ranexa

Objectives: The objective of the current study was to develop an extended release (XR) tablet formulation for ranolazine using Eudragit L 100-55 and hydroxypropylmethylcellulose (HPMC) K100M in an appropriate composition. Ranolazine, an anti-anginal agent, is mainly used for treating chronic stable angina pectoris. The main advantage of this drug that it exhibits anti-ischemic effect, which was not influenced by either blood pressure or heart rate. Materials and Methods: XR tablets of ranolazine were prepared using variable amounts of Eudragit L 100-55 and HPMC K100M in various proportions as per 32 factorial design by direct compression technique...

The antianginal agent ranolazine (Ranexa®) is metabolized primarily by cytochrome P450-3A (CYP3A) enzymes. Coadministration with strong CYP3A inhibitors, such as ketoconazole and posaconazole, is contraindicated due to risk of QT prolongation from high levels of ranolazine. This study evaluated the time course of recovery from the posaconazole drug interaction in normal-weight and otherwise healthy obese subjects. Subjects received single doses of ranolazine in the baseline control condition, again during coadministration of posaconazole, and at 4 additional time points during the 2 weeks after posaconazole discontinuation...

Extended-release ranolazine (ranolazine ER) [Ranexa(®)] is an antianginal agent that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP). This article reviews the efficacy, safety and tolerability of ranolazine ER as add-on therapy in patients with chronic stable angina pectoris, as well as summarizing its pharmacological properties and its use in non-ST-elevation acute coronary syndromes. In the CARISA and ERICA trials, add-on therapy with ranolazine ER improved exercise tolerance and/or reduced angina frequency and nitroglycerin use in patients with chronic stable angina; benefits were seen across a variety of patient subgroups...

A range of experimental and clinical data suggests strongly (i) that metastatic progression in carcinomas is accompanied (maybe even preceded) by upregulation of functional voltage-gated sodium channels (VGSCs) and (ii) that VGSC activity enhances cancer cell invasiveness. First, this review outlines the available in vitro and in vivo evidence for the VGSC expression and its proposed pathophysiological role. Second, we question the mechanism(s) whereby VGSC activity can induce such a cancer-promoting effect...

Atrial fibrillation is the most common arrhythmia seen in clinical practice, and novel pharmacological approaches for treatment are sought. Ranolazine (Ranexa; N-(2,6-dimethylphenyl)-2-[4-(2-hydroxy-3-[2-methoxyphenoxy]propyl)piperazin-1-yl]acetamide) is used clinically for the treatment of angina pectoris. Evidence is reviewed from both pre-clinical and clinical studies, which suggests that ranolazine also exhibits antiarrhythmic activity with growing evidence for atrio-selectivity. Further work is required in order to explore more fully the potential of ranolazine in the treatment of atrial fibrillation...

No abstract text is available yet for this article.

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...

More than 6 million people in the United States are affected by chronic angina. On January 27, 2006, the US Food and Drug Administration (FDA) approved a new medication for the treatment of chronic stable angina called ranolazine (Ranexa). This is the first angina drug approved by the FDA in over a decade. The unique thing about this drug is that it falls into a new class of therapies in that it works at the level of cellular metabolism in decreasing demand on the cardiac tissue. There are many factors to consider when prescribing this medication including past studies, dosing, and education...

Inhibition of the persistent or late Na current (INa) using ranolazine (Ranexa) represents a novel mechanism of action that was approved in the United States in 2006 and only recently in the European Union for use in patients with stable angina pectoris. In general, myocardial ischemia is associated with reduced adenosine triphosphate fluxes and decreased energy supply, resulting in severe disturbances of intracellular ion homeostasis in cardiac myocytes. In the recent years, increased late INa was suggested to contribute to this phenomenon by elevating intracellular Na concentration with subsequent rise in diastolic Ca levels by means of the sarcolemmal Na-Ca exchange system...

Extended-release ranolazine (ranolazine ER) [Ranexa] is a piperazine derivative with a novel mechanism of action that was recently approved in the EU for use as add-on therapy in patients with stable angina pectoris. Ranolazine ER achieves its antianginal effect without affecting heart rate or blood pressure (BP) to a clinically significant extent. Results of well designed, placebo-controlled, short-term studies demonstrate that add-on therapy with ranolazine ER in patients with chronic stable angina improves exercise performance, and reduces anginal frequency and nitroglycerin use...

Ranolazine [Ranexa; (+/-)-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine] is novel anti-ischemic agent that has been shown to inhibit late I(Na) and I(Kr) and to have antiarrhythmic effects in various preclinical in vitro models. This study was undertaken to investigate the effects of ranolazine on drug-induced Torsade de Pointes (TdP) in vivo. TdP was induced by an I(Kr) blocker, clofilium, in anesthetized, alpha(1)-agonist-sensitized rabbits. Clofilium prolonged QT interval corrected for heart rate (QTc) (52 +/- 9%) and monophasic action potential duration (MAPD)(90) (56 +/- 9%) and caused TdP in eight of eight rabbits...

Chronic Angina resistant to medical treatment with hemodynamically acting agents is a major problem in clinical setup. For such patients, large number of clinical trials have documented the beneficial effect of Ranolazine. It acts as an anti-anginal agent that controls myocardial ischemia through intracellular metabolic changes. Ranolazine is a partial fatty acid oxidation inhibitor which shifts cardiac energy metabolism from fatty acid oxidation to glucose oxidation. Since the oxidation of glucose requires less oxygen than the oxidation of fatty acids, ranolazine can help maintain myocardial function in times of ischemia...

(1) Ranolazine-- an adjunctive treatment to beta-blockers, calcium channel blockers, or long-acting nitrates-- is indicated for patients with chronic stable angina who have not responded to standard anti-anginal therapy. (2) In three randomized controlled trials (RCTs), ranolazine, in combination with standard anti-anginal medications, led to modest but statistically significant improvements in exercise duration, and reductions in the frequency of angina episodes and nitroglycerin consumption, when compared to standard anti-anginal medications only...

Ranolazine (Ranexa), a piperazine derivative, is a new antianginal agent approved for the treatment of chronic stable angina pectoris for use as combination therapy when angina is not adequately controlled with other antianginal agents. While the exact mechanism of action of ranolazine is not known, its antianginal and anti-ischemic effects do not appear to depend upon changes in BP or heart rate. An extended-release (ER) oral formulation of ranolazine has been developed to facilitate twice-daily administration whilst maintaining therapeutically effective plasma concentrations...

No abstract text is available yet for this article.

Ranolazine (Ranexa), a piperazine derivative, is a new antianginal agent approved for the treatment of chronic stable angina pectoris for use as combination therapy when angina is not adequately controlled with other antianginal agents. While the exact mechanism of action of ranolazine is not known, its antianginal and anti-ischaemic effects do not appear to depend upon changes in blood pressure or heart rate. An extended-release (ER) oral formulation of ranolazine has been developed to facilitate twice-daily administration whilst maintaining therapeutically effective plasma concentrations...

CV Therapeutics, under license from Roche (formerly Syntex), is developing ranolazine (Ranexa), a metabolic modulator and a partial fatty acid oxidation inhibitor, for the potential treatment of angina and acute coronary syndromes. By October 2004, enrollment in the phase III MERLIN TIMI-36 study was ongoing and the company anticipated completion by the end of the first quarter of 2005.