Trimetazidine
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Trimetazidine
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| Systematic (IUPAC) name | |
| 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C14H22N2O3 |
| Mol. mass | 266.336 g/mol |
| SMILES | search in , |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Trimetazidine is a drug for angina pectoris sometimes referred to by the brand name Vastarel MR®. Each tablet contains 35 mg of trimetazidine. Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, that improves myocardial glucose utilization through inhibition of Fatty acid metabolism.
By preserving the energy metabolism in cells exposed to hypoxia or ischemia, trimetazidine prevents a decrease in intracellular [[Adenosine triphosphate ]] levels, thereby ensuring the proper functioning of ionic pumps and transmembranous sodium-potassium flow whilst maintaining cellular homeostasis.
Controlled studies in angina patients have shown that trimetazidine increases coronary flow reserve, thereby delaying the onset of ischemia associated with exercise, limits rapid swings in blood pressure without any significant variations in heart rate, significantly decreases the frequency of angina attacks, and leads to a significant decrease in the use of nitrates.
It improves left ventricular function in diabetic patients with coronary artery disease. Recently, it has been shown to be effective in patients with heart failure of different etiologies.
It is described as the first cytoprotective anti-ischemic agent, acts by directly counteracting all the major metabolic disorders occurring within the ischemic cell. The actions of trimetazidine include limitation of intracellular acidosis, correction of disturbances of transmembrane ion exchanges, and prevention of excessive production of free radicals.
It is usually prescribed as a long-term treatment of Angina pectoris, Ménière's disease and Tinnitus.
Vastarel MR is also distributed as: Vastarel 35mg, Vastarel LM, Vastarel LP, Preductal MR, Flavedon MR and Trizedon MR.
[edit] References
1. Sellier P, Broustet JP. Am J Cardiovasc Drugs. 2003;3:361-369. 2. Génissel P, Chodjania Y, Demolis JL, Ragueneau I, Jaillon P. Eur J Drug Metab Pharmacokinet. 2004;29: 61-68. 3. Kantor PF, Lucien A, Kozak R, Lopaschuk GD. Circ Res. 2000;86:580-588.
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