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Evaluating Response to Metrifonate

Pierre N. Tariot, M.D.

Published: June 1, 1998

Article Abstract

Metrifonate, administered orally to patients with probable Alzheimer’s disease in a oncedailydose, readily enters the brain and inhibits brain acetylcholinesterase (AChE) activity in a dosedependentfashion. Metrifonate is a prodrug, converted non-enzymatically to 2,2-dichlorovinyl dimethylphosphate, a long-acting inhibitor of AChE that produces stable enzyme inhibition over time.In combination, these pharmacologic characteristics lead to a reduced side effect profile in comparisonwith several other cholinesterase inhibitors. Both preliminary and confirmatory pivotal studieshave shown that significant cognitive improvement is achieved with this medication in comparisonwith placebo in patients with probable Alzheimer’s disease. Moreover, these studies also have demonstratedthat metrifonate benefits the global function—a measure comprising domains of cognition,function, activities of daily living, and behavior—of patients with Alzheimer’s disease. The medicationis generally well tolerated, and no significant laboratory abnormalities occur. Therefore,metrifonate is a useful treatment for the symptoms of Alzheimer’s disease.

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Volume: 59

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