Description
Latin name
Deprenorm MV
Release form
Long-acting film-coated tablets.
Packaging
In a blister pack of 15 tablets. In a cardboard box 2 blisters.
Pharmacological action
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 transfer of potassium and sodium ions and preservation 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 determines the protection of the myocardium from ischemia. Switching energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine.
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 resulting from ischemia
reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused heart tissue
has no direct effect on hemodynamic parameters.
In patients with angina pectoris, trimetazidine:
increases 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 for short-acting nitroglycerin
improves left ventricular contractility in patients with ischemic dysfunction.
Pharmacokinetics
After oral administration, trimetazidine is absorbed from the gastrointestinal tract and reaches its maximum plasma concentration after about 5 hours. Over 24 hours, the plasma concentration 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.
Distribution volume is 4.8 l / kg, which indicates a good distribution of trimetazidine in the tissues (the degree of binding to blood plasma proteins is quite low, about 16% in vitro). Trimetazidine is excreted mainly by the kidneys, mainly in unchanged form. Renal clearance of trimetazidine directly correlates with creatinine clearance (CC), hepatic clearance decreases with the age of the patient.
Indications
Coronary heart disease:
prevention of attacks of stable angina (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 either sex. The drug is contraindicated during pregnancy due to the lack of clinical data on the safety of its use.
There is no data on the release of trimetazidine or its metabolites into breast milk. The risk to the newborn / child cannot be excluded. Do not use Deprenorm ® MV while breastfeeding.
Composition
1 film-coated sustained-release tablet contains:
Active ingredient:
trimetazidine dihydrochloride 70 mg.
Excipients:
hypromellose (hydroxypropyl methylcellulose) 171 mg
carbomer 2 mg silicon dioxide colloidal 6 mg
magnesium stearate 3 mg
hydrogenated vegetable oil 3 mg
microcrystalline cellulose 195 mg.
Film composition:
Opadray II pink 15 mg, including:
polyvinyl alcohol 6 mg,
polyethylene glycol (macrogol) 3.03 mg,
talc 2.22 mg,
titanium dioxide 2.8395 mg,
solar dye sunset yellow 0.381 mg,
dye indigo carmine 0.2175 mg,
dye crimson [Ponceau 4R] 0.312 mg.
Dosage and Administration
Inside, with meals.
Deprenorm ® MB take 1 tablet of 70 mg once a day (in the morning). The course of treatment is recommended by a doctor.
Side effects of
The frequency of side effects noted with 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 1/100)
rarely (more than 1/10000, less than 1/1000)
very rare (less than 1/10000, including individual messages)
of unspecified frequency (the frequency cannot be calculated from 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 the unsteadiness of the gait, restless legs syndrome, other motor disorders associated with them, usually reversible after discontinuation of therapy. Sleep disorders (insomnia, drowsiness).
From the cardiovascular system: rarely – orthostatic hypotension, flushing of blood to the skin of the face, palpitations, extrasystole, tachycardia, marked decrease in blood pressure.
From the circulatory and lymphatic systems: unspecified frequency – agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
From the digestive system: often – abdominal pain, diarrhea, dyspepsia, nausea, vomiting. Unspecified frequency – constipation.
From the liver and biliary tract: unspecified frequency – hepatitis.
From the skin: often – skin rash, itching, urticaria. Unspecified frequency – acute generalized exanthematous pustulosis, Quincke’s edema.
General disorders: often – asthenia.
No drug interaction
There are no data on interaction with other drugs.
Overdose
There is only limited information on the overdose of trimethazidine. In case of overdose, symptomatic therapy should be performed.
Storage conditions
Store in a dry, dark place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Expiration
2 years.
Active substance
Trimetazidine
pharmacy leave sdflfp16 prescription p16rod16 p17products p17prp16 p17product p17pdrp16 vocational
Dosage form
Dosage form
tablets prolong.
Canonfarma, Russia
