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In vitro activity of sparfloxacin compared with those of five other quinolones.

机译:与其他五个喹诺酮类药物相比司帕沙星的体外活性更高。

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摘要

The in vitro activity of sparfloxacin, a new difluorinated quinolone, was evaluated against 857 gram-positive and gram-negative clinical isolates and compared with those of ciprofloxacin, norfloxacin, ofloxacin, fleroxacin, and lomefloxacin. The MIC of sparfloxacin for 90% of the members of the family Enterobacteriaceae tested was 0.5 microgram/ml (range, 0.06 to 4.0 micrograms/ml); only for members of the genera Serratia, Citrobacter, and Providencia were MICs above 1 microgram/ml. Some 90% of Pseudomonas aeruginosa isolates were inhibited by 8 micrograms of the drug per ml. The MICs for 90% of Staphylococcus spp. and Enterococcus faecalis were 0.12 and 2 micrograms/ml, respectively. All (100%) Streptococcus pneumoniae strains were inhibited by 0.5 microgram/ml. The inoculum size had little effect on either the MIC or the MBC of sparfloxacin. An increase in the magnesium concentration from 1.1 to 8.4 mM increased the MIC between 2 and 10 times, depending on the genus tested. Sparfloxacin was less active at pH 5. The antibacterial activity of sparfloxacin against gram-positive bacteria was generally higher than those of the quinolones with which it was compared; against Streptococcus pneumoniae, sparfloxacin was four- and eightfold more active than ofloxacin and ciprofloxacin, respectively. The activity of sparfloxacin against gram-negative rods was generally comparable to that of ciprofloxacin except against Enterobacter and Acinetobacter spp., Pseudomonas cepacia, Xanthomonas maltophilia, and Alcaligenes and Flavobacterium spp., against which sparfloxacin was the most active quinolone.
机译:司帕沙星是一种新型的二氟喹诺酮,其体外活性针对857克阳性和革兰氏阴性临床分离株进行了评估,并与环丙沙星,诺氟沙星,氧氟沙星,氟罗沙星和洛美沙星进行了比较。被测肠杆菌科成员中90%的司帕沙星的MIC为0.5微克/毫升(范围为0.06至4.0微克/毫升);仅对于沙雷氏菌属,柠檬酸杆菌属和普罗维登西亚属的成员而言,MIC均高于1微克/毫升。每毫升8微克药物可抑制约90%的铜绿假单胞菌分离物。 90%葡萄球菌属菌种的MIC。粪肠球菌和粪肠球菌分别为0.12和2微克/毫升。所有(100%)肺炎链球菌菌株均被0.5微克/毫升抑制。接种量对司帕沙星的MIC或MBC影响很小。镁浓度从1.1 mM增加到8.4 mM,使MIC增加2到10倍,具体取决于测试的属。司帕沙星在pH 5时活性较低。司帕沙星对革兰氏阳性细菌的抗菌活性通常高于与之相比的喹诺酮类。对于肺炎链球菌,司帕沙星的活性分别是氧氟沙星和环丙沙星的四倍和八倍。除对肠杆菌和不动杆菌属,假单胞菌脓毒杆菌,产黄单胞菌的嗜麦芽孢杆菌和产碱杆菌和黄杆菌属的菌而言,司帕沙星对革兰氏阴性菌的活性通常与环丙沙星相当,而对后者而言,对司帕沙星的活性最高。

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