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

Excipients: hypromellose (hydroxypropylmethylcellulose) 171 mg; Carbomer 2 mg; silicon dioxide colloidal 6 mg; magnesium stearate 3 mg; vegetable vegetable hydrogenated 3 mg; cellulose microcrystalline 195 mg

composition of film shell: Pink Opadry II 15 mg, including: polyvinyl alcohol 6mg, polyethylene glycol (macrogol) 3.03 mg talc 2.22 mg, 2.8395 mg of titanium dioxide, dye sunset yellow 0.381 mg, 0.2175 mg of dye indigo carmine , colourant dye [Ponso 4R] 0.312 mg.

Description:

Tablets are round, biconvex, covered with a film coat of pink color. The cross section is almost white.

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:

Has antihypoxic effect. Trimetazidine prevents the reduction of intracellular concentration of adenosine triphosphate (ATP) by maintaining the energy metabolism of cells in the 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 oxidation of fatty acids due to selective inhibition of the enzyme 3-ketoacyl-CoA thiolase (3-KAT) mitochondrial isoform long chain fatty acids, which leads to increased oxidation of glucose and acceleration of glycolysis to glucose oxidation, which is responsible for protecting the myocardium from ischemia.Switching energy metabolism from the oxidation of fatty acids to glucose oxidation underlies the pharmacological properties of trimetazidine.

It is experimentally confirmed that trimetazidine has the following properties:

- maintains the energy metabolism of the heart and neurosensory tissues during ischemia;

- reduces the intensity of intracellular acidosis and changes in the transmembrane ion flow that occur with ischemia;

- reduces the level of migration and infiltration of polynucleated neutrophils in ischemic and reperfused heart tissues;

- reduces the size of myocardial damage;

- does not directly affect the parameters of hemodynamics.

In patients with angina pectoris, trimetazidine:

- increases the coronary reserve, thereby slowing the onset of ischemia caused by physical exertion, starting from the 15th day of therapy;

- limits blood pressure fluctuations caused by physical exertion, without significant changes in heart rate;

- reduces the incidence of angina attacks and the need for short-acting nitroglycerin;

- improves the contractile function of the left ventricle in patients with ischemic dysfunction.

Pharmacokinetics:

After oral administration trimetazidine is absorbed from the gastrointestinal tract and reaches a maximum concentration in the blood plasma after about 5 hours. 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 trimetazidine.

The volume of distribution is 4.8 l / kg, which indicates a good distribution of trimetazidine in 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), the hepatic clearance decreases with the age of the patient.

Indications:

Ischemic heart disease: prevention of attacks of stable angina pectoris (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 parkinsonism, tremor, restless leg syndrome and other associated motor disorders.

- pregnancy;

- the period of breastfeeding;

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

Carefully:

Patients with severe hepatic impairment (clinical data are limited); patients with impaired renal function (creatinine clearance more than 30 ml / min.); patients older than 75 years.

Pregnancy and lactation:Data on the use of the drug Deprenorm® CF in pregnant women is absent. Studies in animals have not revealed the presence of direct or indirect reproductive toxicity. Studies of reproductive toxicity have shown no effect of trimetazidine on reproductive function in rats of both sexes. A drug contraindicated in pregnancy due to lack of clinical data on the safety of its use.

Data on the release of trimetazidine or its metabolites in breast milk are not available. The risk to a newborn / child can not be ruled out. Do not use the drug Deprenorm® MB during breastfeeding.

Dosing and Administration:

Inside, with food.

Deprenorm® MB take 1 tablet 70 mg once a day (in the morning). The course of treatment is recommended by a doctor.

Side effects:

The frequency of side effects noted with the administration of trimetazidine is given in the following grades:

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 (frequency can not be calculated from available data).

From the central nervous system

Often: dizziness, headache.

Unspecified frequency: symptoms of parkinsonism (tremor, akinesia, tone increase), instability in Romberg's posture and gait unsteadiness, restless leg syndrome, other associated motor disorders, usually reversible after cessation of therapy. Sleep disturbances (insomnia, drowsiness).

From the side of the cardiovascular system

Rarely: Orthostatic hypotension, "tides" of blood to the skin of the face, sensation heart beat, extrasystole, tachycardia, marked decrease in blood pressure.

From the side of the blood and lymphatic system

Unspecified frequency: agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

From the digestive system

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

Unspecified frequency: constipation.

From the liver and biliary tract

Unspecified frequency: hepatitis.

From the skin

Often: skin rash, itching, hives.

Unspecified frequency: acute generalized exanthematous pustulosis, angioedema.

Common violations

Often: asthenia.

Overdose:

There is only limited information on the overdose of trimetazidine. In case of an overdose, symptomatic therapy should be given.

Interaction:

There are no data on interactions with other drugs.

Special instructions:

Deprenorm® MV is not intended for arresting 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 case of an angina attack, treatment should be reviewed and adapted (drug therapy or revascularization).

The drug can cause or worsen symptoms of parkinsonism (tremor, akinesia, tone increase), therefore, regular monitoring of patients, especially the elderly, should be carried out.

When motor disorders such as Parkinsonism symptoms, restless legs syndrome, tremor, Romberg pose instability and gait unsteadiness occur, Deprenorm® MF should be discontinued.

Such cases are rare and symptoms usually go away after discontinuation of therapy, in most patients within 4 months after drug withdrawal. If the 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 the "shakiness" of the gait or arterial hypotension, especially in patients taking antihypertensive drugs (see the "Side effect" section).

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

In connection with the possible development of dizziness and other side effects with the use of the drug Deprenorm® CF, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of prolonged action, film-coated, 70 mg.

Packaging:

By 7, 10, 14 or 15 tablets in a contour cell pack of film

polyvinylchloride and aluminum foil printed lacquered.

According to 2, 4 contour cell packs of 7 tablets or 1, 3, 6 contour cell packs of 10 tablets or 1,2,4 contour cell packs of 14 tablets or 1, 2, 4 contour cell packs of 15 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002091

Date of registration:04.06.2013

Expiration Date:04.06.2018

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Information update date: & nbsp24.03.2017

Illustrated instructions

Instructions

Deprenorm® MB (Deprenorm MV)