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美罗培南10700,一种新型青霉烯类抗生素:体外活性及其与β-内酰胺酶稳定性、青霉素结合蛋白亲和力和通过细菌细胞壁扩散的相关性。

MEN 10700, a new penem antibiotic: in-vitro activity and its correlation with beta-lactamase stability, PBP affinity and diffusion through the bacterial cell wall.

作者信息

Fontana R, Altamura M, Arcamone F, Mazzariol A, Morandotti G, Sperning R, Cornaglia G

机构信息

Istituto di Microbiologia, Università di Verona, Italy.

出版信息

J Antimicrob Chemother. 1998 May;41(5):513-25. doi: 10.1093/jac/41.5.513.

DOI:10.1093/jac/41.5.513
PMID:9630405
Abstract

The in-vitro activity of MEN 10700, a novel penem, was compared with that of imipenem, ritipenem, ampicillin/sulbactam, cefotaxime, ciprofloxacin and amikacin against 1088 strains taken from 21 genera, including Gram-negative, Gram-positive and anaerobic bacteria. MIC data showed that MEN 10700 was very active against staphylococci and streptococci (MIC90 < or = 0.5 mg/L) and against most members of the Enterobacteriaceae (MIC90 < or = 2 mg/L), with reduced activity only against Providencia stuartii (MIC90 = 8 mg/L). MEN 10700 was also active against anaerobic species such as Clostridium perfringens and Bacteroides fragilis as well as Moraxella catarrhalis. It was moderately active against Enterococcus faecalis and inactive against Pseudomonas aeruginosa, Stenotrophomonas maltophilia, Aeromonas spp. and Acinetobacter spp. Its antibacterial spectrum was thus slightly narrower than that of imipenem, but compared favourably with those of a third-generation cephalosporin and ritipenem. MEN 10700 was highly stable to a number of beta-lactamases and was a poor inducer of class I enzymes. It bound penicillin-binding protein 2 with the highest affinity and easily permeated the outer membrane of Escherichia coli.

摘要

将新型青霉烯类药物MEN 10700的体外活性与亚胺培南、利替培南、氨苄西林/舒巴坦、头孢噻肟、环丙沙星和阿米卡星针对来自21个菌属的1088株菌株(包括革兰氏阴性菌、革兰氏阳性菌和厌氧菌)的活性进行了比较。最低抑菌浓度(MIC)数据表明,MEN 10700对葡萄球菌和链球菌(MIC90≤0.5mg/L)以及大多数肠杆菌科成员(MIC90≤2mg/L)具有很强的活性,仅对斯氏普罗威登斯菌活性降低(MIC90 = 8mg/L)。MEN 10700对诸如产气荚膜梭菌、脆弱拟杆菌以及卡他莫拉菌等厌氧菌也有活性。它对粪肠球菌活性中等,对铜绿假单胞菌、嗜麦芽窄食单胞菌、气单胞菌属和不动杆菌属无活性。因此,其抗菌谱比亚胺培南略窄,但与第三代头孢菌素和利替培南相比具有优势。MEN 10700对多种β-内酰胺酶高度稳定,且是I类酶的弱诱导剂。它以最高亲和力结合青霉素结合蛋白2,并且易于透过大肠杆菌的外膜。

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