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头孢曲松(Ro 13 - 9904)的抗菌活性,一种对β-内酰胺酶稳定的头孢菌素。

Antibacterial activity of ceftriaxone (Ro 13-9904), a beta-lactamase-stable cephalosporin.

作者信息

Neu H C, Meropol N J, Fu K P

出版信息

Antimicrob Agents Chemother. 1981 Mar;19(3):414-23. doi: 10.1128/AAC.19.3.414.

Abstract

The in vitro activity of ceftriaxone (Ro 13-9904), a parenteral cephalosporin, was compared with that of other beta-lactam antibiotics. the compound was less active against Staphylococcus aureus and Staphylococcus epidermidis than was cephalothin or cefamandole, but it was comparable to cefoxitin, cefotaxime, and moxalactam in inhibiting most isolates of S. aureus at 3.1 microgram/ml. Ro 13-9904 inhibited Streptococcus pyogenes and Streptococcus pneumoniae at concentrations below 0.25 microgram/ml, but Streptococcus faecalis required concentrations above 25 microgram/ml. Neisseria gonorrhoeae and Haemophilus influenzae were inhibited at concentrations similar to those of cefotaxime, less than 0.1 microgram/ml. Ro 13-9904 was as active as cefotaxime and moxalactam against most Enterobacteriaceae and was the most active agent tested against Proteus, inhibiting all strains tested at 0.006 microgram/ml. Ro 13-9904 was slightly less active than moxalactam or cefoxitin against Bacteroides fragilis, requiring more than 100 microgram/ml to inhibit 90% of isolates, and it was less active than cefoperazone against Pseudomonas aeruginosa. Presence of serum, alteration of pH, and use of various media did not change the inhibitory levels. Bactericidal concentrations were similar to inhibitory levels. Ro 13-9904 was stable to most plasmid-mediated beta-lactamases, but was hydrolyzed by some Enterobacter, Proteus, and Bacteroides beta-lactamases of chromosomal origin.

摘要

将头孢曲松(Ro 13-9904,一种肠道外使用的头孢菌素)的体外活性与其他β-内酰胺类抗生素进行了比较。该化合物对金黄色葡萄球菌和表皮葡萄球菌的活性低于头孢噻吩或头孢孟多,但在抑制大多数金黄色葡萄球菌分离株方面,其活性与头孢西丁、头孢噻肟和拉氧头孢相当,浓度为3.1微克/毫升。Ro 13-9904在浓度低于0.25微克/毫升时可抑制化脓性链球菌和肺炎链球菌,但粪肠球菌需要浓度高于25微克/毫升。淋病奈瑟菌和流感嗜血杆菌在与头孢噻肟相似的浓度(低于0.1微克/毫升)下被抑制。Ro 13-9904对大多数肠杆菌科细菌的活性与头孢噻肟和拉氧头孢相当,并且是测试的对变形杆菌最具活性的药物,在0.006微克/毫升时可抑制所有测试菌株。Ro 13-9904对脆弱拟杆菌的活性略低于拉氧头孢或头孢西丁,抑制90%的分离株需要超过100微克/毫升,并且对铜绿假单胞菌的活性低于头孢哌酮。血清的存在、pH值的改变以及各种培养基的使用均未改变抑制水平。杀菌浓度与抑制水平相似。Ro 13-9904对大多数质粒介导的β-内酰胺酶稳定,但可被一些染色体来源的肠杆菌、变形杆菌和拟杆菌β-内酰胺酶水解。

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