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恶唑烷酮类化合物依哌唑胺(PNU - 100592)和利奈唑胺(PNU - 100766)与万古霉素相比,对金黄色葡萄球菌、凝固酶阴性葡萄球菌、粪肠球菌和屎肠球菌的体外比较活性及抗生素后效应。

Comparative in vitro activities and postantibiotic effects of the oxazolidinone compounds eperezolid (PNU-100592) and linezolid (PNU-100766) versus vancomycin against Staphylococcus aureus, coagulase-negative staphylococci, Enterococcus faecalis, and Enterococcus faecium.

作者信息

Rybak M J, Cappelletty D M, Moldovan T, Aeschlimann J R, Kaatz G W

机构信息

The Anti-Infective Research Laboratory, Department of Pharmacy Services, Detroit Receiving Hospital/University Health Center, Wayne State University, Michigan 48201, USA.

出版信息

Antimicrob Agents Chemother. 1998 Mar;42(3):721-4. doi: 10.1128/AAC.42.3.721.

Abstract

The activities of the oxazolidinone antibacterial agents eperezolid (PNU-100592) and linezolid (PNU-100766) were compared with that of vancomycin against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus (n = 200), coagulase-negative staphylococci (n = 100), and vancomycin-susceptible and -resistant Enterococcus faecalis and Enterococcus faecium (n = 50). Eperezolid and linezolid demonstrated good in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci (MIC at which 90% of the isolates are inhibited [MIC90] range, 1 to 4 microg/ml) or vancomycin susceptibility for enterococci (MIC90 range, 1 to 4 microg/ml). In time-kill studies, eperezolid and linezolid were bacteriostatic in action. A postantibiotic effect of 0.8+/-0.5 h was demonstrated for both eperezolid and linezolid against S. aureus, S. epidermidis, E. faecalis, and E. faecium.

摘要

将恶唑烷酮类抗菌剂依哌唑胺(PNU - 100592)和利奈唑胺(PNU - 100766)的活性与万古霉素针对甲氧西林敏感和耐药金黄色葡萄球菌(n = 200)、凝固酶阴性葡萄球菌(n = 100)以及万古霉素敏感和耐药粪肠球菌及屎肠球菌(n = 50)的临床分离株进行了比较。无论葡萄球菌对甲氧西林的敏感性(抑制90%分离株的最低抑菌浓度[MIC90]范围为1至4微克/毫升)或肠球菌对万古霉素的敏感性(MIC90范围为1至4微克/毫升)如何,依哌唑胺和利奈唑胺均表现出良好的体外抑制活性。在时间杀菌研究中,依哌唑胺和利奈唑胺具有抑菌作用。依哌唑胺和利奈唑胺对金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌和屎肠球菌均表现出0.8±0.5小时的抗生素后效应。

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