Zeller F P, Spinler S A
Drug Intell Clin Pharm. 1987 Jun;21(6):487-92. doi: 10.1177/106002808702100601.
Bepridil is an investigational calcium channel blocking agent with antianginal activity that has a distinct and complex pharmacologic profile. Bepridil produces significant coronary vasodilation and modest peripheral effects, in addition to negative inotropic and chronotropic effects. Bepridil favorably modifies both myocardial oxygen demand and supply, supporting its use as an antianginal drug. Electrophysiologically, bepridil exhibits classes I, III, and IV antiarrhythmic activity. Five U.S. trials evaluating the short-term antianginal efficacy of bepridil collectively reported that bepridil causes significant improvement in both subjective and objective parameters of efficacy without depressing left ventricular function. In addition, one U.S. trial reported continued antianginal effects of bepridil after long-term use. There are limited data comparing and/or combining bepridil with other antianginal drugs, but the available information is promising. Limited information also exists on the use of bepridil in acute myocardial infarction and arrhythmias. Tolerance to bepridil therapy has been excellent, with the most common adverse effects being diarrhea and dizziness. It is unclear whether bepridil will be used as a first-line agent in the treatment of chronic stable angina pectoris; however, its long half-life, which makes once daily dosing possible, is certainly a significant advantage.
苄普地尔是一种具有抗心绞痛活性的研究性钙通道阻滞剂,其药理特性独特且复杂。苄普地尔除了具有负性肌力和负性变时作用外,还能产生显著的冠状动脉血管舒张作用和适度的外周效应。苄普地尔能有效改善心肌的氧需求和供应,支持其作为抗心绞痛药物的应用。在电生理方面,苄普地尔具有Ⅰ类、Ⅲ类和Ⅳ类抗心律失常活性。美国五项评估苄普地尔短期抗心绞痛疗效的试验共同报告称,苄普地尔能显著改善主观和客观疗效参数,且不降低左心室功能。此外,美国一项试验报告称苄普地尔长期使用后仍有抗心绞痛作用。将苄普地尔与其他抗心绞痛药物进行比较和/或联合使用的数据有限,但现有信息很有前景。关于苄普地尔在急性心肌梗死和心律失常中的应用信息也有限。苄普地尔治疗的耐受性良好,最常见的不良反应是腹泻和头晕。目前尚不清楚苄普地尔是否会被用作治疗慢性稳定型心绞痛的一线药物;然而,其长半衰期使得每日一次给药成为可能,这无疑是一个显著优势。