Lagast H, Husson M, Klastersky J
J Antimicrob Chemother. 1985 Sep;16(3):341-7. doi: 10.1093/jac/16.3.341.
Ten volunteers received three doses of 500 mg ciprofloxacin, orally every 12 hours. After the last dose, mean serum levels were (mg/l +/- SD) 2.4 +/- 0.83 at 1 h; 0.91 +/- 0.30 at 4 h and 0.18 +/- 0.04 at 12 h. At 1 h the median serum bactericidal activity was satisfactory only against the Escherichia coli (1:256) and Klebsiella pneumoniae (1:128). In urine collected from 0 to 4 h and 8 to 12 h after the last dose, the mean ciprofloxacin level was respectively 482.5 +/- 324.7 and 80.9 +/- 48.2 mg/l +/- SD. Bactericidal activity in urine was high even against the least susceptible species tested: Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus faecalis. A post antibiotic effect was demonstrated in 22 out of the 29 strains tested, ranging mainly from 1 to 3 h. Ciprofloxacin 500 mg orally twice a day is a bactericidal regimen against a wide range of urinary pathogens but has a limited systemic activity.
十名志愿者每12小时口服三次500毫克环丙沙星。最后一剂后,1小时时的平均血清水平为(毫克/升±标准差)2.4±0.83;4小时时为0.91±0.30,12小时时为0.18±0.04。1小时时,血清杀菌活性中位数仅对大肠杆菌(1:256)和肺炎克雷伯菌(1:128)令人满意。在最后一剂后的0至4小时和8至12小时收集的尿液中,环丙沙星的平均水平分别为482.5±324.7和80.9±48.2毫克/升±标准差。尿液中的杀菌活性即使对测试的最不易感菌种:铜绿假单胞菌、金黄色葡萄球菌和粪肠球菌也很高。在所测试的29株菌株中,有22株表现出抗生素后效应,主要持续时间为1至3小时。每天口服两次500毫克环丙沙星是针对多种尿路病原体的杀菌方案,但全身活性有限。