User:Mr. Ibrahem/Donepezil
Clinical data | |
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Trade names | Aricept, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a697032 |
License data | |
Pregnancy category |
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Routes of administration | By mouth (tablets) Absorption is not affected by food or time of day.[1] |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 100%[1][2] |
Protein binding | 96%, albumin (about 75%) and alpha1-acid glycoprotein (21%).[2][1] |
Metabolism | CYP2D6, CYP3A4, and glucuronidation.[1] Four major metabolites, two of which are active.[2][1] |
Onset of action | Peak plasma levels in 3–4 h.[2][1] |
Elimination half-life | 70 hours[3] Around 100 hours in elderly patients.[1] |
Duration of action | With daily dosing, steady-state concentration is reached in 15–21 days.[2][1] |
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.[1][2] Steady-state clearance is similar at all ages.[1] |
Identifiers | |
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Chemical and physical data | |
Formula | C24H29NO3 |
Molar mass | 379.500 g·mol−1 |
3D model (JSmol) | |
Chirality | Racemic mixture |
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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]
- ^ 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
- ^ 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.
- ^ 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].
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 27 November 2020. Retrieved 9 September 2020.
- ^ 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.
- ^ 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.
- ^ Swedish Council on Health Technology Assessment (June 2008). "Dementia – Caring, Ethics, Ethnical and Economical Aspects: A Systematic Review". PMID 28876770.
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(help) - ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 300. ISBN 9780857113382.
- ^ 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"
- ^ "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)
- ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
- ^ "Donepezil Hydrochloride – Drug Usage Statistics". ClinCalc. Archived from the original on 8 July 2020. Retrieved 11 April 2020.