Vastarel MR Mechanism of Action

Pharmacology: Pharmacodynamics: 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: After oral administration, maximum concentration is found, on average, 5 hours after taking the tablet. Over 24 hours the plasma concentration remains at levels above or equal to 75% of the maximum concentration for 11 hours. Steady state is reached by the 60th hour, at the latest. The pharmacokinetic characteristics of Trimetazidine (Vastarel MR) are not influenced by meals.
The apparent distribution volume is 4.8 L/kg; protein binding is low: in vitro measurements give value of 16%. Trimetazidine (Vastarel MR) is eliminated primarily in the urine, mainly in the unchanged form. The elimination half-life of Trimetazidine (Vastarel MR) is an average of 7 hours in healthy young volunteers and 12 hours in subjects aged more than 65 years. Total clearance of trimetazidine is the result of major renal clearance which is directly correlated to creatinine clearance and, to a lesser extent, to liver clearance which is reduced with age.