Neu H C, Chin N X
Department of Medicine, College of Physicians & Surgeons, Columbia University, New York, New York 10032.
Eur J Clin Microbiol Infect Dis. 1989 Jul;8(7):644-50. doi: 10.1007/BF01968149.
The activity of PD 117596-2, a novel quinolone, was compared to that of other quinolones, ceftazidime, imipenem and gentamicin. PD 117596-2 inhibited most Enterobacteriaceae at concentrations less than 0.25 micrograms/ml, being equal or superior in activity to ciprofloxacin and 2- to 4-fold more active than ofloxacin. It inhibited ceftazidime-resistant Enterobacter spp., Citrobacter spp. and Serratia marcescens. The MIC90 for Pseudomonas aeruginosa, including strains with imipenem MICs of 8 micrograms/ml and gentamicin MICs greater than 16 micrograms/ml, was 0.25 micrograms/ml. PD 117596-2 was more active than ciprofloxacin against Pseudomonas cepacia and Pseudomonas maltophilia, and it inhibited Neisseria gonorrhoeae and Haemophilus influenzae at less than 0.03 micrograms/ml. PD 117596-2 inhibited staphylococci at 0.5 micrograms/ml, being 2-fold superior to other quinolones, and with an MIC of 0.25 micrograms/ml was more active against group A, B, C and G streptococci and Streptococcus pneumoniae. MICs for Bacteroides spp. were 2 micrograms/ml compared to 8-32 micrograms/ml for other agents. The frequency of spontaneous resistance was low (less than 10(-10]. Differences in MICs and MBCs were within one dilution, and there was a minimal effect of inoculum size. Although PD 117596-2 was less active at pH 5.5, MICs were less than 0.5 micrograms/ml.
将新型喹诺酮类药物PD 117596-2的活性与其他喹诺酮类药物、头孢他啶、亚胺培南和庆大霉素进行了比较。PD 117596-2在浓度低于0.25微克/毫升时可抑制大多数肠杆菌科细菌,其活性与环丙沙星相当或更高,比氧氟沙星高2至4倍。它可抑制对头孢他啶耐药的肠杆菌属、柠檬酸杆菌属和粘质沙雷氏菌。铜绿假单胞菌的MIC90为0.25微克/毫升,包括亚胺培南MIC为8微克/毫升和庆大霉素MIC大于16微克/毫升的菌株。PD 117596-2对洋葱伯克霍尔德菌和嗜麦芽窄食单胞菌的活性比环丙沙星更强,它在浓度低于0.03微克/毫升时可抑制淋病奈瑟菌和流感嗜血杆菌。PD 117596-2在浓度为0.5微克/毫升时可抑制葡萄球菌,比其他喹诺酮类药物强2倍,其MIC为0.25微克/毫升时对A、B、C和G组链球菌及肺炎链球菌的活性更强。拟杆菌属的MIC为2微克/毫升,而其他药物为8至32微克/毫升。自发耐药频率较低(低于10^-10)。MIC和MBC的差异在一个稀释度范围内,接种量大小的影响最小。尽管PD 117596-2在pH 5.5时活性较低,但其MIC低于0.5微克/毫升。