Donepezil

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Abstract
▲ Donepezil is a specific and potent acetylcholinesterase inhibitor according to in vitro data. It displays primarily noncompetitive inhibitory activity. ▲ In vivo, donepezil inhibited acetylcholinesterase activity in human erythrocytes and increased extracellular acetylcholine levels in the cerebral cortex and hippocampus of the rat. ▲ Donepezil demonstrated efficacy in tests of reference memory in animals, but had less consistent activity in tests of working memory. ▲ Donepezil 5 or 10 mg/day was associated with significant improvements in cognitive function [assessed by the Alzheimer’s Disease Assessment Scale — cognitive subscale (ADAS-cog)] after 14 and 30 weeks and patient global function (Clinician’s Interview-based Impression of Change incorporating caregiver input score) after 30 weeks, compared with placebo, in patients with mild to moderate Alzheimer’s disease. ▲ After 2 years, donepezil 5 or 10 mg/day was associated with an ADAS-cog score approximately 4 points better than would be expected in untreated patients with mild to moderate Alzheimer’s disease. ▲ The most common adverse events reported in association with donepezil 5 mg/day were gastrointestinal events (nausea/vomiting, diarrhoea, gastric upset and constipation) and dizziness. No hepatotoxicity was reported after 12 weeks’ treatment.

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