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开发抗心律失常药以延长心肌动作电位时程的Ⅲ类药为主。一项较大规模的临床试验表明,d-索他洛尔有致尖端扭转型室性心动过速(Torsade de pointes,简称 TdP)的副作用。高度选择性阻断快速激活的钾通道组分(I(kr))的Ⅲ类抗心律失常药,不仅有此不良反应,尚有负性频率效应,心率快时药效减弱;还有药效学的局限性,如对缺血性、儿茶酚胺及毒毛花苷G引起的心律失常均无效。本文讨论了当前抗心律失常新药与多种因素影响的关系。在阻断I(kr)的基础上,再结合其他活性,如阻断钾通道的缓慢激活部分(I(kr)),或结合阻断钠通道(I(Na))、钙通道(I(Ca))以及阻滞β受体,以形成复合型Ⅲ类药,将是抗心律失常药的主要发展方向。
The development of antiarrhythmic drugs to prolong the action potential of myocardial action class Ⅲ drugs based. A larger clinical trial has shown that d-Sosalol has the side effects of Torsade de pointes (TdP). Class III anti-arrhythmic agents that selectively block the rapidly activating potassium channel component (I (kr)) not only have this adverse effect, but also have a negative frequency effect with diminished efficacy when the heart rate is fast; Academic limitations, such as ischemic, catecholamines, and ursinin-induced arrhythmias are ineffective. This article discusses the current relationship between antiarrhythmic drugs and various factors. On the basis of blockade of I (kr), in combination with other activities such as blockade of the slow-activating part of the potassium channel (I (kr)) or binding to the blockade of the sodium channel (I (Na) Ca)) and blocking beta receptors to form complex type III drugs, anti-arrhythmic drugs will be the main direction of development.