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QuickView for Donepezil (compound)


PubChem
Name: donepezil
PubChem Compound ID: 1150567
Molecular formula: C24H29NO3
Molecular weight: 379.492 g/mol
Synonyms:
E20; E2020; 1-BENZYL-4-[(5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE
DrugBank
Identification
Name: donepezil
Name (isomeric): DB00843
Drug Type: small molecule
Brand: Aricept, Eranz, Aricept ODT
Category: Parasympathomimetics, Nootropic Agents, Cholinesterase Inhibitors
CAS number: 120014-06-4
Pharmacology
Indication: For the palliative treatment of mild to moderate dementia of the Alzheimer's type.
Pharmacology:
Donepezil is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as...
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Mechanism of Action:
Donepezil is a piperidine derivative that is a centerally active, reversible inhibitor of acetylcholinesterase. This drug is structurally unrelated to other anticholinesterase agents. Donepezil's proposed mechanism of action involves the reversible inhibition of cholinesterases (eg. acetylcholinesterase), which prevents the hydrolysis of acetycholi...
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Absorption: Donepezil is well absorbed with a relative oral bioavailability of 100% and reaches peak plasma concentrations in 3 to 4 hours.
Protein binding: 96%
Biotransformation: Donepezil is metabolized by CYP 450 isoenzymes 2D6 and 3A4 in the liver and also undergoes glucuronidation. The main metabolite, 6-O-desmethyl donepezil, has been reported to inhibit AChE to the same extent as donepezil in vitro.
Route of elimination: Donepezil is both excreted in the urine intact and extensively metabolized to four major metabolites, two of which are known to be active, and a number of minor metabolites, not all of which have been identified.
Half Life: 70 hours
Clearance: apparent plasma cl=0.13 L/hr/kg
Toxicity: Symptoms of overdose include severe nausea, vomiting, salivation, sweating, bradycardia, hypotension, respiratory depression, collapse and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Take without regard to meals.
Drug interaction:
OxybutyninPossible antagonism of action
MesoridazinePossible antagonism of action
DiphenhydraminePossible antagonism of action
TrimeprazinePossible antagonism of action
AzatadinePossible antagonism of action
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Targets


Enzymes