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新型口服活性头孢菌素FR 17027的体外活性及β-内酰胺酶稳定性比较

Comparative in vitro activity and beta-lactamase stability of FR 17027, a new orally active cephalosporin.

作者信息

Neu H C, Chin N X, Labthavikul P

出版信息

Antimicrob Agents Chemother. 1984 Aug;26(2):174-80. doi: 10.1128/AAC.26.2.174.

Abstract

FR 17027, a new orally absorbed cephalosporin ester, inhibited group A and B streptococci and Streptococcus pneumoniae at less than or equal to 0.1 micrograms/ml, which is similar to the inhibition concentration of amoxicillin and cefaclor, and was more active than cephalexin. It was less active (MIC, 25 micrograms/ml) against staphylococci than was cephalexin, and it did not inhibit Streptococcus faecalis or Listeria monocytogenes. FR 17027 inhibited beta-lactamase-producing isolates of Neisseria gonorrhoeae, Haemophilus influenzae, and Branhamella catarrhalis at less than 0.1 micrograms/ml and was more active than cefaclor or cephalexin against these bacteria. FR 17027 inhibited Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Klebsiella oxytoca, Providencia stuartii, Providencia rettgeri, and Citrobacter diversus at less than or equal to 1 microgram/ml, including isolated resistant to amoxicillin, cephalexin, and cefaclor, but it was less active than ceftizoxime. Some strains of Enterobacter cloacae, Enterobacter agglomerans, Citrobacter freundii, and Enterobacter aerogenes were resistant (MIC, greater than 25 micrograms/ml). FR 17027 did not inhibit Pseudomonas aeruginosa, other Pseudomonas species, Acinetobacter species, or Bacteroides species. Activity was minimally affected by growth conditions. FR 17027 was not hydrolyzed by the common beta-lactamases present in many of the pathogens causing respiratory and urinary tract infections in outpatients.

摘要

FR 17027是一种新型口服吸收性头孢菌素酯,对A组和B组链球菌及肺炎链球菌的抑制浓度小于或等于0.1微克/毫升,这与阿莫西林和头孢克洛的抑制浓度相似,且比头孢氨苄活性更强。它对葡萄球菌的活性(最低抑菌浓度为25微克/毫升)低于头孢氨苄,且不抑制粪肠球菌或单核细胞增生李斯特菌。FR 17027对产生β-内酰胺酶的淋病奈瑟菌、流感嗜血杆菌和卡他布兰汉菌的抑制浓度小于0.1微克/毫升,对这些细菌的活性比头孢克洛或头孢氨苄更强。FR 17027对大肠杆菌、肺炎克雷伯菌、奇异变形杆菌、产酸克雷伯菌、斯氏普罗威登斯菌、雷氏普罗威登斯菌和多变柠檬酸杆菌的抑制浓度小于或等于1微克/毫升,包括对阿莫西林、头孢氨苄和头孢克洛耐药的菌株,但活性低于头孢唑肟。阴沟肠杆菌、聚团肠杆菌、弗氏柠檬酸杆菌和产气肠杆菌的一些菌株耐药(最低抑菌浓度大于25微克/毫升)。FR 17027不抑制铜绿假单胞菌、其他假单胞菌属、不动杆菌属或拟杆菌属。生长条件对其活性影响极小。FR 17027不会被门诊患者呼吸道和尿路感染的许多病原体中常见的β-内酰胺酶水解。

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