title: Electrophysiologic basis for the antiarrhythmic actions of ranolazine.
abstract: Ranolazine is a Food and Drug Administration-approved antianginal agent. Experimental and clinical studies have shown that ranolazine has antiarrhythmic effects in both ventricles and atria. In the ventricles, ranolazine can suppress arrhythmias associated with acute coronary syndrome, long QT syndrome, heart failure, ischemia, and reperfusion. In atria, ranolazine effectively suppresses atrial tachyarrhythmias and atrial fibrillation (AF). Recent studies have shown that the drug may be effective and safe in suppressing AF when used as a pill-in-the pocket approach, even in patients with structurally compromised hearts, warranting further study. The principal mechanism underlying ranolazine's antiarrhythmic actions is thought to be primarily via inhibition of late I(Na) in the ventricles and via use-dependent inhibition of peak I(Na) and I(Kr) in the atria. Short- and long-term safety of ranolazine has been demonstrated in the clinic, even in patients with structural heart disease. This review summarizes the available data regarding the electrophysiologic actions and antiarrhythmic properties of ranolazine in preclinical and clinical studies.
authors.affiliation: Masonic Medical Research Laboratory, Utica, New York, USA. ca@mmrl.edu
authors.forename: Charles
authors.initials: C
authors.lastname: Antzelevitch
authors.forename: Alexander
authors.initials: A
authors.lastname: Burashnikov
authors.forename: Serge
authors.initials: S
authors.lastname: Sicouri
authors.forename: Luiz
authors.initials: L
authors.lastname: Belardinelli
mesh_terms: D000083:Acetanilides / Q000494:pharmacology*; D000200:Action Potentials; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D001145:Arrhythmias, Cardiac / Q000188:drug therapy* / Q000503:physiopathology; D015220:Calcium Channels / Q000187:drug effects; D022062:Electrophysiologic Techniques, Cardiac; D006321:Heart / Q000503:physiopathology*; D006325:Heart Atria / Q000187:drug effects / Q000503:physiopathology; D006352:Heart Ventricles / Q000166:cytology / Q000187:drug effects; D006801:Humans; D007473:Ion Channels / Q000187:drug effects; D008564:Membrane Potentials; D032383:Myocytes, Cardiac / Q000187:drug effects / Q000502:physiology; D010879:Piperazines / Q000494:pharmacology*; D015221:Potassium Channels / Q000187:drug effects; D000069458:Ranolazine; D013045:Species Specificity
chemical_list: D000083:Acetanilides; D000889:Anti-Arrhythmia Agents; D015220:Calcium Channels; D007473:Ion Channels; D010879:Piperazines; D015221:Potassium Channels; D000069458:Ranolazine