Hoellman D B, Lin G, Jacobs M R, Appelbaum P C
Department of Pathology, Hershey Medical Center, PA 17033, USA.
J Antimicrob Chemother. 1999 May;43(5):645-9. doi: 10.1093/jac/43.5.645.
An agar dilution MIC method was used to test the activity of gatifloxacin, a new broad-spectrum fluoroquinolone, compared with ciprofloxacin, levofloxacin, sparfloxacin, trovafloxacin, amoxycillin, cefuroxime, ceftriaxone and clarithromycin against 71 penicillin-susceptible, 81 penicillin-intermediate and 55 penicillin-resistant pneumococci. Quinolone activity was unaffected by penicillin susceptibility, with MIC50/MIC90s (mg/L) of 0.25/0.5 for gatifloxacin; 1/2 for ciprofloxacin; 1/2 for levofloxacin; 0.25/0.5 for sparfloxacin; 0.125/0.25 for trovafloxacin. beta-Lactam and clarithromycin MICs rose with those of penicillin G; MIC50/MIC90 values (mg/L) for penicillin-susceptible, -intermediate and -resistant strains were: 0.03/0.06, 0.25/1, 2/4 for penicillin G; 0.03/0.03, 0.125/1, 2/4 for amoxycillin; 0.03/0.125, 0.5/4, 8/16 for cefuroxime; 0.03/0.03, 0.25/0.5, 2/4 for ceftriaxone; 0.03/0.06, 0.03/>64, 1/>64 for clarithromycin. Time-kill testing of four penicillin-susceptible, four -intermediate and four -resistant strains showed that levofloxacin at the MIC, gatifloxacin and sparfloxacin at 2 x MIC, and trovafloxacin and ciprofloxacin at 4 x MIC, were bactericidal (99.9% killing) for all strains after 12 h and 24 h. By contrast, amoxycillin, cefuroxime and ceftriaxone showed bactericidal activity after 24 h against all strains at 4, 8 and 4 x MIC, respectively. Against ten organisms with clarithromycin MICs of 0.03-4.0 mg/L, clarithromycin was bactericidal against seven strains at 8 x MIC after 24 h. Quinolones showed more rapid killing at lower concentrations and earlier time periods than did beta-lactams and clarithromycin.
采用琼脂稀释法测定了新型广谱氟喹诺酮类药物加替沙星与环丙沙星、左氧氟沙星、司帕沙星、曲伐沙星、阿莫西林、头孢呋辛、头孢曲松和克拉霉素对71株青霉素敏感、81株青霉素中介和55株青霉素耐药肺炎球菌的活性。喹诺酮类药物的活性不受青霉素敏感性的影响,加替沙星的MIC50/MIC90(mg/L)为0.25/0.5;环丙沙星为1/2;左氧氟沙星为1/2;司帕沙星为0.25/0.5;曲伐沙星为0.125/0.25。β-内酰胺类药物和克拉霉素的MIC随青霉素G的MIC升高而升高;青霉素敏感、中介和耐药菌株的MIC50/MIC90值(mg/L)分别为:青霉素G为0.03/0.06、0.25/1、2/4;阿莫西林为0.03/0.03、0.125/1、2/4;头孢呋辛为0.03/0.125、0.5/4、8/16;头孢曲松为0.03/0.03、0.25/0.5、2/4;克拉霉素为0.03/0.06、0.03/>64、1/>64。对4株青霉素敏感、4株中介和4株耐药菌株进行的时间杀菌试验表明,左氧氟沙星在MIC浓度、加替沙星和司帕沙星在2倍MIC浓度、曲伐沙星和环丙沙星在4倍MIC浓度时,在12小时和24小时后对所有菌株均有杀菌作用(杀菌率达99.9%)。相比之下,阿莫西林、头孢呋辛和头孢曲松分别在4倍、8倍和4倍MIC浓度时,24小时后对所有菌株均显示杀菌活性。对于10株克拉霉素MIC为0.03 - 4.0 mg/L的菌株,克拉霉素在8倍MIC浓度时,24小时后对7株菌株有杀菌作用。喹诺酮类药物在较低浓度和较短时间内比β-内酰胺类药物和克拉霉素显示出更快的杀菌作用。