Donepezil

Donepezil

Clinical data
Trade names	Aricept
AHFS/Drugs.com	Monograph
MedlinePlus	a697032
Pregnancy category	C
Routes of administration	By mouth (tablets)
ATC code	N06DA02 (WHO)
Legal status
Legal status	US: ℞-only ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	100%
Protein binding	96%
Biological half-life	70 hours
Excretion	0,11-0,13 (l/h/kg)
Identifiers
IUPAC name (RS)-2-[(1-Benzyl-4-piperidyl)methyl]- 5,6-dimethoxy-2,3-dihydroinden-1-one
CAS Number	120014-06-4 Y
PubChem (CID)	3152
IUPHAR/BPS	6599
DrugBank	DB00843 Y
ChemSpider	3040 Y
UNII	8SSC91326P Y
KEGG	D07869 Y
ChEBI	CHEBI:53289 Y
ChEMBL	CHEMBL502 Y
PDB ligand ID	E20 (PDBe, RCSB PDB)
ECHA InfoCard	100.125.198
Chemical and physical data
Formula	C24H29NO3
Molar mass	379.492 g/mol
3D model (Jmol)	Interactive image
Chirality	Racemic mixture
SMILES O=C2c1cc(OC)c(OC)cc1CC2CC4CCN(Cc3ccccc3)CC4
InChI InChI=1S/C24H29NO3/c1-27-22-14-19-13-20(24(26)21(19)15-23(22)28-2)12-17-8-10-25(11-9-17)16-18-6-4-3-5-7-18/h3-7,14-15,17,20H,8-13,16H2,1-2H3 Y Key:ADEBPBSSDYVVLD-UHFFFAOYSA-N Y

Donepezil, marketed under the trade name Aricept, is a medication used in the palliative treatment of Alzheimer's disease. Donepezil is used to improve cognition and behavior of people with Alzheimer's, but does not slow the progression of or cure the disease.

Common side effects include loss of appetite, gastrointestinal upset, diarrhea, difficulty sleeping, vomiting, or muscle cramping.

It was developed by Eisai and Pfizer and is sold as a generic by multiple suppliers. Donepezil acts as a centrally acting reversible acetylcholinesterase inhibitor.

There is no evidence that donepezil or other similar agents alters the course or progression of Alzheimer's disease (AD). 6 to 12-month controlled studies have shown modest benefits in cognition and/or behavior. The UK National Institute for Clinical Excellence (NICE) recommends donepezil as an option in the management of mild to moderate Alzheimer's disease. The person should, however, be reviewed frequently and if there is no significant benefit it should be stopped. In 2006 the U.S. Food and Drug Administration also approved donepezil for treatment of mild, moderate and severe dementia in Alzheimer's disease.

In clinical trials the most common adverse events leading to discontinuation were nausea, diarrhea, and vomiting. Other side effects included difficulty sleeping, muscle cramps and anorexia. Most side effects were observed in patients taking the 23 mg dose compared to 10 mg or lower doses. Side effects improved with continued use.

Donepezil should be used with caution in people with heart disease, cardiac conduction disturbances, chronic obstructive pulmonary disease, asthma, severe cardiac arrhythmias and sick sinus syndrome.