Abstract
The goals of pharmacological treatment of stable angina pectoris are to improve quality of life by reducing the severity and/or frequency of symptoms and also the long-term prognosis. Patients with coronary artery disease have viable but dysfunctional myocardium. The metabolism of the ischemic myocardium is characterized by a shift from fatty acid to glucose as a preferred substrate and a decline in the levels of ATP. Targeting myocardial metabolism as a pharmacologic approach for chronic angina is based on the concept that metabolic adaptive mechanisms during ischemia resemble fetal energy metabolism by shifting substrate use towards glucose metabolism. Potential pharmacologic approaches should target i) the suppression of lipolysis and the plasma fatty acid levels and subsequent uptake and oxidation by the heart, ii) direct inhibition of the enzymes of fatty acid beta-oxidation, iii) inhibition of carnitine palmitoyl transferase- I (CPT-1). Currently, there are no approved medications directly targeting myocardial metabolism. However, in the last two years a number of medications indirectly targeting cardiac metabolism have been tested in small clinical trials, and some of them appear to be promising potential therapies for stable angina. This review summarizes the main aspects of myocardial metabolism and focuses on the therapeutic approaches that could offer clinical benefit in patients with stable angina.
Keywords: Myocardial metabolism, stable angina, free fatty acids, CPT inhibitors, ranolazine, prognosis, lipolysis, clinical trials, fatty acid beta-oxidation, cardiac metabolism
Current Pharmaceutical Design
Title:Targeting Myocardial Metabolism for the Treatment of Stable Angina
Volume: 19 Issue: 9
Author(s): Dimitris Tousoulis, Constantinos Bakogiannis, Alexandros Briasoulis, Nikolaos Papageorgiou, Emmanuel Androulakis, Gerasimos Siasos, George Latsios, Anna-Maria Kampoli, Marietta Charakida, Kostas Toutouzas and Christodoulos Stefanadis
Affiliation:
Keywords: Myocardial metabolism, stable angina, free fatty acids, CPT inhibitors, ranolazine, prognosis, lipolysis, clinical trials, fatty acid beta-oxidation, cardiac metabolism
Abstract: The goals of pharmacological treatment of stable angina pectoris are to improve quality of life by reducing the severity and/or frequency of symptoms and also the long-term prognosis. Patients with coronary artery disease have viable but dysfunctional myocardium. The metabolism of the ischemic myocardium is characterized by a shift from fatty acid to glucose as a preferred substrate and a decline in the levels of ATP. Targeting myocardial metabolism as a pharmacologic approach for chronic angina is based on the concept that metabolic adaptive mechanisms during ischemia resemble fetal energy metabolism by shifting substrate use towards glucose metabolism. Potential pharmacologic approaches should target i) the suppression of lipolysis and the plasma fatty acid levels and subsequent uptake and oxidation by the heart, ii) direct inhibition of the enzymes of fatty acid beta-oxidation, iii) inhibition of carnitine palmitoyl transferase- I (CPT-1). Currently, there are no approved medications directly targeting myocardial metabolism. However, in the last two years a number of medications indirectly targeting cardiac metabolism have been tested in small clinical trials, and some of them appear to be promising potential therapies for stable angina. This review summarizes the main aspects of myocardial metabolism and focuses on the therapeutic approaches that could offer clinical benefit in patients with stable angina.
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Tousoulis Dimitris, Bakogiannis Constantinos, Briasoulis Alexandros, Papageorgiou Nikolaos, Androulakis Emmanuel, Siasos Gerasimos, Latsios George, Kampoli Anna-Maria, Charakida Marietta, Toutouzas Kostas and Stefanadis Christodoulos, Targeting Myocardial Metabolism for the Treatment of Stable Angina, Current Pharmaceutical Design 2013; 19 (9) . https://dx.doi.org/10.2174/1381612811319090006
DOI https://dx.doi.org/10.2174/1381612811319090006 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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