Cooper M A, Andrews J M, Ashby J P, Matthews R S, Wise R
Department of Microbiology, Dudley Road Hospital, Birmingham, UK.
J Antimicrob Chemother. 1990 Nov;26(5):667-76. doi: 10.1093/jac/26.5.667.
The in-vitro activity of sparfloxacin (AT-4140), a new difluorinated quinolone, was compared with those of ciprofloxacin, temafloxacin and selected members of other groups of antimicrobial agents, against 651 recent distinct clinical isolates and strains with known mechanisms of resistance. Three strains of Chlamydia trachomatis were also studied. The MICs for 90% of the Enterobacteriaceae were between 0.06 and 1 mg/l; for Pseudomonas aeruginosa the MIC90 was 2 mg/l. Sparfloxacin was 16-fold more active against Acinetobacter spp. than ciprofloxacin. For Staphylococcus spp., Streptococcus, spp. and Enterococcus faecalis the MIC90 was between 0.25 and 1 mg/l; sparfloxacin was four-fold more active against Str. pneumoniae than ciprofloxacin. Ninety percent of strains of Haemophilus influenzae, Branhamella catarrhalis and Neisseria spp. were inhibited by less than 0.03 mg/l; for Bacteroides fragilis the MIC90 was 1 mg/l. The three strains of Chl. trachomatis were susceptible to 0.06-0.12 mg/l sparfloxacin, which was 16-fold more active than ciprofloxacin. There was cross resistance among the quinolones, but not between the quinolones and other groups of antimicrobials. The protein binding of sparfloxacin was 40% and serum had little effect on its activity.
将新型二氟喹诺酮类药物司帕沙星(AT - 4140)的体外活性与环丙沙星、替马沙星及其他抗菌药物组的选定成员进行比较,以研究651株近期分离出的不同临床菌株及具有已知耐药机制的菌株。还对三株沙眼衣原体菌株进行了研究。90%的肠杆菌科细菌的最低抑菌浓度(MIC)在0.06至1毫克/升之间;铜绿假单胞菌的MIC90为2毫克/升。司帕沙星对不动杆菌属的活性比环丙沙星高16倍。对于葡萄球菌属、链球菌属和粪肠球菌,MIC90在0.25至1毫克/升之间;司帕沙星对肺炎链球菌的活性比环丙沙星高4倍。90%的流感嗜血杆菌、卡他布兰汉菌和奈瑟菌属菌株被低于0.03毫克/升的浓度所抑制;脆弱拟杆菌的MIC90为1毫克/升。三株沙眼衣原体菌株对0.06 - 0.12毫克/升的司帕沙星敏感,其活性比环丙沙星高16倍。喹诺酮类药物之间存在交叉耐药性,但喹诺酮类药物与其他抗菌药物组之间不存在交叉耐药性。司帕沙星的蛋白结合率为40%,血清对其活性影响很小。