Trimetazidine
2038711
225957268
2008-07-16T05:16:39Z
202.164.189.22
/* Brand names */
{{drugbox |
| IUPAC_name = 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine
| image = Trimetazidine.svg
| CAS_number = 5011-34-7
| ATC_prefix = C01
| ATC_suffix = EB15
| PubChem = 21109
| DrugBank =
| C = 14 | H = 22 | N = 2 | O = 3
| molecular_weight = 266.336 g/mol
| smiles = COC1=C(C(=C(C=C1)CN2CCNCC2)OC)OC
| bioavailability =
| protein_bound =
| metabolism =
| elimination_half-life =
| excretion = mainly renal '''(unchanged)'''
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category=
| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S5 / S6 / S7 / S8 / S9 -->
| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status =
| routes_of_administration = 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 [[myocardium|myocardial]] glucose utilization through stopping of [[fatty acid metabolism]].
By preserving the energy metabolism in cells exposed to [[Hypoxia (medical)|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 [[Glyceryl trinitrate (pharmacology)|nitrates]].
It improves [[left ventricle|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 [[radical (chemistry)|free radical]]s.
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.
== 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. In the Philippines, a local brand is called Vestar.
==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.
==External links==
* [http://www.vastarelmr.com/ Official homepage]
[[Category:Antianginals]]
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[[hu:Trimetazidin]]
[[pl:Trimetazydyna]]