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新型口服活性头孢烯抗生素FK 027的体外和体内抗菌特性

In vitro and in vivo antibacterial properties of FK 027, a new orally active cephem antibiotic.

作者信息

Kamimura T, Kojo H, Matsumoto Y, Mine Y, Goto S, Kuwahara S

出版信息

Antimicrob Agents Chemother. 1984 Jan;25(1):98-104. doi: 10.1128/AAC.25.1.98.

Abstract

FK 027 was more active than cefaclor, cephalexin, and amoxicillin against stock strains of a wide variety of gram-negative bacteria, including such opportunistic pathogens as Citrobacter and Enterobacter species and Serratia marcescens. FK 027 was significantly more active than the three reference drugs against clinical isolates of Escherichia coli, Klebsiella pneumoniae, indole-positive and -negative Proteus species, Providencia species, Haemophilus influenzae, and Neisseria gonorrhoeae. It was less active than cefaclor, cephalexin, and amoxicillin against staphylococci, but it was similar to cefaclor in its activity against streptococci. With few exceptions, FK 027 was active against strains of E. coli, K. pneumoniae, and Proteus mirabilis that were resistant to the reference agents. The bactericidal activity of FK 027 against various gram-negative bacteria, including Proteus species, Citrobacter freundii, Enterobacter aerogenes, and S. marcescens, was greater than that of cefaclor, cephalexin, and amoxicillin. The therapeutic activities of FK 027 in mice infected with gram-negative bacilli were far superior to the activities of cefaclor, cephalexin, and amoxicillin, but they were inferior to the activities of these reference drugs against infection with Staphylococcus aureus.

摘要

FK 027对多种革兰氏阴性菌的标准菌株的活性比头孢克洛、头孢氨苄和阿莫西林更强,这些革兰氏阴性菌包括柠檬酸杆菌属、肠杆菌属等机会致病菌以及粘质沙雷氏菌。FK 027对大肠杆菌、肺炎克雷伯菌、吲哚阳性和阴性变形杆菌属、普罗威登斯菌属、流感嗜血杆菌和淋病奈瑟菌临床分离株的活性明显高于这三种参比药物。它对葡萄球菌的活性低于头孢克洛、头孢氨苄和阿莫西林,但对链球菌的活性与头孢克洛相似。除少数例外,FK 027对耐参比药物的大肠杆菌、肺炎克雷伯菌和奇异变形杆菌菌株有活性。FK 027对包括变形杆菌属、弗氏柠檬酸杆菌、产气肠杆菌和粘质沙雷氏菌在内的各种革兰氏阴性菌的杀菌活性大于头孢克洛、头孢氨苄和阿莫西林。FK 027在感染革兰氏阴性杆菌的小鼠中的治疗活性远优于头孢克洛、头孢氨苄和阿莫西林,但在抗金黄色葡萄球菌感染方面不如这些参比药物的活性。

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