Ranolazine (Ranexa) in the treatment of chronic stable angina.
Ischemic heart disease is the major cause of morbidity and mortality in the Western world. Patients often suffer a reduction in quality of life due to chronic stable angina, but therapeutic options can be limited due to concerns for heart rate and blood pressure, as well as side effect profiles. Even revascularization therapy has its limitations and newer agents are required to help in this battle for symptomatic relief. Ranolazine (Ranexa(R), A. Menarini Pharma UK, High Wycombe, UK) is a drug with a novel mechanism of action that has been shown in several large trials to be an efficacious adjunctive agent in reducing symptoms of chronic stable angina. It is thought to work by inhibiting the late sodium current in cardiac myocytes, thereby reducing sodium and calcium overload that follows ischemia. This improves myocardial relaxation and reduces left ventricular diastolic stiffness, which in turn enhances myocardial contractility and perfusion. The drug is generally well tolerated and the evidence so far is encouraging, with a clear clinical benefit achieved in the target groups. Its main strength is that it does not appear to affect either heart rate or blood pressure. This review provides an insight into this treatment option, describes the clinical trials evidence, proposed mechanism of action, and pharmacokinetics, and outlines the indications for its use in chronic stable angina.
Aslam
Sajid
S
Division of Cardiovascular Medicine, University Hospital, Nottingham, UK.
Gray
David
D
D000083:Acetanilides / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000787:Angina Pectoris / Q000188:drug therapy* / Q000601:surgery; D002317:Cardiovascular Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D002908:Chronic Disease; D001026:Coronary Artery Bypass; D004359:Drug Therapy, Combination; D006801:Humans; D010879:Piperazines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016032:Randomized Controlled Trials as Topic; D000069458:Ranolazine
D000083:Acetanilides; D002317:Cardiovascular Agents; D010879:Piperazines; D000069458:Ranolazine