Yourassowsky E, Van der Linden M P, Crokaert F, Glupczynski Y
J Antimicrob Chemother. 1986 Apr;17 Suppl B:19-28. doi: 10.1093/jac/17.suppl_b.19.
Pefloxacin is a new quinolone carboxylic acid with a broad spectrum of antibacterial activity. A comparison was made of the in-vitro activity of pefloxacin and that of nine other antibiotics (ampicillin, ticarcillin, piperacillin, cefazolin, cefotaxime, ceftazidime, gentamicin, amikacin and norfloxacin). The MIC90 of pefloxacin against 500 strains of Enterobacteriaceae ranged from 0.25 mg/l (Escherichia coli, indole + Proteus spp., Enterobacter cloacae, Salmonella spp. and Shigella spp.) to 1 mg/l (Klebsiella pneumoniae). Pefloxacin inhibited 90% of 52 strains of Pseudomonas aeruginosa at 2.5 mg/l (range 0.25 mg/l-4 mg/l). The MIC90 of pefloxacin against 100 Staphylococcus aureus strains (78 oxacillin resistant strains) was 0.4 mg/l (range 0.12-0.5 mg/l). It was markedly less active against Streptococcus faecalis and Str. pneumoniae (37 strains of each species) the MIC90 being 4 mg/l against both species. Overall, pefloxacin was at least as active as the third-generation cephalosporins against Enterobacteriaceae and was more active than any other antibiotic tested against P. aeruginosa, S. epidermidis, and S. aureus. Against E. coli, pefloxacin had a more rapid anti-bacterial activity than piperacillin. A paradoxical effect was observed with pefloxacin. An optimal killing rate was observed at concentrations of pefloxacin compatible with those one can expect in blood of patients treated with this drug.
培氟沙星是一种新型喹诺酮羧酸,具有广谱抗菌活性。对培氟沙星与其他九种抗生素(氨苄西林、替卡西林、哌拉西林、头孢唑林、头孢噻肟、头孢他啶、庆大霉素、阿米卡星和诺氟沙星)的体外活性进行了比较。培氟沙星对500株肠杆菌科细菌的MIC90范围为0.25mg/L(大肠杆菌、吲哚阳性变形杆菌属、阴沟肠杆菌、沙门菌属和志贺菌属)至1mg/L(肺炎克雷伯菌)。培氟沙星在2.5mg/L(范围0.25mg/L - 4mg/L)时可抑制52株铜绿假单胞菌中的90%。培氟沙星对100株金黄色葡萄球菌(78株耐苯唑西林菌株)的MIC90为0.4mg/L(范围0.12 - 0.5mg/L)。它对粪肠球菌和肺炎链球菌(每种37株)的活性明显较低,两种菌的MIC90均为4mg/L。总体而言,培氟沙星对肠杆菌科细菌的活性至少与第三代头孢菌素相当,并且对铜绿假单胞菌、表皮葡萄球菌和金黄色葡萄球菌的活性比所测试的任何其他抗生素都更强。对大肠杆菌而言,培氟沙星的抗菌活性比哌拉西林更快。观察到培氟沙星有一个矛盾效应。在与使用该药治疗的患者血液中预期浓度相当的培氟沙星浓度下观察到了最佳杀菌率。