Department of Anaesthesiology and Intensive Care Medicine, Køge University Hospital, Lykkebækvej, DK-4600, Køge, Denmark,
Eur J Clin Pharmacol. 2013 Nov;69(11):1951-4. doi: 10.1007/s00228-013-1566-9. Epub 2013 Jul 31.
In healthy individuals upwards of 90 % of an injected dose of terbutaline is excreted in the urine. The purpose of this study is to determine the pharmacokinetic properties of terbutaline in patients with severe renal impairment as defined by a glomerular filtration rate (GFR) below 30 mL/min.
Ten patients were included in the study. GFR was measured with Cr-EDTA clearance. They were given an intravenous injection of 0.500 mg of terbutaline. Blood samples were collected at intervals for 60 h and urine samples were collected for 96 h. The concentration of terbutaline in the blood and in the urine was used to calculate pharmacokinetic parameters.
In patients with normal renal function the total clearance of terbutaline is 2.23-3 mL/min/kg. In our population the total clearance of terbutaline was found to be 1.72 (SD: 0.49) mL/min/kg of which approximately 15 % (0.25 mL/min/kg) was renal clearance. We calculated a distribution volume at steady state of 0.74 (SD: 0.22) L/kg with a terminal half-life of 7.93 (SD: 4.06) hours. The mean residence time (MRT) was 8.35 (SD: 4.93) hours.
In healthy individuals the excretion of terbutaline is foremost renal but this study shows that severe renal impairment does not lower the total clearance of terbutaline to a degree that might be expected from the Cr-EDTA clearance. However, more research is needed to determine if dosage adjustment is warranted in patients with CKD.
在健康个体中,超过 90%的注射剂量的特布他林以尿液形式排泄。本研究的目的是确定肾小球滤过率(GFR)低于 30ml/min 的严重肾功能不全患者特布他林的药代动力学特性。
本研究纳入 10 名患者。GFR 采用 Cr-EDTA 清除率测定。他们接受 0.500mg 特布他林静脉注射。在 60 小时内间隔采集血液样本,在 96 小时内采集尿液样本。利用特布他林在血液和尿液中的浓度计算药代动力学参数。
在肾功能正常的患者中,特布他林的总清除率为 2.23-3ml/min/kg。在我们的人群中,特布他林的总清除率为 1.72(SD:0.49)ml/min/kg,其中约 15%(0.25ml/min/kg)为肾清除率。我们计算出稳态时的分布容积为 0.74(SD:0.22)L/kg,终末半衰期为 7.93(SD:4.06)小时。平均驻留时间(MRT)为 8.35(SD:4.93)小时。
在健康个体中,特布他林的排泄主要通过肾脏,但本研究表明,严重肾功能不全不会使特布他林的总清除率降低到与 Cr-EDTA 清除率预期的程度。然而,需要进一步研究以确定在 CKD 患者中是否需要调整剂量。