See Available Brands of Donepezil in India
P - Contraindicated in pregnancy
L - Contraindicated in lactation
Donepezil (also misspelled donezepil), marketed under the trade name Aricept by its developer Eisai and partner Pfizer, is a centrally acting reversible acetylcholinesterase inhibitor.[1] Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. Its binding to the acetylcholinesterase can be seen at Proteopedia 1eve. It has an oral bioavailability of 100% and easily crosses the blood-brain barrier. Because it has a half life of about 70 hours, it can be taken once a day. Initial dose is 5mg per day, which can be increased to 10mg per day after an adjustment period of at least 4 weeks.
Pharmacodynamics
Pharmacokinetics
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.
Donepezil Indications / Donepezil Uses
Information Not Available
Donepezil Adverse Reactions / Donepezil Side Effects
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.
Precautions
Monitor
eva luate patient's mental status, cognitive function, and activities of daily living prior to initiation of therapy and periodically thereafter during prolonged treatment. Monitor for signs and symptoms of GI bleed.
Overdosage
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).
Special 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.
Other 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.
Other Interactions
Food Interactions: Ginkgo biloba may increase the adverse effects of donepezil.
Dosage
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.
Food(before/after)
May be taken with or without food
List of Contraindications
Donepezil and Pregnancy
Contraindicated in pregnancy.
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Donepezil and Lactation
Contraindicated in lactation
Donepezil and Children
Information Not Available
Donepezil and Geriatic
Information Not Available
Donepezil and Other Contraindications
Hypersensitivity
Storage
Oral: Store below 30°C
Lab interference
Information Not Available
