Donepezil

Donepezil
Clinical data
Trade names	Aricept, Adlarity, others
Other names	Donepezil hydrochloride (USAN US)
AHFS/Drugs.com	Monograph
MedlinePlus	a697032
License data	US DailyMed: Donepezil;
Pregnancy; category	AU: B3;
Routes of; administration	By mouth, transdermal
ATC code	N06DA02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); BR: Class C1 (Other controlled substances); UK: POM (Prescription only); US: ℞-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	100%
Protein binding	96%, albumin (about 75%) and alpha1-acid glycoprotein (21%).
Metabolism	CYP2D6, CYP3A4, and glucuronidation. Four major metabolites, two of which are active.
Onset of action	Peak plasma levels in 3–4 h.
Elimination half-life	70 hours Around 100 hours in elderly patients.
Duration of action	With daily dosing, steady-state concentration is reached in 15–21 days.
Excretion	0.11–0.13 (L/h/kg); excreted mostly by the kidneys. Around 17% is excreted unchanged in the urine. About 15% to 20% is excreted in feces. Steady-state clearance is similar at all ages.
Identifiers
	IUPAC name (RS)-2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one;
CAS Number	120014-06-4 ;
PubChem CID	3152;
IUPHAR/BPS	6599;
DrugBank	DB00843 ;
ChemSpider	3040 ;
UNII	8SSC91326P;
KEGG	D07869 ;
ChEBI	CHEBI:53289 ;
ChEMBL	ChEMBL502 ;
PDB ligand	E20 (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID8048317 ;
ECHA InfoCard	100.125.198
Chemical and physical data
Formula	C24H29NO3
Molar mass	379.500 g·mol−1
3D model (JSmol)	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 ; Key:ADEBPBSSDYVVLD-UHFFFAOYSA-N ;
	(verify)

Donepezil, sold under the brand name Aricept among others, is a medication used to treat dementia of the Alzheimer's type. It appears to result in a small benefit in mental function and ability to function. Use, however, has not been shown to change the progression of the disease. Treatment should be stopped if no benefit is seen. It is taken by mouth or via a transdermal patch.

Common side effects include nausea, trouble sleeping, aggression, diarrhea, feeling tired, and muscle cramps. Serious side effects may include abnormal heart rhythms, urinary incontinence, and seizures. Donepezil is a centrally acting reversible acetylcholinesterase inhibitor and structurally unrelated to other anticholinesterase agents.

Donepezil was approved for medical use in the United States in 1996. It is available as a generic medication. In 2021, it was the 131st most commonly prescribed medication in the United States, with more than 4 million prescriptions.

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