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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
Galantamine (Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is used for the treatment of mild to moderate Alzheimer’s disease and various other memory impairments, in particular those of vascular origin. It is an alkaloid that is obtained synthetically or from the bulbs and flowers of Galanthus Caucasicus (Caucasian snowdrop, Voronov’s snowdrop), Galanthus woronowii (Amaryllidaceae) and related genera like Narcissus (daffodil)), Leucojum (snowflake), and Lycoris including Lycoris radiata (Red Spider Lily).
Studies of usage in modern medicine began in the Soviet Union in the 1950s. The active ingredient was extracted, identified, and studied, in particular in relation to its acetylcholinesterase (AChE)-inhibiting properties. The bulk of the work was carried out by Soviet pharmacologists Mashkovsky and Kruglikova-Lvova, beginning in 1951. The work of Mashkovsky and Kruglikova-Lvova was the first published work that demonstrated the AChE-inhibiting properties of galantamine.
The first industrial process was developed in Bulgaria by prof. Paskov in 1959 (Nivalin, Sopharma) from a species traditionally used as a popular medicine in Eastern Europe, and, thus, the idea for
Memantine is the first in a novel class of Alzheimer's disease medications acting on the glutamatergic system by blocking NMDA-type glutamate receptors. It was first synthesized by Eli Lilly and Company in 1968. Memantine is marketed under the brands Axura and Akatinol by Merz, Namenda by Forest, Ebixa and Abixa by Lundbeck and Memox by Unipharm. Memantine has been shown to have a modest effect in moderate-to-severe Alzheimer's disease. Despite years of research, there is little evidence of effect in mild Alzheimer's disease.
Memantine is approved by the U.S. FDA and the European Medicines Agency for treatment of moderate-to-severe Alzheimer's disease, and has now received a limited recommendation by the UK's National Institute for Clinical Excellence for patients who fail other treatment options. Within the new guidance memantine is recommended as an option for managing Alzheimer’s disease for people with: moderate Alzheimer’s disease who are intolerant of or have a contraindication to AChE (acetylcholinesterase) inhibitors or those with severe Alzheimer’s disease.
Memantine has been associated with a moderate decrease in clinical deterioration with only a small positive effect on