吗氯贝胺...
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抗抑郁药物单胺氧化酶抑制剂氯代芳烴苯酰胺类吗啉
美国英国澳大利亚罗氏南非酪胺抗胆碱剂医学导航心理学精神病学心理历程障碍opmpads症状齐名涉及评估治疗N5A5B5C6A6B6D
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| 系统（IUPAC）命名名称 | |
|---|---|
4-chloro-N-(2-morpholin-4-ylethyl)benzamide | |
| 临床数据 | |
| 商品名 | Amira, Aurorix, Clobemix, Depnil, Manerix |
| Drugs.com | Micromedex详细消费者药物信息 |
| 妊娠分级 |
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| 给药途径 | oral |
| 合法狀態 | |
| 合法状态 |
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药代动力学数据 | |
| 生物利用度 | 55-95% (increases with repeat administration)[1] |
| 蛋白结合度 | 50%[2] |
| 代谢 | Hepatic |
| 生物半衰期 | 1-2 hours, 4 hours (elderly)[3][4] |
| 排泄 | Renal, Faecal (<5%)[2] |
| 识别信息 | |
| CAS注册号 | 71320-77-9  |
| ATC代码 | N06AG02 |
| PubChem | CID 4235 |
| IUPHAR/BPS | 7428 |
| DrugBank | DB01171 |
| ChemSpider | 4087 |
| UNII | PJ0Y7AZB63 |
| KEGG | D02561 |
| ChEBI | CHEBI:83531  |
| ChEMBL | CHEMBL86304 |
| 化学信息 | |
| 化学式 | C13H17ClN2O2 |
| 摩尔质量 | 268.739 g/mol |
SMILES
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InChI
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吗氯贝胺（商品名也作Amira、Aurorix、[5]Clobemix、Depnil或Manerix）是主要用于治疗抑郁症和社交焦虑的单胺氧化酶A（RIMA）药物的可逆抑制剂。[6]它在美国不被允许使用，但在其它西方国家，例如英国和澳大利亚（TGA于2000年12月）是被批准使用的。[7]它由罗氏公司的附属公司生产。起初，Aurorix也在南非由罗氏公司供应，但在专利期满之后撤回，Cipla Medpro's Depnil和Pharma Dynamic's Clorix的成本减半。
当吗氯贝胺与胺类混用时，如含酪胺的食物或升压胺类药物，不会出现显著的血压升高，这与较老的非选择性和不可逆单胺氧化酶抑制剂（MAOI）不同，后者的混用会导致血压严重上升。由于不会造成抗胆碱剂、心血管、认知与精神运动损伤，吗氯贝胺在老年人以及心血管疾病患者中是有利的。[6]
参考文献
^ Fitton, A; Faulds, D; Goa, KL. Moclobemide. A review of its pharmacological properties and therapeutic use in depressive illness. Drugs. April 1992, 43 (4): 561–596. PMID 1377119. doi:10.2165/00003495-199243040-00009.
^ 2.02.1 Schoerlin, MP; Mayersohn, M; Korn, A; Eggers, H. Disposition kinetics of moclobemide, a monoamine oxidase-A enzyme inhibitor: single and multiple dosing in normal subjects. Clinical Pharmacology and Therapeutics. October 1987, 42 (4): 395–404. PMID 3665338.
^ Freeman, H. Moclobemide. Lancet. December 1993, 342 (8886-8887): 1528–1532. PMID 7902906. doi:10.1016/S0140-6736(05)80090-X.
^ Gex-Fabry, M; Balant-Gorgia, AE; Balant, LP. Potential of concentration monitoring data for a short half-life drug: analysis of pharmacokinetic variability for moclobemide. Therapeutic Drug Monitoring. February 1995, 17 (1): 39–46. PMID 7725375. doi:10.1097/00007691-199502000-00007.
^ Scheen AJ. [Drug of the month. Moclobemide (Aurorix)]. Rev Med Liege. May 1994, 49 (5): 291–2. PMID 8023056 （法语）.
^ 6.06.1 Fulton B, Benfield P. Moclobemide. An update of its pharmacological properties and therapeutic use. Drugs. September 1996, 52 (3): 450–74. PMID 8875133. doi:10.2165/00003495-199652030-00013.
^ PRODUCT INFORMATION MOCLOBEMIDE SANDOZ® 150mg and 300mg TABLETS. TGA eBusiness Services. Sandoz. 6 March 2012 [16 October 2013].
拓展阅读
- Scientific Information on Aurorix (German)
PubChem Substance Summary: Moclobemide National Center for Biotechnology Information.
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