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 languageEnglish (US)
Pages (from-to)161-180
Number of pages20
JournalExpert Opinion on Pharmacotherapy
Volume5
Issue number1
DOIs
StatePublished - Jan 1 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)

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