Donepezil
Donepezil
Aricept (oral), Adlarity (transdermal patch)
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Summary
Common uses
Alzheimer disease dementia, mild to moderate (FDA)0, Alzheimer disease dementia, severe (FDA, 23 mg/day formulation)0, Lewy body dementia (off-label)0, Parkinson disease dementia (off-label)0
Pharmacy
Starting dose
5 mg PO once daily at bedtime; titrate to 10 mg/day after 4-6 weeks. Severe Alzheimer disease: may escalate to 23 mg/day. Adlarity patch: 5 or 10 mg/day applied weekly
Preparations
Oral tablets 5, 10, 23 mg; ODT 5, 10 mg; Adlarity transdermal patch 5, 10 mg/day (weekly application)
US FDA Max
23 mg/day
Pharmacology
Routes
Oral, transdermal
Onset
Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose
Duration
24 hours (once-daily dosing)
Half-life
~70 hours (long, supports once-daily dosing without peak-trough variation)[1]
Bioavailability
~100% (oral)[1]
Pregnancy
Limited human data; rarely indicated in pregnancy given the patient population.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Selective, reversible acetylcholinesterase inhibitor with central nervous system penetration. Increases synaptic acetylcholine in cortical and hippocampal circuits, partially compensating for the characteristic cholinergic deficit of Alzheimer disease.0 The effect is symptomatic only: donepezil does not alter the underlying neurodegenerative trajectory. CYP3A4 and CYP2D6 metabolism. Cholinergic adverse effects (nausea, diarrhea, vomiting, vivid dreams, bradycardia, syncope) are dose-limiting; bradyarrhythmia and syncope are clinically important, with risk elevated by concurrent β-blockers or non-dihydropyridine calcium channel blockers. The bedtime dosing convention minimizes nausea and vivid-dream burden[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Aricept (donepezil hydrochloride), Eisai/Pfizer, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020690s039lbl.pdf