Piddock L J, Zhu M
Antimicrobial Agents Research Group, Medical School, University of Birmingham, United Kingdom.
Antimicrob Agents Chemother. 1991 Nov;35(11):2423-7. doi: 10.1128/AAC.35.11.2423.
The inhibition of DNA synthesis by sparfloxacin; accumulation of sparfloxacin into members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and staphylococci; induction of recA in Escherichia coli; and the optimum bactericidal concentration (OBC) were measured, and killing kinetics at the OBC were estimated. The OBC and maximum recA-inducing concentration in E. coli were both 1 microgram of sparfloxacin per ml. Accumulation was rapid; two- to threefold more sparfloxacin than ciprofloxacin accumulated in staphylococci and more sparfloxacin accumulated in staphylococci than in gram-negative bacteria. Laboratory mutants with decreased susceptibilities to quinolones alone or multiply resistant were selected from the Enterobacteriaceae and Staphylococcus aureus by using sparfloxacin.
测定了司帕沙星对DNA合成的抑制作用;司帕沙星在肠杆菌科细菌、铜绿假单胞菌和葡萄球菌中的蓄积情况;大肠杆菌中recA的诱导情况以及最佳杀菌浓度(OBC),并估计了在OBC时的杀菌动力学。大肠杆菌中的OBC和recA诱导的最大浓度均为每毫升1微克司帕沙星。蓄积迅速;葡萄球菌中司帕沙星的蓄积量比环丙沙星多两到三倍,且葡萄球菌中司帕沙星的蓄积量比革兰氏阴性菌多。通过使用司帕沙星,从肠杆菌科细菌和金黄色葡萄球菌中筛选出了对喹诺酮类药物敏感性降低或多重耐药的实验室突变株。