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头孢布烯:抗菌活性、抗菌谱及其他微生物学特性综述

Ceftibuten: a review of antimicrobial activity, spectrum and other microbiologic features.

作者信息

Jones R N

机构信息

Division of Medical Microbiology, University of Iowa College of Medicine, Iowa City 52242-1009, USA.

出版信息

Pediatr Infect Dis J. 1995 Jul;14(7 Suppl):S77-83.

PMID:7567314
Abstract

Ceftibuten is a new, orally administered cephalosporin with exceptional beta-lactamase stability and potency against commonly isolated Gram-negative pathogens. More than 90% of recent Enterobacteriaceae clinical isolates were inhibited by < or = 8 micrograms/ml of ceftibuten. In only five enteric species (Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Morganella morganii, Serratia marcescens) were more than 15% of strains resistant (minimal inhibitory concentrations (MIC, with percent of strains inhibited in subscript numbers) > 16 micrograms/ml) to ceftibuten. Enteritis-producing bacteria such as Salmonella, Shigella, Escherichia coli and Yersinia were very ceftibuten-susceptible (MIC50 < or = 0.13 microgram/ml). Fastidious Gram-negative species causing respiratory tract or genital infections had very low ceftibuten MICs, including beta-lactamase-positive Haemophilus influenzae (MIC90 0.06 to 2 micrograms/ml), Moraxella catarrhalis (MIC90 0.25 to 4 micrograms/ml), and Neisseria gonorrhoeae (MIC90 0.015 to 0.5 microgram/ml). Beta-hemolytic streptococci and penicillin-susceptible pneumococci were also inhibited by ceftibuten. Staphylococci, enterococci, Pseudomonas species and Gram-negative anaerobic bacteria were generally resistant to ceftibuten. Ceftibuten has demonstrated bactericidal activity against susceptible pathogens, has high affinity for several lethal penicillin-binding proteins and possesses stability to common plasmid- or chromosomal-mediated beta-lactamases, including those enzymes that hydrolyze parenteral third generation cephalosporins. The microbiologic features for ceftibuten indicate its clinical potential as chemotherapy for community-acquired respiratory tract infections.

摘要

头孢布烯是一种新型口服头孢菌素,对常见的革兰氏阴性病原体具有出色的β-内酰胺酶稳定性和抗菌效力。近期分离出的肠杆菌科临床菌株中,超过90%被≤8微克/毫升的头孢布烯所抑制。仅在五种肠道菌(弗氏柠檬酸杆菌、产气肠杆菌、阴沟肠杆菌、摩根摩根菌、粘质沙雷菌)中,超过15%的菌株对头孢布烯耐药(最低抑菌浓度(MIC,下标数字为被抑制菌株的百分比)>16微克/毫升)。引起肠炎的细菌,如沙门氏菌、志贺氏菌、大肠杆菌和耶尔森氏菌对头孢布烯非常敏感(MIC50≤0.13微克/毫升)。引起呼吸道或生殖道感染的苛养革兰氏阴性菌的头孢布烯MIC值非常低,包括β-内酰胺酶阳性的流感嗜血杆菌(MIC90为0.06至2微克/毫升)、卡他莫拉菌(MIC90为0.25至4微克/毫升)和淋病奈瑟菌(MIC90为0.015至0.5微克/毫升)。β-溶血性链球菌和对青霉素敏感的肺炎球菌也被头孢布烯所抑制。葡萄球菌、肠球菌、假单胞菌属和革兰氏阴性厌氧菌通常对头孢布烯耐药。头孢布烯已证明对敏感病原体具有杀菌活性,对几种致死性青霉素结合蛋白具有高亲和力,并且对常见的质粒或染色体介导的β-内酰胺酶具有稳定性,包括那些水解胃肠外第三代头孢菌素的酶。头孢布烯的微生物学特性表明其作为社区获得性呼吸道感染化疗药物的临床潜力。

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