Trimetazidine MB, 35 mg 60 pcs

Pharmacodynamics

It has an antihypoxic effect. Trimetazidine prevents reduction of intracellular adenosine triphosphate (ATP) concentration by maintaining energy metabolism of cells under hypoxia.

In this way, the drug ensures normal functioning of membrane ion channels, transmembrane transport of potassium and sodium ions and preservation of cellular homeostasis. Trimetazidine inhibits fatty acid oxidation through selective inhibition of the enzyme 3-ketoacyl-CoA-thiolase (3-CAT) mitochondrial long-chain fatty acid isoform, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation, which leads to myocardial protection from ischemia.

The switch of energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine.

Trimetazidine has been experimentally confirmed to have the following properties:

• maintains energy metabolism of cardiac and neurosensory tissues during ischemia;
• reduces the severity of intracellular acidosis and changes in transmembrane ion flow that occur during ischemia;
• reduces the size of myocardial damage;
• does not directly affect hemodynamic parameters.

In patients with angina pectoris, trimetazidine:

• increases coronary reserve, thereby delaying the onset of exercise-induced ischemia from day 15 of therapy;
• limits exercise-induced blood pressure fluctuations without significant changes in heart rate;
• reduces the frequency of angina attacks and the need for short-acting nitroglycerin;
• improves left ventricular contractile function in patients with coronary dysfunction.

Pharmacokinetics

After oral administration, trimetazidine is absorbed from the gastrointestinal tract and reaches maximum plasma concentration after approximately 5 hours. Above 24 hours, plasma concentrations remain above the 75% concentration determined after 11 hours. The equilibrium state is reached after 60 hours. Food intake does not affect the bioavailability of trimetazidine.

The volume of distribution is 4.8 l/kg, which indicates good distribution of trimetazidine in tissues (the degree of binding to plasma proteins is quite low, about 16 % in vitro). Trimetazidine is mainly excreted by the kidneys, mainly unchanged. Renal clearance of trimetazidine directly correlates with creatinine clearance (CK), hepatic clearance decreases with patient age.

Indications

Active ingredient

Composition

1 long-acting film-coated tablet contains:

The active ingredient:

trimetazidine dihydrochloride 35 mg.

Associates:

calcium hydrophosphate dihydrate,

microcrystalline cellulose,

colloidal silicon dioxide (aerosil),

hydroxypropyl cellulose Clucel LF,

hydroxypropyl methylcellulose,

Plasdon S-630,

magnesium stearate.

The composition of the film coating:

Selecoat (hydroxypropyl methylcellulose, plasdon S-630, polyethylene glycol, talcum, iron oxide red, titanium dioxide).

How to take, the dosage

Special Instructions

Contraindications

Side effects

Overdose

Similarities