Vastarel 20

Vastarel 20 Mechanism of Action





Full Prescribing Info
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: Absorption: After oral administration, absorption of trimetazidine is rapid and the plasma peak is reached in less than 2 hours. After a single oral dose of 20 mg of trimetazidine, the peak plasma concentration is approximately 55 During repeated administration, the steady state is reached after 24 to 36 hours and remains very stable throughout treatment.
Distribution: The apparent distribution volume is 4.8 l/kg, which suggests good tissue diffusion. Protein binding is low: in vitro measurements give a value of 16%.
Elimination: Trimetazidine is eliminated primarily in the urine, mainly in the unchanged form. The mean elimination half-life is 6 hours.
Linearity: Trimetazidine pharmacokinetics is linear following single dose administration up to 100 mg. Repeated doses showed a time-linear pharmacokinetic response.
Elderly: Trimetazidine exposure may be increased in elderly patients due to an age-related decrease in renal function. A pharmacokinetics study performed specifically in elderly (75-84 years) and very elderly (≥85 years) participants showed that in the event of moderate renal impairment (creatinine clearance between 30 and 60 ml/min) trimetazidine exposure was increased by a factor of 1.0 and 1.3, respectively in comparison with younger participants (30-65 years) with moderate renal impairment. No safety concerns were observed in the elderly subjects as compared with the general population.
Renal impairment: On average, trimetazidine exposure is multiplied by 1.7 in patients with moderate renal impairment (creatinine clearance between 30 and 60 ml/min) and by 3.1 in patients with severe renal impairment (creatinine clearance below 30 ml/min) compared with healthy young volunteers with normal renal function. No safety concerns were observed in this population as compared with the general population.
Pediatric population: The pharmacokinetics of trimetazidine have not been studied in the pediatric population (<18 years).
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