Department of Cardiology & Pneumology, Georg-August-University Göttingen, Germany.
Pharmacol Ther. 2012 Mar;133(3):311-23. doi: 10.1016/j.pharmthera.2011.11.003. Epub 2011 Nov 26.
Ranolazine which is currently approved as an antianginal agent reduces the Na-dependent Ca overload via inhibition of the late sodium current (late I(Na)) and thus improves diastolic tone and oxygen handling during myocardial ischemia. According to accumulating evidence ranolazine also exerts beneficial effects on diastolic and systolic heart failure where late I(Na) was also found to be elevated. Moreover, late I(Na) plays a crucial role as an arrhythmic substrate. Ranolazine has been described to have antiarrhythmic effects on ventricular as well as atrial arrhythmias without any proarrythmia or severe organ toxicity as it is common for several antiarrhythmic drugs. In patients with diabetes, treatment with ranolazine led to a significant improvement of glycemic control. In this article possible new clinical indications of the late I(Na)-inhibitor ranolazine are reviewed. We summarize novel experimental and clinical studies and discuss the significance of the available data.
雷诺嗪是一种目前被批准用于抗心绞痛的药物,它通过抑制晚期钠电流(晚期 INa)来减少 Na 依赖性 Ca 超载,从而改善心肌缺血时的舒张功能和氧处理。根据越来越多的证据,雷诺嗪对舒张性和收缩性心力衰竭也有有益的作用,在这些心力衰竭中也发现晚期 INa 升高。此外,晚期 INa 作为心律失常的基质起着至关重要的作用。雷诺嗪已被描述为对心室和房性心律失常具有抗心律失常作用,而没有任何致心律失常或严重的器官毒性,因为这是几种抗心律失常药物的常见情况。在糖尿病患者中,雷诺嗪治疗可显著改善血糖控制。本文综述了晚期 INa 抑制剂雷诺嗪的可能新的临床适应证。我们总结了新的实验和临床研究,并讨论了现有数据的意义。