Trimetazidine

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Available since: 2019-09-19

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Clinical Pharmacology

Pharmacodynamics

It has an antihypoxic effect. Trimetazidine prevents the decrease in 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 transfer of potassium and sodium ions and the preservation of cellular homeostasis. Trimetazidine inhibits fatty acid oxidation by selectively inhibiting the enzyme 3-ketoacyl-CoA thiolase (3-CAT) mitochondrial long-chain fatty acid isoform, which leads to increased glucose oxidation and accelerated glycolysis with glucose oxidation, which causes myocardial protection against 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 energy metabolism of the heart and neurosensory tissues during ischemia;
reduces the severity of intracellular acidosis and changes in transmembrane ion flow arising from ischemia;
reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused cardiac tissues;
reduces the size of myocardial damage;
It has no direct effect 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 exercise, without significant changes in heart rate;
reduces the frequency of strokes and the need for short-acting nitroglycerin;
improves the contractile function of the left ventricle in patients with ischemic dysfunction.

Pharmacokinetics

After ingestion, trimetazidine is absorbed from the gastrointestinal tract and reaches a maximum plasma concentration in about 5 hours. Over 24 hours, plasma concentration remains at a level in excess of 75% of the concentration determined after 11 hours. The equilibrium state is reached after 60 hours. Eating does not affect the bioavailability of trimetazidine.

The volume of distribution 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 correlates directly with creatinine clearance (CK), hepatic clearance decreases with the patient's age.

Indications

- Ischemic heart disease: prevention of angina attacks (in combination therapy);

Composition

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

Active ingredient: Trimetazidine dihydrochloride 35 mg.

Excipients: calcium hydrophosphate dihydrate, microcrystalline cellulose, colloidal silicon dioxide (aerosil), hydroxypropyl cellulose Klucel LF, hydroxypropylmethyl cellulose, plasdone S-630, magnesium stearate.

The composition of the film shell: Selyout (hydroxypropylmethylcellulose, plasdone S-630, polyethylene glycol, talc, ferric oxide red, titanium dioxide).

Trimetazidine is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Trimetazidine MB			pills
Preductal OD	Pharmstandard	Russia	capsules
Trimetazidine	Teva	Israel	pills
Deprenorm MB	Canonpharma	Russia	pills
Antisten	Ozon	Russia	pills
Rimecor MW	Nizhpharm	Russia	pills
Trimetazidine-Teva	Teva	Israel	pills
Trimetazidine	Canonpharma	Russia	pills
Predizin	Gedeon Richter	Hungary	pills
Trimectal MV	Vertex	Russia	pills
Angiozil retard	Replepharm	Macedonia	pills
Rimecor	Nizhpharm	Russia	pills
Preductal MR	Servier	Russia	pills

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Dosage and Administration

Inside, while eating.

Depren® MB take 1 tablet of 70 mg 1 time per day (in the morning). The course of treatment is recommended by the doctor.

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, including individual messages);
unspecified frequency (frequency cannot be calculated from 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 legs syndrome, other related motor disorders, usually reversible after cessation of therapy. Sleep disturbances (insomnia, drowsiness).

Since the cardiovascular system: rarely - orthostatic hypotension, "flush" of blood to the skin of the face, feeling of heartbeat, extrasystole, tachycardia, marked reduction in blood pressure.

On the part of the circulatory and lymphatic systems: unspecified frequency - agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

On the part of the digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting. Unspecified frequency - constipation.

On the part of the liver and biliary tract: unspecified frequency - hepatitis.

For the part of the skin: often - skin rash, itching, hives. Unspecified frequency - acute generalized exantmatous pustus, angioedema.

General disorders: often - asthenia.

With care: patients with severe liver failure (clinical data are limited); patients with impaired renal function (creatinine clearance more than 30 ml / min.); patients over 75 years old.

Drug interactions

There are no data on the interaction with other drugs.

Pregnancy and Lactation

Data on the use of the drug Deprenorm® MV in pregnant women are missing. 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 the newborn / child cannot be excluded. Do not use the drug Deprenorm® MV during breastfeeding.

Special instructions

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

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

The drug can cause or worsen parkinsonism symptoms (tremor, akinesia, increased tone), therefore, patients should be regularly monitored, especially the elderly. When motor disorders such as parkinsonism symptoms, restless legs syndrome, tremor, instability in the Romberg position and shakiness of the gait occur, deprenorm® MV should be permanently reversed.

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 "shaky" gait or hypotension may be noted, especially in patients taking antihypertensive drugs (see the section "Side Effects").

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

In connection with the possible development of dizziness and other side effects when using the drug Deprenorm® MB, caution should be exercised when driving vehicles and practicing other potentially dangerous activities that require increased concentration and psychomotor speed.