Uses and Side effects of Trimetazidine

Trimetazidine is a piperazine derivative indicated for the symptomatic treatment of stable angina pectoris in patients inadequately controlled or intolerant to first line therapies.Trimetazidine has been studied as a treatment for angina pectoris since the late 1960s.

Uses

Trimetazidine has been treated as a drug with a high safety and tolerability profile.

Information is scarce about trimetazidine's effect on mortality, cardiovascular events, or quality of life. Long-term, randomized, controlled trials comparing trimetazidine against standard antianginal agents, using clinically important outcomes would be justifiable.Recently, an international multicentre retrospective cohort study has indeed shown that in patients with heart failure of different etiologies, the addition of trimetazidine on conventional optimal therapy can improve mortality and morbidity.

Mechanism of action

Trimetazidine inhibits beta-oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase, which enhances glucose oxidation.In an ischaemic cell, energy obtained during glucose oxidation requires less oxygen consumption than in the beta-oxidation process. Potentiation of glucose oxidation optimizes cellular energy processes, thereby maintaining proper energy metabolism during ischaemia. 

By preserving energy metabolism in cells exposed to hypoxia or ischaemia, trimetazidine prevents a decrease in intracellular ATP levels, thereby ensuring the proper functioning of ionic pumps and transmembrane sodium-potassium flow whilst maintaining cellular homeostasis.

Side effects

The EMA recommends that doctors should no longer prescribe trimetazidine for the treatment of patients with tinnitus, vertigo, or disturbances in vision.The recent EMA evaluation also revealed rare cases (3.6/1 000 000 patient years) of parkinsonian (or extrapyramidal) symptoms (such as tremor, rigidity, akinesia, hypertonia), gait instability, restless leg syndrome, and other related movement disorders; most patients recovered within 4 months after treatment discontinuation, so doctors are advised not to prescribe the medicine either to patients with Parkinson disease, parkinsonian symptoms, tremors, restless leg syndrome, or other related movement disorders, or to patients with severe renal impairment.