Trimetazidin

General characteristics. Structure:

Active agent: a trimetazidina dihydrochloride — 20 mg
excipients: hypro rod (hydroxypropyl cellulose) of 0,7 mg, starch of corn 16 mg, silicon dioxide colloid (aerosil) of 3,13 mg, lactoses monohydrate (sugar milk) 89,47 mg, magnesium stearate of 0,7 mg.
structure of a film cover: селекоат AQ–01673 — 6 mg: gipromelloz (gidroksipropilme-tiltsellyuloz) of 2,4 mg, macrogoal-400 (polyethyleneglycol-400) of 0,6 mg, macrogoal-6000 (polyethyleneglycol-6000) of 0,6 mg, dye crimson [Ponso 4 R] 0,6 mg, titanium dioxide of 1,8 mg.

Description:
Tablets are round biconvex, film coated, pink color; on cross section — white or almost white color.

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 content of intracellular adenosinetriphosphate and creatine phosphate. In the conditions of acidosis normalizes functioning of membrane ion channels, interferes with accumulation of calcium ions 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 stable stenocardia триметазидин reduces the frequency of attacks (consumption of nitrates decreases), in 2 weeks of treatment tolerance to an exercise stress increases, sharp fluctuations of arterial pressure decrease. Dizziness and a sonitus decreases. At vascular pathology of eyes improves functional activity of a retina of an eye.

Pharmacokinetics. After intake 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 makes about 55 ng/ml. Communication with proteins of plasma — 16%. Distribution volume — 4,8 l/kg. Easily passes through gistogematichesky barriers. The elimination half-life makes 4,5–5 h. It is removed by kidneys (about 60% — in not changed look).
The renal clearance of a trimetazidin directly correlates with the clearance of creatinine (CC), the hepatic clearance decreases with age.

Indications to use:

- coronary heart disease: prevention of attacks of stable stenocardia (as a part of a combination therapy);
- chorioretinal disturbances with an ischemic component;
- cochleovestibular disturbances of the ischemic nature, such as dizziness, 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/days). Therapy course duration — according to the recommendation of the doctor.

Features of use:

Drug is not intended for stopping of attacks of stenocardia, for an initial course of therapy of stable stenocardia or a myocardial infarction.
In case of development of an attack of stenocardia it is necessary to reconsider and adapt treatment.

It is necessary to be careful at control of vehicles and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of the side effects noted at reception of a trimetazidin is specified in the following gradation: very often (more than 1/10); often (more than 1/100, less than 1/10); infrequently (more than 1/1000, less than 1/100); seldom (more than 1/10000, less than 1/1000); very seldom (less than 1/10000), including, separate messages.
From the alimentary system:
Often: abdominal pain, diarrhea, dyspepsia, nausea, vomiting.
General disturbances:
Often: adynamy.
From the central nervous system:
Often: dizziness, headache.
Very seldom: extrapyramidal frustration (a tremor, rigidity, an akineziya), reversible after drug withdrawal.
From integuments:
Often: skin rash, itch, small tortoiseshell.
From cardiovascular system:
Seldom: orthostatic hypotension, "inflows" of blood to face skin.

Interaction with other medicines:

There are no data.

Contraindications:

Hypersensitivity to any component of drug; deficit of lactase; lactose intolerance; glyukozo-galaktozny malabsorption; heavy renal insufficiency (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).

Use during pregnancy and during breastfeeding: Administration of drug is contraindicated during pregnancy and during breastfeeding.

Overdose:

The overdoses given about cases are limited. In case of overdose it is necessary to carry out symptomatic therapy.

Storage conditions:

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

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 20 mg.
On 10 or 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished.
On 1, 2, 3, 6 blister strip packagings on 10 tablets or on 1, 2, 3, 4 blister strip packagings on 30 tablets together with the application instruction place in a pack from a cardboard.