Deprenorm MV prolonged-release tablets p / o 35mg, No. 30

Ischemic heart disease: prevention of attacks of stable angina pectoris (as part of combination therapy);

chorioretinal disorders with an ischemic component;

vestibulocochlear disorders of an ischemic nature, such as dizziness, tinnitus, hearing impairment

Inside, during meals.
DeprenormЃ MB is taken 1 tablet 35 mg 2 times a day (morning and evening).

The course of treatment is according to the doctor's recommendation.

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

active substance :

trimetazidine dihydrochloride 35 mg;

Excipients:

calcium hydrogen phosphate dihydrate - 34.6 mg;

hyprolose (hydroxypropyl cellulose) - 6 mg;

hypromellose (hydroxypropyl methylcellulose) - 64 mg;

copovidone - 4.2 mg;

colloidal silicon dioxide (aerosil) - 6.4 mg;

magnesium stearate - 0.8 mg;

microcrystalline cellulose - 59 mg

film sheath:

Selecoat AQ-01673 (hypromellose (hydroxypropyl methylcellulose) - 2.8 mg,

macrogol - 400 (polyethylene glycol - 400) - 0.7 mg,

macrogol - 6000 (polyethylene glycol - 6000) - 0.7 mg,

aluminum varnish based on crimson dye (Ponso 4R) (E124) - 0.7 mg,

titanium dioxide - 2.1 mg) - 7 mg

• hypersensitivity to any component of the drug;

• severe renal failure (CC less than 30 ml / min);

• Parkinson's disease, Parkinson's symptoms, tremors, restless legs syndrome and other associated movement disorders.

• pregnancy;

• breastfeeding period;

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

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

Trade name of the drug : DeprenormЃ MB

International Non-Proprietary Name (INN) : Trimetazidine

Dosage form : prolonged-release film-coated tablets

Ingredients :

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

active substance :

trimetazidine dihydrochloride 35 mg;

Excipients:

calcium hydrogen phosphate dihydrate - 34.6 mg;

hyprolose (hydroxypropyl cellulose) - 6 mg;

hypromellose (hydroxypropyl methylcellulose) - 64 mg;

copovidone - 4.2 mg;

colloidal silicon dioxide (aerosil) - 6.4 mg;

magnesium stearate - 0.8 mg;

microcrystalline cellulose - 59 mg

film sheath:

Selecoat AQ-01673 (hypromellose (hydroxypropyl methylcellulose) - 2.8 mg,

macrogol - 400 (polyethylene glycol - 400) - 0.7 mg,

macrogol - 6000 (polyethylene glycol - 6000) - 0.7 mg,

aluminum varnish based on crimson dye (Ponso 4R) (E124) - 0.7 mg,

titanium dioxide - 2.1 mg) - 7 mg

Description:
Tablets are round, biconciform, film-coated pink. The cross section is almost white.

Pharmacotherapeutic group:

antihypoxic agent.

Pharmacological properties
Pharmacodynamics:
Has 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 maintenance of cellular homeostasis. Trimetazidine inhibits fatty acid oxidation by selectively inhibiting the enzyme 3-ketoacyl-CoA thiolase (3-CAT) of the mitochondrial long-chain fatty acid isoform, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation, which is responsible for 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 neurosensory tissues during ischemia;

• reduces the severity of intracellular acidosis and changes in the transmembrane ion flow 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 pectoris, trimetazidine:

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

• limits the fluctuations in blood pressure caused by exercise, without significant changes in heart rate;

• reduces the frequency of angina attacks and the need to take short-acting nitroglycerin;

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

Pharmacokinetics

After oral administration, trimetazidine is absorbed from the gastrointestinal tract and reaches its maximum plasma concentration after 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. 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 blood plasma proteins is quite low, about 16% in vitro).
Trimetazidine is excreted mainly by the kidneys, mainly unchanged.
Renal clearance of trimetazidine directly correlates with creatinine clearance (CC), hepatic clearance decreases with the age of the patient.

Indications for use:
Ischemic heart disease: prevention of attacks of stable angina pectoris (as part of combination therapy);

chorioretinal disorders with an ischemic component;

vestibulocochlear disorders of an ischemic nature, such as dizziness, tinnitus, hearing impairment.

Contraindications:

• hypersensitivity to any component of the drug;

• severe renal failure (CC less than 30 ml / min);

• Parkinson's disease, Parkinson's symptoms, tremors, restless legs syndrome and other associated movement disorders.

• pregnancy;

• breastfeeding period;

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

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

Application during pregnancy and lactation: There are no
data on the use of DeprenormЃ MB in pregnant women. Animal studies have shown no direct or indirect reproductive toxicity. Reproductive toxicity studies have shown no 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.
There are no data on the excretion of trimetazidine or its metabolites into breast milk. The risk to the newborn / child cannot be excluded. You should not use the drug DeprenormЃ MB during breastfeeding.

Method of administration and dosage:
Inside, with meals.
DeprenormЃ MB is taken 1 tablet 35 mg 2 times a day (morning and evening).

The course of treatment is according to the doctor's recommendation.

Side effect:
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, including individual messages);
unspecified frequency (frequency cannot be estimated from available data).

From the side of the central nervous system
Often: dizziness, headache.
Unspecified frequency: symptoms of parkinsonism (tremor, akinesia, increased tone), unsteadiness in the Romberg position and 'unsteady' gait, 'restless' legs syndrome, other associated movement disorders, usually reversible after discontinuation of therapy. Sleep disturbances (insomnia, drowsiness).
From the side of the cardiovascular system
Rarely: orthostatic hypotension, 'hot flushes' of blood to the skin of the face, palpitations, extrasystole, tachycardia, marked decrease in blood pressure.
From the circulatory and lymphatic system of
Unspecified frequency: agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
From the digestive system
Often: abdominal pain, diarrhea, dyspepsia, nausea, vomiting.
Unspecified frequency: constipation.
Liver and biliary tract
disorders Unspecified frequency: hepatitis.
On the part of the skin
Often: skin rash, itching, urticaria.
Unspecified frequency: acute generalized exanthematous pustulosis, Quincke's edema.
General disorders
Often: asthenia.

Overdose:
There is only limited information on trimetazidine overdose. In case of overdose, symptomatic therapy should be carried out.

Interaction with other medicinal products:
There are no data on interaction with other medicinal products.

Special instructions:
DeprenormЃ MB is not intended for the relief of angina attacks, for the initial course of therapy for unstable angina pectoris or myocardial infarction, as well as in preparation for hospitalization or in its first days.
If an attack of angina pectoris develops, treatment (drug therapy or revascularization) should be reviewed and adapted.
The drug can cause or worsen the symptoms of parkinsonism (tremor, akinesia, increased tone), therefore, patients should be regularly monitored, especially the elderly.
If movement disorders such as parkinsonism symptoms, restless legs syndrome, tremors, instability in the Romberg position and unsteadiness of gait appear, the drug DeprenormЃ MB should be finally 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, a neurologist should be consulted.
There may be cases of falls associated with instability in the Romberg position and 'unsteadiness' of gait or arterial hypotension, especially in patients taking antihypertensive drugs (see section 'Side effects').

Influence on the ability to drive vehicles and perform work requiring a high speed of psychomotor reactions:
Due to the possible development of dizziness and other side effects when using the drug DeprenormЃ MB, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and the speed of psychomotor reactions.

Release form:
Tablets of prolonged action, film-coated, 35 mg.

Storage conditions:
In a dry, dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Expiration date:
2 years.
Do not use after the expiration date.

Vacation conditions:
By prescription.