Edelstein P H, Edelstein M A, Weidenfeld J, Dorr M B
Department of Pathology, University of Pennsylvania School of Medicine, Philadelphia 19104-4283.
Antimicrob Agents Chemother. 1990 Nov;34(11):2122-7. doi: 10.1128/AAC.34.11.2122.
The activities of sparfloxacin, ciprofloxacin, and erythromycin for 21 clinical Legionella isolates were determined by agar and broth dilution susceptibility testing and by growth inhibition assays in guinea pig alveolar macrophages (sparfloxacin and ciprofloxacin). All three antimicrobial agents had roughly equivalent activities when buffered charcoal yeast extract agar medium supplemented with 0.1% alpha-ketoglutarate was used as the test medium; the MICs for 90% of strains were 1.0 micrograms/ml for erythromycin and sparfloxacin and 0.5 microgram/ml for ciprofloxacin. Buffered charcoal yeast extract medium supplemented with 0.1% alpha-ketoglutarate inhibited the activities of all the antimicrobial agents tested, as judged by the susceptibility of a control Staphylococcus aureus strain. Broth macrodilution MICs for two L. pneumophila strains in buffered yeast extract supplemented with 0.1% alpha-ketoglutarate were less than or equal to 0.03 microgram/ml for sparfloxacin, 0.06 microgram/ml for ciprofloxacin, and 0.25 microgram/ml for erythromycin; only erythromycin was inhibited by this medium. Ciprofloxacin and sparfloxacin (both 0.25 microgram/ml) reduced bacterial counts of two L. pneumophila strains grown in guinea pig alveolar macrophages by 2 log10 CFU/ml, but regrowth occurred over a 3-day period. Sparfloxacin, but not ciprofloxacin (both 1 microgram/ml), caused a 3- to 4-day postantibiotic effect. Pharmacokinetic and therapy studies of sparfloxacin were performed in guinea pigs with L. pneumophila pneumonia. For the pharmacokinetic study, sparfloxacin was given (10 mg/kg of body weight) to infected guinea pigs by the intraperitoneal route; peak levels in serum and lung were 2.6 micrograms/ml and 1.6 micrograms/g, respectively, at 1 h, with a terminal-phase half-life of elimination from serum of 5 h.(ABSTRACT TRUNCATED AT 250 WORDS)
通过琼脂和肉汤稀释药敏试验以及豚鼠肺泡巨噬细胞中的生长抑制试验（针对司帕沙星和环丙沙星），测定了司帕沙星、环丙沙星和红霉素对21株临床嗜肺军团菌分离株的活性。当使用添加0.1%α-酮戊二酸的缓冲活性炭酵母提取物琼脂培养基作为测试培养基时，这三种抗菌剂的活性大致相当；90%菌株对红霉素和司帕沙星的MIC为1.0微克/毫升，对环丙沙星的MIC为0.5微克/毫升。根据对照金黄色葡萄球菌菌株的药敏情况判断，添加0.1%α-酮戊二酸的缓冲活性炭酵母提取物培养基抑制了所有测试抗菌剂的活性。在添加0.1%α-酮戊二酸的缓冲酵母提取物中，两株嗜肺军团菌菌株的肉汤大稀释MIC，司帕沙星小于或等于0.03微克/毫升，环丙沙星为0.06微克/毫升，红霉素为0.25微克/毫升；只有红霉素被该培养基抑制。环丙沙星和司帕沙星（均为0.25微克/毫升）使豚鼠肺泡巨噬细胞中生长的两株嗜肺军团菌菌株的细菌计数降低2 log10 CFU/毫升，但在3天内出现再生长。司帕沙星（1微克/毫升）而非环丙沙星产生了3至4天的抗生素后效应。在患有嗜肺军团菌肺炎的豚鼠中进行了司帕沙星的药代动力学和治疗研究。在药代动力学研究中，通过腹腔途径给感染的豚鼠注射司帕沙星（10毫克/千克体重）；1小时时血清和肺中的峰值水平分别为2.6微克/毫升和1.6微克/克，血清消除的终末相半衰期为5小时。（摘要截短至250字）
