Vastarel 35 what is it for

Contact for assistance: Vastarel MR Tablet 35 mg quantity. Category: Trimetazidine Dihydrochloride. Description Reviews 0 Trimetazidine Dihydrochloride Indications. Long-term treatment of Ischaemic heart disease angina pectoris, sequelae of infarction. Trimetazidine is an anti-ischemic anti-anginal metabolic agent, which improves myocardial glucose utilization through inhibition of long-chain 3-ketoacyl CoA thiolase activity, which results in a reduction in fatty acid oxidation and a stimulation of glucose oxidation.

High fatty acid oxidation rates are detrimental during ischemia due to an inhibition of glucose oxidation leading to uncoupling of glycolysis and an increase in proton production, which has the potential to accelerate sodium and calcium overload in the heart.

This leads to an exacerbation of ischemic injury and decreased cardiac efficiency during reperfusion. One 20 mg tablet thrice daily after meals. No dosage adjustments are required in patients with impaired renal and hepatic function. Pharmacology: Pharmacodynamics: Mechanism of action: 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.

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-ischemic effects are achieved without concomitant haemodynamic effects. Clinical efficacy and safety: Clinical studies have demonstrated the efficacy and safety of trimetazidine in the treatment of patients with chronic angina, when the benefit from other antianginal medicinal products was insufficient.

In a patients randomized, double blind, placebo-controlled study Sellier , one 35 mg trimetazidine modified release tablet b. No significant difference between groups could be found for the other secondary endpoints total exercise duration, total workload and clinical endpoints. In the overall population, including both asymptomatic and symptomatic patients, trimetazidine failed to demonstrate a benefit on both ergometric total exercise duration, time to onset of 1mm ST and time to onset angina and clinical endpoints.

Pharmacokinetics: After oral administration, maximum concentration is found, on average, 5 hours after taking the tablet. Steady state is reached by the 60 th hour, at the latest.

The pharmacokinetic characteristics of Vastarel 35mg are not influenced by meals. The apparent distribution volume is 4. Trimetazidine is eliminated primarily in the urine, mainly in the unchanged form. The elimination half-life of Vastarel 35mg 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.

Special populations: Elderly subjects: A specific clinical study carried out in an elderly population using a dosage of 2 tablets per day taken in 2 doses, analysed by a population pharmacokinetics approach, showed an increase in plasma exposure. The elderly may have increased trimetazidine exposure due to age-related decrease in renal function. Renal impairment: Trimetazidine exposure is increased on average by 1.

No safety concerns were observed in this population as compared with the general population. Toxicology: Preclinical safety data: Chronic toxicity studies conducted by the oral route in dogs and rats, showed a good safety profile.

The genotoxic potential was assessed in in vitro studies, including evaluation of the mutagenic and clastogenic potential, and one in vivo study. All the tests were negative. Reproductive toxicity studies in mice, rabbits and rats showed no embryotoxicity or teratogenicity. Trimetazidine Dihydrochloride inhibits fatty acid pathway by inhibiting 3-keto acyl CoA thiolase enzyme and transfers oxygen to glucose pathway.

Since glucose pathway is more efficient in producing energy, the same oxygen produces more energy and makes the heart more active. Moreover, the aerobic oxidation of glucose stops production of lactic acid, which prevents angina pectoris. The recommended dose of Trimetazidine is 35 mg twice daily or 20 mg tablet thrice daily during meals.

The benefit of the treatment should be assessed after three months and Trimetazidine should be discontinued if there is no treatment response. No drug interaction so far has been reported. In particular, no interaction has been reported with beta-blockers, calcium antagonists, nitrates, heparin, hypolipidemic agents or digitalis preparation. Trimetazidine is contraindicated in patients who have hypersensitivity to the active substance or to any of the excipients.