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Review
. 2010;37(6):641-7.

Ranolazine: a new approach to treating an old problem

Bharath M Reddy  1 , Howard S Weintraub, Arthur Z Schwartzbard
Affiliations
Review

Ranolazine: a new approach to treating an old problem

Bharath M Reddy et al. Tex Heart Inst J. 2010.

Abstract

Chronic angina pectoris affects millions of patients every year. During the past 2 decades, advances in medical therapy have led to substantial reductions in the symptoms of angina. Nonetheless, many patients continue to experience persistent angina that causes debilitating symptoms and lifestyle changes. Moreover, many current therapeutic agents cause side effects that can induce substantial morbidity on their own. In major clinical trials, the drug ranolazine has been shown to bring symptomatic relief to large numbers of patients who have chronic angina. Herein, we review the physiology of the sodium channel; the pharmacology of ranolazine; clinical trials that support use of the drug; recent evidence about ranolazine's therapeutic effect on diastolic heart failure, glycemic control, and atrial fibrillation and other arrhythmias; officially approved clinical indications; and avenues of future study.

Keywords: Angina pectoris/drug therapy/prevention & control; anti-arrhythmia agents/pharmacology/therapeutic use; cardiovascular agents/pharmacology/therapeutic use; clinical trials as topic; coronary disease/drug therapy; dose-response relationship, drug; heart conduction system/drug effects/metabolism/physiopathology; myocardial ischemia/drug therapy; piperazines/therapeutic use; ranolazine/administration & dosage; sodium channel blockers/pharmacology/therapeutic use; sodium channels/drug effects/metabolism/physiology.

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Figures

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Fig. 1 Late inhibition of inward sodium channel current (INaL) under normal and pathologic increased states. Adapted from: Hasenfuss G, Maier LS. Mechanism of action of the new anti-ischemia drug ranolazine. Clin Res Cardiol 2008;97(4):222–6. Used by permission.
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Fig. 2 Presumed effect of ranolazine on myocardial oxygen demand–supply mismatch. LVEDP = left ventricular end-diastolic pressure; INaL = late inward sodium channel current Adapted from: Stone PH. Ranolazine: new paradigm for management of myocardial ischemia, myocardial dysfunction, and arrhythmias. Cardiol Clin 2008;26(4):603–14. Used by permission.
See this image and copyright information in PMC

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