Deprenorm MB Prolonged pills 35mg, 30pcs

Composition

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

Active ingredient:

Trimetazidine dihydrochloride 35 mg.

Auxiliary substances:

Calcium hydrophosphate dihydrate;

Microcrystalline cellulose;

Colloidal silicon dioxide (aerosil);

Hydroxypropyl Cellulose Klucel LF;

Hydroxypropylmethylcellulose, plasdon S-630;

Magnesium stearate.

Composition of the film shell:

Selekout (hydroxypropylmethylcellulose, plasdon S-630, polyethylene glycol, talc, iron oxide red, titanium dioxide).

Pharmacological action

Pharmacodynamics

It has an 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 preservation of cellular homeostasis. Trimetazidine inhibits the oxidation of fatty acids by selectively inhibiting the enzyme 3-ketoacyl-CoA-thiolase (3-CAT) of the mitochondrial long-chain isoform of fatty acids, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation, which determines 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 sensorineural tissues during ischemia;
• reduces the severity of intracellular acidosis and changes in the transmembrane ion flux 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 trimetazidine:

• increases coronary reserve, thereby slowing the onset of ischemia caused by physical activity, starting from the 15th day of therapy;
• limit fluctuations in blood pressure, caused by physical activity, without significant changes in heart rate;
• reduces the frequency of angina attacks and the need for nitroglycerin short action;
• improves contractile function of the left ventricle in patients with coronary dysfunction.

Pharmacokinetics

After oral use, trimetazidine is absorbed from the gastrointestinal tract and reaches its maximum plasma concentration after approximately 5 hours. For more than 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 plasma proteins is quite low, about 16% in vitro). Trimetazidine is mainly excreted by the kidneys, mainly in unchanged form. Renal clearance of trimetazidine is directly correlated with creatinine clearance (CC), and hepatic clearance decreases with age.

Indications

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

Use during pregnancy and lactation

There are no data on the use of Deprenorm MV in pregnant women. Animal studies have not revealed the presence of direct or indirect reproductive toxicity. Reproductive toxicity studies have not shown the effect of trimetazidine on reproductive function in rats of both sexes. The drug is contraindicated during 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 in breast milk. The risk to the newborn/child cannot be excluded. Do not use Deprenorm MB during breastfeeding.

Contraindications

• Hypersensitivity to any of the components of the drug;
• Severe renal insufficiency (creatinine clearance less than 30 ml / min);
• Parkinson’s disease, symptoms of Parkinsonism, tremors, restless legs syndrome, and other related motor disorders.
• Pregnancy;
• Breast-feeding period;
• Age up to 18 years (efficacy and safety have not been established).

With caution:

• Patients with severe hepatic insufficiency (clinical data are limited);

• Patients with impaired renal function (creatinine clearance greater than 30 ml / min);

• Patients over 75 years of age.

Side effects

the Frequency of side effects noted in the admission of Trimetazidine in the following gradation: very often (>1/10); often (>1/100, <1/10); infrequently (>1/1000, <1/100); rare (>1/10 000, <1/1000); very rare (<1/10 000, including individual messages); unspecified frequency (frequency cannot be estimated according to the available data).

From 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 legs syndrome, and other associated motor disorders, usually reversible after discontinuation of therapy. Sleep disorders (insomnia, drowsiness).

From the cardiovascular system: rarely-orthostatic hypotension, “flushes” of blood to the skin of the face, palpitation, extrasystole, tachycardia, marked decrease in blood pressure.

From the circulatory and lymphatic system: 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.

From the side of the skin: often – skin rash, pruritus, urticaria. Unspecified frequency – acute generalized exanthematous pustulosis, angioedema.

General violations: often-asthenia.

Interaction

There are no data on interactions with other drugs.

How to take, course of use and dosage

Inside, while eating.

Deprenorm MB is taken 1 tablet of 70 mg once a day (in the morning).

The course of treatment is based on the doctor’s recommendation.

Overdose

There is only limited information about trimetazidine overdose.

In case of overdose, symptomatic therapy should be performed.

Special instructions

Deprenorm ® MB is not intended for the management of angina attacks, for the initial course of treatment for unstable angina or myocardial infarction, or in preparation for hospitalization or in the first days of it.

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

The drug may cause or worsen the symptoms of parkinsonism (tremor, akinesia, increased tone), so patients, especially the elderly, should be regularly monitored. If motor disorders such as Parkinsonism symptoms, restless legs syndrome, tremor, instability in the Romberg position, and unsteadiness of gait occur, Deprenorm MB should be permanently discontinued.

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

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Due to the possible development of dizziness and other side effects when using Deprenorm MB, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Long-acting, film-coated tablets.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf

life is 3 years.

Active ingredient

Trimetazidine

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Purpose

For adults as directed by your doctor

Indications

Angina