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GR - 20263:一种对假单胞菌属和肠杆菌科具有高活性的新型氨基噻唑基头孢菌素。

GR-20263: a new aminothiazolyl cephalosporin with high activity against Pseudomonas and Enterobacteriaceae.

作者信息

Verbist L, Verhaegen J

出版信息

Antimicrob Agents Chemother. 1980 May;17(5):807-12. doi: 10.1128/AAC.17.5.807.

Abstract

The in vitro activity of GR-20263, a new aminothiazolyl cephalosporin, was compared with the activities of other beta-lactam antibiotics by using 800 clinical bacterial isolates. GR-20263 was highly active (inhibition of 90% of the isolates between 0.03 and 1 microgram/ml) against the common Enterobacteriaceae and 5 to 20 times more active than cefuroxime, cefoxitin, and cephalothin. GR-20263 was three to six times less active than cefotaxime against Escherichia coli, Klebsiella pneumoniae, Salmonella, and Shigella, but three to four times more active than cefotaxime against Proteus vulgaris and Serratia marcescens. The activity of GR-20263 against Pseudomonas aeruginosa (with minimal inhibitory concentrations of 2 and 8 micrograms/ml for 90 and 100% of the isolates, respectively) was similar to that of tobramycin, 2 times that of cefsulodin, 5 times that of piperacillin, and 10 times that of cefotaxime. Against Haemophilus influenzae GR-20263 was three time more active than ampicillin. The beta-lactamase-producing strains were as susceptible to GR-20263 as the beta-lactamase-negative strains. GR-20263 was less active than cefotaxime and ampicillin against Staphylococcus aureus.

摘要

通过使用800株临床分离菌,将新型氨噻唑基头孢菌素GR-20263的体外活性与其他β-内酰胺类抗生素的活性进行了比较。GR-20263对常见肠杆菌科细菌具有高活性(抑制90%的分离菌所需浓度在0.03至1微克/毫升之间),其活性比头孢呋辛、头孢西丁和头孢噻吩高5至20倍。GR-20263对大肠杆菌、肺炎克雷伯菌、沙门菌和志贺菌的活性比对头孢噻肟低三至六倍,但对普通变形杆菌和粘质沙雷菌的活性比对头孢噻肟高三至四倍。GR-20263对铜绿假单胞菌的活性(90%和100%的分离菌的最低抑菌浓度分别为2和8微克/毫升)与妥布霉素相似,是头孢磺啶的2倍、哌拉西林的5倍和头孢噻肟的10倍。对流感嗜血杆菌,GR-20263的活性比氨苄西林高三倍。产β-内酰胺酶的菌株与不产β-内酰胺酶的菌株对GR-20263同样敏感。GR-20263对金黄色葡萄球菌的活性比对头孢噻肟和氨苄西林低。

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