Instruction for use: Trimetazidine

International Nonproprietary Name (INN): Trimetazidine

Pharmaceutic group: Antihypoxic

Presentation:

Film-coated tablets 20 mg ¹30, ¹60

Available with prescription

Indications for Trimetazidine

Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through inhibition of fatty acid metabolism, also known as fatty acid oxidation inhibitor.

By preserving the energy metabolism in cells exposed to hypoxia or ischemia, trimetazidine prevents a decrease in intracellular adenosine triphosphate levels, thereby ensuring the proper functioning of ionic pumps and transmembranous sodium-potassium flow whilst maintaining cellular homeostasis. It also inhibits oxidation of fatty acid in blood vessels.

Controlled studies in angina patients have shown that trimetazidine increases coronary flow reserve, thereby delaying the onset of ischemia associated with exercise, limits rapid swings in blood pressure without any significant variations in heart rate, significantly decreases the frequency of angina attacks, and leads to a significant decrease in the use of nitrates.

It improves left ventricular function in diabetic patients with coronary heart disease. Recently, it has been shown to be effective in patients with heart failure of different etiologies (5-6).

Trimetazidine is described as the first cytoprotective anti-ischemic agent developed and marketed by Les Laboratoires Servier (France). It acts by directly counteracting all the major metabolic disorders occurring within the ischemic cell. The actions of trimetazidine include limitation of intracellular acidosis, correction of disturbances of transmembrane ion exchanges, and prevention of excessive production of free radicals.

Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus and dizziness. It is taken twice a day.

Trimetazidine has high safety and tolerability profile. It has no known drug interactions.

Trade name of the drug – Trimetazidine

Dosage Form: tablets

Active substance:

trimetazidine dihydrochloride - 20 mg;

Excipients: lactose monohydrate - 81.00 mg Povidone - 3.00 mg Crospovidone - 3.00 mg magnesium stearate - 1.00 g of polyvinyl alcohol - 1.80 mg macrogol (polyethylene glycol) - 0.90 mg talc - 0.70 mg titanium dioxide - 0.20 mg carmine dye [Ponceau 4R] - 0,18 mg dye sunset yellow - 0.01 mg aluminum lake - 0.71 mg.

Description:

Tablets biconvex shape, covered with a foil coated red.

Pharmacotherapeutic group: Antihypoxic

ATX code: C01EB15

Pharmacological Properties of Trimetazidine

Pharmacodynamics

Trimetazidine has anti-hypoxic action.

Directly affecting cardiomyocytes and neurons in the brain, improves their metabolism and function. Cytoprotective effect is due to an increase in energy potential, activation of oxidative decarboxylation and rationalization of consumption of oxygen (aerobic glycolysis and strengthen the blockade of fatty acid oxidation).

It supports myocardial contractility, prevents a decrease in intracellular adenosine triphosphate and phosphocreatine. The conditions of acidosis normalizes the functioning of membrane ion channels, prevents the accumulation of calcium and sodium in cardiomyocytes, normalizes intracellular concentration of potassium ions.

Reduces intracellular acidosis and elevated phosphate levels caused by myocardial ischemia and reperfusion. It prevents the damaging action of free radicals, preserves the integrity of cellular membranes, prevents activation of neutrophils in the ischemic area, increases the electric potential decreases the yield of the cells and creatine severity of ischemic myocardial injury.

When reducing the frequency of attacks of angina (nitrates reduced consumption), after 2 weeks of treatment, increases exercise capacity, reduced blood pressure drops. Improves hearing and vestibular trial results in patients with pathology of upper respiratory tract, reduces dizziness and tinnitus. In vascular pathology eyes restores functional activity of the retina eyes.

Pharmacokinetics

Upon receiving the trimetazidine is rapidly and almost completely absorbed in the gastrointestinal tract. Bioavailability - 90%. The time to reach maximum plasma concentration - 2 h. The maximum concentration after a single dose of 20 mg of trimetazidine about 55 ng / ml. Relationship to plasma proteins - 16%. Easily penetrates the blood-tissue barriers. The half-life is 4.5-5 hours excreted by the kidneys (60% - unchanged).

Indications for Trimetazidine

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

Chorioretinal vascular disorders;

Vertigo of vascular origin;

vestibular disorders ischemic nature (tinnitus, hearing impairment).

Contraindications for Trimetazidine

Hypersensitivity to any component of the drug; renal impairment (creatinine clearance less than 15 mL / min); expressed human liver; pregnancy; lactation; age of 18 years (effectiveness and safety have been established). Due to the presence of lactose preparation, it is contraindicated in congenital lactose intolerance, lactase deficiency if, when glucose-galactose malabsorption.

Trimetazidine Dosage and Administration

Inside, during a meal.

The recommended dosing regime - 1 tablet (20 mg), 2-3 times a day (40-60 mg per day).

The course of treatment recommended by the doctor.

Side effect ofTrimetazidine

Allergic reactions (itchy skin). Rare: headache, feeling of palpitations; from the gastrointestinal tract - weak dyspeptic symptoms (nausea, vomiting, gastralgia).

overdose

No cases of overdose.

Interaction

No information.

special instructions for Trimetazidine

Do not use for the relief of angina attacks!

Against the background of treatment in patients with coronary heart disease is a significant decrease in daily requirement of nitrates.

Use of the drug has no effect on the ability to drive a car and perform activities that require a high rate of psychomotor reactions.

Release form of Trimetazidine

Tablets, coated on a foil wrapper 20 mg.

10 tablets in blisters. 1, 2, 3, 4, 5 or 6, the contour of cellular packaging together with instructions for use are placed in a pile of cardboard.

100 tablets in a jar polymer, each jar along with instructions for use are placed in a pile of cardboard.

Storage conditions of Trimetazidine

In a dry, dark place at a temperature no higher than 25 ° C.

Keep out of the reach of children.

Shelf life of Trimetazidine

3 years.

Do not use beyond the expiration date printed on the package.

Conditions of supply of Trimetazidine from pharmacies

With prescription.