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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTI-DEMENTIA DRUGS › Anticholinesterases
donepezil
N06DA02
Forms & Strengths
- Oral tablets: 5 mg, 10 mg, 23 mg
- Orally disintegrating tablets (ODT): 5 mg, 10 mg
Adult Dosing
- Mild to moderate Alzheimer's disease: Start 5 mg once daily at bedtime; may increase to 10 mg once daily after 4 to 6 weeks.
- Moderate to severe Alzheimer's disease: Can increase to 23 mg once daily after at least 3 months of treatment on 10 mg once daily.
Pediatric Dosing
- Not indicated for pediatric use.
Indications
- Treatment of dementia of the Alzheimer's type (mild, moderate, and severe).
Mechanism of Action
- Reversible and noncompetitive inhibitor of centrally active acetylcholinesterase, increasing acetylcholine concentrations in the cerebral cortex.
Contraindications
- Known hypersensitivity to donepezil or piperidine derivatives.
Adverse Reactions
- Nausea
- Diarrhea
- Insomnia
- Vomiting
- Muscle cramps
- Fatigue
- Anorexia
- Bradycardia
- Syncope
Drug Interactions
- Strong CYP3A4 and CYP2D6 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease donepezil concentrations.
- Strong CYP3A4 inhibitors (e.g., ketoconazole) and CYP2D6 inhibitors (e.g., quinidine) may increase donepezil exposure.
- Cholinesterase inhibitors and succinylcholine-type neuromuscular blocking agents may have synergistic effects.
- Beta-blockers may enhance bradycardia risk.
Curated Content: Needs Vetting Before Put to Clinical Use