Dunbar Lala M, Wunderink Richard G, Habib Michael P, Smith Leon G, Tennenberg Alan M, Khashab Mohammed M, Wiesinger Barbara A, Xiang Jim X, Zadeikis Neringa, Kahn James B
Louisiana State University Medical Center, New Orleans, Louisiana, USA.
Clin Infect Dis. 2003 Sep 15;37(6):752-60. doi: 10.1086/377539. Epub 2003 Aug 28.
Levofloxacin demonstrates concentration-dependent bactericidal activity most closely related to the pharmacodynamic parameters of the ratio of area under the concentration-time curve (AUC) to minimum inhibitory concentration (MIC) and the ratio of peak plasma concentration (C(max)) to MIC. Increasing the dose of levofloxacin to 750 mg exploits these parameters by increasing peak drug concentrations, allowing for a shorter course of treatment without diminishing therapeutic benefit. This was demonstrated in a multicenter, randomized, double-blind investigation that compared levofloxacin dosages of 750 mg per day for 5 days with 500 mg per day for 10 days for the treatment of mild to severe community-acquired pneumonia (CAP). In the clinically evaluable population, the clinical success rates were 92.4% (183 of 198 persons) for the 750-mg group and 91.1% (175 of 192 persons) for the 500-mg group (95% confidence interval, -7.0 to 4.4). Microbiologic eradication rates were 93.2% and 92.4% in the 750-mg and 500-mg groups, respectively. These data demonstrate that 750 mg of levofloxacin per day for 5 days is at least as effective as 500 mg per day for 10 days for treatment of mild-to-severe CAP.
左氧氟沙星表现出浓度依赖性杀菌活性，这与浓度-时间曲线下面积（AUC）与最低抑菌浓度（MIC）的比值以及血浆峰浓度（C(max)）与MIC的比值等药效学参数最为相关。将左氧氟沙星剂量增加至750mg可通过提高药物峰浓度来利用这些参数，从而允许采用更短疗程的治疗且不降低治疗效果。这在一项多中心、随机、双盲研究中得到了证实，该研究比较了每天750mg共5天与每天500mg共10天的左氧氟沙星剂量用于治疗轻至重度社区获得性肺炎（CAP）的效果。在可进行临床评估的人群中，750mg组的临床成功率为92.4%（198人中的183人），500mg组为91.1%（192人中的175人）（95%置信区间为-7.0至4.4）。750mg组和500mg组的微生物清除率分别为93.2%和92.4%。这些数据表明，每天750mg共5天治疗轻至重度CAP至少与每天500mg共10天一样有效。
