Therapeutic Classification: anti-Alzheimers's agents
Pharmacologic Classification: cholinergics (cholinesterase inhibitors)
Absorption: Well absorbed after oral administration. Bioavailability of transdermal formulation comparable to that of oral tablets.
Distribution: Widely distributed to extravascular tissues.
Protein Binding: 96%.
Metabolism/Excretion: Partially metabolized by the liver (CYP2D6 and CYP3A4 isoenyzmes) and partially excreted by kidneys (17% unchanged). Two metabolites are pharmacologically active. The CYP2D6 enzyme system exhibits genetic polymorphism (7% of population may be poor metabolizers and may have significantly ↑ donepezil concentrations and an ↑ risk of adverse effects).
Half-life: Oral: 70 hr. Transdermal: 91 hr.
(improvement in symptoms)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | unknown | several wk | 6 wk† |
| Transdermal | unknown | several wk | 6 wk† |
†Return to baseline after discontinuation.
Contraindicated in:
Use Cautiously in:
CV: atrial fibrillation, hypertension, hypotension, vasodilation.
Derm: allergic contact dermatitis (transdermal), ecchymoses.
Endo: hot flashes.
GI: diarrhea, nausea, anorexia, vomiting.
GU: frequent urination.
Metab: weight loss.
MS: arthritis, muscle cramps.
Neuro: headache, abnormal dreams, depression, dizziness, drowsiness, fatigue, insomnia, syncope.
Drug-Drug:
Drug-Natural Products:
Mild to Moderate Alzheimer's Disease
Severe Alzheimer's Disease
(Generic available)
Adlarity, Aricept, Aricept ODT
NDC Code*