Role of ranolazine in angina, heart failure, arrhythmias, and diabetes

Pharmacol Ther. 2012 Mar;133(3):311-23. doi: 10.1016/j.pharmthera.2011.11.003. Epub 2011 Nov 26.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetanilides / therapeutic use*
  • Animals
  • Cardiovascular Agents / therapeutic use*
  • Diabetes Mellitus / drug therapy*
  • Diabetes Mellitus / physiopathology
  • Heart Diseases / drug therapy*
  • Heart Diseases / physiopathology
  • Humans
  • Piperazines / therapeutic use*
  • Ranolazine

Substances

  • Acetanilides
  • Cardiovascular Agents
  • Piperazines
  • Ranolazine