Oral Mild dementia in Alzheimer's disease, Moderate dementia in Alzheimer's disease, Severe dementia in Alzheimer's disease
Adult: Initially, 5 mg once daily at bedtime, may increase after 1 mth to 10 mg once daily, if necessary. Max: 10 mg daily. Elderly: Initially, 5 mg daily at bedtime, increase if necessary up to 10 mg once daily at bedtime after 4-6 wk.
May be taken with or without food.
Patient w/ history of asthma or COPD, sick sinus syndrome, supraventricular conduction abnormalities, susceptibility to peptic ulcer, seizures, GI or urinary tract obstruction. Hepatic impairment. Pregnancy and lactation.
Monitor mental status, wt, pulse, symptoms of GI intolerance or bleeding.
Symptoms: Cholinergic crisis characterised by severe nausea, vomiting, salivations, sweating, bradycardia, hypotension, resp depression, collapse, convulsion, muscle weakness. Management: Supportive treatment and use of anticholinergic such as IV atropine.
Increased risk of neuroleptic malignant syndrome w/ antipsychotics. Synergistic effect w/ succinylcholine, similar neuromuscular blocking agents, or cholinergic agonists (e.g. bethanechol). May interfere w/ the activity of anticholinergic medications. Increased plasma concentration when used w/ CYP3A4 inhibitors (e.g. ketoconazole, erythromycin) and CYP 2D6 inhibitors (e.g. fluoxetine, quinidine). Decreased plasma concentrations w/ enzyme inducers (e.g. rifampicin, phenytoin).
Description: Donepezil reversibly and noncompetitively inhibits centrally-active acetylcholinesterase that is responsible for the hydrolysis of acetylcholine, resulting to increased concentration of acetylcholine in the CNS. Pharmacokinetics: Absorption: Well absorbed from the GI tract. Time to peak plasma concentration: 3-4 hr. Distribution: Volume of distribution: 12-16 L/kg. Protein binding: Approx 96% (to albumin (75%) and α1-acid glycoprotein (21%). Metabolism: Extensively metabolised in the liver, mainly by CYP3A4 isoenzyme and to a lesser extent by CYP2D6, into 4 major metabolites. Excretion: Via urine (57%, as unchanged drug and metabolites) and faeces (15%). Elimination half-life: Approx 70 hr.
N06DA02 - donepezil ; Belongs to the class of anticholinesterases. Used in the management of dementia.
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