美沙唑侖

美沙唑侖
臨床資料
商品名（英語：Drug nomenclature）	Melex、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	N05BA25 (WHO) ;
法律規範狀態
法律規範	加：Schedule IV;
藥物動力學數據
藥物代謝	肝（CYP3A4）
排泄途徑	腎
識別資訊
	IUPAC命名法 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	4177;
ChemSpider	4033 ;
UNII	S5969B6237;
KEGG	D01316 ;
CompTox Dashboard（英語：CompTox Chemicals Dashboard） (EPA)	DTXSID9057715 ;
化學資訊
化學式	C18H16Cl2N2O2
摩爾質量	363.24 g·mol−1
3D模型（JSmol（英語：JSmol））	交互式圖像;
	SMILES Clc1ccccc1C42OCC(N2CC(=O)Nc3c4cc(Cl)cc3)C;
	InChI 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) ; Key:ANUCDXCTICZJRH-UHFFFAOYSA-N ;

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、阿托伐他汀和西立伐他汀抑制美沙唑侖的代謝，^[4]但普伐他汀無法抑制。^[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]

參見

參考資料

^ DE Patent 1954065
^ Benzodiazepine Names. non-benzodiazepines.org.uk. [2009-04-05]. （原始內容存檔於2008-12-08）.
^ 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  .
^ 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  .
^ 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.
^ 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）.
^ 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.

[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.

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