Trimetazidine MB - instructions for use, dose, side effects, contraindications

Excipients: kollidone SR [80% polyvinyl acetate, 19% povidone, 0.8% sodium lauryl sulfate, silica, 0.2%] - 99 mg Microcrystalline cellulose - 61.8 mg Hypromellose (Methocel K 100 M) - 22 mg colloidal silicon dioxide ( aerosil) -1.1 mg, magnesium stearate 1.1 mg.

Shell accessories: fall off II Pink [polyvinylalcohol - 2.6400 mg of titanium dioxide - 1.6124 mg macrogol - 1.3332 mg talc - 0.9768 mg carmine red dye - 0,0250 mg Yellow iron oxide - 0.0099 mg iron oxide black - 0.0027 mg] - 6.6 mg.

Description:

Round, biconvex tablets, covered with a pink film membrane.

On the cross-section, two layers are visible: the core is white or almost white and the shell is pink.

Roughness of the surface of tablets is allowed.

Pharmacotherapeutic group:antihypoxic agent

ATX: & nbsp

C.01.E.B Other drugs for the treatment of heart disease

C.01.E.B.15 Trimetazidine

Pharmacodynamics:

Trimetazidine has an antihypoxic effect.

Trimetazidine prevents a decrease in intracellular adenosine triphosphate (ATP) by maintaining the energy metabolism of the cells in a state of hypoxia. Directly affecting the cardiomyocytes and neurons of the brain, it optimizes their metabolism and function.

The cytoprotective effect is due to an increase in the energy potential, activation of oxidative decarboxylation, and rationalization of oxygen consumption (enhancement of aerobic glycolysis and fat oxidation blockade). Supports contractility of the myocardium, prevents the decrease in intracellular content of ATP and phosphocreatinine. Under conditions of acidosis, it normalizes the functioning of membrane ion channels, prevents the accumulation of calcium and sodium ions in cardiomyocytes, normalizes the intracellular concentration of potassium ions.

Reduces intracellular acidosis and phosphate content, caused by myocardial ischemia and reperfusion.

It prevents the damaging action of free radicals, preserves the integrity of cellular membranes, prevents activation of neutrophils in the ischemic area, increases the electric potential decreases the yield of creatine from the cells and the severity of ischemic myocardial injury.

When angina pectoris reduces the frequency of attacks (reduces the consumption of nitrates), after 2 weeks of treatment, tolerance to physical activity increases, blood pressure drops decrease.

Pharmacokinetics:

After ingestion trimetazidine quickly absorbed and reaches a maximum concentration in the blood plasma after about 5 hours. Bioavailability is 90%.

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. Eating does not affect the bioavailability of the drug.

The volume of the distribution is 4.8 l / kg, which indicates a good distribution of trimetazidine in tissues (a relationship with blood plasma proteins is about 16%).

Trimetazidine is excreted from the body mainly by the kidneys in an unchanged form (about 60%). Half-life in young healthy volunteers is about 7 hours, in patients older than 75 years - about 12 hours.

Renal clearance of trimetazidine directly correlates with creatinine clearance (CC), the hepatic clearance decreases with the age of the patient.

It is shown that in elderly patients when taken in a dose - 1 tablet 2 times a day, an increase in the exposure in the blood plasma does not lead to any more pronounced effects compared to placebo.

Indications:ANDShemical heart disease: prevention of attacks of stable angina (in monotherapy and as part of combination therapy).

Contraindications:

- Hypersensitivity to any of the components of the drug;

- severe renal failure (creatinine clearance less than 30 ml / min);

- Parkinson's disease, extrapyramidal disorders, Parkinsonism symptoms, restless leg syndrome and other associated motor disorders;

- pregnancy;

- the period of breastfeeding;

- age to 18 years (efficacy and safety not established).

Carefully:

- Severe hepatic insufficiency (clinical data are limited);

- moderate renal failure (creatinine clearance 30-60 ml / min);

- elderly people with moderate renal insufficiency;

- age over 75 years.

Pregnancy and lactation:

There are no data on the use of trimetazidine in pregnant women. Studies in animals have not revealed the presence of direct or indirect reproductive toxicity. The study of reproductive toxicity did not show the effect of trimetazidine on the reproductive function of rats of both sexes. As a precautionary measure, it is not recommended to use Trimetazidine MB during pregnancy.

The use of Trimetazidine MV in the period of breastfeeding, due to the lack of data on the penetration of trimetazidine into breast milk,it is contraindicated. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Tablets take whole, not liquid, squeezed with water.

The duration of treatment is determined by the doctor.

The drug is taken orally, while eating 1 tablet 2 times a day (morning and evening). The maximum daily dose is 70 mg.

Patients with impaired renal function

In patients with moderate renal impairment (creatinine clearance 30-60 ml / min), the recommended dose is 35 mg (1 tablet) in the morning during breakfast.

Elderly patients

In elderly patients, there may be an increased exposure of trimetazidine due to age-related decline in kidney function. In patients with moderate renal impairment (creatinine clearance 30-60 ml / min), the recommended dose is 35 mg (1 tablet) in the morning during breakfast.

Side effects:

The frequency of side effects noted with the administration of trimetazidine is given in the following gradation according to the classification of the World Health Organization: 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; frequency is unknown - can not be calculated based on available data.

From the digestive system

Often: abdominal pain, diarrhea, indigestion, nausea, vomiting.

Common violations

Often: asthenia.

From the central nervous system

Often: dizziness, headache.

Very rarely: extrapyramidal symptoms (tremor, rigidity, akinesia), reversible after drug withdrawal.

The frequency is unknown: symptoms of parkinsonism (tremor, increase in tone), instability in Romberg's posture and the "unsteadiness" of the gait, restless legs syndrome, and other related motor disorders of sleep (insomnia, drowsiness).

From the liver and biliary tract

Frequency unknown: hepatitis.

From the skin

Often: skin rash, itching, hives.

The frequency is unknown: acute generalized exanthematous pustulosis, angioedema.

From the side of the cardiovascular system

Rarely: sensation of palpitations, extrasystole, tachycardia, marked decrease in blood pressure, orthostatic hypotension,which can be accompanied by general weakness, dizziness or loss of balance, especially with the simultaneous use of antihypertensive drugs, "tides" of blood to the skin of the face.

On the part of the blood and lymphatic system

The frequency is unknown: agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

Overdose:

Currently, information on cases of drug overdose is limited. If necessary, conduct symptomatic therapy.

Interaction:

Drug interaction is not currently described.

In clinical studies of trimetazidine, it has been shown that it promotes an increase in anti-ischemic activity of antianginal agents.

Special instructions:

It should be borne in mind that Trimetazidine MV is not intended for relief of angina attacks and is not indicated for the initial course of therapy for unstable angina or myocardial infarction.

Do not use Trimetazidine MV in preparation for hospitalization or in its first days.

In the case of an attack of angina pectoris, the treatment should be reviewed and adapted.

Trimetazidin MB can cause or worsen symptoms of parkinsonism (tremor, akinesia, tone increase),therefore, regular monitoring of patients, especially of the elderly, should be carried out. In doubtful cases, patients should be referred to a neurologist for an appropriate examination. When motor disorders such as Parkinsonism symptoms, restless legs syndrome, tremor, Romberg pose instability and gait unsteadiness occur, Trimetazidine MB should be finally abolished. Such cases are rare, and the symptoms usually go away after the abolition of therapy: in most patients - within 4 months after discontinuation of the drug. If the symptoms of parksinsonism persist for more than 4 months after drug withdrawal, you should consult a neurologist. There may be falls associated with instability in the Romberg position and the "shakiness" of the gait or a marked decrease in blood pressure, especially in patients taking antihypertensive drugs.

Patients with severe hepatic insufficiency (clinical data are limited), with moderate renal insufficiency (creatinine clearance 30-60 ml / min), elderly people with moderate renal insufficiency and over 75 years of age, take with caution.

If you skip one or more doses of the drug, you can not take a higher dose to the next dose!

Effect on the ability to drive transp. cf. and fur:

Trimetazidine MB does not significantly affect the ability to drive vehicles, mechanisms and perform work that requires an increased speed of physical and mental reactions.

In connection with the possible development of dizziness and other side effects, care should be taken when controlling vehicles, mechanisms and performing work that requires a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets with modified release, film-coated, 35 mg.

Packaging:

For 15 tablets in a contour mesh package.

2, 4 contoured cell packs together with instructions for use are placed in a pack of cardboard.

Storage conditions:

Store in a dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003456

Date of registration:16.02.2016

Expiration Date:16.02.2021

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Representation: & nbspTATHIMFARM PREPARATIONS OJSC TATHIMFARM PREPARATIONS OJSC Russia

Information update date: & nbsp31.07.2016

Illustrated instructions

Instructions

Trimetazidine MB (Trimetazidine MR)