Trimetazidine MB sustained release pills 35mg, 60pcs

Composition

1 tablet of prolonged action, film-coated, contains:

Active ingredient:

trimetazidine dihydrochloride 35 mg.

Auxiliary substances:

calcium hydrophosphate dihydrate,

microcrystalline cellulose,

colloidal silicon dioxide (aerosil),

hydroxypropylcellulose Klucel LF,

hydroxypropylmethylcellulose,

plasdon S-630,

magnesium stearate.

Composition of the film shell:

Selekout (hydroxypropylmethylcellulose, plasdon S-630, polyethylene glycol, talc, iron oxide red, titanium dioxide).

Pharmacological action

Pharmacodynamics

It has an antihypoxic effect. Trimetazidine prevents a decrease in the intracellular concentration of adenosine triphosphate (ATP) by maintaining the energy metabolism of cells in a state of hypoxia.

Thus, the drug ensures the normal functioning of membrane ion channels, transmembrane transport of potassium and sodium ions, and the preservation of cellular homeostasis. Trimetazidine inhibits the oxidation of fatty acids by selectively inhibiting the enzyme 3-ketoacyl-CoA-thiolase (3-CAT) of the mitochondrial long-chain isoform of fatty acids, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation, which determines the protection of the myocardium from ischemia.

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

It has been experimentally confirmed that trimetazidine has the following properties: :

• supports the energy metabolism of the heart and sensorineural tissues during ischemia;
• reduces the severity of intracellular acidosis and changes in the transmembrane ion flux that occur during ischemia;
• reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused heart tissues;
• reduces the size of myocardial damage;
• does not directly affect hemodynamic parameters.

In patients with angina trimetazidine:

• increases coronary reserve, thereby slowing the onset of ischemia caused by physical activity, starting from the 15th day of therapy;
• limit fluctuations in blood pressure, caused by physical activity, without significant changes in heart rate;
• reduces the frequency of angina attacks and the need for nitroglycerin short action;
• improves contractile function of the left ventricle in patients with coronary dysfunction.

Pharmacokinetics

After oral use, trimetazidine is absorbed from the gastrointestinal tract and reaches its maximum plasma concentration after approximately 5 hours. For more than 24 hours, the concentration in the blood plasma remains at a level exceeding 75% of the 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 a 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 in unchanged form. Renal clearance of trimetazidine is directly correlated with creatinine clearance (CC), and hepatic clearance decreases with age.

Indications

-Coronary heart disease: prevention of angina attacks (in complex therapy);- Chorioretinal vascular disorders;- Cochlea-vestibular disorders of an ischemic nature (tinnitus, hearing impairment, dizziness).

Contraindications

-Hypersensitivity to any component of the drug;- Renal insufficiency (creatinine clearance less than 15 ml / min); – Severe liver function disorders;- Pregnancy;- Breast-feeding period;- Age up to 18 years (efficacy and safety have not been established);- Patients with lactase deficiency, galacgozemia or glucose-galactose malabsorption syndrome.

Side effects

Rarely – nausea, vomiting, possible allergic reactions.

How to take, course of use and dosage

Trimetazidine MV is prescribed 1 tablet 2 times a day with meals in the morning and evening. The duration of therapy is set individually.

Overdose

Currently, no cases of overdose of the drug have been reported.

Special instructions

It is not used to stop angina attacks and is not indicated for the initial course of treatment for unstable angina or myocardial infarction, as well as in preparation for hospitalization or in the first days of it. If an angina attack develops, treatment should be reviewed and adapted (drug therapy or revascularization). Influence on the ability to drive vehicles and mechanisms: The use of the drug does not affect the ability to drive a car and perform work that requires a high speed of mental and physical reactions.

Form of production

Long-acting, film-coated tablets.

Storage conditions

Keep out of the reach of children in a dark place at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Trimetazidine

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets