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Ranolazine for the Treatment of Chronic Angina and Potential Use in Other Cardiovascular Conditions

Ranolazine for the Treatment of Chronic Angina and Potential Use in Other Cardiovascular Conditions New Drugs and Technologies Ranolazine for the Treatment of Chronic Angina and Potential Use in Other Cardiovascular Conditions Bernard R. Chaitman, MD hronic angina, a condition that impairs quality of life and is Ranolazine Metabolism C associated with decreased life expectancy, affects 6.4 Exposure to ranolazine is not affected by food. Oral bioavail- million Americans. Current therapies that reduce angina fre- ability is in the range of 30% to 55%. Plasma protein binding quency and nitrate consumption and increase the threshold at (mainly to 1-acid glycoprotein) is 65%. The cytochrome which demand-induced myocardial ischemic symptoms become P450 (CYP) 3A4 –mediated pathway accounts for the major- 16 –18 evident include drugs (nitrates, -blockers, calcium antagonists), ity of ranolazine biotransformation. Additional pathways exercise conditioning, enhanced external counterpulsation, and include metabolism by CYP2D6 (10% to 15%), glucuronida- 1–3 coronary revascularization. Several new investigational drugs tion (5%), and excretion of unchanged ranolazine by the 4–9 are being tested for the treatment of chronic angina. This kidneys (5%) (Figure 1). Three phase I metabolites (CVT- review will focus on sustained-release ranolazine, a drug that 2512, CVT-2514, CVT-2738) and 1 phase II metabolite of reduces angina symptoms, with a mechanism of action different ranolazine in http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Circulation Wolters Kluwer Health

Ranolazine for the Treatment of Chronic Angina and Potential Use in Other Cardiovascular Conditions

Circulation , Volume 113 (20) – May 1, 2006

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ISSN
0009-7322
eISSN
1524-4539
DOI
10.1161/CIRCULATIONAHA.105.597500
pmid
16717165
Publisher site
See Article on Publisher Site

Abstract

New Drugs and Technologies Ranolazine for the Treatment of Chronic Angina and Potential Use in Other Cardiovascular Conditions Bernard R. Chaitman, MD hronic angina, a condition that impairs quality of life and is Ranolazine Metabolism C associated with decreased life expectancy, affects 6.4 Exposure to ranolazine is not affected by food. Oral bioavail- million Americans. Current therapies that reduce angina fre- ability is in the range of 30% to 55%. Plasma protein binding quency and nitrate consumption and increase the threshold at (mainly to 1-acid glycoprotein) is 65%. The cytochrome which demand-induced myocardial ischemic symptoms become P450 (CYP) 3A4 –mediated pathway accounts for the major- 16 –18 evident include drugs (nitrates, -blockers, calcium antagonists), ity of ranolazine biotransformation. Additional pathways exercise conditioning, enhanced external counterpulsation, and include metabolism by CYP2D6 (10% to 15%), glucuronida- 1–3 coronary revascularization. Several new investigational drugs tion (5%), and excretion of unchanged ranolazine by the 4–9 are being tested for the treatment of chronic angina. This kidneys (5%) (Figure 1). Three phase I metabolites (CVT- review will focus on sustained-release ranolazine, a drug that 2512, CVT-2514, CVT-2738) and 1 phase II metabolite of reduces angina symptoms, with a mechanism of action different ranolazine in

Journal

CirculationWolters Kluwer Health

Published: May 1, 2006

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