Trimetazidine

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Trimetazidine
Systematic (IUPAC) name
1-[(2,3,4-trimethoxyphenyl)methyl]piperazine
Identifiers
CAS number	5011-34-7
ATC code	C01EB15
PubChem	21109
Chemical data
Formula	C₁₄H₂₂N₂O₃
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 stopping 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.

Trimetazine is described as the first cytoprotective anti-ischemic agent. 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.

Trimetazine 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.

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

[edit] Brand names

Vastarel MR is also distributed as: Vastarel 35 mg, Vastarel 20 mg, Vastarel LM, Vastarel LP, Preductal MR, Flavedon MR, Cardaptan, Idaptan, Carvidon MR and Trizedon MR.

[edit] References

Sellier P, Broustet JP. Am J Cardiovasc Drugs. 2003;3:361-369.
Génissel P, Chodjania Y, Demolis JL, Ragueneau I, Jaillon P. Eur J Drug Metab Pharmacokinet. 2004;29: 61-68.
Kantor PF, Lucien A, Kozak R, Lopaschuk GD. Circ Res. 2000;86:580-588.
Stanley WC, Marzilli M. Trimetazidine for the treatment of stable angina: biochemical mechanisms and clinical efficacy. Fundamental Clin Pharmacol. 17:133–145, 2003.