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A Novel Mechanism for the Treatment of Angina, Arrhythmias, and Diastolic Dysfunction: Inhibition of Late INa Using Ranolazine
Journal of Cardiovascular Pharmacology, 08/26/09
Maier LS – In the recent years, increased late INa was suggested to contribute to this phenomenon by elevating intracellular Na concentration with subsequent rise in diastolic Ca levels by means of the sarcolemmal Na–Ca exchange system. Ranolazine, a specific inhibitor of late INa, reduces Na influx and hence ameliorates disturbed Na and Ca homeostasis. This is associated with a symptomatic improvement of angina in patients unlike other antianginal drugs without affecting heart rate or systemic blood pressure as shown in placebo–controlled studies. Therefore, ranolazine is a useful new option for patients with chronic stable angina not only as an add–on therapy. New clinical and experimental studies even point to potential antiarrhythmic effects, beneficial effects in diastolic heart failure, and under hyperglycemic conditions.
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