目的 对22例肾功能正常与受损患者单剂量静滴环丙沙星（ciprofloxacin, CPFX）的药动学进行研究。方法 按肾功能测定结果将患者分成4组：第1组（肾功能正常组），肌酐清除率（CLCR）＞80 mL·min-1，n=6；第2组（肾功能轻度受损组），CLCR 51～80 mL·min-1，n＝5；第3组（肾功能中度受损组)，CLCR 20～50 mL·min-1,n＝6；第4组（肾功能重度受损组), CLCR＜20 mL·min-1，n＝5。第1，2，3组CPFX的滴注剂量为400 mg，第4组为300 mg，滴注时间均为1 h。用微生物法测定CPFX的浓度。结果 与肾功能正常组相比，其他各组的表观分布容积(Vc)各组之间均无显著改变，第2组的各药动学参数亦无显著改变;但第3，4组（肾功能中、重度受损组）的AUC，t1/2α，t1/2β及CLS与第1组相比均显著改变，其中AUC分别升高到第1组的2.8和5.5倍, t1/2α分别延长到第1组的2.8和2.9倍，t1/2β分别延长到第1组的1.8和2.7倍,CLS分别比第1组降低了60％和81％。结论 当CLCR＜50 mL·min-1时,应调整给药方案。对于严重肾衰的患者(CLCR＜20 mL·min-1)静脉滴注CPFX时，建议采用每日一次，剂量为200 mg的给药方案。
Abstract
OBJECTIVE The pharmacokinetics of ciprofloxacin (CPFX) was studied in 22 patients with normal and impaired renal function after a single intravenous administration.METHODS The patients were randomly devided into four groups, basing on their creatinine clearance (CLCR) : group 1 (normal renal function), CLCR＞80 mL·min-1, n=6;group 2 (mild renal impairment), CLCR51～80 mL·min-1,n=5; group 3 (moderate renal impairment), CLCR20～50 mL·min-1,n=6;group 4 (severe renal impairment), CLCR＜20 mL·min-1,n=5.All patients in group 1, 2 and 3 received a single dose of 400 mg, and group 4 at 300 mg,respectively.CPFX were infused intravenously for 1 h.The serum concentrations of CPFX were determined by bioassay.RESULTS The apparent volumes of distribution were not significantly different from each other in the four groups (P＞0.05 ).AUC was 2.8 and 5.5 fold,t1/2αwas 2.8 and 2.9 fold, and t1/2β was 1.8 and 2.7 fold higher in groups 3 and 4 than those in group 1, significantly and respectively.CLS was 60% and 81% lower in group 3 and 4 than those in group 1.CONCLUSION A dose of 200 mg CPFX daily was suggested for patients with severely impaired renal function (CR＜20 mL·min-1).
关键词
环丙沙星 /
肾功能受损 /
药动学 /
微生物法
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Key words
ciprofloxacin /
impaired renal function /
pharmacokinetics /
bioassay
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参考文献
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脚注
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基金
河北省科技攻关项目（00276182D）
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