Abstract
Ranolazine has primarily been developed and so far approved as an antianginal drug. However, it also has potentially interesting and relevant antiarrhythmic properties. Its antiarrhythmic effects are mainly based on the blockade of sodium currents, in particular of the late sodium current. Experimental and clinical studies have revealed an antiarrhythmic effect of ranolazine in atrial fibrillation as chronic or “pill in the pocket” therapy. Of note, this effect was preserved in the setting of chronic heart failure. Furthermore, an antiarrhythmic effect has also been shown in experimental models of ventricular tachyarrhythmias. In addition, prevention of ventricular tachyarrhythmias has been demonstrated in patients with structural heart disease. A few late sodium current inhibitors are evaluated for antiarrhythmic properties in experimental studies. However, randomized clinical data is not yet available for these recently developed agents and larger controlled trials are necessary before recommending ranozaline as a novel antiarrhythmic drug.
Keywords: Atrial fibrillation, late sodium current, post-repolarization refractoriness, proarrhythmia, ranolazine, ventricular fibrillation
Current Medicinal Chemistry
Title:Late Sodium Current Inhibition: The Most Promising Antiarrhythmic Principle in the Near Future?
Volume: 21 Issue: 11
Author(s): G. Frommeyer, P. Milberg, L.S. Maier and L. Eckardt
Affiliation:
Keywords: Atrial fibrillation, late sodium current, post-repolarization refractoriness, proarrhythmia, ranolazine, ventricular fibrillation
Abstract: Ranolazine has primarily been developed and so far approved as an antianginal drug. However, it also has potentially interesting and relevant antiarrhythmic properties. Its antiarrhythmic effects are mainly based on the blockade of sodium currents, in particular of the late sodium current. Experimental and clinical studies have revealed an antiarrhythmic effect of ranolazine in atrial fibrillation as chronic or “pill in the pocket” therapy. Of note, this effect was preserved in the setting of chronic heart failure. Furthermore, an antiarrhythmic effect has also been shown in experimental models of ventricular tachyarrhythmias. In addition, prevention of ventricular tachyarrhythmias has been demonstrated in patients with structural heart disease. A few late sodium current inhibitors are evaluated for antiarrhythmic properties in experimental studies. However, randomized clinical data is not yet available for these recently developed agents and larger controlled trials are necessary before recommending ranozaline as a novel antiarrhythmic drug.
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Frommeyer G., Milberg P., Maier L.S. and Eckardt L., Late Sodium Current Inhibition: The Most Promising Antiarrhythmic Principle in the Near Future?, Current Medicinal Chemistry 2014; 21 (11) . https://dx.doi.org/10.2174/09298673113209990220
DOI https://dx.doi.org/10.2174/09298673113209990220 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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