Foster J K, Lentino J R, Strodtman R, DiVincenzo C
Antimicrob Agents Chemother. 1986 Dec;30(6):823-7. doi: 10.1128/AAC.30.6.823.
Quinolone antibiotics have been proposed as possible alternatives to vancomycin for methicillin-resistant Staphylococcus aureus infections. We investigated the activities of amifloxacin, ciprofloxacin, norfloxacin, and vancomycin by time-kill kinetic studies. Antibiotic concentrations of 0, 1.0, and 4.0 times the MIC were used against four strains of gentamicin- and methicillin-resistant S. aureus. Staphylococci were plated onto ciprofloxacin-containing agar at all time points, in repeat time-kill kinetic studies. Macrobroth dilution MICs and MBCs were determined. Ciprofloxacin levels were measured by bioassay. Replica plating was performed from the original susceptible inoculum (MIC, 0.125 micrograms/ml) onto ciprofloxacin-supplemented agar. At 4.0 times the MIC, only with ciprofloxacin was there regrowth at 24 and 48 h. All four strains of staphylococci grew on agar supplemented with 1 microgram of ciprofloxacin per ml; three of four grew on agar supplemented with 2 micrograms of ciprofloxacin per ml. MICs and MBCs for these resistant clones ranged from 8 to 32 micrograms/ml. No degradation in activity or amount of ciprofloxacin could be detected in the bioassay. Replica-plated staphylococci grew on agar containing 1 microgram/ml but not higher concentrations of ciprofloxacin at 48 h. Amifloxacin and norfloxacin sustained bactericidal activity comparable to that of vancomycin. We conclude that heteroresistant subpopulations of gentamicin- and methicillin-resistant S. aureus can emerge under antibiotic selection pressure. Such resistant clones may then mutate in the presence of subinhibitory concentrations of antibiotic to higher levels of ciprofloxacin resistance.
喹诺酮类抗生素已被提议作为耐甲氧西林金黄色葡萄球菌感染时替代万古霉素的可能选择。我们通过时间杀菌动力学研究考察了阿米氟沙星、环丙沙星、诺氟沙星和万古霉素的活性。使用0、1.0和4.0倍MIC的抗生素浓度作用于4株耐庆大霉素和耐甲氧西林的金黄色葡萄球菌。在重复的时间杀菌动力学研究中,在所有时间点将葡萄球菌接种到含环丙沙星的琼脂平板上。测定了微量肉汤稀释法的MIC和MBC。通过生物测定法测量环丙沙星水平。从原始敏感接种物(MIC,0.125微克/毫升)进行影印接种到补充环丙沙星的琼脂平板上。在4.0倍MIC时,仅环丙沙星在24小时和48小时出现再生长。所有4株葡萄球菌在每毫升补充1微克环丙沙星的琼脂上生长;4株中有3株在每毫升补充2微克环丙沙星的琼脂上生长。这些耐药克隆的MIC和MBC范围为8至32微克/毫升。在生物测定中未检测到环丙沙星的活性或量有降解。影印接种的葡萄球菌在48小时时能在含1微克/毫升但不含更高浓度环丙沙星的琼脂上生长。阿米氟沙星和诺氟沙星维持了与万古霉素相当的杀菌活性。我们得出结论,在抗生素选择压力下,耐庆大霉素和耐甲氧西林的金黄色葡萄球菌可能会出现异质性耐药亚群。然后,这种耐药克隆可能在亚抑菌浓度的抗生素存在下发生突变,对环丙沙星产生更高水平的耐药性。