Deprenorm mv pills 70mg №30

Pills: round, biconvex, film-coated pink.

In cross section: almost white.

Mechanism of action

pharmachologic effect - antihypoxic.

It has an antihypoxic effect. Trimetazidine prevents a decrease in the intracellular concentration of 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 transfer of potassium and sodium ions and the preservation of cellular homeostasis.Trimetazidine inhibits fatty acid oxidation by selectively inhibiting the 3-ketoacyl-CoA thiolase enzyme in the mitochondrial long-chain fatty acid isoform, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation and causes myocardial protection from ischemia. Switching energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine.

It was experimentally confirmed that trimetazidine has the following properties:

- supports the energy metabolism of the heart and neurosensory tissues during ischemia;

- reduces the severity of intracellular acidosis and changes in transmembrane ion flow arising during ischemia;

- reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused cardiac tissues;

- reduces the size of myocardial damage;

- does not have a direct impact on hemodynamic parameters.

In patients with angina pectoris, trimetazidine:

- increases coronary reserve, thereby slowing the onset of ischemia caused by exercise, starting from the 15th day of therapy;

- limits blood pressure fluctuations caused by physical activity, without significant changes in heart rate;

- reduces the frequency of strokes and the need for taking short-acting Nitroglycerin;

- improves the contractile function of the left ventricle in patients with ischemic dysfunction.

After ingestion, trimetazidine is absorbed from the gastrointestinal tract, T_max in the blood plasma - approximately 5 hours. Over 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. Eating does not affect the bioavailability of trimetazidine.

V_d is 4.8 l / kg, which indicates a good distribution of trimetazidine in the tissues (the degree of binding to plasma proteins is rather low, about 16% in vitro).

Trimetazidine is excreted mainly by the kidneys, mainly unchanged.

The kidney clearance of trimetazidine directly correlates with creatinine clearance, and hepatic clearance decreases with the patient's age.

Indications and usage

Coronary heart disease: prevention of attacks of stable angina (as part of combination therapy).

Contraindications

hypersensitivity to any of the components of the drug;

severe renal impairment (Cl creatinine less than 30 ml / min);

Parkinson's disease, symptoms of parkinsonism, tremor, restless legs syndrome and other related motor disorders;

pregnancy;

breastfeeding period;

age up to 18 years (efficacy and safety have not been established).

Carefully: severe hepatic impairment (clinical data are limited); impaired renal function (Cl creatinine more than 30 ml / min); patients over 75 years old.

Pregnancy and Breastfeeding

Data on the use of the drug Deprenorm^® MB in pregnant women are absent. Animal studies have not revealed direct or indirect reproductive toxicity. Reproductive toxicity studies did not show the effect of trimetazidine on reproductive function in rats of both sexes. The drug is contraindicated in pregnancy due to the lack of clinical data on the safety of its use.

Data on the allocation of trimetazidine or its metabolites in breast milk are not available. The risk for a newborn / child cannot be excluded. Do not use the drug Deprenorm^® MB while breastfeeding.

Adverse reactions

The frequency of side effects noted when taking trimetazidine is given 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; rarely more than 1/10000, less than 1/1000; very rarely - less than 1/10000, incl. individual messages; unspecified frequency - the frequency cannot be calculated from the available data.

From the side of the central nervous system: often - dizziness, headache; unspecified frequency - symptoms of parkinsonism (tremor, akinesia, increased tone), instability in the Romberg position and shaky gait, restless leg syndrome, and other motor disturbances associated with them, usually reversible after discontinuation of therapy. Sleep disturbances (insomnia, drowsiness).

From the CCC: rarely - orthostatic hypotension, flushing of the skin of the face, feeling of heartbeat, extrasystole, tachycardia, marked reduction in blood pressure.From the circulatory and lymphatic systems; unspecified frequency - agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

Gastrointestinal: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting; unspecified frequency - constipation.

Liver and biliary tract: unspecified frequency - hepatitis.

From the skin: often - skin rash, itching, urticaria; of unspecified frequency - acute generalized exantmatous pustus, angioedema.

General violations: often - asthenia.

Drug interactions

There are no data on the interaction with other drugs.

Dosage and administration

Inside while eating.

Deprenorm^® MB take 1 tab. 70 mg once a day (in the morning). The course of treatment is recommended by the doctor.

Overdosage

Only limited information is available on trimetazidine overdose. In case of overdose, symptomatic therapy should be carried out.

Deprenorm^® MB is not intended for the relief of strokes, the initial course of treatment of unstable angina or myocardial infarction, as well as in preparation for hospitalization or during its first days.

If an attack of angina occurs, the treatment (drug therapy or revascularization) should be reviewed and adapted.

The drug can cause or worsen the symptoms of parkinsonism (tremor, akinesia, increased tone), so you should regularly monitor patients, especially the elderly.

With the appearance of motor disorders such as parkinsonism symptoms, restless legs syndrome, tremor, instability in the Romberg position and unsteadiness of gait, the drug Deprenorm^® MB should be permanently canceled.

Such cases are rare and symptoms usually disappear after discontinuation of therapy in most patients within 4 months after discontinuation of the drug. If the symptoms of parkinsonism persist for more than 4 months after discontinuation of the drug, you should consult a neurologist.

Cases of falling associated with instability in the Romberg position and unsteady gait or arterial hypotension may be noted, especially in patients taking antihypertensive drugs (see “Side Effects”).

Influence on ability to drive vehicles and to perform the works demanding high speed of psychomotor reactions. In connection with the possible development of dizziness and other side effects when using the drug Deprenorm^® MB should be careful when driving and other potentially hazardous activities that require high concentration of attention and psychomotor reactions.

Tablets of the prolonged action, film coated, 70 mg. In a blister strip packaging of PVC film and aluminum printed lacquer foil in 7, 10, 14 or 15 pcs. 2, 4 blister packs of 7 pcs. or 1, 3, 6 blister packs of 10 pcs.or 1, 2, 4 blister packs of 14 each, or 1, 2, 4 blister packs of 15 each. in a pack of cardboard.

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