Abstract
This article reviews the piperidine derivative, donepezil hydrochloride (E2020, Aricept®), a reversible central acetylcholinesterase inhibitor currently approved for treatment of mild-to-moderate Alzheimer's disease. Donepezil is well absorbed orally, unaffected by food or by time of administration; it reaches therapeutic levels in doses of 5 - 10 mg/day and peak plasma concentrations are obtained 3 - 4 h after oral administration. A single bedtime dose is recommended due to the long elimination half-life of the drug (70 h). Donepezil does not cause liver toxicity or significant drug interactions and is relatively well-tolerated. Initial side effects include nausea, vomiting, diarrhoea, insomnia, muscle cramps, fatigue, anorexia and syncope. Caution is advised in patients with bradycardia. Long-term use of donepezil in AD has been found to delay nursing-home placement and to result in caregiver respite. Donepezil also slows deterioration of cognition and global function in patients with moderate-to-severe AD, with improvement of abnormal behaviours. In addition to AD, donepezil demonstrates significant improvement in cognition, global function and activities of daily living in comparison with placebo-treated patients with vascular dementia and has potential therapeutic benefit for other neurological conditions.
Original language | English (US) |
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Pages (from-to) | 161-180 |
Number of pages | 20 |
Journal | Expert Opinion on Pharmacotherapy |
Volume | 5 |
Issue number | 1 |
DOIs | |
State | Published - Jan 2004 |
Keywords
- Alzheimer's disease
- Aphasia
- Autism
- Cholinergic transmission
- Cholinesterase inhibitors
- Dementia donepezil
- Down's syndrome
- Drowsiness
- Head injury
- Lewy body
- Memory
- Migraine
- Opioid drowsiness
- Parkinson's disease
- Schizophrenia
- Seizures
- Stroke
- Tardive dyskinesia
- Vascular dementia
ASJC Scopus subject areas
- Pharmacology (medical)
- Pharmacology, Toxicology and Pharmaceutics(all)