Donepezil
Nama sistematis (IUPAC) | |
---|---|
(RS)-2-[(1-Benzyl-4-piperidyl)methyl]-5,6-dimethoxy-2,3-dihydroinden-1-one | |
Data klinis | |
Nama dagang | Aricept, others |
AHFS/Drugs.com | monograph |
MedlinePlus | a697032 |
Data lisensi | US Daily Med:pranala |
Kat. kehamilan | B3(AU) C(US) |
Status hukum | Harus dengan resep dokter (S4) (AU) ℞-only (US) ℞ Preskripsi saja |
Rute | By mouth (tablets) Absorption is not affected by food or time of day.[1] |
Data farmakokinetik | |
Bioavailabilitas | 100%[1][2] |
Ikatan protein | 96%, albumin (about 75%) and alpha1-acid glycoprotein (21%).[2][1] |
Metabolisme | CYP2D6, CYP3A4, and glucuronidation.[1] Four major metabolites, two of which are active.[2][1] |
Waktu paruh | 70 hours[3] Around 100 hours in elderly patients.[1] |
Ekskresi | 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] |
Pengenal | |
Kode ATC | ? |
Data kimia | |
Rumus | C24H29NO3 |
SMILES | eMolecules & PubChem |
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Donepezil adalah obat yang digunakan untuk mengatasipenyakit Alzheimer . [4] Donepezil bisa memberikan cukup manfaat untuk fungsi mental. [5] Sayangnya penggunaan obat ini masih belum terbukti dalam mengubah penyakit alzheimer. [6] Penggunaan harus dihentikan jika tidak memiliki manfaat atau perubahan yang terlihat. [7] Rute pemberian obat ini melalui oral. [4]
Kejadian efek samping yang umum pada penggunaan obat ini seperti , rasa lelah,sulit tidur, agresi, diare, mual dan kram otot. [4] [7] Kejadian efek samping yang serius pada penggunaan obat ini meliputi aritmia, retensi urin, dan sawan . [4] Obati ini merupakan golongan inhibitor asetilkolinesterase reversibel yang memiliki mekanisme kerja secara terpusat dan secara struktural tidak berkaitan dengan agen antikolinesterase lainnya. [4] [1]
Obat donepezil disetujui dalam penggunaan medis di Amerika Serikat pada tahun 1996. [4] Donepezil sudah tersedia dalam bentuk obat generik. [7]
Referensi
[sunting | sunting sumber]- ^ a b c d e f g h i Kumar, A; Sharma, S (2020), "article-20656", Donepezil, Treasure Island (FL): StatPearls Publishing, PMID 30020629, diarsipkan dari versi asli tanggal 2021-08-28, diakses tanggal 2020-04-12
- ^ a b c d Seltzer, Ben (2005-09-29). "Donepezil: a review". Expert Opinion on Drug Metabolism & Toxicology. Informa Healthcare. 1 (3): 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. 35. Elsevier. hlm. 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].
- ^ a b c d e f "Donepezil Hydrochloride Monograph for Professionals". Drugs.com (dalam bahasa Inggris). American Society of Health-System Pharmacists. Diarsipkan dari versi asli tanggal 26 July 2019. Diakses tanggal 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.
- ^ a b c British national formulary : BNF 76 (edisi ke-76). Pharmaceutical Press. 2018. hlm. 300. ISBN 9780857113382.