight, and partial molecular structure. He also gave it the name Progesterone derived from Progestational Steroidal ketone.
Like other steroids, progesterone consists of four interconnected cyclic hydrocarbons. Progesterone contains ketone and oxygenated functional groups, as well as two methyl branches. Like all steroid hormones, it is hydrophobic.
Progesterone is produced in the ovaries (by the corpus luteum), the adrenal glands (near the kidney), and, during pregnancy, in the placenta. Progesterone is also stored in adipose (fat) tissue.
In humans, increasing amounts of progesterone are produced
Marketed formulations:Simvastatin 10 film coated tablet
Simvastatin (INN) ( /ˈsɪmvəstætɨn/) is a hypolipidemic drug used to control elevated cholesterol, or hypercholesterolemia. It is a member of the statin class of pharmaceuticals.
Simvastatin is a synthetic derivative of a fermentation product of Aspergillus terreus. The drug is marketed generically and under the trade name Zocor.
The primary uses of simvastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels sufficiently.
Common side effects (>1% incidence) may include abdominal pain, diarrhea, indigestion, and a general feeling of weakness. Rare side effects include joint pain, memory loss, and muscle cramps. Cholestatic hepatitis, hepatic cirrhosis, rhabdomyolysis (destruction of muscles and blockade of renal system) and myositis have been reported in patients receiving the drug chronically.
A type of DNA variant known as a single nucleotide polymorphism (SNP) may help predict individuals prone to developing myopathy when taking simvastatin; a study ultimately including 32,000 patients concluded the carriers of
Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.
It is also an effective preventive medication for migraine. It is a class 3 antianginal drug, and a class IV antiarrhythmic. It is a common adulterant of cocaine seized in the UK, and has been found to reduce cocaine cravings in rats, indicating it may prolong the "high" (see below). It incites minimal reflex sympathetic changes. It is based upon a 1,4-thiazepine ring.
Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.
Diltiazem is a potent vasodilator, increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. Its pharmacological activity is somewhat similar to verapamil.
It is a potent vasodilator of coronary and peripheral vessels, which reduces peripheral resistance and afterload.
Because of its negative inotropic effect, diltiazem causes a modest decrease in heart muscle contractility and reduces myocardium oxygen consumption. Its negative chronotropic effect results in a modest lowering of heart rate, due to
Marketed formulations:Valdecoxib 10 film coated tablet
Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is a cyclooxygenase-2 selective inhibitor.
Valdecoxib was manufactured and marketed under the brand name Bextra by G. D. Searle & Company. It was approved by the United States Food and Drug Administration on November 20, 2001, and was available by prescription in tablet form until 2005, when it was removed from the market due to concerns about possible increased risk of heart attack and stroke.
In the United States, the Food and Drug Administration (FDA) approved valdecoxib for the treatment of osteoarthritis, adult rheumatoid arthritis, and primary dismennorhea.
Valdecoxib was also used off-label for controlling accute pain and various types of surgical pain, though Pfizer was penalized for promoting such uses in US.
On April 7, 2005, Pfizer withdrew Bextra from the U.S. market on recommendation by the FDA, citing an increased risk of heart attack and stroke and also the risk of a serious, sometimes fatal, skin reaction. This was a result of recent attention to prescription NSAIDs, such as Merck's Vioxx.
Desflurane (1,2,2,2-tetrafluoroethyl difluoromethyl ether) is a highly fluorinated methyl ethyl ether used for maintenance of general anesthesia. Like halothane, enflurane and isoflurane, it is a racemic mixture of (R) and (S) optical isomers (enantiomers). Together with sevoflurane, it is gradually replacing isoflurane for human use, except in the third world, where its high cost precludes its use. It has the most rapid onset and offset of the volatile anesthetic drugs used for general anesthesia due to its low solubility in blood.
Some drawbacks of desflurane are its low potency, its pungency and its high cost. It may cause tachycardia and airway irritability when administered at concentrations greater than 10 vol%. Due to this airway irritability, desflurane is infrequently used to induce anesthesia via inhalation techniques.
Additionally, desflurane is a greenhouse gas. Anesthesia gases used globally contribute the equivalent of 1 million cars to global warming. Desflurane has a global warming potential of 3714. One tonne of desflurane emitted is equivalent to 3714 tonnes of carbon dioxide in the atmosphere, much higher than sevoflurane or isoflurane. Taking into account the
Escitalopram (trade names Nexito, Anxiset-E (India),Cipralex (Pakistan) Lexapro, Cipralex, Seroplex, Elicea, Lexamil, Lexam, Entact, Losita (Bangladesh), Reposil (Chile), Animaxen (Colombia)), is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is approved by the U.S. Food and Drug Administration (FDA) for the treatment of adults and children over 12 years of age with major depressive disorder and generalized anxiety disorder . Escitalopram is the (S)-stereoisomer (enantiomer) of the earlier Lundbeck drug citalopram, hence the name escitalopram. Escitalopram is noted for its high selectivity with serotonin reuptake inhibition. Its side effects are typical for the SSRI class. Only one independent study has shown that escitalopram is more effective than citalopram, but in October 2011 it was reported that the company that sponsored the study had links to Lundbeck, the makers. The similarity between escitalopram and citalopram has led to accusations of "evergreening", an accusation that Lundbeck has rejected.
Escitalopram is primarily used for the treatment of major depressive disorder and general anxiety disorder in adults. However, it has also been
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. Unlike acetylcholine, bethanechol is not hydrolyzed by cholinesterase and will therefore have a long duration of action. Bethanechol does not involve the action of the muscarinic M3 receptor subtype in-vitro (Benavides-Haro et al. (2003))
Bethanechol is sold under the brand names Duvoid (Roberts), Myotonachol (Glenwood), Urecholine (Merck Frosst) and Urocarb (Hamilton).
Bethanechol is sometimes given orally or subcutaneously to treat urinary retention resulting from general anesthetic or diabetic neuropathy of the bladder, or to treat gastrointestinal atony (lack of muscular tone). The muscarinic receptors in the bladder and gastrointestinal tract stimulate contraction of the bladder and expulsion of urine, and increased gastrointestinal motility, respectively. Bethanechol should be used to treat these disorders only after mechanical obstruction is ruled out as a possible cause.
Its potential benefit in the treatment of cerebral palsy has been investigated. Bethanechol is a powerful cholinergic agent which efficiently crosses the blood -
Bupropion (/bjuːˈproʊpi.ɒn/ bew-PROH-pee-on; marketed as Wellbutrin, Zyban, Voxra, Budeprion, Prexaton, Elontril or Aplenzin; and formerly known as amfebutamone) is an atypical antidepressant and smoking cessation aid. Its chemical name is β-keto-3-chloro-N-tert-butylamphetamine, a substituted cathinone (β-ketoamphetamine), as well as substituted amphetamine. The drug therefore is a mild psychostimulant. Its primary pharmacological action is thought to be norepinephrine-dopamine reuptake inhibition. It binds selectively to the dopamine transporter, but its behavioural effects have often been attributed to its inhibition of norepinephrine reuptake. It also acts as a nicotinic acetylcholine receptor antagonist. Bupropion belongs to the chemical class of aminoketones and is similar in structure to stimulants cathinone and diethylpropion, and to phenethylamines in general. Medically, bupropion serves as a non-tricyclic antidepressant fundamentally different to most commonly prescribed antidepressants such as SSRIs.
Initially researched and marketed as an antidepressant, bupropion was subsequently found to be effective as a smoking cessation aid. With over 20 million retail
Chloral hydrate is an unapproved, Schedule IV sedative and hypnotic drug as well as a chemical reagent and precursor. The name chloral hydrate indicates that it is formed from chloral (trichloroacetaldehyde) by the addition of one molecule of water. Its chemical formula is C2H3Cl3O2.
It was discovered through the chlorination of ethanol in 1832 by Justus von Liebig in Gießen. Its sedative properties were first published in 1869 and subsequently, because of its easy synthesis, its use was widespread. It was widely used recreationally and misprescribed in the late 19th century. Chloral hydrate is soluble in both water and alcohol, readily forming concentrated solutions. A solution of chloral hydrate in alcohol called "knockout drops" was used to prepare a Mickey Finn. More reputable uses of chloral hydrate include its use as a clearing agent for chitin and fibers and as a key ingredient in Hoyer's mounting medium, which is used to prepare permanent or semipermanent microscope slides of small organisms, histological sections, and chromosome squashes.
It is, together with chloroform, a minor side-product of the chlorination of water when organic residues are present in the water,
Diclofenac (marketed under many trade names) is a nonsteroidal anti-inflammatory drug (NSAID) taken to reduce inflammation and as an analgesic reducing pain in certain conditions.
The name is derived from its chemical name: 2-(2,6-dichloranilino) phenylacetic acid.
In the United Kingdom, India, Brazil and the United States, it may be supplied as either the sodium or potassium salt, in China most often as the sodium salt, while in some other countries only as the potassium salt. Diclofenac is available as a generic drug in a number of formulations; including Dichlofenac diethylammonium under the trade name Voltarol Emulgel applied topically to joints. Over-the-counter (OTC) use is approved in some countries for minor aches and pains and fever associated with common infections.
Diclofenac is used to treat pain, inflammatory disorders, and dysmenorrhea.
Inflammatory disorder may include musculoskeletal complaints, especially arthritis, rheumatoid arthritis, polymyositis, dermatomyositis, osteoarthritis, dental pain, TMJ, spondylarthritis, ankylosing spondylitis, gout attacks, and pain management in cases of kidney stones and gallstones. An additional indication is the treatment of
γ-Hydroxybutyric acid (GHB), also known as 4-hydroxybutanoic acid and sodium oxybate (INN), is a naturally occurring substance found in the human central nervous system, as well as in wine, beef, small citrus fruits, and almost all animals in small amounts. It is also categorized as an illegal drug in many countries. It is currently regulated in Australia and New Zealand, Canada, most of Europe and in the US. GHB as the sodium salt, known as sodium oxybate, is sold by Jazz Pharmaceuticals under the name Xyrem to treat cataplexy and excessive daytime sleepiness in patients with narcolepsy.
GHB has been used in a medical setting as a general anesthetic, to treat conditions such as insomnia, clinical depression, narcolepsy, and alcoholism, and to improve athletic performance. It is also used as an intoxicant (illegally in many jurisdictions) or as a date rape drug. GHB is naturally produced in the human body's cells and is structurally related to the ketone body beta-hydroxybutyrate. As a supplement/drug, it is used most commonly in the form of a salt, for example sodium gamma-hydroxybutyrate (Na.GHB, sodium oxybate, or under the brand name Xyrem.) or potassium gamma-hydroxybutyrate
Marketed formulations:Hydromorphone hydrochloride 2 film coated tablet
Hydromorphone, a more common synonym for dihydromorphinone, commonly a hydrochloride (brand names Palladone, Dilaudid, and numerous others) is a very potent centrally acting analgesic drug of the opioid class. It is a derivative of morphine, to be specific, a hydrogenated ketone thereof, and it can be said that hydromorphone is to morphine as hydrocodone is to codeine and, therefore, a semi-synthetic drug. It is, in medical terms, an opioid analgesic and, in legal terms, a narcotic. Hydromorphone is commonly used in the hospital setting, mostly intravenously (IV) because its bioavailability orally, rectally, and intranasally is very low.
Hydromorphone is used in medicine as an alternative to morphine for analgesia and as a second- or third-line narcotic antitussive (cough suppressant) for cases of dry, painful, paroxysmal coughing resulting from continuing bronchial irritation after influenza and other ailments, inhalation of fungus, and other causes. In general, it is considered the strongest of the antitussive drugs and was developed shortly after diacetylmorphine (heroin) was removed from clinical use for this purpose in most of the world and banned outright in many countries.
Tissue plasminogen activator (abbreviated tPA or PLAT) is a protein involved in the breakdown of blood clots. It is a serine protease (EC 18.104.22.168) found on endothelial cells, the cells that line the blood vessels. As an enzyme, it catalyzes the conversion of plasminogen to plasmin, the major enzyme responsible for clot breakdown. Because it works on the clotting system, tPA is used in clinical medicine to treat embolic or thrombotic stroke. Use is contraindicated in hemorrhagic stroke and head trauma.
tPA may be manufactured using recombinant biotechnology techniques. tPA created this way may be referred to as recombinant tissue plasminogen activator (rtPA).
tPA and plasmin are the key enzymes of the fibrinolytic pathway in which tPA mediated plasmin generation occurs. To be specific, tPA cleaves the zymogen, plasminogen at its Arg560 - Val561 peptide bond, into the serine protease plasmin.
Increased enzymatic activity causes hyperfibrinolysis, which manifests as excessive bleeding. Decreased activity leads to hypofibrinolysis which can result in thrombosis or embolism.
Tissue plasminogen activator also plays a role in cell migration and tissue remodeling.
Captopril (rINN) ( /ˈkæptəprɪl/) is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. Captopril is commonly marketed by Bristol-Myers Squibb under the trade name Capoten.
Captopril's main uses are based on its vasodilation and inhibition of some renal function activities. These benefits are most clearly seen in the following conditions:
2) Cardiac conditions such as congestive heart failure and after myocardial infarction
3) Preservation of kidney function in diabetic nephropathy
Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although there has been one negative study. Formal clinical trials in depressed patients have not been reported.
It has also been investigated for use in the treatment of cancer.
Captopril was developed in 1975 by three
Dimenhydrinate (in US marketed under brand names Dramamine, Driminate, Gravol, Gravamin, Vomex, and Vertirosan) is an over-the-counter drug used to prevent nausea and motion sickness. It is marketed in Brazil as Dramin, in Canada as Gravol, in Ecuador as Anautin, in Hungary as Daedalon, in Italy as Xamamina, in Indonesia as Antimo, in Portugal as Viabom, and in Thailand as ไดเมนนีน (Dị men nīn). It is most commonly used as pills, although it is also available in liquid form and in suppositories. Chemically, dimenhydrinate is a salt of two drugs: diphenhydramine, and 8-chlorotheophylline, a chlorinated derivative of theophylline.
The effects of dimenhydrinate are very similar to those of diphenhydramine. The main differences are a lower potency, and a longer latency. 50 mg dimenhydrinate contains 27.2 mg of diphenhydramine, so it is less potent at equal doses. Also, dimenhydrinate must dissociate into diphenhydramine and its counterion in the body before it is active, so it produces effects more slowly than diphenhydramine. The drug typically takes a minimum of 4 hours to fully take effect.
Theophylline was added in order to counteract drowsiness. Theophylline is very closely
Hyoscyamine (also known as daturine) is a tropane alkaloid. It is a secondary metabolite found in certain plants of the Solanaceae family, including henbane (Hyoscyamus niger), mandrake (Mandragora officinarum), jimsonweed (Datura stramonium), tomato (Solanum lycopersicum) and deadly nightshade (Atropa belladonna). It is the levorotary isomer of atropine (third of the three major nightshade alkaloids) and thus sometimes known as levo-atropine. Hyoscyamine should not be confused with hyoscine, an older alternate name for the related nightshade-derived anticholinergic scopolamine for which it is the precursor of.
Brand names for hyoscyamine include Symax, HyoMax, Anaspaz, Egazil, Buwecon, Cystospaz, Levsin, Levbid, Levsinex, Donnamar, NuLev, Spacol T/S and Neoquess.
Hyoscyamine can be extracted from plants of the Solanaceae family, notably Datura stramonium. As hyoscyamine is a direct precursor in the plant biosynthesis of scopolamine, it is produced via the same metabolic pathway.
The biosynthesis of scopolamine begins with the decarboxylation of L-ornithine to putrescine by ornithine decarboxylase (EC 22.214.171.124). Putrescine is methylated to N-methylputrescine by putrescine
Marketed formulations:Maprotiline hydrochloride 50 film coated tablet
Maprotiline (sold as Deprilept, Ludiomil, Psymion) is a tetracyclic antidepressant (TeCA). However, Maprotiline's fourth ring is spurious, as formed by a bridge across the central tricyclic ring. It is a strong norepinephrine reuptake inhibitor with only weak effects on serotonin and dopamine reuptake.
It exerts blocking effects at the following postsynaptic receptors:
The pharmacologic profile of Maprotiline explains its antidepressant, sedative, anxiolytic, and sympathomimetic activities. Additionally, it shows a strong antagonism against Reserpine-induced effects in animal studies, as do the other 'classical' antidepressants. Although Maprotiline behaves in most regards as a 'first generation antidepressant' it is commonly referred to as 'second generation antidepressant'.
Sedation has a fast onset (the same day), while remission of the depression itself is noted usually after a latent period of one to four weeks.
Maprotiline does not improve mood in nondepressed persons.
Maprotiline was developed and has been marketed by the Swiss manufacturer Geigy (now Novartis) since the early 1980s under the brand name Ludiomil. Generics are widely available.
Maprotiline is used in the
Olanzapine (trade name Zyprexa or in combination with fluoxetine Symbyax) is an atypical antipsychotic, approved by the U.S. Food and Drug Administration (FDA) for the treatment of schizophrenia and bipolar disorder. Olanzapine is structurally similar to clozapine, but is classified as a thienobenzodiazepine. The olanzapine formulations are manufactured and marketed by the pharmaceutical company Eli Lilly and Company; the drug went generic in 2011. Sales of Zyprexa in 2008 were $2.2B in the US alone, and $4.7B in total.
In 2002, British and Japanese regulatory agencies warned that Zyprexa may be linked to diabetes, but even after the FDA issued a similar warning in 2003, Lilly did not publicly disclose their own findings. Eli Lilly agreed on January 4, 2007 to pay up to $500 million to settle 18,000 lawsuits from people who claimed they developed diabetes or other diseases after taking Zyprexa. On January 15, 2009 Eli Lilly pled guilty to a criminal misdemeanor charge of illegally marketing Zyprexa for off-label use, and agreed to pay $1.4 billion. Although Lilly had evidence that it is not effective for dementia, Zyprexa was marketed for elderly Alzheimer's patients. The drug
Phenylpropanolamine (PPA; Accutrim), also known as the stereoisomers norephedrine and norpseudoephedrine, is a psychoactive drug of the phenethylamine and amphetamine chemical classes which is used as a stimulant, decongestant, and anorectic agent. It is commonly used in prescription and over-the-counter cough and cold preparations. In veterinary medicine, it is used to control urinary incontinence in dogs under trade names Propalin and Proin.
In the United States, PPA is no longer sold without a prescription due to a proposed increased risk of stroke in younger women. In a few countries in Europe, however, it is still available by either prescription or sometimes over-the-counter. In Canada, it was withdrawn from the market on May 31, 2001. In India human use of PPA and its formulations were banned on 10 February 2011.
Phenylpropanolamine acts as a potent and selective releasing agent of norepinephrine and epinephrine, or as a norepinephrine releasing agent (NRA). It also acts as a dopamine releasing agent (DRA) to a lesser extent. It works by mimicking the effects of endogenous catecholamines such as epinephrine and norepinephrine, and to a lesser degree dopamine.
Amlodipine (Norvasc (Pfizer) and generics) (as besylate, mesylate or maleate) is a long-acting calcium channel blocker (dihydropyridine (DHP) class) used as an anti-hypertensive and in the treatment of angina. Like other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle (although DHP-class calcium channel blockers are more selective for arteries than myocardium, as the cardiac calcium channels are not of the dihydropyridine-type).
Amlodipine is used in the management of hypertension, and coronary artery disease.
Adverse side effects of the use of amlodipine may be:
The acute oral toxicity (LD50) of amlodipine in mice is 37 mg/kg.
Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are
Brompheniramine (Bromfed, Dimetapp, Bromfenex, Dimetane, BPN, Lodrane), commonly marketed as its salt brompheniramine maleate, is an antihistamine drug of the propylamine (alkylamine) class. It is readily available over the counter and is indicated for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing. It is a first-generation antihistamine.
Brompheniramine is part of a series of antihistamines including pheniramine (Naphcon) and its halogenated derivatives and others including fluorpheniramine, chlorpheniramine, dexchlorpheniramine (Polaramine), deschlorpheniramine, dipheniramine (also known as triprolidine with the trade name Actifed), and iodopheniramine.
The halogenated alkylamine antihistamines all exhibit optical isomerism and brompheniramine products contain racemic brompheniramine maleate whereas dexbrompheniramine (Drixoral) is the dextrorotary (right-handed) stereoisomer.
Brompheniramine has antidepressant properties, inhibiting reuptake of the neurotransmitter serotonin. Based on this knowledge, Arvid Carlsson and his colleagues, working at the Swedish company Astra AB, were able to derive
Cerivastatin (brand names: Baycol, Lipobay) is a synthetic member of the class of statins used to lower cholesterol and prevent cardiovascular disease. It was marketed by the pharmaceutical company Bayer A.G. in the late 1990s, competing with Pfizer's highly successful atorvastatin (Lipitor). Cerivastatin was voluntarily withdrawn from the market worldwide in 2001, due to reports of fatal rhabdomyolysis.
During post-marketing surveillance, 52 deaths were reported in patients using cerivastatin, mainly from rhabdomyolysis and its resultant renal failure. Risks were higher in patients using fibrates, mainly gemfibrozil (Lopid), and in patients using the highest (0.8 mg/day) dose of cerivastatin. Bayer A.G. added a contraindication for the concomitant use of cerivastatin and gemfibrozil to the package 18 months after the drug interaction was found. The frequency of deadly cases of rhabdomyolysis with cerivastatin was 16 to 80 times higher than with other statins. Another 385 nonfatal cases of rhabdomyolysis were reported. This put the risk of this (rare) complication at 5-10 times that of the other statins. Cerivastatin also induced myopathy in a dose-dependent manner when
Doxapram hydrochloride (marketed as Dopram, Stimulex or Respiram) is a respiratory stimulant. Administered intravenously, doxapram stimulates an increase in tidal volume, and respiratory rate.
Doxapram stimulates chemoreceptors in the carotid bodies of the carotid arteries, which in turn, stimulates the respiratory centre in the brain stem.
Doxapram is a white to off-white, odorless, crystalline powder that is stable in light and air. It is soluble in water, sparingly soluble in alcohol and practically insoluble in ether. Injectable products have a pH from 3.5-5. Benzyl alcohol or chlorobutanol is added as a preservative agent in the commercially available injections.
Doxapram is used in intensive care settings to stimulate the respiratory rate in patients with respiratory failure. It may be useful for treating respiratory depression in patients who have taken excessive doses of drugs such as buprenorphine which may fail to respond adequately to treatment with naloxone.
It is equally effective as pethidine in suppressing shivering after surgery.
High blood pressure, panic attacks, tachycardia (rapid heart rate), tremor, sweating and vomiting may occur. Convulsions have been
Ephedrine ( /ɨˈfɛdrɪn/ or /ˈɛfɨdriːn/; not to be confused with ephedrone) is a sympathomimetic amine commonly used as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia.
Ephedrine is similar in structure to the (semi-synthetic) derivatives amphetamine and methamphetamine. Chemically, it is an alkaloid derived from various plants in the genus Ephedra (family Ephedraceae). It works mainly by increasing the activity of noradrenaline on adrenergic receptors. It is most usually marketed in the hydrochloride and sulfate forms.
In traditional Chinese medicine, the herb má huáng (麻黄, Ephedra sinica) contains ephedrine and pseudoephedrine as its principal active constituents. The same is true of other herbal products containing extracts from some of the other Ephedra species.
Ephedrine exhibits optical isomerism and has two chiral centres, giving rise to four stereoisomers. By convention the pair of enantiomers with the stereochemistry (1R,2S and 1S,2R) is designated ephedrine, while the pair of enantiomers with the stereochemistry (1R,2R and 1S,2S) is called pseudoephedrine.
Ephedrine is a substituted amphetamine and a
Nitrofurantoin is an antibiotic which is marketed under the following brand names; Niftran, Furadantin, Furabid, Macrobid, Macrodantin, Nitrofur Mac, Nitro Macro, Nifty-SR, Martifur-MR, Martifur-100 (in India), Urantoin, Nifuran (in Macedonia) and Uvamin (in Middle East). It is usually used in treating urinary tract infection. It is often used against E. coli.
Resistance to other antibiotics has led to increased interest in this agent.
It is sometimes described as being appropriate to use in pregnant patients (along with other agents such as sulfisoxazole or cephalexin). This is in contrast to agents such as trimethoprim and ciprofloxacin which may not be appropriate for pregnant women.
Organisms are said to be susceptible to nitrofurantoin if their minimum inhibitory concentration (MIC) is 32 μg/mL or less. The peak blood concentration of nitrofurantoin following an oral dose of nitrofurantoin 100 mg, is less than 1 μg/mL and may be undetectable; tissue penetration is negligible; the drug is well concentrated in the urine: 75% of the dose is rapidly metabolised by the liver, but 25% of the dose is excreted in the urine unchanged, reliably achieving levels of 200 μg/ml or more. For
Oxytetracycline was the second of the broad-spectrum tetracycline group of antibiotics to be discovered.
Oxytetracycline works by interfering with the ability of bacteria to produce essential proteins. Without these proteins, the bacteria cannot grow, multiply and increase in numbers. Oxytetracycline therefore stops the spread of the infection and the remaining bacteria are killed by the immune system or eventually die.
Oxytetracycline is a broad-spectrum antibiotic, active against a wide variety of bacteria. However, some strains of bacteria have developed resistance to this antibiotic, which has reduced its effectiveness for treating some types of infections.
Oxytetracycline is still used to treat infections caused by Chlamydia (e.g. the chest infection psittacosis, the eye infection trachoma, and the genital infection urethritis) and infections caused by Mycoplasma organisms (e.g. pneumonia).
Oxytetracycline is also used to treat acne, due to its activity against the bacteria on the skin that cause acne (Propionibacterium acnes). It is used to treat flare-ups of chronic bronchitis, due to its activity against the bacteria usually responsible, Haemophilus
Pantoprazole (sold under various brand names including Somac, Tecta, Pantoloc, Protium, Protonix, Pantecta, Pantoheal, Pantpas, Ppi-40, and Neoppi) is a proton pump inhibitor drug that inhibits gastric acid secretion.
Pantoprazole is used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. Initial treatment is generally of eight weeks' duration, after which another eight week course of treatment may be considered if necessary. It can be used as a maintenance therapy for long term use after initial response is obtained.
This medication may affect the results of certain lab tests, such as drug screenings (pantoprazole can cause a false positive for THC, the psychoactive component of cannabis.
Pantoprazole is metabolized in the liver by the cytochrome P450 system. Metabolism mainly consists of demethylation by CYP2C19 followed by sulfation. Another metabolic pathway is oxidation by CYP3A4. Pantoprazole metabolites are not thought to have any pharmacological significance. Pantoprazole is relatively free of drug interactions; however, it may alter the absorption of other medications that depend on the amount of acid in the
Sertindole (brand names: Serdolect, and Serlect) is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company H. Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. It is classified chemically as a phenylindole derivative.
Sertindole is not approved for use in the United States.
Sertindole has restricted receptor and brain site activity. It mainly affects dopamine D2, serotonin 5-HT2 and α1-adrenergic receptors. The effect on D2 receptors is more pronounced in the limbic dopamine system compared with the nigrostriatal system. This is supported by findings from clinical trials that provide evidence for significantly fewer extra pyramidal side effects than haloperidol and olanzapine. Weight gain is moderate, there is no diabetogenic effect, or effects on cholesterol and triglycerides, or prolactin blood levels reported. Sertindole has been shown to block hERG in the low nanomolar range.
In contrast to other antipsychotics, sertindole is not associated with sedative effects; sedation may add to the
Metronidazole (INN) ( /mɛtrəˈnaɪdəzoʊl/) (Flagyl, and others) is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. Metronidazole is an antibiotic, amebicide, and antiprotozoal. It is the drug of choice for first episodes of mild-to-moderate Clostridium difficile infection. It is marketed in the U.S.A. by Pfizer and globally by Sanofi under the trade name Flagyl, and is also sold under other brand names. Metronidazole was developed in 1960.
Metronidazole is used also as a gel preparation in the treatment of the dermatological conditions such as rosacea (Rozex and MetroGel by Galderma) and fungating tumours (Anabact, Cambridge Healthcare Supplies).
Metronidazole is indicated for the treatment of:
Metronidazole has also been used in women to prevent preterm birth associated with bacterial vaginosis, amongst other risk factors including the presence of cervicovaginal fetal fibronectin (fFN). A randomised controlled trial demonstrated that metronidazole was ineffective in preventing preterm delivery in high-risk pregnant women and, conversely, the incidence of preterm delivery was actually higher in women treated with metronidazole.
In a study
Marketed formulations:Propafenone hydrochloride 225 film coated tablet
Propafenone ( /proʊˈpæfɨnoʊn/ proh-PAF-i-nohn; brand name Rythmol SR or Rytmonorm) is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.
Propafenone works by slowing the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitability of the cells. Propafenone is more selective for cells with a high rate, but also blocks normal cells more than class Ia or Ib. Propafenone differs from the prototypical class Ic antiarrhythmic in that it has additional activity as a beta-adrenergic blocker which can cause bradycardia and bronchospasm.
Propafenone is metabolized primarily in the liver. Because of its short half-life, it requires dosing two or three times daily to maintain steady blood levels. The long-term safety of propafenone is unknown. Because it is structurally similar to another anti-arrhythmic medicine, flecainide, similar cautions should be exercised in its use. Flecainide and propafenone, like other antiarrhythmic drugs have been shown to increase the occurrence of arrhythmias (5.3% for propafenone, Teva physician prescribing information), primarily in patients with
Marketed formulations:Albuterol sulfate 4 extended release film coated tablet
Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names.
Salbutamol was the first selective β2-receptor agonist to be marketed — in 1968. It was first sold by Allen & Hanburys under the brand name Ventolin. The drug was an instant success, and has been used for the treatment of asthma ever since.
Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebulizer or other proprietary delivery devices (e.g. Rotahaler or Autohaler). In these forms of delivery, the maximal effect of salbutamol can take place within five to 20 minutes of dosing, though some relief is immediately seen. It can also be given orally, as an inhalant, or intravenously.
Salbutamol is typically used to treat bronchospasm (due to either allergen asthma or exercise-induced), as well as chronic obstructive pulmonary disease.
Other uses include in cystic fibrosis, along with ipratropium bromide, acetylcysteine, and
Marketed formulations:Mirtazapine 45 film coated tablet
Mirtazapine (Remeron, Avanza, Zispin) is a noradrenergic and specific serotonergic antidepressant (NaSSA) which was introduced by Organon International in the United States in 1990 and is used primarily in the treatment of depression. It is also commonly used as an anxiolytic, hypnotic, antiemetic, and appetite stimulant. Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).
Mirtazapine's primary use is the treatment of major depressive disorder and other mood disorders.
However, it has also been found useful in alleviating the following conditions and may be prescribed off-label for their treatment:
Mirtazapine has had literature published on its efficacy in the experimental treatment of the following conditions:
In clinical studies, mirtazapine has been found to be an effective antidepressant with a generally tolerable side effect profile relative to other antidepressants.
In a major systematic review published in 2009 which compared the efficacy and tolerability of 12 popular antidepressants, mirtazapine was found to be superior to all of the included selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake
Dofetilide is a class III antiarrhythmic agent.
It is marketed under the trade name Tikosyn by Pfizer, and is available in the United States in capsules containing 125, 250, and 500 µg of dofetilide.
Due to the pro-arrhythmic potential of dofetilide, it is only available by prescription by physicians who have undergone specific training in the risks of treatment with dofetilide. In addition, it is only available by mail order or through specially trained local pharmacies to individuals who are prescribed dofetilide by a properly registered physician.
It is used for the maintenance of sinus rhythm in individuals prone to the formation of atrial fibrillation and flutter, and for the chemical cardioversion to sinus rhythm from atrial fibrillation and flutter.
The elimination half-life of dofetilide is roughly 10 hours, however this is variable based on many physiologic factors (most significantly creatinine clearance), and ranges from 4.8 to 13.5 hours.
Dofetilide works by selectively blocking the rapid component of the delayed rectifier outward potassium current (IKr).
This causes the refractory period of atrial tissue to increase, hence its effectiveness in the treatment of atrial
Suramin is a drug developed by Oskar Dressel and Richard Kothe of Bayer, Germany in 1916, and is still sold by Bayer under the brand name Germanin.
According to the National Cancer Institute there are no active clinical trials (as of April 1, 2008). Completed and closed clinical trials are listed here:
In addition to Germanin, the National Cancer Institute also lists the following "Foreign brand names": 309 F or 309 Fourneau, Bayer 205, Moranyl, Naganin, Naganine.
It is used for treatment of human sleeping sickness caused by trypanosomes.
It has been used in the treatment of onchocerciasis.
It has been investigated as treatment for prostate cancer.
The molecular formula of suramin is C51H34N6O23S6. It is a symmetric molecule in the center of which lies urea, NH-CO-NH. Suramin contains 8 benzene rings, 4 of which are fused in pairs (naphthalene), 4 amide groups in addition to the one of urea and six sulfonate groups. When given as drug it usually contains six sodium ions that form a salt with the six sulfonate groups.
Suramin is administered by a single weekly intravenous injection for six weeks. The dose per injection is 1 g.
The most frequent adverse reactions are nausea and
Marketed formulations:Divalproex sodium 125 coated pellets in capsule
Active moieties:Valproic acid
Valproic acid (VPA), an acidic chemical compound, has found clinical use as an anticonvulsant and mood-stabilizing drug, primarily in the treatment of epilepsy, bipolar disorder, and, less commonly, major depression. It is also used to treat migraine headaches and schizophrenia. VPA is a liquid at room temperature, but it can be reacted with a base such as sodium hydroxide to form the salt sodium valproate, which is a solid. The acid, salt, or a mixture of the two (valproate semisodium) are marketed under the various brand names Depakote, Depakote ER, Depakene, Depakene Crono (extended release in Spain), Depacon, Depakine, Valparin and Stavzor.
Approved uses of the various formulations vary by country; e.g., valproate semisodium is used as a mood stabilizer and also in the US as an anticonvulsant.
VPA is a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.
As an anticonvulsant, valproic acid is used to control absence seizures, tonic-clonic seizures (grand mal), complex partial seizures, juvenile myoclonic epilepsy, and the seizures associated with Lennox-Gastaut syndrome. It is also used in treatment of myoclonus. In some countries,
Estradiol (E2 or 17β-estradiol, also oestradiol) is a sex hormone. Estradiol is abbreviated E2 as it has two hydroxyl groups in its molecular structure. Estrone has one (E1) and estriol has three (E3). Estradiol is about 10 times as potent as estrone and about 80 times as potent as estriol in its estrogenic effect. Except during the early follicular phase of the menstrual cycle, its serum levels are somewhat higher than that of estrone during the reproductive years of the human female. Thus it is the predominant estrogen during reproductive years both in terms of absolute serum levels as well as in terms of estrogenic activity. During menopause, estrone is the predominant circulating estrogen and during pregnancy estriol is the predominant circulating estrogen in terms of serum levels. Estradiol is also present in males, being produced as an active metabolic product of testosterone. The serum levels of estradiol in males (14 - 55 pg/mL) are roughly comparable to those of postmenopausal women (
Naloxone is an opioid inverse agonist drug developed by Sankyo in the 1960s. Naloxone is a drug used to counter the effects of opiate overdose, for example heroin or morphine overdose. Naloxone is specifically used to counteract life-threatening depression of the central nervous system and respiratory system. Naloxone is also experimentally used in the treatment for congenital insensitivity to pain with anhidrosis (CIPA), an extremely rare disorder (1 in 125 million) that renders one unable to feel pain. It is marketed under various trademarks including Narcan, Nalone, and Narcanti, and has sometimes been mistakenly called "naltrexate." It is not to be confused with naltrexone, an opioid receptor antagonist with qualitatively different effects, used for dependence treatment rather than emergency overdose treatment.
Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system. Naloxone is a μ-opioid receptor competitive antagonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- and δ-opioid receptors.
Naloxone is synthesized from
Verapamil (brand names: Isoptin, Verelan, Verelan PM, Calan, Bosoptin, Covera-HS) is an L-type calcium channel blocker of the phenylalkylamine class. It has been used in the treatment of hypertension, angina pectoris, cardiac arrhythmia, and most recently, cluster headaches. It is also an effective preventive medication for migraine. Verapamil has also been used as a vasodilator during cryopreservation of blood vessels. It is a class IV antiarrhythmic, more effective than digoxin in controlling ventricular rate and was approved by the U.S. Food and Drug Administration (FDA) in March 1982.
Verapamil's mechanism in all cases is to block voltage-dependent calcium channels.
In cardiac pharmacology, calcium channel blockers are considered class IV antiarrhythmic agents. Since calcium channels are especially concentrated in the sinoatrial and atrio-ventricular nodes, these agents can be used to decrease impulse conduction through the AV node, thus protecting the ventricles from atrial tachyarrhythmias.
Calcium channels are also present in the smooth muscle that lines blood vessels. By relaxing the tone of this smooth muscle, calcium-channel blockers dilate the blood vessels. This has led
Marketed formulations:Atorvastatin calcium trihydrate 10 film coated tablet
Atorvastatin (INN) ( /əˌtɔrvəˈstætən/), marketed by Pfizer as a calcium salt under the trade name Lipitor, is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammatory and other mechanisms. Like all statins, atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.
Atorvastatin was first synthesized in 1985 by Bruce Roth of Parke-Davis Warner-Lambert Company (now Pfizer). The best selling drug in pharmaceutical history, sales of Lipitor since it was approved in 1996 exceed US$125 billion, and the drug has topped the list of best-selling branded pharmaceuticals in the world for nearly a decade. Generic atorvastatin, manufactured only by generic drugmakers Watson Pharmaceuticals and India's Ranbaxy Laboratories, became available in the United States on November 30, 2011, but prices for the generic version did not drop to the level of other generics—$10 or less for a month's supply—until other manufacturers were able to supply in May 2012.
The primary uses of atorvastatin is for the treatment of
Hydroxyzine ( /haɪˈdrɒksɨziːn/; sold as Vistaril, Atarax) is a first-generation antihistamine of the diphenylmethane and piperazine classes. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year, and is still in widespread use today.
Due to its antagonistic effects on several receptor systems in the brain, Hydroxyzine has strong anxiolytic and mild antiobsessive as well as antipsychotic properties. Today it is used primarily for the symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested. Because of its antihistamine effects it can also be used for the treatment of severe cases of itching, hyperalgesia and motion sickness-induced nausea. Even though it is an effective sedative, hypnotic, analgesic, and tranquilizer, it shares virtually none of the abuse, dependence, addiction, and toxicity potential of other drugs used for the same range of therapeutic reasons.
Hydroxyzine is used with opioid analgesics to increase the pain-killing ability of a given dose of opioid, reduce the quantity needed to stop a given level of
Midazolam ( /mɪˈdæzəlæm/, marketed in English-speaking countries under the trade names Dormicum, Hypnovel, and Versed, is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potent anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant, and sedative properties. Midazolam has a fast recovery time and is the most commonly used benzodiazepine as a premedication for sedation; less commonly it is used for induction and maintenance of anesthesia. Flumazenil, a benzodiazepine antagonist drug, can be used to treat an overdose of midazolam, as well as to reverse sedation. However, flumazenil can trigger seizures in mixed overdoses and in benzodiazepine-dependent individuals, so is not used in most cases.
Administration of midazolam by the intranasal or the buccal route (absorption via the gums and cheek) as an alternative to rectally administered diazepam is becoming increasingly popular for the emergency treatment of seizures in children. Midazolam is also used for
Paclitaxel is a mitotic inhibitor used in cancer chemotherapy. It was discovered in a U.S. National Cancer Institute program at the Research Triangle Institute in 1967 when Monroe E. Wall and Mansukh C. Wani isolated it from the bark of the Pacific yew tree, Taxus brevifolia and named it taxol. Later it was discovered that endophytic fungi in the bark synthesize paclitaxel.
When it was developed commercially by Bristol-Myers Squibb (BMS) the generic name was changed to paclitaxel and the BMS compound is sold under the trademark Taxol. In this formulation, paclitaxel is dissolved in Cremophor EL and ethanol, as a delivery agent. A newer formulation, in which paclitaxel is bound to albumin, is sold under the trademark Abraxane.
Paclitaxel is now used to treat patients with lung, ovarian, breast, head and neck cancer, and advanced forms of Kaposi's sarcoma. Paclitaxel is also used for the prevention of restenosis.
Paclitaxel stabilizes microtubules and as a result, interferes with the normal breakdown of microtubules during cell division. Together with docetaxel, it forms the drug category of the taxanes. It was the subject of a notable total synthesis by Robert A. Holton.
Phenacetin is an analgesic, once widely used; its use has declined because of its adverse effects.
Phenacetin was introduced in 1887, and was used principally as an analgesic; it was one of the first synthetic fever reducers to go on the market. It is also known historically to be one of the first non-opioid analgesics without anti-inflammatory properties.
Its analgesic effects are due to its actions on the sensory tracts of the spinal cord. In addition, phenacetin has a depressant action on the heart, where it acts as a negative inotrope. It is an antipyretic, acting on the brain to decrease the temperature set point. It is also used to treat rheumatoid arthritis (subacute type) and intercostal neuralgia.
It is metabolised in the body to paracetamol.
The first synthesis was reported in 1878 by Harmon Northrop Morse.
Phenacetin may be synthesized as an example of the Williamson ether synthesis: ethyl iodide, paracetamol, and anhydrous potassium carbonate are refluxed in 2-butanone to give the crude product, which is recrystallized from water.
Phenacetin was widely used until the third quarter of the twentieth century, often in the form of an "A.P.C." or aspirin-phenacetin-caffeine
Propofol (INN, marketed as Diprivan by AstraZeneca) is a short-acting, intravenously administered hypnotic agent. Its uses include the induction and maintenance of general anesthesia, sedation for mechanically ventilated adults, and procedural sedation. Propofol is also commonly used in veterinary medicine. Propofol is approved for use in more than 50 countries, and generic versions are available.
Chemically, propofol is unrelated to barbiturates and has largely replaced sodium thiopental (Pentothal) for induction of anesthesia because recovery from propofol is more rapid and "clear" when compared with thiopental. Propofol is not considered an analgesic, so opioids such as fentanyl may be combined with propofol to alleviate pain. Propofol has been referred to as "milk of amnesia" (a play on words of milk of magnesia), because of the milk-like appearance of its intravenous preparation.
Propofol is used for induction and maintenance of anesthesia, having largely replaced sodium thiopental for this indication. Propofol is also used to sedate individuals who are receiving mechanical ventilation. In critically ill patients propofol has been found to be superior to lorazepam both in
Marketed formulations:Sildenafil citrate 25 film coated tablet
Sildenafil citrate, sold as Viagra, Revatio and under various other trade names, is a drug used to treat erectile dysfunction and pulmonary arterial hypertension (PAH). It was originally developed by British scientists and then brought to market by the US-based pharmaceutical company Pfizer. It acts by inhibiting cGMP-specific phosphodiesterase type 5, an enzyme that promotes degradation of cGMP, which regulates blood flow in the penis. Since becoming available in 1998, sildenafil has been the prime treatment for erectile dysfunction; its primary competitors on the market are tadalafil (Cialis) and vardenafil (Levitra).
The primary indication of sildenafil is treatment of erectile dysfunction (inability to sustain a satisfactory erection to complete intercourse). Its use is now standard treatment for erectile dysfunction in all settings, including diabetes.
People on antidepressants may experience sexual dysfunction, either as a result of their illness or as a result of their treatment. A 2003 study showed that sildenafil improved sexual function in men in this situation. Following up reports from 1999, the same researchers found that sildenafil improved sexual function in female
Marketed formulations:Thioridazine hydrochloride 10 film coated tablet
Thioridazine (Mellaril, Novoridazine, Thioril) is a piperidine typical (but see next paragraph, below) antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. Due to concerns about cardiotoxicity and retinopathy at high doses this drug is not commonly prescribed, reserved for patients who have failed to respond to, or have contraindications for, more widely used antipsychotics. A serious side effect is the potentially fatal neuroleptic malignant syndrome. It exerts its actions through a central adrenergic-blocking, a dopamine-blocking, and minor anticholinergic activity.
In older references, it is sometimes described as atypical, but more recently it is usually described as typical, with the term "atypical" usually reserved for agents showing D4 selectivity or serotonin antagonism.
Previous additional indications were agitated depression, tension and anxiety linked to alcohol withdrawal and dysphoria of epileptic patients. It was even indicated in Europe for the treatment of psychosis in children and adolescents as Melleretten (10 mg to 60 mg daily).
It was also given off-label for the treatment of
Venlafaxine (brand name: Effexor or Efexor) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class. First introduced by Wyeth in 1993, now marketed by Pfizer, it is licensed for the treatment of major depressive disorder (MDD), as a treatment for generalized anxiety disorder, and comorbid indications in certain anxiety disorders with depression. In 2007, venlafaxine was the sixth most commonly prescribed antidepressant on the U.S. retail market, with 17.2 million prescriptions.
Venlafaxine is used primarily for the treatment of depression, general anxiety disorder, social phobia, panic disorder, and vasomotor symptoms.
At low doses (150 mg/day), it acts on serotonergic and noradrenergic systems, whereas at high doses (>300 mg/day), it also affects dopaminergic neurotransmission.
Multiple double blind studies show venlafaxine's effectiveness in treating depression. Venlafaxine has similar efficacy to the tricyclic antidepressants amitriptyline (Elavil) and imipramine, and is better tolerated than amitriptyline. Its efficacy is similar to or better than sertraline (Zoloft) and
Benzphetamine (Didrex) is an anorectic drug marketed under this brand in the USA by Pharmacia. Benzphetamine is used as a short term adjunct in management of exogenous obesity. It is closely related to amphetamine.
Benzphetamine is a sympathomimetic amine and is classified as an anorectic. The drug's main function is to reduce appetite, which in turn reduces caloric intake. Benzphetamine can cause vivid hallucinations if taken for the wrong purpose.
Although the mechanism of action of the sympathomimetic appetite suppressants in the treatment of obesity is not fully known, these medications have pharmacological effects similar to those of amphetamines. Amphetamine and related sympathomimetic medications (such as benzphetamine) are thought to stimulate the release of norepinephrine and/or dopamine from storage sites in nerve terminals of the lateral hypothalamic feeding center, thereby producing a decrease in appetite. This release is mediated through the binding of benzphetamine to VMAT2 and inhibiting its function, causing a release of these neurotransmitters into the synaptic cleft through their reuptake transporters. Tachyphylaxis and tolerance have been demonstrated with all
Celecoxib INN (/sɛlɨˈkɒksɪb/ SE-lə-KOK-sib) is a sulfa non-steroidal anti-inflammatory drug (NSAID) and selective COX-2 inhibitor used in the treatment of osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, and to reduce numbers of colon and rectum polyps in patients with familial adenomatous polyposis. It is marketed by Pfizer. It is known under the brand name Celebrex or Celebra for arthritis and Onsenal for polyps. Celecoxib is available by prescription in capsule form.
Celecoxib is licensed for use in osteoarthritis, rheumatoid arthritis, acute pain, painful menstruation and menstrual symptoms, ankylosing spondylitis and to reduce the number of colon and rectal polyps in patients with familial adenomatous polyposis. It was originally intended to relieve pain while minimizing the gastrointestinal adverse effects usually seen with conventional NSAIDs. In practice, its primary indication is in patients who need regular and long term pain relief; there is probably no advantage to using celecoxib for short term or acute pain relief over conventional NSAIDs, except in the situation where non-selective NSAIDs or aspirin cause cutaneous
Cisapride is a gastroprokinetic agent, a drug which increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It has been sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the U.S.). It was discovered by Janssen Pharmaceutica in 1980. In many countries, it has been either withdrawn from the market or had its indications limited because of side effects.
The commercial preparations of this drug are the racemic mixture of both enantiomers of the compound. The (+) enantiomer itself has the major pharmacologic effects and does not induce many of the detrimental side effects of the mixture.
Cisapride increases muscle tone in the esophageal sphincter in people with gastroesophageal reflux disease. It also increases gastric emptying in people with diabetic gastroparesis. It has been used to treat bowel constipation.
In many countries, it has been either withdrawn or had its indications limited because of reports of the side effect long QT syndrome, which predisposes to
Clonidine is a sympatholytic medication used to treat medical conditions, such as high blood pressure, some pain conditions, ADHD and anxiety/panic disorder. It is classified as a centrally acting α2 adrenergic agonist. An alternative hypothesis that has been proposed is that clonidine acts centrally as an imidazoline receptor agonist.
Clonidine has been investigated and prescribed first as an antihypertensive drug in the 1950s. It has found new uses later, including treatment of some types of neuropathic pain, opioid detoxification, sleep hyperhidrosis, and as veterinary anaesthetic drug. Clonidine is used to treat anxiety and panic disorder. It is also FDA approved to treat ADHD in an extended release form. It is becoming a more accepted treatment for insomnia, as well as for relief of menopausal symptoms.
Clonidine is increasingly used in conjunction with stimulants to treat attention-deficit hyperactivity disorder (ADHD), for which it is administered in late afternoon or evening for sleep, and because it sometimes helps moderate ADHD-associated impulsive and oppositional behavior, and may reduce tics, a problem in which a part of the body moves repeatedly and suddenly.
Dicyclomine, also known as dicycloverine, is an anticholinergic that blocks muscarinic receptors. Dicycloverine was first synthesized in the United States circa 1947.
Dicyclomine is used to treat intestinal hypermotility and the symptoms of Irritable Bowel Syndrome (IBS) (also known as spastic colon). It relieves muscle spasms and cramping in the gastrointestinal tract by blocking the activity of acetylcholine on cholinergic (or muscarinic) receptors on the surface of muscle cells. It is a smooth muscle relaxant.
in the UK it is ingredient of a multi-ingredient preparation, together with an antiflatulent (simethicone) and two antacids, under the trade name Kolanticon.
It is also marketed as Meftal-SPAS containing mefenamic acid along with dicyclomine hydrochloride as an analgesic and antispasmodic.
Dicyclomine can cause a range of anticholinergic side effects such as dry mouth, nausea, and, at higher doses, deliriant effects. Recreational use of this drug for its anticholinergic effects has been rarely reported.
Breastfeeding is not recommended while using this drug. Users should use care when operating vehicles and/or dangerous machines.
Tramadol hydrochloride (trademarked as Conzip, Ryzolt, Ultracet, Ultram in the USA, Ralivia and Zytram XL in Canada) is a centrally acting synthetic analgesic used to treat moderate to moderately-severe pain. The drug has a wide range of applications, including treatment of rheumatoid arthritis, restless legs syndrome and fibromyalgia. It was launched and marketed as Tramal by the German pharmaceutical company Grünenthal GmbH in 1977.
Tramadol is a very weak μ-opioid receptor agonist, induces serotonin release, and inhibits the reuptake of norepinephrine. Tramadol is converted to O-desmethyltramadol, a significantly more potent μ-opioid agonist. The opioid agonistic effect of tramadol and its major metabolite(s) is almost exclusively mediated by such μ-opioid receptors. This further distinguishes tramadol from opioids in general (including morphine), which do not possess tramadol's degree of receptor subtype selectivity and which are much stronger opiate-receptor agonists. Similarly, the habituating properties of tramadol (such as they are) are arguably mainly due to μ-opioid agonism with contributions from serotonergic and noradrenergic effects.
Tramadol is used similarly to
Trastuzumab (INN; trade name Herceptin) is a monoclonal antibody that interferes with the HER2/neu receptor. Its main use is to treat certain breast cancers.
The HER receptors are proteins that are embedded in the cell membrane and communicate molecular signals from outside the cell to inside the cell, and turn genes on and off. The HER proteins regulate cell growth, survival, adhesion, migration, and differentiation—functions that are amplified or weakened in cancer cells. In some cancers, notably some breast cancers, HER2 is over-expressed, and causes breast cells to reproduce uncontrollably.
Antibodies are molecules from the immune system that bind selectively to different proteins. Trastuzumab is an antibody that binds selectively to the HER2 protein. When it binds to defective HER2 proteins, the HER2 protein no longer causes cells in the breast to reproduce uncontrollably. This increases the survival of people with cancer. However, cancers usually develop resistance to trastuzumab.
The original studies of trastuzumab showed that it improved overall survival in late-stage (metastatic) breast cancer from 20.3 to 25.1 months, but there is controversy over whether trastuzumab is
Clindamycin rINN ( /klɪndəˈmaɪsɨn/) is a lincosamide antibiotic. It is usually used to treat infections with anaerobic bacteria but can also be used to treat some protozoal diseases, such as malaria. It is a common topical treatment for acne and can be useful against some methicillin-resistant Staphylococcus aureus (MRSA) infections.
The most severe common adverse effect of clindamycin is Clostridium difficile-associated diarrhea (the most frequent cause of pseudomembranous colitis). Although this side effect occurs with almost all antibiotics, including beta-lactam antibiotics, it is classically linked to clindamycin use.
Clindamycin is marketed under various trade names, including Dalacin, ''Daclin''. Combination products include Duac, BenzaClin, Clindoxyl and Acanya (in combination with benzoyl peroxide), and Ziana (with tretinoin). Clindamycin is also available as a generic drug.
Clindamycin is used primarily to treat anaerobic infections caused by susceptible anaerobic bacteria, including dental infections, and infections of the respiratory tract, skin and soft tissue infections, and peritonitis. In patients with hypersensitivity to penicillins, clindamycin may be used to
Heparin (from Ancient Greek ηπαρ (hepar), liver), also known as unfractionated heparin, a highly sulfated glycosaminoglycan, is widely used as an injectable anticoagulant, and has the highest negative charge density of any known biological molecule. It can also be used to form an inner anticoagulant surface on various experimental and medical devices such as test tubes and renal dialysis machines.
Although it is used principally in medicine for anticoagulation, its true physiological role in the body remains unclear, because blood anti-coagulation is achieved mostly by heparan sulfate proteoglycans derived from endothelial cells. Heparin is usually stored within the secretory granules of mast cells and released only into the vasculature at sites of tissue injury. It has been proposed that, rather than anticoagulation, the main purpose of heparin is defense at such sites against invading bacteria and other foreign materials. In addition, it is conserved across a number of widely different species, including some invertebrates that do not have a similar blood coagulation system.
Native heparin is a polymer with a molecular weight ranging from 3 kDa to 30 kDa, although the average
Ampicillin is a beta-lactam antibiotic that is part of the aminopenicillin family and is roughly equivalent to its successor, amoxicillin in terms of spectrum and level of activity. It can sometimes result in reactions that range in severity from a rash (in the case of patients that may unwittingly have mononucleosis) to potentially lethal allergic reactions such as anaphylaxis. However, as with other penicillin drugs, it is relatively non-toxic and adverse effects of a serious nature are encountered only rarely.
Belonging to the penicillin group of beta-lactam antibiotics, ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin only by the presence of an amino group. That amino group helps the drug penetrate the outer membrane of gram-negative bacteria.
Ampicillin acts as a competitive inhibitor of the enzyme transpeptidase, which is needed by bacteria to make their cell walls. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis. Ampicillin has received FDA approval for its mechanism of action.
Ampicillin, like other β-lactam antibiotics, not only blocks the
Aripiprazole ( /ˌɛərɨˈpɪprəzoʊl/ AIR-i-PIP-rə-zohl; brand names: Abilify, Aripiprex) is a partial dopamine agonist of the third generation class of atypical antipsychotics with additional antidepressant properties that is used in the treatment of schizophrenia, bipolar disorder, and clinical depression. It was approved by the US Food and Drug Administration (FDA) for schizophrenia on November 15, 2002 and the European Medicines Agency on 4 June 2004; for acute manic and mixed episodes associated with bipolar disorder on October 1, 2004; as an adjunct for major depressive disorder on November 20, 2007; and to treat irritability in children with autism on 20 November 2009. Aripiprazole was developed by Otsuka in Japan, and in the United States, Otsuka America markets it jointly with Bristol-Myers Squibb.
Aripiprazole is used for the treatment of schizophrenia or bipolar disorder.
In the United States, the FDA has approved aripiprazole for the treatment of schizophrenia in adults and adolescents (aged 13–17), of manic and mixed episodes associated with Bipolar I Disorder with or without psychotic features in adults, children and adolescents (aged 10–17), of irritability associated
Dehydroepiandrosterone (DHEA; brand name Fidelin), also known as androstenolone or prasterone (INN), as well as 3β-hydroxyandrost-5-en-17-one or 5-androsten-3β-ol-17-one, is an important endogenous steroid hormone. It is the most abundant circulating steroid in humans, in whom it is produced in the adrenal glands, the gonads, and the brain, where it functions predominantly as a metabolic intermediate in the biosynthesis of the androgen and estrogen sex steroids. However, DHEA also has a variety of potential biological effects in its own right, binding to an array of nuclear and cell surface receptors, and acting as a neurosteroid.
In women with adrenal insufficiency and the healthy elderly there is insufficient evidence to support the use of DHEA.
Evidence is inconclusive in regards to the effect of DHEA on strength in the elderly.
In middle-aged men, no statistically significant effect of DHEA supplementation on lean body mass, strength, or testosterone levels was found in a randomized placebo-controlled trial.
DHEA supplementation has not been found to be useful for memory function in normal middle aged or older adults. It has been studied as a treatment for Alzheimer's disease,
Diphenhydramine ( /ˌdaɪfɛnˈhaɪdrəmiːn/; abbreviated DPH, sometimes DHM) is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason is often used as a non-prescription sleep aid; especially in the form of diphenhydramine citrate. It is produced and marketed under the trade name Benadryl by McNeil-PPC (a division of Johnson & Johnson) in the U.S., Canada and South Africa (other trade names in other countries: Dimedrol, Daedalon). It is also available as a generic or store brand medication. It is also found in the name-brand products Nytol, Unisom, Tylenol PM, Excedrin PM, Midol PM, Zzzquil and Advil PM, though some Unisom products contain doxylamine instead. It is available as an over-the-counter (OTC) or prescribed HCl injectable. It may also be used for the treatment of extrapyramidal side-effects of many antipsychotics, such as the tremors that haloperidol can cause. In addition, injectable diphenhydramine can be used for life-threatening reactions (anaphylaxis) to allergens
Fludrocortisone (also called 9α-fluorocortisol or 9α-fluorohydrocortisone) is a synthetic corticosteroid with moderate glucocorticoid potency and much greater mineralocorticoid potency. The brand name in the U.S. and Canada is Florinef.
Fludrocortisone has been used in the treatment of cerebral salt wasting. It is used primarily to replace the missing hormone aldosterone in various forms of adrenal insufficiency such as Addison's disease and the classic salt wasting (21-hydroxylase deficiency) form of congenital adrenal hyperplasia. Fludrocortisone is the first line of treatment for orthostatic intolerance and Postural Tachycardia Syndrome as well.
Fludrocortisone is also a confirmation test for diagnosing Conns Syndrome (aldosterone producing-adrenal adenoma), the fludrocortisone suppression test. Loading the patient with fludrocortisone would suppress serum aldosterone level in a normal patient, whereas the level will not be altered in a Conns patient. Its effects on increasing Na+ levels, and therefore blood volume, make it useful as an off label treatment for postural orthostatic tachycardia syndrome (POTS)
Fludrocortisone is available in 0.1 mg tablets. Typical daily doses for
Marketed formulations:Glimepiride 2 film coated tablet
Glimepiride is a medium- to long-acting sulfonylurea antidiabetic drug. It is marketed as Amaryl by Sanofi-Aventis, GLIMPID by Ranbaxy Laboratories(Cardiovascular) and GLIMY by Dr.Reddy's Labs.
It is sometimes classified as either the first third-generation sulfonylurea, or as second-generation.
Glimepiride is indicated to treat type 2 diabetes mellitus; its mode of action is to increase insulin production by the pancreas. It is not used for type 1 diabetes because the pancreas is no longer able to produce insulin.
Its use is contraindicated in patients with hypersensitivity to glimepiride or other sulfonylureas, and during pregnancy.
Side effects from taking glimepiride include gastrointestinal tract (GI) disturbance, and rarely thrombocytopenia, leukopenia, hemolytic anemia, and occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased. Alcohol consumption and exposure to sunlight should be restricted in patients taking it because they can worsen the side effects.
With glimepiride, GI absorption is complete, with no interference of meals. Significant absorption was seen within 1 hour, and distributed throughout the body,
Mefloquine hydrochloride (Lariam, Mephaquin or Mefliam) is an orally administered medication used in the prevention and treatment of malaria. Mefloquine was developed in the 1970s at the United States Department of Defense's Walter Reed Army Institute of Research as a synthetic analogue of quinine. The brand name drug, Lariam, is manufactured by the Swiss company Hoffmann–La Roche. In August 2009, Roche stopped marketing Lariam in the United States. Generic mefloquine from other manufacturers is still widely available. Rare but serious neuropsychiatric problems have been associated with its use.
Mefloquine is used to both prevent and treat certain forms of malaria.
Mefloquine is useful for the prevention of malaria in all areas except for those where parasites may have resistance to multiple drugs. It is typically taken for one to two weeks before entering an area with malaria. Doxycycline and atovaquone/proguanil provide protection within one to two days and may be better tolerated. If a person becomes ill with malaria despite prophylaxis with mefloquine, the use of halofantrine and quinine for treatment may be ineffective.
Once a person has contracted malaria, mefloquine is
Marketed formulations:Minocycline hydrochloride 75 film coated tablet
Minocycline (INN) is a broad-spectrum tetracycline antibiotic, and has a broader spectrum than the other members of the group. It is a bacteriostatic antibiotic, classified as a long-acting type. As a result of its long half-life it generally has serum levels 2–4 times that of the simple water-soluble tetracyclines (150 mg giving 16 times the activity levels compared with 250 mg of tetracycline at 24–48 hours).
Minocycline is the most lipid-soluble of the tetracycline-class antibiotics, giving it the greatest penetration into the prostate and brain, but also the greatest amount of central nervous system (CNS)-related side effects, such as vertigo. A common side effect is diarrhea. Uncommon side effects (with prolonged therapy) include skin discolouration and autoimmune disorders that are not seen with other drugs in the class.
Minocycline is a relatively poor tetracycline-class antibiotic choice for urinary pathogens sensitive to this antibiotic class, as its solubility in water, and levels in the urine, are less than all other tetracyclines. Minocycline is metabolized by the liver and has poor urinary excretion.
Minocycline is not a naturally-occurring antibiotic, but was
Pimozide (Teva's Orap) is an antipsychotic drug of the diphenylbutylpiperidine class. It was discovered at Janssen Pharmaceutica in 1963. It has a high potency compared to chlorpromazine (ratio 50-70:1). On a weight basis it is even more potent than haloperidol. It also has special neurologic indications for Tourette syndrome and resistant tics. The side effects include akathisia, tardive dyskinesia, and, more rarely, neuroleptic malignant syndrome and prolongation of the QT interval.
Pimozide is used in its oral preparation in schizophrenia and chronic psychosis (on-label indications in Europe only), Tourette syndrome and resistant tics (Europe, USA and Canada). In Germany the 1 mg tablet is indicated for the treatment of some forms of reactive depression.
Pimozide has been used in the treatment of delusional disorder and paranoid personality disorder.
It has been used for delusions of parasitosis.
Use as a Listeria monocytogenes inhibitor has been described.
Plasma levels of pimozide can vary widely between patients, and in insufficient response therapeutic drug monitoring may be required to ascertain that the patient is developing adequate plasma levels before withdrawing the
Sertraline hydrochloride (trade names Zoloft and Lustral, among others) is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It was discovered by Pfizer. Sertraline is primarily used to treat major depression in adult outpatients as well as obsessive–compulsive, panic, and social anxiety disorders in both adults and children. In 2007, it was the most prescribed antidepressant on the U.S. retail market, with 29,652,000 prescriptions.
The efficacy of sertraline for depression is similar to that of older tricyclic antidepressants, but its side effects are much less pronounced. Differences with newer antidepressants are subtler and also mostly confined to side effects. Evidence suggests that sertraline may work better than fluoxetine (Prozac) for some subtypes of depression. Cognitive behavioral therapy in combination with sertraline is a better treatment for obsessive-compulsive disorder than sertraline alone. Although approved for social phobia and posttraumatic stress disorder, sertraline leads to only modest improvement in these conditions. Sertraline also alleviates the symptoms of premenstrual dysphoric disorder and can be used in sub-therapeutic doses
Xylometazoline (also known as xylomethazoline) is a drug which is used as a topical nasal decongestant. It is applied directly into the nose, either as a spray or as drops.
Xylometazoline is marketed under many brand names (see below), with the typical adult solution strength being 0.1% w/v xylometazoline, and the dose for children under 12 being 0.05%.
It should not be used for too long a period of time, or rebound effect may occur after discontinuation (see: Rhinitis medicamentosa).
The drug works by constricting the blood vessels in the nose. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made. (If the colour of the nasal passage is observed, it is visibly paler after dosage.)
Xylometazoline is an imidazole derivative which is designed to mimic the molecular shape of adrenaline. It binds to alpha-adrenergic receptors in the nasal mucosa. Due to its sympathomimetic effects, it should not be used by people with high blood pressure, or other heart problems.
Extended usage of xylometazoline can result in decreased effectiveness or a build up of tolerance against the drug. The number of receptors
Marketed formulations:Amphotericin b 5 injectable lipid complex
Active moieties:Amphotericin B
Amphotericin B (Fungilin, Fungizone, Abelcet, AmBisome, Fungisome, Amphocil, Amphotec) is a polyene antifungal drug, often used intravenously for systemic fungal infections. It was originally extracted from Streptomyces nodosus, a filamentous bacterium, in 1955 at the Squibb Institute for Medical Research from cultures of an undescribed streptomycete isolated from the soil collected in the Orinoco River region of Venezuela. Its name originates from the chemical's amphoteric properties. Two amphotericins, amphotericin A and amphotericin B are known, but only B is used clinically, because it is significantly more active in vivo. Amphotericin A is almost identical to amphotericin B (having a double C=C bond between the 27th and 28th carbons), but has little antifungal activity. Currently, the drug is available as plain amphotericin B, as a cholesteryl sulfate complex (ABCD), as a lipid complex (ABLC), and as a liposomal formulation (LAmB). The latter formulations have been developed to improve tolerability for the patient, but may show considerably different pharmacokinetic characteristics compared to plain amphotericin B.
The natural route to synthesis includes polyketide synthase
Benzocaine is a local anesthetic commonly used as a topical pain reliever or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is also combined with antipyrine to form A/B Otic Drops to relieve ear pain and remove earwax.
Benzocaine is the ethyl ester of p-aminobenzoic acid (PABA). It can be prepared from PABA and ethanol by Fischer esterification or via the reduction of ethyl p-nitrobenzoate. Benzocaine is sparingly soluble in water; it is more soluble in dilute acids and very soluble in ethanol, chloroform and ethyl ether. The melting point of benzocaine is 88-90 degrees Celsius, and the boiling point is about 310 °C. The density of benzocaine is 1.17 g/cm.
Benzocaine was first synthesized in 1890 by the German chemist Eduard Ritsert (1859-1946), in the town of Eberbach and introduced to the market in 1902 under the name "Anästhesin".
Pain is caused by the stimulation of free nerve endings. When the nerve endings are stimulated, sodium enters the neuron, causing depolarization of the nerve and subsequent initiation of an action potential. The action potential is propagated down the nerve toward the
Fluvastatin (trade names Lescol, Canef, Vastin) is a member of the drug class of statins, used to treat hypercholesterolemia and to prevent cardiovascular disease.
It has also been shown to exhibit antiviral activity against Hepatitis C in a study with 31 patients. This effect has been described as modest, variable, and often short-lived by the authors.
Halothane (trademarked as Fluothane) is an inhalational general anesthetic. Its IUPAC name is 2-bromo-2-chloro-1,1,1-trifluoroethane. It is the only inhalational anesthetic agent containing a bromine atom; there are several other halogenated anesthesia agents which lack the bromine atom and do contain the fluorine and chlorine atoms present in halothane. It is colorless and pleasant-smelling, but unstable in light. It is packaged in dark-colored bottles and contains 0.01% thymol as a stabilizing agent. Halothane is a core medicine in the World Health Organization's "Essential Drugs List", which is a list of minimum medical needs for a basic health care system. Its use in developed countries, however, has been almost entirely superseded by newer inhalational anaesthetic agents.
It is a potent anesthetic with a minimum alveolar concentration of 0.74. Its blood/gas partition coefficient of 2.4 makes it an agent with moderate induction and recovery time. It is not a good analgesic and its muscle relaxation effect is moderate.
This halogenated hydrocarbon was first synthesized by C. W. Suckling of Imperial Chemical Industries (ICI) in 1951 and was first used clinically by M. Johnstone
Marketed formulations:Levetiracetam 500 extended release film coated tablet
Levetiracetam (INN) ( /lɛvɨtɪˈræsɨtæm/) is an anticonvulsant medication used to treat epilepsy. It is the S-enantiomer of etiracetam, structurally similar to the prototypical nootropic drug piracetam.
Levetiracetam is marketed under the trade name Keppra. Keppra is manufactured by UCB Pharmaceuticals Inc. Since November 2008 the drug has been available as a generic brand in the United States.
Levetiracetam has been approved in the European Union as a monotherapy treatment for epilepsy in the case of partial seizures, or as an adjunctive therapy for partial, myoclonic and tonic-clonic seizures. It is also used in veterinary medicine for similar purposes.
Levetiracetam has potential benefits for other psychiatric and neurologic conditions such as Tourette syndrome, Alzheimer's Disease, autism, bipolar disorder and anxiety disorder. However, its most serious adverse effects are behavioral, and its benefit-risk ratio in these conditions is not well understood.
Along with other anticonvulsants like gabapentin, it is also sometimes used to treat neuropathic pain. It has not been found to be useful for essential tremors.
Levetiracetam is generally well tolerated, but may cause drowsiness,
Morphine (INN) ( /ˈmɔrfiːn/; MS Contin, MSIR, Avinza, Kadian, Oramorph, Roxanol, Kapanol) is a potent opiate analgesic drug that is used to relieve severe pain. It was first isolated in 1804 by Friedrich Sertürner, first distributed by him in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more widely used after the invention of the hypodermic needle in 1857. It took its name from the Greek god of dreams Morpheus (Greek: Μορφέας).
Morphine is the most abundant alkaloid found in opium, the dried sap (latex) derived from shallowly slicing the unripe seedpods of the opium, or common and/or edible, poppy, Papaver somniferum. Morphine was the first active principle purified from a plant source and is one of at least 50 alkaloids of several different types present in opium, poppy straw concentrate, and other poppy derivatives. Morphine is generally 8 to 14 percent of the dry weight of opium, although specially bred cultivars reach 26 percent or produce little morphine at all, under 1 percent, perhaps down to 0.04 percent. The latter varieties, including the 'Przemko' and 'Norman' cultivars of the opium poppy, are used to
Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eyedrops. The discovery of neomycin dates back to 1949. It was discovered in the lab of Selman Waksman, who was later awarded the Nobel Prize in Physiology and medicine in 1951. Neomycin belongs to aminoglycoside class of antibiotics that contain two or more aminosugars connected by glycosidic bonds. Neamine (two rings), ribostamycin (three rings), paromomycin (four rings), and lividomycin (five rings) are some other examples of aminoglycosides. They have shown tremendous potential as antibacterials. One of them, gentamicin, has been used extensively in clinical practice. Due to the inherent oto- and nephrotoxicity of these substances, systemic use has declined, as safer alternatives have become available.
Neomycin is overwhelmingly used as a topical preparation, such as Neosporin. It can also be given orally, where it is usually combined with other antibiotics. Neomycin is not absorbed from the gastrointestinal tract and has been used as a preventive measure for hepatic encephalopathy and hypercholesterolemia. By killing bacteria in the intestinal tract, it keeps ammonia
Tacrolimus (also FK-506 or fujimycin, trade names Prograf, Advagraf, Protopic) is an immunosuppressive drug that is mainly used after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, and the skin condition vitiligo.
It is a 23-membered macrolide lactone discovered in 1984 from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. It reduces interleukin-2 (IL-2) production by T-cells.
Tacrolimus was discovered in 1984; it was among the first macrolide immunosuppressants discovered, preceded by the discovery of rapamycin (sirolimus) on Rapa Nui (Easter Island) in 1975. It is produced by a type of soil bacterium, Streptomyces tsukubaensis. The name tacrolimus is derived from 'Tsukuba macrolide immunosuppressant'.
Tacrolimus was first approved by the Food and Drug Administration (FDA) in 1994 for use in liver transplantation; this has been extended to include kidney, heart, small
Tetracycline (INN) ( /ˌtɛtrəˈsaɪkliːn/) is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Tetracyclines bind to the 30S subunit of microbial ribosomes. They inhibit protein synthesis by blocking the attachment of charged aminoacyl-tRNA to the A site on the ribosome. Thus, they prevent introduction of new amino acids to the nascent peptide chain. The action is usually inhibitory and reversible upon withdrawal of the drug. Resistance to the tetracyclines results
Adenosine (ADO) is a purine nucleoside comprising a molecule of adenine attached to a ribose sugar molecule (ribofuranose) moiety via a β-N9-glycosidic bond. In the USA, it is marketed as Adenocard.
Adenosine plays an important role in biochemical processes, such as energy transfer—as adenosine triphosphate (ATP) and adenosine diphosphate (ADP)—as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter, believed to play a role in promoting sleep and suppressing arousal, with levels increasing with each hour an organism is awake.
Adenosine is an endogenous purine nucleoside that modulates many physiological processes. Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3).
Extracellular adenosine concentrations from normal cells are approximately 300 nM; however, in response to cellular damage (e.g. in inflammatory or ischemic tissue), these concentrations are quickly elevated (600–1,200 nM). Thus, in regard to stress or injury, the function of adenosine is primarily that of cytoprotection preventing tissue damage during instances of hypoxia, ischemia, and seizure
Alprazolam /ælˈpræzəlæm/ (trade name Xanax, available among other generic names) is a short-acting anxiolytic of the benzodiazepine class of psychoactive drugs. Alprazolam, like other benzodiazepines, binds to specific sites on the GABAA gamma-amino-butyric acid receptor. Alprazolam is commonly used and FDA approved for the medical treatment of panic disorder, and anxiety disorders, such as generalized anxiety disorder (GAD) or social anxiety disorder (SAD). Alprazolam is available for oral administration in compressed tablet (CT) and extended-release capsule (XR) formulations. Alprazolam possesses anxiolytic, sedative, hypnotic, skeletal muscle relaxant, anticonvulsant, and amnestic properties.
Alprazolam has a fast onset of action and symptomatic relief. Ninety percent of peak benefits are achieved within the first hour (Although onset may begin at 8-25 minutes of ingestion) of using either preparation for panic disorder, and full peak benefits are achieved in 1.5 and 1.6 hours respectively. Peak benefits achieved for generalized anxiety disorder (GAD) may take up to a week. Tolerance does not appear to develop to the anxiolytic effects but may develop to the sedative effects
Bromocriptine (INN; trade names Parlodel, Cycloset), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes.
Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug. Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal. In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset (VeroScience). It is currently unknown how this drug improves glycemic control, but it has been shown to reduce HbA1c by ~0.5 percentage points.
Bromocriptine is a potent agonist at dopamine D2 receptors and various serotonin receptors. It also inhibits the release of glutamate, by reversing the glutamate GLT1 transporter.
Bromocriptine agonizes the following monoamine receptors:
Other properties for serotonin are yet unknown.
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through
Carbamazepine (CBZ) is an anticonvulsant and mood-stabilizing drug used primarily in the treatment of epilepsy and bipolar disorder, as well as trigeminal neuralgia. It is also used off-label for a variety of indications, including attention-deficit hyperactivity disorder (ADHD), schizophrenia, phantom limb syndrome, complex regional pain syndrome, paroxysmal extreme pain disorder, neuromyotonia, intermittent explosive disorder, borderline personality disorder, and post-traumatic stress disorder.
It has been seen as safe for pregnant women to use carbamazepine as a mood stabilizer, but, like other anticonvulsants, intrauterine exposure is associated with spina bifida and neurodevelopmental problems.
Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. It may be used as a second line treatment for bipolar disorder and along with antipsychotic agents in schizophrenia.
In the United States, the FDA-approved indications are epilepsy (including partial seizures and tonic-clonic seizures), trigeminal neuralgia, and manic and mixed episodes of bipolar I disorder. Although data are still lacking, carbamazepine appears to be as effective and safe as
Carbamide peroxide (CH6N2O3), also called urea peroxide, urea hydrogen peroxide (UHP), and percarbamide, is an adduct of hydrogen peroxide and urea.
Like hydrogen peroxide, carbamide peroxide is an oxidizer. This compound is a white crystalline solid which dissolves in water to give free hydrogen peroxide; the solubility of commercial samples varies from 0.05 g/mL to more than 0.6 g/mL. The solid state structure of this adduct at the right has been determined by neutron diffraction.
This compound is cheaply available; it is produced on a scale of several hundred tonnes a year by the dissolution of urea in excess concentrated hydrogen peroxide solution, followed by crystallization. The laboratory synthesis is analogous.
Carbamide peroxide is mainly used as a disinfecting and bleaching agent in cosmetics and pharmaceuticals. As a drug, this compound is used in some preparations for the whitening of teeth. It is also used to relieve minor inflammation of gums, oral mucosal surfaces and lips including canker sores and dental irritation, and to emulsify and disperse ear wax.
In tooth bleaching, the hydrogen peroxide produced acts to oxidise interprismatic extrinsic staining within tooth
Chlorphenamine (INN) or chlorpheniramine (USAN, former BAN), commonly marketed in the form of chlorpheniramine maleate (Chlorphen-12), is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria. Its sedative effects are relatively weak compared to other first-generation antihistamines. Chlorphenamine is one of the most commonly used antihistamines in small-animal veterinary practice as well. Although not generally approved as an antidepressant or anti-anxiety medication, chlorphenamine appears to have these properties as well (see below).
Chlorphenamine is part of a series of antihistamines including pheniramine (Naphcon) and its halogenated derivatives and others including fluorpheniramine, dexchlorpheniramine (Polaramine), brompheniramine (Dimetapp), dexbrompheniramine (Drixoral), deschlorpheniramine, dipheniramine (also known as triprolidine with the trade name Actifed), and iodopheniramine.
The halogenated alkylamine antihistamines all exhibit optical isomerism, and chlorphenamine in the indicated products is racemic chlorphenamine maleate, whereas dexchlorpheniramine is the dextrorotary
Ciprofloxacin (INN) is a synthetic antibiotic of the fluoroquinolone drug class. It is a second-generation fluoroquinolone antibacterial. It kills bacteria by interfering with the enzymes that cause DNA to rewind after being copied, which stops synthesis of DNA and of protein.
Ciprofloxacin was first patented in 1983 by Bayer A.G. and subsequently approved by the U.S. Food and Drug Administration (FDA) in 1987. Ciprofloxacin has 12 FDA-approved human uses and other veterinary uses, but it is often used for unapproved uses (off-label). Ciprofloxacin interacts with other drugs, herbal and natural supplements, a characteristic it shares with other widely used antibacterial drugs such as amoxicillin, trimethoprim, azithromycin, cephalexin, and doxycycline.
As of 2011 the FDA has added two black box warnings for this drug in reference to spontaneous tendon ruptures and the fact that ciprofloxacin may cause worsening of myasthenia gravis symptoms, including muscle weakness and breathing problems. Such an adverse reaction is a potentially life-threatening event and may require ventilatory support.
Ciprofloxacin is used to treat a number of infections including: infections of bones and
Diethylcarbamazine (DEC) is an anthelmintic drug that does not resemble other antiparasitic compounds. It is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements.
DEC is indicated for treatment of individual patients with certain filarial diseases. These diseases include: lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori; tropical pulmonary eosinophilia, and loiasis.
In cases of onchocerciasis, another common filarial parasite, the drug is not used. This is because of the intense and unbearable itching associated with the dead subcutaneous parasites.
DEC continues to be the mainstay for treatment of patients with lymphatic filariasis and loiasis. DEC is also used in the prevention of dog heartworm Dirofilaria immitis.
DEC is an inhibitor of arachidonic acid metabolism in filarial microfilaria. This makes the microfilaria more susceptible to immune attack.
Epinephrine (also known as adrenaline or adrenalin) is a hormone and a neurotransmitter. Epinephrine has many functions in the body, regulating heart rate, blood vessel and air passage diameters, and metabolic shifts; epinephrine release is a crucial component of the fight-or-flight response of the sympathetic nervous system. In chemical terms, epinephrine is one of a group of monoamines called the catecholamines. It is produced in some neurons of the central nervous system, and in the chromaffin cells of the adrenal medulla from the amino acids phenylalanine and tyrosine.
This chemical is widely referred to as "adrenaline" outside the United States; however, its United States Adopted Name and International Nonproprietary Name is epinephrine. Epinephrine was chosen as the generic name in the United States because John Abel, who prepared extracts from the adrenal glands in 1897, used that name for his extracts. In 1901, Jokichi Takamine patented a purified adrenal extract, and called it "adrenalin", which was trademarked by Parke, Davis & Co in the U.S. In the belief that Abel's extract was the same as Takamine's, a belief since disputed, epinepherine became the generic name in the
Famotidine (INN) ( /fəˈmɒtɪdiːn/) is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). It is commonly marketed by Johnson & Johnson/Merck under the trade names Pepcidine and Pepcid and by Astellas under the trade name Gaster. Unlike cimetidine, the first H2 antagonist, famotidine has no effect on the cytochrome P450 enzyme system, and does not appear to interact with other drugs.
Famotidine was developed by Yamanouchi Pharmaceutical Co. It was licensed in the mid-80s by Merck & Co. and is marketed by a joint venture between Merck and Johnson & Johnson. The imidazole-ring of cimetidine was replaced with a 2-guanidinothiazole ring. Famotidine proved to be 30 times more active than cimetidine.
It was first marketed in 1981. Pepcid RPD orally-disintegrating tablets (that are not swallowed) were released in 1999. Generic preparations became available in 2001, e.g. Fluxid (Schwarz) or Quamatel (Gedeon Richter Ltd.).
In the United States, a product called Pepcid Complete is available that combines famotidine with an antacid in a chewable tablet to
Heroin (diacetylmorphine or morphine diacetate (INN)), also known as diamorphine (BAN), is an opiate analgesic synthesized by C.R. Alder Wright in 1874 by adding two acetyl groups to the molecule morphine found in the opium poppy. It is the 3,6-diacetyl ester of morphine, and functions as a morphine prodrug (meaning that it is metabolically converted to morphine inside the body in order for it to work).
When used in medicine it is typically used to treat severe pain, such as that resulting from a heart attack or a severe injury. The name "heroin" is only used when being discussed in its illegal form. When it is used in a medical environment, it is referred to as Diamorphine. The white crystalline form considered "pure heroin" is usually the hydrochloride salt, diacetylmorphine hydrochloride.
Illegally supplied heroin however is more often in freebase form, dulling the sheen and consistency to a matte-white powder. Because of its lower boiling point, the freebase form of heroin is also smokable. It is prevalent in heroin coming from Afghanistan, which as of 2004 produced roughly 87% of the world supply in illicit raw opium. However, production in Mexico has risen six-fold from 2007
Isoniazid (Laniazid, Nydrazid), also known as isonicotinylhydrazine (INH), is an organic compound that is the first-line medication in prevention and treatment of tuberculosis. The compound was first synthesized in the early 20th century, but its activity against tuberculosis was first reported in the early 1950s, and three pharmaceutical companies attempted unsuccessfully to simultaneously patent the drug (the most prominent one being Roche, which launched its version, Rimifon, in 1952). With the introduction of isoniazid, a cure for tuberculosis was first considered reasonable.
Isoniazid is available in tablet, syrup, and injectable forms (given intramuscularly or intravenously). It is available worldwide, is inexpensive and is generally well tolerated. It is manufactured from isonicotinic acid, which is produced from 4-methylpyridine.
Isoniazid may be prepared by the base hydrolysis of 4-cyanopyridine to give the amide, followed by displacement of ammonia by hydrazine:
Isoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex.
Ketoprofen, (RS)2-(3-benzoylphenyl)-propionic acid (chemical formula C16H14O3) is one of the propionic acid class of nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin.
Ketoprofen was available over-the-counter in the United States in the form of 12.5 mg coated tablets (Orudis KT and Actron), but this form has been discontinued. It is available by prescription as 50, 75, 100, 150, and 200 mg capsules.
Ketoprofen is available also as a 2.5% gel for topical application.
Brand names in the US are Orudis and Oruvail. It is available in the UK as Ketoflam and Oruvail, in Finland as Ketorin, Keto, Ketomex, and Orudis'; in France as Profénid, Bi-Profénid and Ketum, in Italy as Ketodol, Fastum Gel, Lasonil, Orudis or Oki, in Poland, Serbia, Slovenia and Croatia as Knavon or Ketonal, in Romania as Ketonal, in Mexico as Arthril, in Norway as Zon or Orudis, in Russia as ОКИ (OKI) and Ketonal, in Spain as Actron and in Venezuela as Ketoprofeno under an injectable solution of 100 mg and 150 mg capsules.
In Lithuania, ketoprofen is called Ketoprofenum and/or Ketoprofenas. For topical application: the
Marketed formulations:Loperamide hydrochloride 2 film coated tablet
Loperamide ( /loʊˈpɛrəmaɪd/; R-18553), a synthetic piperidine derivative, is an opioid drug used against diarrhea resulting from gastroenteritis or inflammatory bowel disease. In most countries it is available generically and under brand names such as Lopex, Imodium, Dimor, Fortasec, Lopedium, and Pepto Diarrhea Control. It was developed at Janssen Pharmaceutica.
Loperamide is effective for the treatment of a number of types of diarrhea.
Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine; by itself it does not affect the central nervous system.
It works by decreasing the activity of the myenteric plexus, which, like morphine, decreases the tone of the longitudinal smooth muscles but increases the tone of circular smooth muscles of the intestinal wall. This increases the amount of time substances stay in the intestine, allowing for more water to be absorbed out of the fecal matter. Loperamide also decreases colonic mass movements and suppresses the gastrocolic reflex.
Concurrent administration of P-glycoprotein inhibitors such as quinidine and its other isomer quinine (although much higher doses must be used),
Lorazepam (initially marketed under the brand names Ativan and Temesta) is a high-potency, short- to intermediate-acting, 3-hydroxy benzodiazepine drug that has all six intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant. Lorazepam is used for the short-term treatment of anxiety, insomnia, acute seizures including status epilepticus and sedation of hospitalized patients, as well as sedation of aggressive patients.
Lorazepam is considered to be a short-acting drug which, similar to other benzodiazepines, exerts its therapeutic, as well as adverse, effects via its interaction at benzodiazepine binding sites, which are located on GABAA receptors in the central nervous system. After its introduction in 1977, lorazepam's principal use was in treating anxiety. Among benzodiazepines, lorazepam has a relatively high addictive potential. Lorazepam also has abuse potential; the main types of misuse are for recreational purposes or continued use against medical advice. Its sedative-hypnotic and anterograde amnesia properties are sometimes used for criminal purposes.
Long-term effects of benzodiazepines include tolerance,
Marketed formulations:Metformin hydrochloride 1000 extended release film coated tablet
Metformin (BP, pronounced /mɛtˈfɔrmɨn/, met-FAWR-min; originally sold as Glucophage) is an oral antidiabetic drug in the biguanide class. It is the first-line drug of choice for the treatment of type 2 diabetes, in particular, in overweight and obese people and those with normal kidney function. Its use in gestational diabetes has been limited by safety concerns. It is also used in the treatment of polycystic ovary syndrome, and has been investigated for other diseases where insulin resistance may be an important factor. Metformin works by suppressing glucose production by the liver.
Metformin is the only antidiabetic drug that has been conclusively shown to prevent the cardiovascular complications of diabetes. It helps reduce LDL cholesterol and triglyceride levels, and is not associated with weight gain. As of 2010, metformin is one of only two oral antidiabetics in the World Health Organization Model List of Essential Medicines (the other being glibenclamide).
When prescribed appropriately, metformin causes few adverse effects (the most common is gastrointestinal upset) and is associated with a low risk of hypoglycemia. Lactic acidosis (a buildup of lactate in the blood) can be
Nifedipine (brand names Adalat, Nifediac, Cordipin, Nifedical, and Procardia) is a dihydropyridine calcium channel blocker. Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive, although a large number of other indications have recently been found for this agent, such as Raynaud's phenomenon, premature labor, and painful spasms of the esophagus such as in cancer and tetanus patients. It is also commonly used for the small subset of pulmonary hypertension patients whose symptoms respond to calcium channel blockers.
The recommended starting dose for immediate-release nifedipine capsules is 10 mg, taken 3 times daily. With the extended-release version, the recommended starting nifedipine dosage is 30 to 60 mg, taken once daily. Nifedipine rapidly lowers blood pressure, and patients are commonly warned they may feel dizzy or faint after taking the first few doses. Tachycardia (fast heart rate) may occur as a reaction. These problems are much less frequent in the sustained-release preparations of nifedipine (such as Adalat OROS). A more novel release system is GITS (Gastro-Intestinal Therapeutic System), which - according to Bayer - provides
Pentamidine (formulated as a salt, pentamidine diisethionate or dimesilate) is an antimicrobial medication given for prevention and treatment of Pneumocystis pneumonia (PCP) caused by Pneumocystis jirovecii (formerly known as Pneumocystis carinii), a severe interstitial type of pneumonia often seen in patients with HIV infection. The drug is also the mainstay of treatment for stage I infection with Trypanosoma brucei gambiense (West African Trypanosomiasis).
Pentamidine is also used as a prophylactic against PCP in patients receiving chemotherapy, as they also have a depressed immune system as a direct side-effect of the drugs used. The mortality of untreated PCP is very high. Additionally, pentamidine has good clinical activity in treating leishmaniasis, and yeast infections caused by the organism Candida albicans. Pentamidine is also used as a prophylactic antibiotic for children undergoing treatment for leukemia.
The exact mechanism of its anti-protozoal action is unknown (though it may involve reactions with ubiquitin), despite the fact that it is a basic therapeutic modality (in concurrence with multiple antifungal medications) when treating Acanthamoeba infections in the
Piracetam (sold under many brand names) is a nootropic drug. Piracetam's chemical name is 2-oxo-1-pyrrolidine acetamide; it shares the same 2-oxo-pyrrolidone base structure with 2-oxo-pyrrolidine carboxylic acid (pyroglutamate). Piracetam is a cyclic derivative of GABA. It is one of the group of racetams. Piracetam is prescribed by doctors for some conditions, mainly myoclonus, but is used off-label for a much wider range of applications.
Popular trade names for Piracetam in Europe are "Nootropil" and "Lucetam", among many others. In Argentina, it is made by GlaxoSmithKline S.A. laboratories and sold under the trade name of "Noostan" (800 mg or 1200 mg). In Venezuela and Ecuador, Piracetam is produced by Laboratorios Farma S.A. and sold under the brand name of "Breinox".
There is very little data on piracetam's effect on healthy people, with most studies focusing on people with seizures, dementia, concussions, or other neurological problems. A two week regimen of piracetam was reported in 1976 to enhance verbal memory in healthy college students in a double-blind, placebo-controlled study.
Numerous positive individual studies supported the use of piracetam in people suffering from
Pravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used for lowering cholesterol and preventing cardiovascular disease.
The primary uses of prevastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.
Pravastatin has undergone over 112,000 patient-years of double-blind randomized trials utilizing the 40mg once daily dose and placebos. These trials indicate that pravastatin is well tolerated and displays few non-cardiovascular abnormalities in patients.
However, side effects may occur. A doctor should be consulted if symptoms such as heartburn or headache are severe and do not go away. The following is a list of uncommon side effects that may require attention:
Pravastatin acts as a lipoprotein-lowering drug through two pathways. In the major pathway, pravastatin inhibits the function of hydroxymethylglutaryl-CoA (HMG-CoA) reductase. As a reversible competitive inhibitor, pravastatin sterically hinders the action of HMG-CoA reductase by occupying the active site of the
Prednisone is a glucocorticoid prodrug that is converted by 11beta-hydroxysteroid dehydrogenase in the liver into the active form, prednisolone. It is used to treat certain inflammatory diseases (such as severe allergic reactions) and (at higher doses) some types of cancer, but has many significant adverse effects. It is usually taken orally but can be delivered by intramuscular injection or intravenous injection.
Prednisone is used for many different indications including: asthma, COPD, CIDP, rheumatic disorders, allergic disorders, ulcerative colitis and Crohn’s disease, adrenocortical insufficiency, hypercalcemia due to cancer, thyroiditis, laryngitis, severe tuberculosis, lipid pneumonitis, multiple sclerosis, nephrotic syndrome, myasthenia gravis, and as part of a drug regimen to prevent rejection post organ transplant.
Prednisone has also been used in the treatment of migraine headaches and cluster headaches and for severe aphthous ulcer. Prednisone is used as an antitumor drug. Prednisone is important in the treatment of acute lymphoblastic leukemia, Non-Hodgkin lymphomas, Hodgkin's lymphoma, multiple myeloma and other hormone-sensitive tumors, in combination with other
Quinine (US /ˈkwaɪnaɪn/, UK /ˈkwɪniːn/ or /kwɪˈniːn/ KWIN-een) is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), and anti-inflammatory properties and a bitter taste. It is a stereoisomer of quinidine which, unlike quinine, is an antiarrhythmic. Quinine contains two major fused-ring systems: the aromatic quinoline and the bicyclic quinuclidine.
Though it has been synthesized in the lab, quinine occurs naturally in the bark of the cinchona tree. The medicinal properties of the cinchona tree were originally discovered by the Quechua, who are indigenous to Peru and Bolivia; later, the Jesuits were the first to bring the cinchona to Europe.
Quinine was the first effective treatment for malaria caused by Plasmodium falciparum, appearing in therapeutics in the 17th century. It remained the antimalarial drug of choice until the 1940s, when other drugs replaced it that have less unpleasant side effects. Since then, many effective antimalarials have been introduced, although quinine is still used to treat the disease in certain critical circumstances, such as severe malaria, and in impoverished regions due to its low cost.
Trifluoperazine (Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, Triftazin) is a typical antipsychotic of the phenothiazine chemical class.
The primary application of trifluoperazine is for schizophrenia. Other official indications may vary country by country, but generally it is also indicated for use in agitation and patients with behavioural problems, severe nausea and vomiting as well as severe anxiety. Its use in many parts of the world has declined because of highly frequent and severe early and late tardive dyskinesia, a type of extrapyramidal symptom. The annual development rate of tardive dyskinesia may be as high as 4%.
A 2006 study suggested that trifluoperazine may be able to reverse addiction to opioids.
A multi-year UK study by the Alzheimer's Research Trust suggested that this and other antipsychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often make their condition worse. The study concluded that
Trifluoperazine has central antiadrenergic, antidopaminergic, and minimal anticholinergic effects. It is believed to work by blockading dopamine D1 and D2 receptors in the mesocortical and mesolimbic
Marketed formulations:Vancomycin hydrochloride 4 lyophilized powder for injectable solution
Vancomycin INN ( /væŋkɵˈmaɪsɨn/) is a glycopeptide antibiotic used in the prophylaxis and treatment of infections caused by Gram-positive bacteria. Vancomycin was first isolated in 1953 at Eli Lilly, from a soil sample collected from the interior jungles of Borneo by a missionary. It is a naturally occurring antibiotic made by the soil bacterium Actinobacteria species Amycolatopsis orientalis (formerly designated Nocardia orientalis). It is a complex chemical compound and an example of a comparatively rare haloorganic natural compound, containing two organically bonded chlorine atoms.
The compound was industrially produced by fermentation and given the generic name vancomycin, derived from the term "vanquish." The original indication for vancomycin was for the treatment of penicillin-resistant Staphylococcus aureus, a use kept alive for many years by the fact that compound had to be given intravenously and was thus not abused outside hospitals, and the fact that organisms were relatively slow to evolve to adapt to it, even in experiments.
For many years since its initial use, vancomycin has traditionally been reserved as a drug of "last resort", used only after treatment with other
Zolpidem (sold under the brand names Ambien, Ambien CR, Stilnox, and Sublinox) is a prescription medication used for the treatment of insomnia, as well as some brain disorders. It is a short-acting nonbenzodiazepine hypnotic of the imidazopyridine class that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to GABAA receptors at the same location as benzodiazepines. It works quickly (usually within 15 minutes) and has a short half-life (two to three hours).
Zolpidem has not adequately demonstrated effectiveness in maintaining sleep (unless delivered in a controlled-release form); however, it is effective in initiating sleep. Its hypnotic effects are similar to those of the benzodiazepine class of drugs, but it is molecularly distinct from the classical benzodiazepine molecule and is classified as an imidazopyridine. Flumazenil, a benzodiazepine receptor antagonist, which is used for benzodiazepine overdose, can also reverse zolpidem's sedative/hypnotic and memory-impairing effects.
As an anticonvulsant and muscle relaxant, the drug's effects are not evident until dosages 10 and 20 times those required for sedation, respectively, are reached.