Abstract

Donepezil is an acetylcholinesterase inhibitor used to treat Alzheimer's disease. It has been shown to be effective in the treatment of cognitive symptoms, functional impairment and behavioral problems at mild, moderate and severe stages of the disease. Donepezil treatment results in modest short-term (6- to 9-month) improvement in some measures and attenuates the downward course of the disease for 1–3 years. Donepezil reaches peak plasma levels 3–4 h after ingestion and, with daily dosing, steady-state concentration in 14–21 days. The elimination half-life is approximately 70 h, and it is principally excreted unchanged in the urine. There is a linear relationship between plasma level and both red blood cell acetylcholinesterase inhibition and certain cognitive outcome measures. Donepezil is generally safe and well tolerated and, because of its dosing schedule, convenient to prescribe. Ongoing studies are examining the use of donepezil in combination with other drugs for Alzheimer's disease and for other conditions involving cognitive dysfunction.

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