Name: | donepezil |
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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
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Name: | donepezil |
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Name (isomeric): | DB00843 |
Drug Type: | small molecule |
Brand: | Aricept, Eranz, Aricept ODT |
Category: | Parasympathomimetics, Nootropic Agents, Cholinesterase Inhibitors |
CAS number: | 120014-06-4 |
Indication: | For the palliative treatment of mild to moderate dementia of the Alzheimer's type. |
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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 |
Food interaction: |
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Drug interaction: |
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