Gu J W, Neu H C
Department of Medicine, College of Physicians and Surgeons, Columbia University, New York, New York 10032.
Antimicrob Agents Chemother. 1990 Feb;34(2):189-95. doi: 10.1128/AAC.34.2.189.
The in vitro activity of Ro 23-9424, which is desacetyl-cefotaxime linked to fleroxacin, was compared with the activities of cefotaxime, desacetyl-cefotaxime, fleroxacin, ofloxacin, and ciprofloxacin. It inhibited the majority of members of the family Enterobacteriaceae, except for some Serratia marcescens, Citrobacter freundii, and Enterobacter cloacae strains, at less than or equal to 0.25 microgram/ml and had an MIC for 90% of strains tested (MIC90) of 8 micrograms/ml against Pseudomonas aeruginosa. Most group A, B, C, and G streptococci and Streptococcus pneumoniae were inhibited at less than or equal to 0.25 microgram/ml. Ninety percent of the staphylococci were inhibited at less than or equal to 4 micrograms/ml, except for some methicillin-resistant Staphylococcus aureus isolates. The MIC90S of Ro 23-9424 for Enterococcus faecalis and Listeria monocytogenes were greater than or equal to 16 micrograms/ml. Ninety percent of Clostridium perfringens isolates were inhibited by less than or equal to 2 micrograms/ml, whereas Bacteroides fragilis had an MIC90 of 32 micrograms/ml. There was a minimal inoculum size effect. The MICs and MBCs were either identical or within a twofold dilution. The MICs of Ro 23-9424 for Escherichia coli, Klebsiella pneumoniae, Serratia marcescens, Enterobacter cloacae, Citrobacter freundii, Pseudomonas aeruginosa, and Staphylococcus aureus increased 16- to 128-fold after 2 weeks of transfer in the presence of Ro 23-9424, showing that the presence of two agents does not prevent resistance.
将去乙酰头孢噻肟与氟罗沙星相连的Ro 23-9424的体外活性,与头孢噻肟、去乙酰头孢噻肟、氟罗沙星、氧氟沙星和环丙沙星的活性进行了比较。它能抑制大多数肠杆菌科成员,除了一些粘质沙雷氏菌、弗氏柠檬酸杆菌和阴沟肠杆菌菌株,其抑制浓度小于或等于0.25微克/毫升,对铜绿假单胞菌的90%受试菌株的最低抑菌浓度(MIC90)为8微克/毫升。大多数A、B、C和G组链球菌以及肺炎链球菌在小于或等于0.25微克/毫升时被抑制。90%的葡萄球菌在小于或等于4微克/毫升时被抑制,除了一些耐甲氧西林金黄色葡萄球菌分离株。Ro 23-9424对粪肠球菌和单核细胞增生李斯特菌的MIC90大于或等于16微克/毫升。90%的产气荚膜梭菌分离株在小于或等于2微克/毫升时被抑制,而脆弱拟杆菌的MIC90为32微克/毫升。接种量效应极小。MIC和MBC要么相同,要么在两倍稀释范围内。在Ro 23-9424存在的情况下传代2周后,Ro 23-9424对大肠杆菌、肺炎克雷伯菌、粘质沙雷氏菌、阴沟肠杆菌、弗氏柠檬酸杆菌、铜绿假单胞菌和金黄色葡萄球菌的MIC增加了16至128倍,表明两种药物同时存在并不能阻止耐药性产生。