Caron J, Libersa C
Centre Régional de Pharmacovigilance, Service de Pharmacologie Hospitalière, Faculté de Médecine, Université Droit et Santé, Lille, France.
Drug Saf. 1997 Jul;17(1):8-36. doi: 10.2165/00002018-199717010-00002.
Class I antiarrhythmic drugs are characterised by their ability to block the fast inward sodium current in cardiac muscle tissue. However, at the same time, they can be responsible for various effects involving other organs and systems. Although some of these effects can be helpful in specific situations, most of them, such as their pro-arrhythmic propensity, are deleterious. Some of the adverse effects of class I antiarrhythmic drugs are directly linked to sodium-channel blockade (conduction disorders haemodynamic perturbations, and digestive and neurological effects), while others are linked to other specific pharmacological properties (e.g. atropinic, or alpha- or beta-adrenergic blockade) or to nonspecific properties (idiosyncratic hypersensitivity, and haematological, dermatological or hepatic reactions). Other adverse effects are associated with complex interactions between class I antiarrhythmics and individual predisposing factors, trigger mechanisms and physiological factors (including concomitant drug treatment). These numerous variations and interactions within a specific environment and underlying disorder might be of pharmacological or/and pharmacokinetic origin, making analysis of the true liability of the class I drugs very difficult when adverse effects occur.
I类抗心律失常药物的特点是能够阻断心肌组织中的快速内向钠电流。然而,与此同时,它们可能会对涉及其他器官和系统产生各种影响。虽然其中一些影响在特定情况下可能是有益的,但大多数影响,如促心律失常倾向,是有害的。I类抗心律失常药物的一些不良反应与钠通道阻滞直接相关(传导障碍、血流动力学紊乱以及消化和神经学影响),而其他不良反应则与其他特定药理特性(如抗胆碱能、α或β肾上腺素能阻滞)或非特异性特性(特发性超敏反应以及血液学、皮肤病学或肝脏反应)有关。其他不良反应与I类抗心律失常药物与个体易感因素、触发机制和生理因素(包括合并药物治疗)之间的复杂相互作用有关。在特定环境和潜在疾病中,这些众多的变化和相互作用可能源于药理学或/和药代动力学,当出现不良反应时,很难分析I类药物的真正不良反应。