Van der Auwera P, Klastersky J, Lieppe S, Husson M, Lauzon D, Lopez A P
Antimicrob Agents Chemother. 1986 Feb;29(2):230-4. doi: 10.1128/AAC.29.2.230.
Serum bactericidal activities (SBAs) were studied after intravenous administration of pefloxacin (8 mg/kg) and amikacin (7.5 mg/kg) alone or in combination to 15 human volunteers. About 10 strains each of Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus were tested. The serum levels of pefloxacin were measured microbiologically by using E. coli KP 1976-712 as the test organism at 0, 30, 60, 120, and 720 min after infusion; at 0, 30, 60, and 720 min these levels were 7 +/- 1.4, 5 +/- 0.8, 4.5 +/- 0.7, and 2.1 +/- 0.6 mg/liter (mean +/- standard deviation), respectively, with a terminal half-life of 10 h. The serum levels of pefloxacin in the presence of amikacin were measured similarly; 1% sodium polyanethol sulfonate was added to the agar to inactivate amikacin. Treatment with pefloxacin alone resulted in high SBAs against E. coli, K. pneumoniae strains susceptible to cephalothin, and Staphylococcus aureus at the peak concentration; 81 to 100% of the sera had SBAs of greater than or equal to 1:8. However, treatment with pefloxacin alone resulted in low SBAs against K. pneumoniae strains resistant to cephalothin and P. aeruginosa; only 34% of the sera had SBAs of greater than or equal to 1:8. At trough concentrations the percentages of sera with SBAs greater than or equal to 1:8 were 75 to 83% (E. coli), 9 to 27% (K. pneumoniae), 0% (P. aeruginosa), and 10% (S. aureus). The combination of pefloxacin plus amikacin was most often additive; the peak activity was due to amikacin, and the trough activity was due to pefloxacin. Occasionally antagonism occurred with P. aeruginosa, K. pneumoniae, and S. aureus strains. These observations were confirmed by the killing curves in pooled serum obtained at peak and trough levels. Regrowth was observed for seven strains of P. aeruginosa treated with pefloxacin alone; amikacin seemed to prevent this phenomenon.
对15名人类志愿者静脉注射培氟沙星（8mg/kg）和阿米卡星（7.5mg/kg）单独使用或联合使用后，研究了血清杀菌活性（SBA）。对大约10株大肠杆菌、肺炎克雷伯菌、铜绿假单胞菌和金黄色葡萄球菌进行了测试。通过使用大肠杆菌KP 1976 - 712作为测试菌株，在输注后0、30、60、120和720分钟通过微生物学方法测量培氟沙星的血清水平；在0、30、60和720分钟时，这些水平分别为7±1.4、5±0.8、4.5±0.7和2.1±0.6mg/升（平均值±标准差），终末半衰期为10小时。在存在阿米卡星的情况下，类似地测量培氟沙星的血清水平；向琼脂中加入1%的聚茴香脑磺酸钠以灭活阿米卡星。单独使用培氟沙星治疗在峰值浓度时对大肠杆菌、对头孢噻吩敏感的肺炎克雷伯菌菌株和金黄色葡萄球菌产生高SBA；81%至100%的血清SBA大于或等于1:8。然而，单独使用培氟沙星治疗对耐头孢噻吩的肺炎克雷伯菌菌株和铜绿假单胞菌产生低SBA；只有34%的血清SBA大于或等于1:8。在谷浓度时，SBA大于或等于1:8的血清百分比分别为75%至83%（大肠杆菌）、9%至27%（肺炎克雷伯菌）、0%（铜绿假单胞菌）和10%（金黄色葡萄球菌）。培氟沙星加阿米卡星的联合使用最常为相加作用；峰值活性归因于阿米卡星，谷活性归因于培氟沙星。偶尔在铜绿假单胞菌、肺炎克雷伯菌和金黄色葡萄球菌菌株中出现拮抗作用。这些观察结果通过在峰值和谷值水平获得的混合血清中的杀菌曲线得到证实。单独用培氟沙星治疗的7株铜绿假单胞菌观察到再生长；阿米卡星似乎可防止这种现象。
