Amtaz Mechanism of Action

Pharmacologic category: Anti-angina.
Pharmacology: Pharmacodynamics: Trimetazidine inhibits oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase, which enhances glucose oxidation. In an ischemic cell, energy obtained during glucose oxidation requires less oxygen consumption than in the oxidation process. Potentiation of glucose oxidation optimizes cellular energy processes, thereby maintaining proper energy metabolism during ischemia.
Pharmacodynamic effects: In patients with ischemic heart disease, trimetazidine acts as a metabolic agent, preserving the myocardial high-energy phosphate intracellular levels. Anti-ischemic effects are achieved without concomitant hemodynamic effects.
Pharmacokinetics: Absorption: Trimetazidine after oral administration and absorption from the digestive tract reaches the maximum concentration in the serum after about 5 hours from administration of the drug. The steady concentration of the drug in the serum is reached after 60 hours and is stable throughout the period of treatment. No interactions with foodstuffs have been found.
Distribution: The drug binds to plasma proteins at about 16%. The volume of distribution is 4.8 L/kg, which means good penetration of the drug into the tissues.
Elimination: Trimetazidine is eliminated mainly in the urine, in unchanged form. The average half-life is 7 hours, in patients over age 65 years it increases to 12 hours.
Pharmacokinetics in special populations: No pharmacokinetic data are available for the use of trimetazidine in hepatically impaired patients.