Ene M D, Roberts C J
Department of Medicine, University of Bristol, England.
J Clin Pharmacol. 1987 Dec;27(12):1001-4. doi: 10.1002/j.1552-4604.1987.tb05604.x.
Presented are the results of a study in which ten healthy subjects and seven patients with hepatic cirrhosis were given 10 mg nifedipine orally; plasma concentrations of the drug were measured over 24 hours. The drug was also administered intravenously, but those results were unsatisfactory for presentation. The rate of absorption and peak plasma concentrations were similar in the two groups. There was a fourfold increase in the elimination half-life (434 +/- 74 minutes in the cirrhotics compared with 102 +/- 11 minutes in the healthy subjects). A twofold increase in the area under the plasma concentration-time curve occurred in the cirrhotic group. The study confirmed that there is clinically significant alteration in the kinetics of nifedipine in patients who have hepatic cirrhosis and that there is considerable risk of accumulation. No adverse effects were observed despite high plasma levels of nifedipine.
本文呈现了一项研究结果,该研究让10名健康受试者和7名肝硬化患者口服10毫克硝苯地平;在24小时内测量了该药物的血浆浓度。该药物也通过静脉给药,但那些结果不适合展示。两组的吸收速率和血浆峰值浓度相似。消除半衰期增加了四倍(肝硬化患者为434±74分钟,而健康受试者为102±11分钟)。肝硬化组的血浆浓度-时间曲线下面积增加了两倍。该研究证实,肝硬化患者硝苯地平的动力学存在临床上显著的改变,且有相当大的蓄积风险。尽管硝苯地平血浆水平很高,但未观察到不良反应。