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两种口服头孢菌素头孢替胺(Ro 19-5247)和头孢他美酯(Ro 15-8074)的体外活性及β-内酰胺酶稳定性

In vitro activity and beta-lactamase stability of two oral cephalosporins, ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074).

作者信息

Neu H C, Chin N X, Labthavikul P

出版信息

Antimicrob Agents Chemother. 1986 Sep;30(3):423-8. doi: 10.1128/AAC.30.3.423.

Abstract

Ceftetrame (Ro 19-5247) and cefetamet (Ro 15-8074), two new orally administered aminothiazolyl imimomethoxy cephalosporins, inhibited hemolytic streptococci and Streptococcus pneumoniae at less than or equal to 0.5 micrograms/ml but were less active against staphylococci than were cephalexin and cefaclor. They did not inhibit S. faecalis, S. faecium, Listeria monocytogenes, Corynebacterium JK species, or Pseudomonas aeruginosa. Haemophilus influenzae, Branhamella catarrhalis, and Neisseria gonorrhoeae, including ampicillin-resistant isolates, were inhibited at less than 0.25 micrograms/ml. Both agents inhibited Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Proteus mirabilis, Salmonella species, Shigella species, Citrobacter diversus, and Aeromonas hydrophila resistant to ampicillin, cephalexin, and cefaclor at less than or equal to 2 micrograms/ml, although many isolates of Enterobacter cloacae, Citrobacter freundii, and Serratia marcescens resistant to cefotaxime were not inhibited by these agents. A marked inoculum effect was noted for Enterobacteriaceae carrying the Richmond-Sykes type 1A chromosomally mediated beta-lactamases, but plasmid-mediated beta-lactamases did not hydrolyze the compounds. Both drugs inhibited the chromosomally mediated beta-lactamase of E. cloacae, P99.

摘要

头孢曲嗪(Ro 19 - 5247)和头孢他美酯(Ro 15 - 8074)是两种新型口服氨噻唑基亚胺甲氧基头孢菌素,对溶血性链球菌和肺炎链球菌的抑制浓度小于或等于0.5微克/毫升,但对葡萄球菌的活性低于头孢氨苄和头孢克洛。它们对粪肠球菌、屎肠球菌、单核细胞增生李斯特菌、JK棒状杆菌或铜绿假单胞菌无抑制作用。流感嗜血杆菌、卡他布兰汉菌和淋病奈瑟菌,包括耐氨苄西林菌株,在浓度小于0.25微克/毫升时被抑制。两种药物对大肠杆菌、肺炎克雷伯菌、产酸克雷伯菌、奇异变形杆菌、沙门菌属、志贺菌属、弗氏柠檬酸杆菌和对氨苄西林、头孢氨苄及头孢克洛耐药的嗜水气单胞菌的抑制浓度小于或等于2微克/毫升,不过许多对头孢噻肟耐药的阴沟肠杆菌、弗氏柠檬酸杆菌和粘质沙雷菌分离株不受这些药物抑制。对于携带里士满 - 赛克斯1A 型染色体介导的β - 内酰胺酶的肠杆菌科细菌,观察到明显的接种量效应,但质粒介导的β - 内酰胺酶不会水解这些化合物。两种药物均抑制阴沟肠杆菌的染色体介导的β - 内酰胺酶P99。

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