Akaniro J C, Vidaurre C E, Stutman H R, Marks M I
Department of Pediatrics, Memorial Miller Children's Hospital, Long Beach, California 90806.
Antimicrob Agents Chemother. 1990 Oct;34(10):1880-4. doi: 10.1128/AAC.34.10.1880.
We evaluated fleroxacin, a newer fluoroquinolone, against isolates from sputum from patients with cystic fibrosis. These isolates included rough and mucoid Pseudomonas aeruginosa, Pseudomonas cepacia, Staphylococcus aureus, Haemophilus influenzae, and Escherichia coli. Selected isolates were tested by the broth microdilution method to examine the influence of various pHs, inoculum sizes, and biological fluids (serum or sputum from patients with cystic fibrosis). Fleroxacin MICs for 50 and 90% of isolates of P. aeruginosa were 2.0 and 4 micrograms/ml, those for P. cepacia were 2 and 16 micrograms/ml, those for S. aureus were 0.5 and 1 microgram/ml, those for H. influenzae were 0.06 and 0.06 micrograms/ml, and those for E. coli were 0.01 and 0.03 micrograms/ml, respectively. Fleroxacin activity against mucoid P. aeruginosa was similar to the activities of enoxacin and ofloxacin but eightfold lower than that of ciprofloxacin. It was twofold more active than norfloxacin and enoxacin but was twofold less active than ciprofloxacin, ofloxacin, and nafcillin against S. aureus. Fleroxacin inhibitory activity against P. cepacia was two- to fourfold lower than that of ciprofloxacin but eightfold greater than those of the other quinolones tested. Alterations in pH, diluent, and inoculum size did not significantly affect fleroxacin activity. These results, combined with available pharmacokinetic and tissue distribution data, support the need for clinical evaluation of fleroxacin in pulmonary infections in patients with cystic fibrosis.
我们评估了新型氟喹诺酮类药物氟罗沙星对囊性纤维化患者痰液分离菌株的抗菌活性。这些分离菌株包括粗糙型和黏液型铜绿假单胞菌、洋葱伯克霍尔德菌、金黄色葡萄球菌、流感嗜血杆菌和大肠杆菌。通过肉汤微量稀释法对选定的分离菌株进行检测,以考察不同pH值、接种量以及生物液体(血清或囊性纤维化患者的痰液)的影响。氟罗沙星对50%和90%的铜绿假单胞菌分离菌株的最低抑菌浓度(MIC)分别为2.0和4微克/毫升,对洋葱伯克霍尔德菌的MIC分别为2和16微克/毫升,对金黄色葡萄球菌的MIC分别为0.5和1微克/毫升,对流感嗜血杆菌的MIC分别为0.06和0.06微克/毫升,对大肠杆菌的MIC分别为0.01和0.03微克/毫升。氟罗沙星对黏液型铜绿假单胞菌的活性与依诺沙星和氧氟沙星相似,但比环丙沙星低8倍。它对金黄色葡萄球菌的活性比诺氟沙星和依诺沙星高2倍,但比环丙沙星、氧氟沙星和萘夫西林低2倍。氟罗沙星对洋葱伯克霍尔德菌的抑菌活性比环丙沙星低2至4倍,但比其他受试喹诺酮类药物高8倍。pH值、稀释剂和接种量的改变对氟罗沙星的活性没有显著影响。这些结果,结合现有的药代动力学和组织分布数据,支持对氟罗沙星在囊性纤维化患者肺部感染中的临床评估的必要性。