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Uses

Alzheimer’s Disease

Palliative treatment of mild to moderate dementia of the Alzheimer’s type (Alzheimer’s disease, presenile or senile dementia).

Comparative studies have not been performed to date, but donepezil does not share the hepatotoxic potential of tacrine and may be preferable to tacrine as a first-line treatment because it can be administered once daily and does not require regular monitoring of liver function.

Dosage and Administration

Administration

Oral Administration

Administer conventional or orally disintegrating tablets orally once daily, usually at bedtime.

Administer with or without food.

Orally disintegrating tablets: Place on tongue and allow to dissolve; follow with water.

Donepezil hydrochloride orally disintegrating and conventional film-coated tablets are bioequivalent.

Dosage

Available as donepezil hydrochloride; dosage expressed in terms of the salt.

Adults

Alzheimer’s Disease

Oral

Initially, 5 mg daily.

Some data suggest the possibility of additional benefit with higher (10 mg daily) dosage in some patients; however, additional benefit with the 10-mg dosage has not been demonstrated in controlled clinical studies. Adverse cholinergic effects are more likely with the 10-mg dosage.

Daily administration of 10 mg should not be considered until patient has received 5 mg daily for 4–6 weeks, since occurrence of adverse effects may be influenced by the rate of increase in dosage.

Special Populations

Dosage in Hepatic Impairment

No specific recommendation for dosage adjustment.

Cautions

Contraindications

• Known hypersensitivity to donepezil or piperidine derivatives or any ingredient in the formulation.

Warnings/Precautions

Warnings

Anesthesia

Potential for exaggerated succinylcholine-type muscle relaxation during anesthesia.

Cardiac Effects

Cholinesterase inhibitors may produce bradycardia or heart block via vagotonic effects on the sinoatrial or AV nodes. May occur in patients with or without known cardiac conduction abnormalities. Syncope reported in patients receiving donepezil.

GI Effects

Possible diarrhea, nausea, and vomiting, particularly at dosage of 10 mg daily.

Potential for increased gastric acid secretion.

Carefully monitor patients, especially those at increased risk for developing ulcers (e.g., those with history of peptic ulcer disease, those receiving concomitant NSAIA therapy), for symptoms of active or occult GI bleeding.

GU Effects

Although not reported in clinical studies with donepezil, cholinomimetic agents may cause bladder outflow obstruction.

Respiratory Effects

Use with caution in patients with a history of asthma or obstructive pulmonary disease.

Neurologic Effects

Cholinomimetic agents may have the potential to cause generalized seizures; however, seizures also may be a manifestation of Alzheimer’s disease.

Specific Populations

Pregnancy

Category C.

Lactation

Not known whether donepezil is distributed into milk. Not indicated for use in nursing women.

Pediatric Use

Safety and efficacy not established.

Geriatric Use

Dementia of the Alzheimer's type occurs principally in patients >55 years of age. The mean age of patients receiving donepezil in clinical studies was 73 years of age. No substantial differences in most adverse effects in patients ≥65 years of age relative to those <65 years of age.

Common Adverse Effects

Nausea, diarrhea, insomnia, vomiting, muscle cramp, fatigue, anorexia.