Stage 8: Cognitive Enhancers & Dementia
Concept 2 of 6
R8.2

Donepezil

Once-daily AChEI — workhorse of Alzheimer's treatment, FDA-approved for severe disease.

Once-daily dosing made possible by long half-life (~70 hours). Adherence advantage especially relevant in dementia. Most prescribed AChEI partly for this reason.

Donepezil — Aricept — is the most prescribed cholinesterase inhibitor. The half-life is long (~70 hours), enabling once-daily dosing, and the FDA approvals span mild, moderate, and severe Alzheimer's disease. For a population that often struggles with medication adherence, the simplicity of once-daily is meaningful.

Drug card
Class
Acetylcholinesterase inhibitor
Mechanism
Selective reversible AChE inhibition (vs butyrylcholinesterase)
Typical dose
5 mg daily for 4-6 weeks, then 10 mg daily; 23 mg for severe disease (higher GI burden)
Half-life
~70 hours
FDA indications
Mild, moderate, and severe Alzheimer's disease
Key adverse effects
GI (nausea, vomiting, diarrhea, anorexia), insomnia/vivid dreams (if AM dosed — switch to bedtime), bradycardia, syncope, muscle cramps

Long half-life allows once-daily dosing. Most prescribed AChEI. FDA approval spans mild to severe disease (broader than rivastigmine, galantamine). Bedtime dosing reduces dream disturbances; AM dosing if causing daytime sedation.

Dosing: start 5 milligrams daily for 4-6 weeks, then increase to 10 milligrams. The 23-milligram formulation is approved for severe disease — extending use into later stages, though with higher GI burden and modest additional cognitive benefit over 10 milligrams.

23 mg formulation for severe Alzheimer's — extends use into later disease stages. Higher GI burden; not all patients tolerate. Modest additional benefit over 10 mg.

Dosing timing matters and varies by patient. Bedtime dosing reduces vivid dreams and nightmares for some patients but worsens sleep onset for others. Morning dosing avoids the sleep concerns but may produce sedation or fatigue during the day. The right time is patient-specific — start with bedtime, adjust if dreams or sleep problems emerge.

Dosing time considerations: bedtime reduces vivid dreams/nightmares but may worsen sleep onset in some; morning if sedation problematic; case-by-case adjustment.

Side effects share the AChEI class profile. GI is most common: nausea, diarrhea, vomiting, anorexia. Slow titration mitigates. Take with food. Monitor weight. Vivid dreams, sleep disturbance, bradycardia, syncope, urinary incontinence, muscle cramps round out the profile.

Mechanism in practice

Donepezil is the most-prescribed cholinesterase inhibitor — once-daily, broadly indicated, with a tolerability profile shaped by its cholinergic mechanism.

Mechanism
Reversible, selective acetylcholinesterase inhibition
Effect
Increased synaptic acetylcholine
Clinical applications
Approved across mild, moderate, and severe Alzheimer's disease — the broadest stage range of the class.
Mechanism
Long half-life (~70h)
Effect
Stable levels; convenient once-daily dosing
Clinical applications
Simple regimen aids adherence; usually dosed in the evening, though timing can be adjusted if sleep is disrupted.
Mechanism
Central cholinergic support
Effect
Modest cognitive and functional stabilization
Clinical applications
Titrate from 5mg to 10mg (to 23mg in some moderate-severe cases) as tolerated; benefit is modest and symptomatic.
Mechanism
Cholinergic peripheral effects
Effect
Nausea, diarrhea, anorexia, vivid dreams, bradycardia
Clinical applications
GI effects often improve with slow titration and food; vivid dreams may respond to morning dosing; cardiac caution with conduction disease.

Mechanism note: Donepezil's once-daily dosing and broad stage approval make it the default cholinesterase inhibitor; manage the cholinergic GI and sleep effects with titration and timing.

For mild-to-moderate Alzheimer's, donepezil is often the AChEI of first choice. Once-daily dosing wins on adherence; the long track record gives families confidence. For severe disease, the 23-milligram formulation can extend use. For most situations, this is the AChEI you reach for first.

Prescribing reality
Cost
Generic: ~$10-30/month.
Generic status
Generic since 2010.
Formulary typical
Tier 1 generic.
Access friction
None for most patients. 23 mg formulation has had access concerns historically.

Prescriber tip: Cheap and accessible workhorse AChEI. For severe disease 23 mg formulation, document mild-to-moderate failure for PA if needed.

The anchor

Donepezil is the workhorse AChEI — once-daily dosing, FDA-approved across mild to severe Alzheimer's, GI side effects manage by slow titration and timing.

Prove it

A patient on donepezil 10 mg HS reports vivid disturbing dreams and waking unrested. What adjustment might help?

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