Pharmacotherapeutic group: Other cardiac preparation.
Pharmacology: Pharmacodynamics: Trimetazidine inhibits β-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 β-oxidation process. Potentiation of glucose oxidation optimizes cellular energy processes, thereby maintaining proper energy metabolism during ischaemia.
Pharmacodynamic effects: In patients with ischaemic heart disease, trimetazidine acts as a metabolic agent, preserving the myocardial high-energy phosphate intracellular levels. Anti-ischaemic effects are achieved without concomitant haemodynamic effects.
Pharmacokinetics: Trimetazidine is rapidly and completely absorbed from the gastrointestinal tract. Plasma protein binding is low and the volume of distribution is 320 L. Four pathways of metabolism are known but metabolism is not extensive, with 51% of unchanged drug eliminated in urine. Elimination is rapid (t½=6 h) and predominantly renal.
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