Trimetazidine

Trimetazidine

Clinical data
Trade names	Vastarel
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral
ATC code	C01EB15 (WHO)
Legal status
Legal status	UK: Controlled Drug
Pharmacokinetic data
Bioavailability	completely absorbed at around 5 hours, steady state is reached by 60th hour
Protein binding	low (16%)
Metabolism	minimal
Biological half-life	7 to 12 hours
Excretion	mainly renal (unchanged), exposure is increased in renal impairment - on average by 4-fold in subjects with severe renal impairment (CrCl <30 ml/min)
Identifiers
IUPAC name 1-(2,3,4-trimethoxybenzyl)piperazine
CAS Number	5011-34-7 N
PubChem (CID)	21109
ChemSpider	19853 Y
UNII	N9A0A0R9S8 Y
ChEMBL	CHEMBL203266 Y
ECHA InfoCard	100.023.355
Chemical and physical data
Formula	C14H22N2O3
Molar mass	266.336 g/mol
3D model (Jmol)	Interactive image
SMILES O(c1ccc(c(OC)c1OC)CN2CCNCC2)C
InChI InChI=1S/C14H22N2O3/c1-17-12-5-4-11(13(18-2)14(12)19-3)10-16-8-6-15-7-9-16/h4-5,15H,6-10H2,1-3H3 Y Key:UHWVSEOVJBQKBE-UHFFFAOYSA-N Y
NY (what is this?)

Trimetazidine is a drug for angina pectoris sold under the brand name Vastarel MR. Trimetazidine is described as the first cytoprotective anti-ischemic agent developed and marketed by Laboratoires Servier (France). Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through inhibition of fatty acid metabolism, also known as fatty acid oxidation inhibitor.

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. In 2012 European Medicines Agency (EMA) finished a review of benefits and risks of trimetazidine and recommended restricting use of trimetazidine-containing medicines just as an additional treatment of angina pectoris in case of inadequate control by or intolerance to first-line antianginal therapies.

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.

Trimetazidine has been treated as a drug with a high safety and tolerability profile. It interacts with monoamine oxidase inhibitors.