Abstract
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.
In patients with chronic stable angina, ranolazine ER monotherapy was shown to improve exercise duration at trough plasma drug concentration in a dose-dependent manner compared with placebo. The drug was effective as adjunctive therapy in patients with chronic stable angina whose condition was not controlled adequately with conventional antianginal therapy. In randomized clinical trials, ranolazine ER was well tolerated, with no overt effects on cardiovascular hemodynamics or conduction, apart from a modest increase in corrected QT interval (but no torsades de pointes). Importantly, the efficacy and tolerability of ranolazine ER were not affected by old age and co-morbid conditions (heart failure or diabetes mellitus).
Comparative trials of ranolazine ER with other antianginal agents and trials examining its effects on long-term morbidity and mortality in patients with ischemic heart disease are required to determine with greater certainty the place of the drug in current antianginal therapy. Nevertheless, ranolazine ER may well prove to be a useful alternative and adjunct to conventional hemodynamic antianginal therapy in the treatment of chronic stable angina.
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The use of trade names is for product identification purposes only and does not imply endorsement.
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Acknowledgments
The full text article in Drugs 2006; 66 (5): 693-710 was reviewed by B.R. Chaitman, Division of Cardiology, Saint Louis University Health Sciences Center, St Louis, Missouri, USA; G. Cocco, University of Ferrara, Ferrara, Italy; G.D. Lopaschuk, Cardiovascular Research Group, Heritage Medical Research Centre, University of Alberta, Edmonton, Alberta, Canada; P.A. McCullough, Divisions of Cardiology, Nutrition, and Preventive Medicine, Department of Medicine, William Beaumont Hospital, Royal Oak, Michigan, USA; J.O. Parker, Department of Medicine, Kingston General Hospital, Kingston, Ontario, Canada; C.J. Pepine, Division of Cardiovascular Medicine, University of Florida College of Medicine, Gainesville, Florida, USA; H. Taegtmeyer, Division of Cardiology, Department of Internal Medicine, University of Texas Health Science Center, Houston, Texas, USA.
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This Spotlight is derived from abstract and summary text of an Adis Drug Evaluation originally published in full in Drugs 2006; 66 (5): 693–710.
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Siddiqui, M.A.A., Keam, S.J. Spotlight on Ranolazine in Chronic Stable Angina Pectoris. Am J Cardiovasc Drugs 6, 357–359 (2006). https://doi.org/10.2165/00129784-200606050-00009
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DOI: https://doi.org/10.2165/00129784-200606050-00009