Donepezil

Indications
 Oral
Mild to moderately severe dementia in Alzheimer's disease
Adult: Initially, 5 mg daily at bedtime, increase if necessary up to 10 mg once daily at bedtime after 4-6 wk.
Elderly: Initially, 5 mg daily at bedtime, increase if necessary up to 10 mg once daily at bedtime after 4-6 wk.
Contraindications
 Hypersensitivity.
Warnings / Precautions
 Caution when used in patients with sick sinus syndrome or cardiac conduction abnormalities. May increase secretion of gastric acid; caution when used in patients at risk of ulcer disease. Patients with COPD, asthma, history of epilepsy, bladder obstruction, prostatic hypertrophy. May cause dose-related diarrhoea, nausea and/or vomiting which usually resolves after 1-3 wk. Safety and efficacy have not been established in children. Pregnancy, lactation.
Adverse Reactions
 Nausea, vomiting, anorexia, wt loss, diarrhoea, insomnia, fatigue, muscle cramps; headache and dizziness; syncope, bradycardia; convulsions; increased liver transaminases; sinoatrial and atrioventricular block; hallucinations, agitation and aggressive behavior; minor increases in plasma creatine kinase; potentially bladder outflow obstruction.
Overdose Reactions
 Overdose may result in cholinergic crisis; symptoms include severe nausea, vomiting, salivation, hypotension, bradycardia, resp depression, collapse and seizures. Muscle weakness may increase and death may occur if resp muscles are involved. Treatment includes supportive measures and use of tertiary anticholinergics (such as atropine).
Drug Interactions
 May increase the neurotoxic effect of antipsychotics. Concurrent use with systemic corticosteroids may increase the adverse effects of donepezil. May increase the neuromuscular-blocking effect of succinylcholine. May increase the adverse effects of cholinergic agonists. May increase the bradycardic effect of β-blockers.
See Below for More donepezil Drug Interactions
Food Interactions
 Ginkgo biloba may increase the adverse effects of donepezil.
Mechanism of Actions
 Donepezil reversibly and noncompetitively inhibits centrally-active acetylcholinesterase. It is used for the symptomatic treatment of Alzheimer's disease.
Absorption: Well absorbed in the GI tract. Plasma levels peak within 3-4 hr after oral admin.
Distribution: Protein binding: About 95% (mainly albumin).
Metabolism: Partially metabolised in the liver mainly by CYP3A4 to 4 major metabolites.
Excretion: Elimination half-life: About 70 hr. Steady-state concentrations are achieved within 3 wk of treatment initiation.
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store below 30°C.
ATC Classification
 N06DA02 - donepezil ; Belongs to the class of anticholinesterases. Used in the management of dementia.
Storage
 Oral: Store below 30°C.
Available As
  • Donepezil 10 mg
  • Donepezil 5 mg

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