Fung-Tomc J, Gradelski E, Huczko E, Minassian B, Bonner D P
Department of Microbiology, Bristol-Myers Squibb Company, 5 Research Parkway, 06492, Wallingford, CT, USA.
Int J Antimicrob Agents. 2001 Jul;18(1):77-80. doi: 10.1016/s0924-8579(01)00356-9.
Gatifloxacin is an 8-methoxy fluoroquinolone. On quinolones, this side chain imparts increased activity against Gram-positive bacteria and enhanced killing. Gatifloxacin was tested against ofloxacin non-susceptible (ofloxacin MIC>2 mg/l) strains of Streptococcus pneumoniae (gatifloxacin MIC(90), 1 mg/l) and methicillin-resistant Staphylococcus aureus (MRSA, gatifloxacin MIC(90), 4 mg/l), and to ciprofloxacin non-susceptible (ciprofloxacin MIC>1 mg/l) strains of Escherichia coli (gatifloxacin MIC(90),>16 mg/l) and ciprofloxacin non-susceptible (ciprofloxacin MIC>0.06 mg/l) Neisseria gonorrhoeae (gatifloxacin MIC(50), 0.12 mg/l and MIC(90), 0.5 mg/l). Though gatifloxacin showed some reduced susceptibility to these populations, the MIC(50) and MIC(90) values suggest that gatifloxacin may be useful against pneumococci and some gonococcal strains not susceptible to other fluoroquinolones. Gatifloxacin did not select for less susceptible variants of MRSA and pneumococci, in contrast to the 10- to 100-fold higher selection frequencies with ciprofloxacin and ofloxacin. The single-step E. coli mutants selected by gatifloxacin and the comparator quinolones had quinolone MICs within the susceptible range. These data suggest that gatifloxacin use may hinder the development of quinolone-resistance, particularly in Gram-positive bacteria.
加替沙星是一种8-甲氧基氟喹诺酮类药物。在喹诺酮类药物中,这个侧链可增强对革兰氏阳性菌的活性并提高杀菌能力。对肺炎链球菌(加替沙星MIC(90)为1mg/l)和耐甲氧西林金黄色葡萄球菌(MRSA,加替沙星MIC(90)为4mg/l)的左氧氟沙星不敏感菌株(左氧氟沙星MIC>2mg/l),以及对大肠杆菌(加替沙星MIC(90)>16mg/l)和环丙沙星不敏感的淋病奈瑟菌(环丙沙星MIC>0.06mg/l,加替沙星MIC(50)为0.12mg/l,MIC(90)为0.5mg/l)的环丙沙星不敏感菌株进行了加替沙星测试。尽管加替沙星对这些菌群体的敏感性有所降低,但MIC(50)和MIC(90)值表明,加替沙星可能对其他氟喹诺酮类药物不敏感的肺炎球菌和一些淋球菌菌株有效。与环丙沙星和左氧氟沙星高10至100倍的选择频率相比,加替沙星未筛选出MRSA和肺炎球菌的低敏感性变异株。加替沙星和对照喹诺酮类药物筛选出的单步大肠杆菌突变体的喹诺酮MIC在敏感范围内。这些数据表明,使用加替沙星可能会阻碍喹诺酮耐药性的发展,尤其是在革兰氏阳性菌中。