Roosendaal R, Bakker-Woudenberg I A, van den Berghe-van Raffe M, Vink-van den Berg J C, Michel M F
Department of Clinical Microbiology and Antimicrobial Therapy, Erasmus University Rotterdam, The Netherlands.
Antimicrob Agents Chemother. 1987 Nov;31(11):1809-15. doi: 10.1128/AAC.31.11.1809.
The antibacterial activities of ciprofloxacin and ceftazidime against Klebsiella pneumoniae in vitro and in vivo were compared. Although there was only a minor difference between the MBCs of both drugs, the bacterial killing rate of ciprofloxacin in vitro was very fast in comparison with that of ceftazidime. Similarly, the intravenous administration of ciprofloxacin at 1 h after bacterial inoculation resulted in effective bacterial killing in the lungs of leukopenic rats. This killing was dose dependent, in contrast to the dose-independent bactericidal effect of ceftazidime. The high antibacterial activity of ciprofloxacin in the lungs as compared with that of ceftazidime was also reflected in its therapeutic efficacy in K. pneumoniae pneumonia and septicemia in leukopenic rats when these infections were treated at 6-h intervals over 4 days, starting at 5 h after bacterial inoculation. Concentrations of ciprofloxacin and ceftazidime in lung tissue were not significantly different. Regarding the antibacterial activity of both drugs against K. pneumoniae in relation to the bacterial growth rate in vitro and in the lungs of leukopenic rats, ciprofloxacin killed K. pneumoniae organisms that were not actively growing, whereas ceftazidime did not. In addition, it was demonstrated that when the intravenous administration of antibiotic was delayed from 1 h up to 24 h after bacterial inoculation, ceftazidime lost its antibacterial activity in the lungs and blood of leukopenic rats, whereas ciprofloxacin was still very effective. These data suggest that the capacity of an antibiotic to kill bacteria at a slow growth rate may be relevant for its therapeutic effect in established infections, in which slowly growing bacteria form a substantial part of the total bacterial population.
比较了环丙沙星和头孢他啶对肺炎克雷伯菌的体外和体内抗菌活性。尽管两种药物的最低杀菌浓度(MBC)之间只有微小差异,但与头孢他啶相比,环丙沙星的体外细菌杀灭率非常快。同样,在细菌接种后1小时静脉注射环丙沙星可有效杀灭白细胞减少大鼠肺部的细菌。这种杀灭作用是剂量依赖性的,与头孢他啶的非剂量依赖性杀菌作用相反。与头孢他啶相比,环丙沙星在肺部的高抗菌活性也体现在其对白细胞减少大鼠肺炎克雷伯菌肺炎和败血症的治疗效果上,这些感染在细菌接种后5小时开始,每隔6小时治疗4天。环丙沙星和头孢他啶在肺组织中的浓度没有显著差异。关于两种药物对肺炎克雷伯菌的抗菌活性与体外和白细胞减少大鼠肺部细菌生长速率的关系,环丙沙星能杀灭非活跃生长的肺炎克雷伯菌,而头孢他啶则不能。此外,还证明当细菌接种后抗生素静脉给药从1小时延迟至24小时时,头孢他啶在白细胞减少大鼠的肺部和血液中失去了抗菌活性,而环丙沙星仍然非常有效。这些数据表明,抗生素在缓慢生长速率下杀灭细菌的能力可能与其对已建立感染的治疗效果相关,在这些感染中,缓慢生长的细菌占总细菌群体的很大一部分。