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Donepezil

ARICEPT

What it isCentrally acting acetylcholinesterase inhibitor; Alzheimer dementia at all stages.

Why this oneUnlike galantamine, its label extends to severe Alzheimer dementia, so it can be continued as disease advances.

What limits itCholinergic effects — bradycardia, syncope, GI upset and vivid dreams. The benefit is symptomatic; it does not alter progression.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Alzheimer's disease, mild–moderateAdults5 mg QHS10 mg QD10 mg QD
Alzheimer's disease, moderate–severeAdults5 mg QHS10–23 mg QD23 mg QD

Titration Increase to 10 mg only after 4–6 wk at 5 mg; increase to 23 mg only after ≥3 mo at 10 mg.

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No adequate human data; animal data show increased stillbirths/decreased offspring survival at clinically relevant doses

Lactation Undefined

NO BOXED WARNINGS

Principal riskBradycardia and syncope

Cost, est. cash$10–$500/month

Generic entry2009

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades3 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityBradycardia, syncope or GI effects for symptomatic drugs; anti-amyloid agents add edema/hemorrhage risk.

Mechanism of action: Donepezil ballicule

Donepezil ballicule: receptor binding, kinetics and half-life diagram

Open Donepezil in the interactive console ↗

Memory aids: mascots and interaction avatars

Donepezil ARICEPT mascot mnemonic cartoon
“Donnie Pez is Air except (for Alzheimer’s brain)”
Light blue → cholinergic / muscarinic
Donepezil CYP2D6 substrate avatar
CYP2D6 substrate

Open Donepezil in the interactive console ↗