Ranolazine (Ranexa) in the treatment of chronic stable angina. 2010

Sajid Aslam, and David Gray
Division of Cardiovascular Medicine, University Hospital, Nottingham, UK.

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.

UI MeSH Term Description Entries
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D002317 Cardiovascular Agents Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume. Cardioactive Agent,Cardioactive Drug,Cardiovascular Agent,Cardiovascular Drug,Cardioactive Agents,Cardioactive Drugs,Cardiovascular Drugs,Agent, Cardioactive,Agent, Cardiovascular,Drug, Cardioactive,Drug, Cardiovascular
D002908 Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2). Chronic Condition,Chronic Illness,Chronically Ill,Chronic Conditions,Chronic Diseases,Chronic Illnesses,Condition, Chronic,Disease, Chronic,Illness, Chronic
D004359 Drug Therapy, Combination Therapy with two or more separate preparations given for a combined effect. Combination Chemotherapy,Polychemotherapy,Chemotherapy, Combination,Combination Drug Therapy,Drug Polytherapy,Therapy, Combination Drug,Chemotherapies, Combination,Combination Chemotherapies,Combination Drug Therapies,Drug Polytherapies,Drug Therapies, Combination,Polychemotherapies,Polytherapies, Drug,Polytherapy, Drug,Therapies, Combination Drug
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000069458 Ranolazine An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS. N-(2,6-dimethylphenyl)-4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)-1-piperazineacetamide,RS 43285,RS 43285-193,RS-43285,Ranexa,Ranolazine Dihydrochloride,Ranolazine HCl,Ranolazine Hydrochloride,Renolazine,43285, RS,Dihydrochloride, Ranolazine,HCl, Ranolazine,Hydrochloride, Ranolazine,RS 43285 193,RS 43285193,RS43285
D000083 Acetanilides Compounds based on N-phenylacetamide, that are similar in structure to 2-PHENYLACETAMIDES. They are precursors of many other compounds. They were formerly used as ANALGESICS and ANTIPYRETICS, but often caused lethal METHEMOGLOBINEMIA. Acetylanilines,N-Phenylacetamides
D000787 Angina Pectoris The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION. Angor Pectoris,Stenocardia,Stenocardias
D001026 Coronary Artery Bypass Surgical therapy of ischemic coronary artery disease achieved by grafting a section of saphenous vein, internal mammary artery, or other substitute between the aorta and the obstructed coronary artery distal to the obstructive lesion. Aortocoronary Bypass,Bypass, Coronary Artery,Bypass Surgery, Coronary Artery,Coronary Artery Bypass Grafting,Coronary Artery Bypass Surgery,Aortocoronary Bypasses,Artery Bypass, Coronary,Artery Bypasses, Coronary,Bypass, Aortocoronary,Bypasses, Aortocoronary,Bypasses, Coronary Artery,Coronary Artery Bypasses
D016032 Randomized Controlled Trials as Topic Works about clinical trials that involve at least one test treatment and one control treatment, concurrent enrollment and follow-up of the test- and control-treated groups, and in which the treatments to be administered are selected by a random process, such as the use of a random-numbers table. Clinical Trials, Randomized,Controlled Clinical Trials, Randomized,Trials, Randomized Clinical

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