Donepezil is a centrally active acetylcholinesterase inhibitor. It has efficacy in mild-to-moderate Alzheimer's disease when given once daily.

Donepezil possesses a high degree of selectivity for central nervous system acetylcholinesterase, with a low propensity for peripheral activity.

Bioavailability: 100%; Protein binding: approximately 96%; Hepatic metabolism: P450 CYP2D6 and CYP3A4, extensive metabolism, glucuronidation; Excretion: Fecal- 15%, Renal- 57%, 17% unchanged; Elimination Half Life: about 71 h.

Hypersensitivity to donepezil or piperidine derivatives. Use with caution in patients with active gastrointestinal diseases, asthma, COPD, seizure, and sick sinus syndrome.

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Infant risk cannot be ruled out.

Adverse effects are nausea, vomiting, diarrhea, muscle cramps, insomnia, fatigue, and anorexia.

Adults: mild-to-moderate Alzheimer's disease: initial, 5 mg orally once daily at bedtime; if suboptimal clinical response, may increase to MAX of 10 mg orally once daily at 4 to 6 weeks