Description
Release form
Long-acting film-coated tablets.
Packaging
In a blister pack of 15 tablets. In a cardboard box 4 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.
It is experimentally confirmed that trimetazidine has the following properties: it supports the energy metabolism of the heart and neurosensory tissues during ischemia the extent of
myocardial damage does not directly affect hemodynamic performance.
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 stable angina attacks (as part of combination therapy).
Contraindications
Hypersensitivity to any of the components of the
drug severe renal failure (CC less than 30 ml / min)
Parkinson’s disease, symptoms of Parkinson’s disease, tremor, restless legs syndrome and other related motor disorders.
pregnancy
breastfeeding period
age 18 years (efficacy and safety not established).
Precautions: patients with severe hepatic insufficiency (clinical data are limited) patients with impaired renal function (creatinine clearance greater than 30 ml / min.) patients older than 75 years.
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.
Special instructions
Deprenorm ® MB is not intended for the relief of angina attacks, for the initial course of therapy for unstable angina or myocardial infarction, as well as in preparation for hospitalization or in its first days.
In the event of an attack of angina pectoris, treatment (drug therapy or revascularization) should be reviewed and adapted.
The drug may cause or worsen symptoms of parkinsonism (tremor, akinesia, increased tone), therefore, regular monitoring of patients, especially the elderly, should be carried out. If motor disturbances appear, such as symptoms of parkinsonism, restless legs syndrome, tremors, instability in the Romberg position and gait shakiness, the drug Deprenorm ® MV should be completely 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 symptoms of parkinsonism persist for more than 4 months after discontinuation of the drug, consult a neurologist. Cases of falling may be noted, associated with instability in the Romberg position and the ² Ñunsteadiness ² Ñ of the gait or arterial hypotension, especially in patients taking antihypertensive drugs (see the section ² ÑSide effects ² Ñ).
Effect 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 requiring increased concentration attention and speed of psychomotor reactions.
Composition
1 sustained-release film-coated tablet contains:
Active ingredient: trimetazidine dihydrochloride 35 mg.
Excipients: calcium hydrogen phosphate dihydrate, microcrystalline cellulose, colloidal silicon dioxide (aerosil), hydroxypropyl cellulose Klucel LF, hydroxypropyl methylcellulose, plasdon S-630, magnesium stearate.
Composition of the film coat: Selecote (hydroxypropyl methylcellulose, S-630 plasdon, polyethylene glycol, talc, iron oxide red, titanium dioxide).
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
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)
is 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, the syndrome of “restless” legs, 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, a feeling of palpitations, extrasystole, tachycardia, a 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.
Drug interaction
There is no data on the 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
Keep dry, protected from light at a temperature not exceeding 25 ° C.
Keep out of the reach of children
Shelf life
2 years
Deystvuyushtee substance
trimetazidine
Terms and conditions
prescription
Dosage form
prolong tablets.
Indications
Indications
Angina
Teva Pharmaceutical Enterprise Co., Ltd., Israel
