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新型口服单环β-内酰胺类药物替吉莫南的体外抗菌活性

Antibacterial activity in vitro of tigemonam, a new oral monobactam.

作者信息

Schito G C, Debbia E, Bandelloni R, Paglia P, Pesce A

机构信息

Institute of Microbiology, University of Genoa Medical School, Italy.

出版信息

J Chemother. 1989 May;1 Suppl 2:41-4.

PMID:2809702
Abstract

Using a broth microdilution method, the antibacterial activity of tigemonam, a novel oral monobactam, was evaluated against 217 gram-negative aerobes freshly isolated from clinical specimens. Reference antibiotics were amoxicillin, amoxicillin-sulbactam, cephalexin, cefaclor, norfloxacin, and co-trimoxazole. At a concentration of less than or equal to 8 mg/L, tigemonam inhibited 88% of the members of the Enterobacteriaceae family. Its activity was poor against the nonfermenter pathogens. In comparison with the other drugs, tigemonam generally exhibited superior antibacterial activity (with the exception of norfloxacin, which showed similar potency against the strains tested). Minimum bactericidal concentrations and time-kill determinations indicated that tigemonam showed remarkable bactericidal activity, with a 9% reduction in colony-forming units after 2 h at a dose corresponding to fourfold its minimum inhibitory concentration. When tigemonam was used in combination with netilmicin and amikacin against susceptible representative isolates of Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens and Escherichia coli, a synergistic effect was obtained.

摘要

采用肉汤微量稀释法,对一种新型口服单环β-内酰胺类药物替吉莫南对217株从临床标本中新鲜分离出的革兰氏阴性需氧菌的抗菌活性进行了评估。对照抗生素为阿莫西林、阿莫西林-舒巴坦、头孢氨苄、头孢克洛、诺氟沙星和复方新诺明。在浓度小于或等于8mg/L时,替吉莫南抑制了88%的肠杆菌科菌属成员。其对非发酵菌病原体的活性较差。与其他药物相比,替吉莫南总体上表现出更强的抗菌活性(诺氟沙星除外,其对测试菌株的效力相似)。最低杀菌浓度和时间杀菌测定表明,替吉莫南显示出显著的杀菌活性,在相当于其最低抑菌浓度四倍的剂量下作用2小时后,菌落形成单位减少了9%。当替吉莫南与奈替米星和阿米卡星联合用于对抗肺炎克雷伯菌、阴沟肠杆菌、粘质沙雷氏菌和大肠杆菌的敏感代表性分离株时,获得了协同效应。

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