美沙唑侖

化合物

美沙唑侖(英語:Mexazolam[1]),以商品名Melex和Sedoxil銷售,[2]是一種苯二氮䓬衍生物藥物。[3]美沙唑侖已針對焦慮進行了試驗,並在一周的隨訪中發現可有效緩解焦慮。美沙唑侖通過CYP3A4途徑代謝。HMG-CoA還原酶抑制劑包括辛伐他汀、辛伐他汀酸、洛伐他汀氟伐他汀阿托伐他汀西立伐他汀抑制美沙唑侖的代謝,[4]普伐他汀無法抑制。[5][6]其主要活性代謝物是地洛西泮(商品名Dadumir)和勞拉西泮(商品名Ativan)。[7]

美沙唑侖
臨床資料
商品名英語Drug nomenclatureMelex、Sedoxil
其他名稱13-chloro- 2-(2-chlorophenyl)- 5-methyl- 3-oxa- 6,9-diazatricyclo[8.4.0.02,6] tetradeca- 1(10),11,13-trien- 8-one
AHFS/Drugs.com國際藥品名稱
給藥途徑口服
ATC碼
法律規範狀態
法律規範
藥物動力學數據
藥物代謝CYP3A4
排泄途徑
識別資訊
  • 10-chloro-11b-(2-chlorophenyl)-3-methyl-2,3,5,7-tetrahydro-[1,3]oxazolo[3,2-d][1,4]benzodiazepin-6-one
CAS號31868-18-5
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C18H16Cl2N2O2
摩爾質量363.24 g·mol−1
3D模型(JSmol英語JSmol
  • Clc1ccccc1C42OCC(N2CC(=O)Nc3c4cc(Cl)cc3)C
  • InChI=1S/C18H16Cl2N2O2/c1-11-10-24-18(13-4-2-3-5-15(13)20)14-8-12(19)6-7-16(14)21-17(23)9-22(11)18/h2-8,11H,9-10H2,1H3,(H,21,23) checkY
  • Key:ANUCDXCTICZJRH-UHFFFAOYSA-N checkY

參見

參考資料

  1. ^ DE Patent 1954065
  2. ^ Benzodiazepine Names. non-benzodiazepines.org.uk. [2009-04-05]. (原始內容存檔於2008-12-08). 
  3. ^ Kurono Y, Kamiya K, Kuwayama T, Jinno Y, Yashiro T, Ikeda K. Kinetics and mechanism of the acid-base equilibrium of mexazolam and comparison with those of other commercial benzodiazepinooxazole drugs. Chemical & Pharmaceutical Bulletin. September 1987, 35 (9): 3831–7. PMID 2893667. doi:10.1248/cpb.35.3831 . 
  4. ^ Mc Donnell CG, Harte S, O'Driscoll J, O'Loughlin C, Van Pelt FN, Shorten GD, Van Pelt FD. The effects of concurrent atorvastatin therapy on the pharmacokinetics of intravenous midazolam. Anaesthesia. September 2003, 58 (9): 899–904. PMID 12911366. S2CID 25382546. doi:10.1046/j.1365-2044.2003.03339.x . 
  5. ^ Ishigami M, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y. Sex difference in inhibition of in vitro mexazolam metabolism by various 3-hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors in rat liver microsomes. Drug Metabolism and Disposition. August 2002, 30 (8): 904–10. PMID 12124308. S2CID 2620104. doi:10.1124/dmd.30.8.904. 
  6. ^ Ishigami M, Honda T, Takasaki W, Ikeda T, Komai T, Ito K, Sugiyama Y. A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. Drug Metabolism and Disposition. March 2001, 29 (3): 282–8 [2023-12-23]. PMID 11181496. (原始內容存檔於2005-01-15). 
  7. ^ Helder Fernandes; Ricardo Moreira. Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety. Neurology and Therapy. 2014, 3 (1): 1–14. PMC 4381915 . PMID 26000220. doi:10.1007/s40120-014-0016-7.