Ranolazine: A Contemporary Review

R anolazine, a piperazine derivative sold under the trade name Ranexa, is a well-tolerated medication that selectively inhibits the late sodium current. Additionally, ranolazine has beneficial metabolic properties and does not affect heart rate or blood pressure. Ranolazine is currently approved in the United States and Europe as a second-line agent in the management of chronic stable angina pectoris (CSAP). It is not currently approved for use by Health Canada and requires an application through the Special Access Programme. CSAP is estimated to affect >7 million North Americans, and is associated with significant morbidity. Several randomized controlled trials (RCTs) have supported the use of ranolazine in this population. This evidence has been incorporated in North American and European guidelines. In addition, the benefit of ranolazine in acute coronary syndrome (ACS), microvascular coronary dysfunction (MCD), arrhythmias, and glycemic control has been evaluated. We present a comprehensive review of the pharmacology, guidelines, and studied uses of ranolazine.