吗氯贝胺

化合物

吗氯贝胺(商品名也作AmiraAurorix[5]ClobemixDepnilManerix)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。

吗氯贝胺
临床资料
商品名英语Drug nomenclatureAmira, Aurorix, Clobemix, Depnil, Manerix
AHFS/Drugs.comMicromedex详细消费者药物信息
怀孕分级
给药途径oral
ATC码
法律规范状态
法律规范
药物动力学数据
生物利用度55-95% (increases with repeat administration)[1]
血浆蛋白结合率50%[2]
药物代谢Hepatic
生物半衰期1-2 hours, 4 hours (elderly)[3][4]
排泄途径Renal, Faecal (<5%)[2]
识别信息
  • 4-chloro-N-(2-morpholin-4-ylethyl)benzamide
CAS号71320-77-9  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.163.935 编辑维基数据链接
化学信息
化学式C13H17ClN2O2
摩尔质量268.739 g/mol
3D模型(JSmol英语JSmol
  • Clc1ccc(cc1)C(=O)NCCN2CCOCC2
  • InChI=1S/C13H17ClN2O2/c14-12-3-1-11(2-4-12)13(17)15-5-6-16-7-9-18-10-8-16/h1-4H,5-10H2,(H,15,17) checkY
  • Key:YHXISWVBGDMDLQ-UHFFFAOYSA-N checkY

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

  1. ^ 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. ^ 2.0 2.1 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. 
  3. ^ Freeman, H. Moclobemide. Lancet. December 1993, 342 (8886-8887): 1528–1532. PMID 7902906. doi:10.1016/S0140-6736(05)80090-X. 
  4. ^ 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. 
  5. ^ Scheen AJ. [Drug of the month. Moclobemide (Aurorix)]. Rev Med Liege. May 1994, 49 (5): 291–2. PMID 8023056 (法语). 
  6. ^ 6.0 6.1 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. 
  7. ^ PRODUCT INFORMATION MOCLOBEMIDE SANDOZ® 150mg and 300mg TABLETS. TGA eBusiness Services. Sandoz. 6 March 2012 [16 October 2013]. (原始内容存档于2020-09-21). 

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