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Trimetazidine
Systematic (IUPAC) name
1-(2,3,4-trimethoxybenzyl)piperazine
Identifiers
CAS number 5011-34-7
ATC code C01EB15
PubChem 21109
Chemical data
Formula C 14H22N2O3  
Mol. mass 266.336 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion mainly renal (unchanged)
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

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, which 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. It also inhibits oxidation of fatty acid in blood vessels.

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 heart disease. Recently, it has been shown to be effective in patients with heart failure of different etiologies (5-6).

Trimetazidine is described as the first cytoprotective anti-ischemic agent developed and marketed by Les Laboratories Servier (France). It 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.

Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus and dizziness. It is taken twice a day.

Trimetazidine has high safety and tolerability profile. It has no known drug interactions.

Contents

Reservations

There is scarce information about trimetazidine's effect on mortality, cardiovascular events or quality of life. Long term trials comparing trimetazidine against standard anti-anginal agents, using clinically important outcomes would be justifiable. [1]

Brand names

Distributed as: Vastarel MR, Vastarel 20 mg, Vastarel LM, Vastarel LP, Preductal MR, Flavedon MR, Flavedon 20 mg, Cardaptan, Idaptan, Carvidon MR and Trizedon MR. In the Philippines, a local brand is called Vestar.

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.
  4. Stanley WC, Marzilli M. Trimetazidine for the treatment of stable angina: biochemical mechanisms and clinical efficacy. Fundamental Clin Pharmacol 2003;17:133–145.
  5. Fragasso G, Palloshi A, Puccetti P, Silipigni C, Rossodivita A, Pala M, Calori G, Alfieri O, Margonato A. A randomized clinical trial of trimetazidine, a partial free fatty acid oxidation inhibitor, in patients with heart failure. J Am Coll Cardiol 2006;48:992-8.
  6. Tuunanen H, Engblom E, Naum A, Någren K, Scheinin M, Hesse B, Juhani Airaksinen KE, Nuutila P, Iozzo P, Ukkonen H, Opie LH, Knuuti J. Trimetazidine, a metabolic modulator, has cardiac and extracardiac benefits in idiopathic dilated cardiomyopathy. Circulation 2008;118:1250-8.

Trizide SR

External links

http://www.cochrane.org/reviews/en/ab003614.html








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