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新型头孢菌素头孢甲肟(SCE - 1365)的β-内酰胺酶稳定性及抗菌活性

Beta-lactamase stability and antibacterial activity of cefmenoxime (SCE-1365), a novel cephalosporin.

作者信息

Okonogi K, Kuno M, Kida M, Mitsuhashi S

出版信息

Antimicrob Agents Chemother. 1981 Aug;20(2):171-5. doi: 10.1128/AAC.20.2.171.

Abstract

Cefmenoxime, a new cephalosporin antibiotic, has been shown to be stable to a Staphylococcus aureus penicillinase and R plasmid-mediated type I and type IV penicillinases. It was also resistant to hydrolysis by most cephalosporinases, but was susceptible to hydrolysis by a Proteus vulgaris beta-lactamase. Cefmenoxime was active against cephaloridine-resistant species, except Pseudomonas aeruginosa, which was moderately resistant to cefmenoxime. Cefmenoxime was an inducer of P. vulgaris beta-lactamase biosynthesis, but 1 microgram or more of the drug per ml, which inhibits most of the clinical isolates of P. vulgaris, was required for the production of detectable amounts of the enzyme. Cefmenoxime was a strong competitive inhibitor of beta-lactamases of Enterobacter cloacae, Citrobacter freundii, P. aeruginosa, and Serratia marcescens, but it did not inhibit penicillinases in spite of its resistance to hydrolysis.

摘要

头孢甲肟,一种新型头孢菌素抗生素,已被证明对金黄色葡萄球菌青霉素酶以及R质粒介导的I型和IV型青霉素酶具有稳定性。它对大多数头孢菌素酶的水解作用也具有抗性,但对普通变形杆菌β-内酰胺酶敏感。头孢甲肟对除铜绿假单胞菌外的头孢菌素耐药菌具有活性,而铜绿假单胞菌对头孢甲肟有中度耐药性。头孢甲肟是普通变形杆菌β-内酰胺酶生物合成的诱导剂,但每毫升需要1微克或更多该药物(才能)抑制普通变形杆菌的大多数临床分离株,以产生可检测量的该酶。头孢甲肟是阴沟肠杆菌、弗氏柠檬酸杆菌、铜绿假单胞菌和粘质沙雷氏菌β-内酰胺酶的强竞争性抑制剂,但尽管它对水解具有抗性,却不抑制青霉素酶。

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