Roden D M
Department of Medicine, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Br J Pharmacol. 2008 Aug;154(7):1502-7. doi: 10.1038/bjp.2008.238. Epub 2008 Jun 16.
Striking QT prolongation and the morphologically distinctive ventricular tachycardia torsades de pointes can occur in up to 5% of patients treated with certain antiarrhythmic drugs. This adverse drug reaction also occurs, albeit far less frequently, during therapy with a range of drugs not used for cardiovascular indications; examples include certain antibiotics, antipsychotics and antihistamines. The common mechanism for drug-induced torsades de pointes is inhibition of a specific repolarizing potassium current, I(Kr). The key question facing clinicians, regulators and those who develop drugs is why torsades de pointes only occurs in some patients exposed to I(Kr) block. This paper reviews the clinical, cellular, molecular and genetic features of the arrhythmia that may provide an answer to this question and proposes future studies in this area.
使用某些抗心律失常药物治疗的患者中,高达5%可能会出现显著的QT间期延长以及形态独特的室性心动过速——尖端扭转型室速。在使用一系列并非用于心血管适应症的药物进行治疗期间,这种药物不良反应也会发生,尽管频率要低得多;例如某些抗生素、抗精神病药物和抗组胺药。药物诱发尖端扭转型室速的常见机制是抑制一种特定的复极化钾电流I(Kr)。临床医生、监管机构以及药物研发人员面临的关键问题是,为什么尖端扭转型室速只发生在某些暴露于I(Kr)阻滞的患者中。本文综述了这种心律失常的临床、细胞、分子和遗传特征,这些特征可能为该问题提供答案,并提出了该领域未来的研究方向。