Back دونيبيزيل Arabic Donepezil Azerbaijani دونپزیل AZB دونپزیل CKB Donepesil Welsh Donepezil German Δονεπεζίλη Greek Donepezilo Spanish دونپزیل Persian Donepetsiili Finnish

Donepezil

Donepezil
Clinical data
Trade namesAricept, Adlarity, others
Other namesDonepezil hydrochloride (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa697032
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth, transdermal
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability100%[5][6]
Protein binding96%, albumin (about 75%) and alpha1-acid glycoprotein (21%).[6][5]
MetabolismCYP2D6, CYP3A4, and glucuronidation.[5] Four major metabolites, two of which are active.[6][5]
Onset of actionPeak plasma levels in 3–4 h.[6][5]
Elimination half-life70 hours[7] Around 100 hours in elderly patients.[5]
Duration of actionWith daily dosing, steady-state concentration is reached in 15–21 days.[6][5]
Excretion0.11–0.13 (L/h/kg); excreted mostly by the kidneys. Around 17% is excreted unchanged in the urine. About 15% to 20% is excreted in feces.[5][6] Steady-state clearance is similar at all ages.[5]
Identifiers
  • (RS)-2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.125.198 Edit this at Wikidata
Chemical and physical data
FormulaC24H29NO3
Molar mass379.500 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C2c1cc(OC)c(OC)cc1CC2CC4CCN(Cc3ccccc3)CC4
  • 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 checkY
  • Key:ADEBPBSSDYVVLD-UHFFFAOYSA-N checkY
  (verify)

Donepezil, sold under the brand name Aricept among others, is a medication used to treat dementia of the Alzheimer's type.[3][4][8] It appears to result in a small benefit in mental function and ability to function.[9] Use, however, has not been shown to change the progression of the disease.[10] Treatment should be stopped if no benefit is seen.[11] It is taken by mouth or via a transdermal patch.[3][4][8]

Common side effects include nausea, trouble sleeping, aggression, diarrhea, feeling tired, and muscle cramps.[8][11] Serious side effects may include abnormal heart rhythms, urinary incontinence, and seizures.[8] Donepezil is a centrally acting reversible acetylcholinesterase inhibitor and structurally unrelated to other anticholinesterase agents.[8][5]

Donepezil was approved for medical use in the United States in 1996.[8] It is available as a generic medication.[11] In 2021, it was the 131st most commonly prescribed medication in the United States, with more than 4 million prescriptions.[12][13]

  1. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  2. ^ "Donepezil Hydrochloride 10 mg Film-coated tablets". Electronic Medicines Compendium. Archived from the original on 8 September 2022. Retrieved 8 September 2022.
  3. ^ a b c "Aricept- donepezil hydrochloride tablet, film coated Aricept ODT- donepezil hydrochloride tablet, orally disintegrating". DailyMed. 23 December 2021. Retrieved 15 March 2022.
  4. ^ a b c "Adlarity- donepezil hydrochloride patch". DailyMed. 11 March 2022. Retrieved 19 June 2022.
  5. ^ a b c d e f g h i j Cite error: The named reference Kum2020 was invoked but never defined (see the help page).
  6. ^ a b c d e f Seltzer B (October 2005). "Donepezil: a review". Expert Opinion on Drug Metabolism & Toxicology. 1 (3). Informa Healthcare: 527–536. doi:10.1517/17425255.1.3.527. PMID 16863459. S2CID 32689288. there is a linear relationship between dose and pharmacodynamic effects, measured as red blood cell acetylcholinesterase inhibition and clinical efficacy. Despite being 96% bound to plasma proteins, it has few interactions with other drugs, and the 5-mg dose can be given safely to patients with mild-to-moderate hepatic and renal-disease.
  7. ^ Asiri YA, Mostafa GA (2010). "Donepezil". Profiles of Drug Substances, Excipients and Related Methodology. Vol. 35. Elsevier. pp. 117–50. doi:10.1016/s1871-5125(10)35003-5. ISBN 978-0-12-380884-4. ISSN 1871-5125. PMID 22469221. S2CID 206178636. Plasma donepezil concentrations decline with a half-life of approximately 70 h. Sex, race, and smoking history have no clinically significant influence on plasma concentrations of donepezil [46–51].
  8. ^ a b c d e f "Donepezil Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 4 February 2019.
  9. ^ Birks JS, Harvey RJ (June 2018). "Donepezil for dementia due to Alzheimer's disease". The Cochrane Database of Systematic Reviews. 2018 (6): CD001190. doi:10.1002/14651858.CD001190.pub3. PMC 6513124. PMID 29923184.
  10. ^ Swedish Council on Health Technology Assessment (June 2008). "Dementia – Caring, Ethics, Ethnical and Economical Aspects: A Systematic Review". SBU Systematic Reviews. PMID 28876770.
  11. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 300. ISBN 978-0-85711-338-2.
  12. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  13. ^ "Donepezil - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.

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