美沙唑仑

美沙唑仑
臨床資料
商品名（英语：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	国际药品名称
给药途径	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
药物代谢	肝（CYP3A4）
排泄途徑	肾
识别信息
	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号	31868-18-5
PubChem CID	4177;
ChemSpider	4033 ;
UNII	S5969B6237;
KEGG	D01316 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID9057715 ;
化学信息
化学式	C18H16Cl2N2O2
摩尔质量	363.24 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	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 ;

美沙唑仑（英语：Mexazolam^[1]），以商品名Melex和Sedoxil销售，^[2]是一种苯二氮䓬衍生物药物。^[3]美沙唑仑已针对焦虑进行了试验，并在一周的随访中发现可有效缓解焦虑。美沙唑仑通过CYP3A4途径代谢。HMG-CoA还原酶抑制剂包括辛伐他汀、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仑的代谢，^[4]但普伐他汀无法抑制。^[5]^[6]其主要活性代谢物是地洛西泮（商品名Dadumir）和劳拉西泮（商品名Ativan）。^[7]

参见

参考资料

^ DE Patent 1954065
^ Benzodiazepine Names. non-benzodiazepines.org.uk. [2009-04-05]. （原始内容存档于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. （原始内容存档于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]. （原始内容存档于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. （原始内容存档于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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