Darmansjah I, Wong E, Setiawati A, Moeloek D, Irawati D, Siagian M, Muchtar A
Clinical Pharmacology Unit, University of Indonesia, Jakarta.
J Clin Pharmacol. 1990 Feb;30(S2):S39-45. doi: 10.1002/j.1552-4604.1990.tb03494.x.
The steady state pharmacokinetics and pharmacodynamics of metoprolol controlled release tablets 100 mg CR/ZOK, was compared with those of metoprolol conventional tablets 100 mg (CT) and atenolol 50 mg (ATL) in ten healthy Oriental men. The study was of double-blind, cross-over placebo controlled design. The three study drugs and placebo were given in a random order once daily for 4 consecutive days with 1-week wash-out between each period. Treadmill exercise tests were performed and blood samples were obtained at fixed intervals after the fourth dose of each treatment. There was less fluctuation in the plasma level-time profile after CR/ZOK than CT and ATL. Plasma concentrations were significantly higher on CR/ZOK than CT at 24 hours after dosing. The relative bioavailability of CR/ZOK to CT was 69.0%. CR/ZOK achieved relatively more uniform beta-blocking effect over the dose interval. Compared to CT and ATL, the peak effect after CR/ZOK was less pronounced and the beta-blockade after 24 hours more effective.
在10名健康的东方男性中，对100 mg CR/ZOK美托洛尔控释片的稳态药代动力学和药效学与100 mg美托洛尔常规片（CT）和50 mg阿替洛尔（ATL）进行了比较。该研究采用双盲、交叉、安慰剂对照设计。三种研究药物和安慰剂按随机顺序每日给药一次，连续给药4天，每个给药期之间有1周的洗脱期。在每种治疗的第四剂给药后，进行跑步机运动试验并在固定时间间隔采集血样。与CT和ATL相比，CR/ZOK给药后血浆浓度-时间曲线的波动较小。给药后24小时，CR/ZOK的血浆浓度显著高于CT。CR/ZOK相对于CT的相对生物利用度为69.0%。CR/ZOK在给药间隔内达到相对更均匀的β受体阻滞作用。与CT和ATL相比，CR/ZOK给药后的峰值效应不那么明显，24小时后的β受体阻滞作用更有效。
