Boelaert J, Daneels R, Schurgers M, Mellows G, Swaisland A J, Lambert A M, Van Landuyt H W
Drugs. 1985;29 Suppl 5:109-13. doi: 10.2165/00003495-198500295-00023.
Temocillin pharmacokinetics in renal impairment were investigated following an intravenous bolus injection of 15 mg/kg. The 28 patients were divided into 5 groups of varying renal function, from normal to uraemic [including a group being treated with haemodialysis and a group on continuous ambulatory peritoneal dialysis (CAPD)]. The distribution of temocillin into the tissues was not affected by renal dysfunction. Uraemia as compared to normal renal function resulted in a 4.3-fold decrease in temocillin clearance and a 3.1-fold decrease in urinary recovery over 24 hours, as well as a 5- and 3.7-fold increase in the beta half-life and the area under the curve (AUC), respectively. Haemodialysis doubled the serum clearance and halved the beta half-life of temocillin in the uraemic subject, but CAPD over 24 hours eliminated only 8% of the temocillin dose, resulting in a minimal change in pharmacokinetics. Temocillin dosage adjustments in renal failure are proposed.
在静脉推注15mg/kg的替莫西林后,研究了其在肾功能损害患者中的药代动力学。28名患者被分为5组,肾功能从正常到尿毒症不等[包括一组接受血液透析治疗的患者和一组持续非卧床腹膜透析(CAPD)患者]。替莫西林在组织中的分布不受肾功能障碍的影响。与正常肾功能相比,尿毒症导致替莫西林清除率降低4.3倍,24小时尿回收率降低3.1倍,β半衰期和曲线下面积(AUC)分别增加5倍和3.7倍。血液透析使尿毒症患者的血清清除率加倍,替莫西林的β半衰期减半,但CAPD在24小时内仅清除了8%的替莫西林剂量,导致药代动力学变化极小。文中提出了肾衰竭时替莫西林的剂量调整建议。