Fass R J
Department of Internal Medicine, Ohio State University College of Medicine, Columbus 43210.
Antimicrob Agents Chemother. 1993 Nov;37(11):2348-57. doi: 10.1128/AAC.37.11.2348.
MICs of Bay y 3118, ciprofloxacin, ofloxacin, clarithromycin, azithromycin, cefuroxime, amoxicillin-clavulanate, and trimethoprim-sulfamethoxazole for 878 recent clinical isolates were determined by broth microdilution methods. Among the three quinolones, Bay y 3118 was the most active against Haemophilus influenzae, Moraxella catarrhalis, Acinetobacter baumannii, Xanthomonas maltophilia, gram-positive cocci, and anaerobes; MICs for 50% of the strains (MIC50s) and MIC90s were < or = 0.015 and < or = 0.015, < or = 0.015 and < or = 0.015, 0.03 and 2, 0.25 and 0.5, 0.06 and 1, and 0.12 and 0.25 micrograms/ml, respectively. For gram-positive cocci and anaerobes, these values were 16- to 32-fold (4 to 5 log2 dilution steps) lower than those for ciprofloxacin and ofloxacin. Bay y 3118 was similar in activity to ciprofloxacin and more active than ofloxacin against members of the family Enterobacteriaceae and Pseudomonas aeruginosa; Bay y 3118 MIC50s and MIC90s were 0.03 and 0.25 and 0.5 and 8 micrograms/ml, respectively. Scattergrams and regression analyses comparing quinolone MICs indicated that, despite differences in activity, organisms relatively susceptible to one were relatively susceptible to all and organisms relatively resistant to one were relatively resistant to all. However, the greater in vitro activity of Bay y 3118 was most pronounced against relatively resistant organisms. Pending pharmacokinetic and safety data for Bay y 3118, there is reasonable anticipation that its enhanced activity against gram-positive cocci and anaerobes would broaden the clinical utility of the quinolone class of antimicrobial agents.
采用肉汤微量稀释法测定了Bay y 3118、环丙沙星、氧氟沙星、克拉霉素、阿奇霉素、头孢呋辛、阿莫西林-克拉维酸和甲氧苄啶-磺胺甲恶唑对878株近期临床分离株的最低抑菌浓度（MIC）。在这三种喹诺酮类药物中，Bay y 3118对流感嗜血杆菌、卡他莫拉菌、鲍曼不动杆菌、嗜麦芽窄食单胞菌、革兰氏阳性球菌和厌氧菌的活性最强；50%菌株的MIC（MIC50）和90%菌株的MIC（MIC90）分别为≤0.015和≤0.015、≤0.015和≤0.015、0.03和2、0.25和0.5、0.06和1以及0.12和0.25微克/毫升。对于革兰氏阳性球菌和厌氧菌，这些数值比环丙沙星和氧氟沙星低16至32倍（4至5个log2稀释步骤）。Bay y 3118对肠杆菌科和铜绿假单胞菌的活性与环丙沙星相似，且比对氧氟沙星更具活性；Bay y 3118的MIC50和MIC90分别为0.03和0.25以及0.5和8微克/毫升。比较喹诺酮类药物MIC的散点图和回归分析表明，尽管活性存在差异，但对一种药物相对敏感的菌株对所有药物都相对敏感，而对一种药物相对耐药的菌株对所有药物也相对耐药。然而，Bay y 3118在体外对相对耐药菌株的活性增强最为明显。在获得Bay y 3118的药代动力学和安全性数据之前，可以合理预期其对革兰氏阳性球菌和厌氧菌增强的活性将拓宽喹诺酮类抗菌药物的临床应用范围。
