Drusano G L, Weir M, Forrest A, Plaisance K, Emm T, Standiford H C
Antimicrob Agents Chemother. 1987 Jun;31(6):860-4. doi: 10.1128/AAC.31.6.860.
We examined the pharmacokinetic behavior of 200 mg of ciprofloxacin administered intravenously to 32 volunteers whose renal function as measured by creatinine clearance ranged from 0 to 8.99 liters/h per 1.73 m2. Serum clearances (mean +/- standard deviation) were 26.8 +/- 5.7 and 15.4 +/- 4.3 liters/h per 1.73 m2 in normal and anephric volunteers, respectively. The half-life (mean +/- standard deviation) increased from 4.3 +/- 0.8 h in normal volunteers to 8.6 +/- 3.3 h in anephric volunteers. There was good correlation between normalized creatinine clearance and both normalized serum and renal clearance. The regression equation for serum clearance (CLS) versus creatinine clearance (CLCR) was CLS = 1.97 X CLCR + 13.23, where r = 0.697; for renal clearance versus creatinine clearance, the equation was CLR = 2.26 X CLCR, where r = 0.845. On the basis of these data, we recommend a maximum 50% reduction in dose when ciprofloxacin is instituted at a renal function of 1.2 to 1.8 liters/h per 1.73 m2 (20 to 30 ml/min per 1.73 m2). Because of the observed variation in ciprofloxacin half-life in our anephric volunteers, we also recommend that a schedule of administration every 12 h be maintained, even for patients without urine output.
我们研究了静脉注射200毫克环丙沙星在32名志愿者体内的药代动力学行为，这些志愿者的肌酐清除率所测肾功能范围为每1.73平方米0至8.99升/小时。正常志愿者和无肾志愿者的血清清除率（平均值±标准差）分别为每1.73平方米26.8±5.7升/小时和15.4±4.3升/小时。半衰期（平均值±标准差）从正常志愿者的4.3±0.8小时增加到无肾志愿者的8.6±3.3小时。标准化肌酐清除率与标准化血清清除率和肾清除率之间均具有良好的相关性。血清清除率（CLS）与肌酐清除率（CLCR）的回归方程为CLS = 1.97×CLCR + 13.23，其中r = 0.697；肾清除率与肌酐清除率的方程为CLR = 2.26×CLCR，其中r = 0.845。基于这些数据，我们建议当环丙沙星用于肾功能为每1.73平方米1.2至1.8升/小时（每1.73平方米20至30毫升/分钟）的患者时，最大剂量减少50%。由于在我们的无肾志愿者中观察到环丙沙星半衰期存在差异，我们还建议即使对于无尿患者也维持每12小时一次的给药方案。
