Journal
PHARMACOLOGY & THERAPEUTICS
Volume 133, Issue 3, Pages 311-323Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.pharmthera.2011.11.003
Keywords
Ranolazine; Late Na current; Ca overload; Ischemia; Angina; Atrial fibrillation; Heart failure; Arrhythmias; Diabetes
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Funding
- Gilead
- Faculty of Medicine, Georg-August-University Gottingen
- Deutsche Forschungsgemeinschaft through a Clinical Research group [MA 1982/2-2]
- Deutsche Forschungsgemeinschaft [MA 1982/4-1]
- Leducq Transatlantic Networks of Excellence
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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. (C) 2011 Elsevier Inc. All rights reserved.
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