Ranolazine: effects on ischemic heart

Recent Pat Cardiovasc Drug Discov. 2013 Dec;8(3):197-203. doi: 10.2174/15748901113089990023.

Abstract

Coronary artery disease is the major cause of mortality and morbidity in the industrialized countries; in the United States of America and in Europe, it is responsible for one of every six deaths per year. In the setting of ischemic heart disease, angina pectoris and chest pain, in particular, are the major causes of emergency department accesses. Angina pectoris is a clinical syndrome characterized by discomfort typically in the chest, neck, chin and left arm induced by physical exertion, emotional stress and cold and is relieved by rest or by taking of nitrates. The main targets of treatment of angina pectoris are to improve quality of life by reducing the frequency and the severity of symptoms, to increase functional capacity and to improve prognosis. Ranolazine is a recent antianginal drug with unique methods of action. It was approved by the US Food and Drug Administration in 2006 as add-on therapy in patients symptomatic for stable angina. With the inhibition of the late sodium current, Ranolazine protects against ion deregulation, prevents cellular calcium overload and the subsequent increase in diastolic tension without impacting heart rate and blood pressure. Short term clinical trials and patent research show that add on therapy with Ranolazine in patients with chronic stable angina significantly improves exercise duration, exercise time to angina and reduces the use of nitro glycerine. Long term clinical trials showed no significant differences in the rate of cardiovascular death and myocardial infarction in patients with non-ST segment elevation acute coronary syndromes but a reduction in terms of recurrent ischemia. Ranolazine is generally well tolerated and even if it increases the duration of QTc interval it is not associated with atrial and ventricular arrhythmias. Therefore Ranolazine represents a good therapeutic approach in patients with chronic stable angina still symptomatic, while on optimal anti-ischemic therapy, or intolerant to traditional anti-ischemic drugs.

Publication types

  • Review

MeSH terms

  • Acetanilides / adverse effects
  • Acetanilides / pharmacokinetics
  • Acetanilides / pharmacology
  • Acetanilides / therapeutic use*
  • Angina, Stable / drug therapy
  • Animals
  • Arrhythmias, Cardiac / drug therapy
  • Clinical Trials as Topic
  • Diabetes Mellitus / drug therapy
  • Drug Interactions
  • Heart Failure / drug therapy
  • Humans
  • Myocardial Ischemia / drug therapy*
  • Piperazines / adverse effects
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology
  • Piperazines / therapeutic use*
  • Ranolazine
  • Sodium Channel Blockers / therapeutic use*

Substances

  • Acetanilides
  • Piperazines
  • Sodium Channel Blockers
  • Ranolazine