Spyker D A, Gober L L, Scheld W M, Sande M A, Bolton W K
Antimicrob Agents Chemother. 1982 Feb;21(2):278-81. doi: 10.1128/AAC.21.2.278.
The pharmacokinetics of cefaclor were characterized in 15 functionally anephric patients on hemodialysis. Each patient received a 500-mg oral dose of cefaclor every 8 h for 10 days. Multiple serum drug levels were measured by bioassay on day 0 (no hemodialysis), day 10 during hemodialysis, and as single determinations 1 h after administration on days 1, 3, and 5. Analysis of cefaclor kinetics in these 15 patients along with kinetics from 24 previously studied patients showed that weight was the best single predictor of volume of distribution. The corrected creatinine clearance (calculated from serum creatinine, age, and sex) proved to be the best predictor of drug half-life (r = 0.969). Thus, a single serum creatinine test provided a better estimated of cefaclor half-life than a 24-h urine collection. Cefaclor was cleared with an average serum half-life of 2.9 h without hemodialysis and 1.5 h during hemodialysis. Cefaclor serum levels measured 1 h after administration on days 0, 1, 3, and 5 showed no evidence of accumulation. Thus, cefaclor may be administered orally in multiple doses without accumulation in functionally anephric patients. In patients on dialysis, dosage interval or quantity should be increased to compensate for doubled drug clearance dialysis.
对15名进行血液透析的功能性无肾患者的头孢克洛药代动力学进行了研究。每位患者每8小时口服500毫克头孢克洛,持续10天。在第0天(未进行血液透析)、第10天血液透析期间通过生物测定法测定多次血清药物水平,并在第1、3和5天给药后1小时进行单次测定。对这15名患者的头孢克洛动力学分析以及之前研究的24名患者的动力学分析表明,体重是分布容积的最佳单一预测指标。校正的肌酐清除率(根据血清肌酐、年龄和性别计算)被证明是药物半衰期的最佳预测指标(r = 0.969)。因此,单次血清肌酐检测比24小时尿液收集能更好地估计头孢克洛的半衰期。未进行血液透析时,头孢克洛的平均血清半衰期为2.9小时,血液透析期间为1.5小时。在第0、1、3和5天给药后1小时测得的头孢克洛血清水平没有累积迹象。因此,头孢克洛可以在功能性无肾患者中口服多剂量而不累积。对于透析患者,应增加给药间隔或剂量以补偿透析导致的药物清除率加倍。