User:Mr. Ibrahem/Donepezil

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Mr. Ibrahem/Donepezil
Clinical data
Trade namesAricept, others
AHFS/Drugs.comMonograph
MedlinePlusa697032
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth (tablets) Absorption is not affected by food or time of day.[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability100%[1][2]
Protein binding96%, albumin (about 75%) and alpha1-acid glycoprotein (21%).[2][1]
MetabolismCYP2D6, CYP3A4, and glucuronidation.[1] Four major metabolites, two of which are active.[2][1]
Onset of actionPeak plasma levels in 3–4 h.[2][1]
Elimination half-life70 hours[3] Around 100 hours in elderly patients.[1]
Duration of actionWith daily dosing, steady-state concentration is reached in 15–21 days.[2][1]
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.[1][2] Steady-state clearance is similar at all ages.[1]
Identifiers
  • (RS)-2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one
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 as the trade name Aricept among others, is a medication used to treat Alzheimer's disease.[5] It appears to result in a small benefit in mental function and ability to function.[6] Use, however, has not been shown to change the progression of the disease.[7] Treatment should be stopped if no benefit is seen.[8] It is taken by mouth.[5]

Common side effects include nausea, trouble sleeping, aggression, diarrhea, feeling tired, and muscle cramps.[5][8] Serious side effects may include abnormal heart rhythms, difficulty emptying urine from the bladder, and seizures.[5] Donepezil is a centrally acting reversible acetylcholinesterase inhibitor and structurally unrelated to other anticholinesterase agents.[5][1]

Donepezil was approved for medical use in the United States in 1996.[5] It is available as a generic medication.[8] In the United Kingdom a typical month's supply costs the NHS about £0.52 as of 2019.[9] The wholesale cost of this amount in the United States is about US$1.38.[10] In 2017, it was the 127th most commonly prescribed medication in the United States, with more than five million prescriptions.[11][12]

References[edit]

  1. ^ a b c d e f g h i j k Kumar, A; Sharma, S (2020), "article-20656", Donepezil, Treasure Island (FL): StatPearls Publishing, PMID 30020629, archived from the original on 2021-08-28, retrieved 2020-04-12
  2. ^ a b c d e f Seltzer, Ben (2005-09-29). "Donepezil: a review". Expert Opinion on Drug Metabolism & Toxicology. 1 (3). Informa Healthcare: 527–36. doi:10.1517/17425255.1.3.527. ISSN 1742-5255. PMID 16863459. 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.
  3. ^ Asiri, Yousif A.; Mostafa, Gamal A.E. (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. 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].
  4. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 27 November 2020. Retrieved 9 September 2020.
  5. ^ a b c d e f "Donepezil Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 26 July 2019. Retrieved 4 February 2019.
  6. ^ Birks JS, Harvey RJ (June 2018). "Donepezil for dementia due to Alzheimer's disease". The Cochrane Database of Systematic Reviews. 6: CD001190. doi:10.1002/14651858.CD001190.pub3. PMC 6513124. PMID 29923184.
  7. ^ Swedish Council on Health Technology Assessment (June 2008). "Dementia – Caring, Ethics, Ethnical and Economical Aspects: A Systematic Review". PMID 28876770. {{cite journal}}: Cite journal requires |journal= (help)
  8. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 300. ISBN 9780857113382.
  9. ^ BNF76 (2018), p. 300 harvp error: multiple targets (3×): CITEREFBNF762018 (help) "Donepezil hydrochloride (Non-proprietary) Donepezil hydrochloride 5 mg Donepezil 5 mg tablets | 28 tablet P £ 59.85 DT = £ 0.52"
  10. ^ "NADAC as of 2019-01-30". Centers for Medicare and Medicaid Services. Archived from the original on 2019-03-27. Retrieved 4 February 2019. 0.04978 (per tablet)
  11. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  12. ^ "Donepezil Hydrochloride – Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.
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