Berndt A, Looby M, Pönicke K, Zipprich B, Weiss M
Department of Internal Medicine, Faculty of Medicine, Martin Luther University Halle-Wittenberg, Germany.
J Clin Pharmacol. 1996 Oct;36(10):897-902. doi: 10.1002/j.1552-4604.1996.tb04756.x.
The pharmacokinetics of trapidil were studied in 15 patients with chronic liver disease (12 with hepatic cirrhosis, 2 with alcoholic fatty liver, 1 with liver fibrosis). Trapidil was administered intravenously as a 100-mg bolus. Serum samples were analyzed for trapidil by means of high-performance liquid chromatography. Mean pharmacokinetic parameters were compared with those found in a previous study of 12 healthy volunteers. Total plasma clearance was decreased significantly in patients with hepatic cirrhosis (96 mL/ min versus 258 mL/min in healthy individuals and 252 mL/min in patients with noncirrhotic liver disease). No difference in clearance was observed between patients with compensated or decompensated cirrhosis, and portal hypertension did not affect this clearance of trapidil. It can be concluded that trapidil clearance is a parameter that is very sensitive to alterations in hepatic clearance caused by liver cirrhosis, and that the dosage of trapidil should be adjusted accordingly in such patients.
对15例慢性肝病患者（12例肝硬化、2例酒精性脂肪肝、1例肝纤维化）进行了曲匹地尔的药代动力学研究。曲匹地尔以100mg静脉推注给药。采用高效液相色谱法分析血清样本中的曲匹地尔。将平均药代动力学参数与先前对12名健康志愿者的研究结果进行比较。肝硬化患者的总血浆清除率显著降低（健康个体为258 mL/分钟，非肝硬化肝病患者为252 mL/分钟，肝硬化患者为96 mL/分钟）。代偿期或失代偿期肝硬化患者的清除率无差异，门静脉高压不影响曲匹地尔的这种清除率。可以得出结论，曲匹地尔清除率是一个对肝硬化引起的肝脏清除率改变非常敏感的参数，在这类患者中应相应调整曲匹地尔的剂量。
