Products
In many countries, no drugs containing trimetazidine are commercially available. In other countries, film-coated tablets of modified release and dropper solutions are available (e.g., Vastarel), among others.
Structure and properties
Trimetazidine (C14H22N2O3, Mr = 266.3 g/mol) is a piperazine derivative. It is present in the drug as trimetazidine dihydrochloride.
Effects
Trimetazidine (ATC C01EB15) has antiischemic, cardioprotective, and cytoprotective properties. It inhibits beta-oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase in mitochondria. As a result, glucose oxidation is enhanced. Energy production by glucose oxidation consumes less oxygen than beta-oxidation in ischemic cells. This maintains energy metabolism and homeostasis during ischemia.
Indications
For the treatment of stable angina.
Dosage
According to the SmPC (depending on the drug).
Abuse
Trimetazidine can be abused as a doping agent. It is banned in professional sports both during and out of competition. See also under meldonium.
Contraindications
- Hypersensitivity
- Parkinson’s disease, Parkinson’s symptoms, tremor, restless legs syndrome.
- Severe limitation of renal function
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are not described in the SmPC. Trimetazidine is excreted mainly unchanged in the urine.
Adverse effects
The most common possible adverse effects include drowsiness, headache, rash, indigestion, and weakness.
