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首页> 外文期刊>International journal of antimicrobial agents >Urinary concentrations and bactericidal activities of newer fluoroquinolones in healthy volunteers
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Urinary concentrations and bactericidal activities of newer fluoroquinolones in healthy volunteers

机译：健康志愿者中新型氟喹诺酮类药物的尿液浓度和杀菌活性

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Eleven healthy male subjects participated in a crossover study to compare the urine concentrations and bactericidal activities of newer fluoroquinolones against common uropathogens. Each volunteer received a single oral dose of gatifloxacin (400 mg), levofloxacin (250 mg), moxifloxacin (400 mg) and trovafloxacin (200 mg), and a urine sample was obtained at 2, 6, 12 and 24 h after the dose. Urine concentrations were highest with gatifloxacin and levofloxacin and lowest with trovafloxacin. Each drug concentration was studied against a levofloxacin susceptible and moderately-susceptible strain of Escherichia coli (minimal inhibitory concentration, MICs: 0.125 and 4 mg/l), K pneumoniae (MICs: 0.125 and 4 mg/l), Pseudomonas aeruginosa (MICs: 0.5 and 4 mg/l) and Enterococcus faecalis (MICs: 0.25 and 4 mg/l). The duration of urine bactericidal activity (UBA) was based upon the median bactericidal titre at each time period. Both gatifloxacin and levofloxacin exhibited prolonged (greater than or equal to6h) UBA against all of the study isolates. Moxifloxacin exhibited prolonged UBA against both isolates of E. coli, K. pneumoniae and E. faecalis but not against either strain of P. aeruginosa. Prolonged UBA was not observed for trovafloxacin against the moderately-susceptible strains with the exception of E. faecalis. Furthermore, UBA was not observed for trovafloxacin against the susceptible strain of P. aeruginosa. Although these newer fluoroquinolones exhibited similar in vitro activity against these uropathogens, only those compounds with the highest urinary concentrations (gatifloxacin and levofloxacin) produced prolonged UBA against both strains of P. aeruginosa. The findings from this study suggest that both microbiological activity and urinary concentrations are important parameters to consider when choosing a fluoroquinolone for empirical treatment of urinary tract infections (UTIs). (C) 2004 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.
机译：十一名健康的男性受试者参加了一项交叉研究，以比较新型氟喹诺酮类药物对常见尿毒症的尿液浓度和杀菌活性。每位志愿者接受加替沙星（400 mg），左氧氟沙星（250 mg），莫西沙星（400 mg）和曲伐沙星（200 mg）的单次口服剂量，并在给药后2、6、12和24小时获得尿液样本。加替沙星和左氧氟沙星的尿液浓度最高，而曲伐沙星的尿液浓度最低。研究了每种药物浓度对左氧氟沙星敏感和中等敏感的大肠杆菌菌株（最低抑菌浓度，MIC：0.125和4 mg / l），肺炎克雷伯菌（MIC：0.125和4 mg / l），铜绿假单胞菌（MICs： 0.5和4 mg / l）和粪肠球菌（MIC：0.25和4 mg / l）。尿液杀菌活性（UBA）的持续时间基于每个时间段的杀菌中位数。加替沙星和左氧氟沙星对所有研究分离株均表现出延长的UBA（大于或等于6h）。莫西沙星对大肠杆菌，肺炎克雷伯菌和粪肠球菌的两种分离株均表现出延长的UBA，但对铜绿假单胞菌的任何菌株均不显示。除粪肠球菌外，曲伐沙星对中度敏感菌株未观察到长时间的UBA。此外，未观察到针对铜绿假单胞菌易感菌株的曲伐沙星的UBA。尽管这些较新的氟喹诺酮类药物对这些尿毒症病原体表现出相似的体外活性，但只有那些尿液浓度最高的化合物（加替沙星和左氧氟沙星）对两种铜绿假单胞菌菌株产生的UBA延长。这项研究的发现表明，在选择氟喹诺酮类药物进行尿路感染（UTI）的经验治疗时，微生物活性和尿液浓度都是重要的参数。 （C）2004年Elsevier B.V.和国际化学疗法学会。版权所有。

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