Trimetazidin

General characteristics. Structure:

Active ingredient: 20 mg of a trimetazidin of dihydrochloride.

Excipients: lactoses monohydrate, povidone, кросповидон, magnesium stearate, polyvinyl alcohol, macrogoal (polyethyleneglycol), talc, titanium dioxide, dye crimson [Ponso 4R], dye sunset yellow, aluminum varnish.

The means improving oxygen absorption fabrics and increasing resistance to oxygen insufficiency. Drug normalizes energy balance of substances in the cells suffering from a hypoxia or affected with ischemia. Prevents decrease in the main source of energy in cells, keeps constancy of structure of the intracellular environment. At ischemia when the need of heart for oxygen is higher, than its receipt, increases resistance of cells of a myocardium to a lack of oxygen. The same effect is observed also at a lack of oxygen to a retina of eyes and their vessels (триметазидин recovers functional activity of a retina), at decrease in auditory acuity (recovers hearing).

Trimetazidin counteracts destructive influence of free radicals, protects cellular membranes from damages, reduces degree of manifestation of ischemic damages.

At the use of drug the frequency of attacks of stenocardia decreases, in two weeks of treatment the patient begins to transfer better exercise stresses, ceases to suffer from differences of arterial pressure. Trimetazidin reduces a sonitus and dizzinesses.

Trimetazidin gives fine opportunities for therapy of elderly patients which organism is more subject to side effects and an adverse effect of medicines, and also patients with a diabetes mellitus. Drug does not influence a hemodynamics, does not break the movement of blood, and in it too – one of its essential advantages.

Pharmacological properties:

Pharmacodynamics. Trimetazidin has anti-hypoxemic effect. Directly influencing cardiomyocytes and neurons of a brain, optimizes their metabolism and function. The cytoprotective effect is caused by increase in energy potential, activation of oxidizing decarboxylation and rationalization of consumption of oxygen (strengthening of aerobic glycolysis and blockade of oxidation of fatty acids).

Maintains contractility of a myocardium, prevents decrease in intracellular content of adenosinetriphosphate and phosphocreatinine. In the conditions of acidosis normalizes functioning of membrane ion channels, interferes with accumulation of calcium and sodium in cardiomyocytes, normalizes the intracellular maintenance of potassium ions.

Reduces the intracellular acidosis and the increased content of phosphates caused by ischemia of a myocardium and reperfusion. Interferes with the damaging action of free radicals, keeps integrity of cellular membranes, prevents activation of neutrophils in an ischemia zone, increases duration of electric potential, reduces a kreatinfosfokinaza exit from cells and expressiveness of ischemic injuries of a myocardium.

At stenocardia reduces the frequency of attacks (consumption of nitrates decreases), in 2 weeks of treatment tolerance to an exercise stress increases, differences of arterial pressure decrease. Improves hearing and results of vestibular tests at patients with pathology of ENT organs, reduces dizziness and a sonitus. At vascular pathology of eyes recovers functional activity of a retina of an eye.

Pharmacokinetics. After reception триметазидин it is quickly and almost completely absorbed in digestive tract. Bioavailability – 90%. Time of achievement of the maximum concentration in a blood plasma – 2 hours. The maximum concentration after a single dose of 20 mg of a trimetazidin about 55 ng/ml. Communication with proteins of plasma – 16%. Easily gets through gistogematichesky barriers. The elimination half-life makes 4,5-5 h. It is removed by kidneys (about 60% – in not changed look).

Indications to use:

Coronary heart disease, prevention of attacks of stenocardia (in complex therapy);

Chorioretinal vascular disorders;

Dizzinesses of a vascular origin;

Cochleovestibular disturbances of the ischemic nature (sonitus, hearing disorder).

Route of administration and doses:

Inside, during food. The recommended dosing mode – 1 tablet (20 mg) 2-3 times a day (40-60 mg a day). A course of treatment according to the recommendation of the doctor

Features of use:

Not to apply to stopping of attacks of stenocardia!

Against the background of treatment by drug patients to coronary heart disease have an essential reduction of daily need for nitrates.

Use of drug does not influence ability to driving and performance of work, the psychomotor reactions demanding high speed.

Side effects:

Allergic reactions (skin itch). Seldom: headache, feeling of strong heartbeat; from digestive tract – the weak dispepsichesky phenomena (nausea, vomiting, a gastralgia).

Interaction with other medicines:

There are no data.

Contraindications:

Hypersensitivity to any component of drug; a renal failure (the clearance of creatinine is lower than 15 ml/min.); the expressed abnormal liver functions; pregnancy; lactation period; age up to 18 years (efficiency and safety are not established). Due to the existence in composition of drug of lactose, it is contraindicated at an inborn lactose intolerance, at insufficiency of lactase, at glyukozo-galaktozny malabsorption.

Overdose:

Now about cases of overdose of drug it was not reported.

Storage conditions:

In the dry place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 20 mg.

On 10 tablets in a blister strip packaging. 1, 2, 3, 4 or 5 blister strip packagings together with the application instruction place in a pack from a cardboard.

On 100 tablets in bank polymeric, each can together with the application instruction is placed in a pack from a cardboard.