比较碳青霉烯的审查。

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Zhanel GG, Wiebe R, Dilay L,汤姆森K, E,鲁宾斯坦贺朋的DJ, Noreddin, Karlowsky农协

比较碳青霉烯的审查。

药。2007;67 (7):1027 - 52。

PubMed ID
17488146 (在PubMed
]
文摘

碳青霉烯是beta-lactam抗菌药物与异常广泛的活动。年长的碳青霉烯,如imipenem,往往容易被酶降解dehydropeptidase-1 (DHP-1)位于肾小管和要求与DHP-1 cilastatin等抑制剂。后添加到类,如meropenem厄他培南DHP-1 doripenem证明增加稳定和管理没有DHP-1抑制剂。像所有beta-lactam抗菌药物,碳青霉烯通过抑制细菌细胞壁合成绑定和灭活penicillin-binding蛋白质(是)。大多数beta-lactamases包括碳青霉烯稳定AmpC beta-lactamases和extended-spectrum beta-lactamases。耐碳青霉烯发展当细菌获取或开发结构性变化在他们的是,当他们获得金属-β-内酰胺酶能够快速降解的碳青霉烯,或者当膜透性的变化产生的结果失去某些特定的外膜名叫孔。碳青霉烯(imipenem meropenem doripenem)具有广谱体外活动,包括活动对许多革兰氏阳性和革兰氏阴性厌氧菌;碳青霉烯缺乏活动对肠球菌都有效,耐甲氧西林金黄色葡萄球菌和Stenotrophomonas maltophilia。与imipenem相比,meropenem doripenem,厄他培南更有限的频谱活动主要是因为它缺乏活动对铜绿假单胞菌和肠球菌spp。imipenem meropenem和doripenem体内一半的生命大约1小时,而厄他培南半衰期约4小时使其适合每日一次。与其他beta-lactam抗菌药物,最重要的药效学参数预测体内功效是血浆药物浓度的时间维持在最低抑制浓度(T >麦克风)。 Imipenem/cilastatin and meropenem have been studied in comparative clinical trials establishing their efficacy in the treatment of a variety of infections including complicated intra-abdominal infections, skin and skin structure infections, community-acquired pneumonia, nosocomial pneumonia, complicated urinary tract infections, meningitis (meropenem only) and febrile neutropenia. The current role for imipenem/cilastatin and meropenem in therapy remains for use in moderate to severe nosocomial and polymicrobial infections. The unique antimicrobial spectrum and pharmacokinetic properties of ertapenem make it more suited to treatment of community-acquired infections and outpatient intravenous antimicrobial therapy than for the treatment of nosocomial infections. Doripenem is a promising new carbapenem with similar properties to those of meropenem, although it appears to have more potent in vitro activity against P. aeruginosa than meropenem. Clinical trials are required to establish the efficacy and safety of doripenem in moderate to severe infections, including nosocomial infections.

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药物
药物靶点
药物 目标 类 生物 药理作用 行动
Imipenem Penicillin-binding蛋白1 蛋白质 大肠杆菌(应变K12)
是的
抑制剂
 细节
Imipenem Penicillin-binding蛋白质1 b 蛋白质 大肠杆菌(应变K12)
是的
抑制剂
 细节
Imipenem Penicillin-binding蛋白2 蛋白质 大肠杆菌(应变K12)
是的
抑制剂
 细节
Imipenem Penicillin-binding蛋白3 蛋白质 枯草芽孢杆菌(168株)
未知的
抑制剂
 细节