Ranolazine: an anti-anginal drug with further therapeutic potential.
Ranolazine is a novel drug approved for the treatment of chronic angina pectoris. In randomized trials, it significantly reduced the frequency of anginal attacks and the need for use of short-acting nitroglycerine. It improved exercise capacity and delayed onset of anginal symptoms or electrocardiographic signs of ischemia during exercise in patients with chronic stable angina. Unlike other drugs used for the treatment of chronic angina, ranolazine has negligible effects on blood pressure and heart rate. A major mechanism believed to contribute to this clinical efficacy is its inhibitory effect on late sodium influx during the cardiac action potential of cardiomyocytes, which is particularly important in ischemic or hypoxic conditions. Ranolazine thereby reduces intracellular sodium and calcium accumulation during ischemia, as shown in various animal research models. In this review we discuss the pharmacological profile of ranolazine and discuss the current and potential future applications in cardiovascular disease for this drug.
Reffelmann
Thorsten
T
Klinik und Poliklinik für Innere Medizin B, Universitätsklinikum der Ernst-Moritz-Arndt-Universität Greifswald, Friedrich-Löffler Strasse 23a, Greifswald, Germany. thorstenreffelmann@web.de
Kloner
Robert A
RA
D000083:Acetanilides / Q000008:administration & dosage* / Q000494:pharmacology; D000787:Angina Pectoris / Q000175:diagnosis / Q000188:drug therapy* / Q000401:mortality; D002908:Chronic Disease; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D017277:Drug Approval; D004359:Drug Therapy, Combination; D005260:Female; D005500:Follow-Up Studies; D006801:Humans; D008297:Male; D005996:Nitroglycerin / Q000627:therapeutic use; D010879:Piperazines / Q000008:administration & dosage* / Q000494:pharmacology; D016032:Randomized Controlled Trials as Topic; D000069458:Ranolazine; D015996:Survival Rate; D016896:Treatment Outcome; D014481:United States
D000083:Acetanilides; D010879:Piperazines; D000069458:Ranolazine; D005996:Nitroglycerin