Medicinal reference book geotar. Antisten: what is it used for and what contraindications does it have? For impaired renal function

In this article you can read the instructions for use of the drug Antisten. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Antisten in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Antisten in the presence of existing structural analogues. Use for the treatment of coronary heart disease and other vascular disorders in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

Antisten- a drug that normalizes the energy metabolism of cells exposed to hypoxia or ischemia. Prevents a decrease in intracellular ATP content, ensures the normal functioning of membrane ion channels, transmembrane transport of potassium and sodium ions and the preservation of cellular homeostasis.

Trimetazidine (the active ingredient of the drug Antisten) slows down the oxidation of fatty acids due to the selective inhibition of long-chain 3-ketoacetyl-CoA thiolase, which leads to increased glucose oxidation and restoration of the coupling between glycolysis and oxidative decarboxylation and has been shown to protect the myocardium from ischemia. The switch from fatty acid oxidation to glucose oxidation underlies the antianginal effect of trimetazidine.

Experimental studies on animals have shown that Antisten supports the energy metabolism of the heart and neurosensory organs during periods of ischemic episodes; reduces the amount of intracellular acidosis and the degree of changes in the transmembrane ion flow that occurs during ischemia; reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfusion tissues of the heart, reduces the size of myocardial damage; however, it does not affect hemodynamics.

Compound

Trimetazidine dihydrochloride + excipients.

Pharmacokinetics

Antisten is quickly and almost completely absorbed by the intestinal mucosa. Bioavailability is 90%. Plasma protein binding is 16%. It is excreted by the kidneys (about 60% unchanged).

Indications

IHD: prevention of angina attacks (in complex therapy);
cochleovestibular disorders of ischemic nature, such as dizziness, tinnitus, hearing impairment;
chorioretinal vascular disorders.

Release forms

Film-coated tablets 20 mg.

Extended-release, film-coated tablets MB 35 mg.

Instructions for use and dosage regimen

Taken orally at a dose of 40-60 mg per day, dosage frequency 2-3 times a day. The duration of therapy is determined individually, depending on the clinical situation.

MB extended-release tablets

Inside, during meals.

Antisten MV is prescribed 1 tablet 2 times a day (morning and evening). The course of treatment is determined by the doctor individually.

Side effect

allergic reactions (including skin rash, itching);
extrapyramidal disorders (tremor, rigidity, akinesia);
dizziness;
headache;
asthenia;
nausea, vomiting;
diarrhea;
dyspepsia;
gastralgia.

Contraindications

pregnancy;
lactation period (breastfeeding);
age under 18 years (efficacy and safety have not been established);
renal failure (creatinine clearance less than 15 ml/min);
hypersensitivity to trimetazidine.

Use during pregnancy and breastfeeding

Animal studies have not revealed a teratogenic effect, however, due to the lack of clinical data on the safety of the drug during pregnancy, the risk of fetal malformations cannot be excluded. The use of Antisten during pregnancy is contraindicated.

It is not known whether Antisten is excreted in breast milk. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Use in children

Contraindicated in children and adolescents under 18 years of age (efficacy and safety have not been established).

special instructions

Do not use to relieve angina attacks!

The drug is not indicated for the initial course of therapy unstable angina or myocardial infarction.

If an attack of angina occurs, treatment should be reviewed and adapted.

If you miss one or more doses of the drug, you should not take a higher dose at the next dose.

Impact on the ability to drive vehicles and operate machinery

The drug Antisten does not have a significant effect on the ability to drive vehicles and perform other work requiring high speed psychomotor reactions.

Drug interactions

There is no information about drug interactions between the drug.

Analogues of the drug Antisten

Structural analogues of the active substance:

Angiosil retard;
Antisten MV;
Deprenorm MV;
Carditrim;
Metaguard;
Predisin;
Preductal;
Preductal MV;
Precard;
Rimecore;
Rimecor MV;
Triducard;
Trimectal;
Trimectal MV;
Trimet;
Trimetazide;
Trimetazidine;
Trimetazidine MB;
Trimetazidine dihydrochloride;
Trimitard MV.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.

Dosage form: extended-release film-coated tablets Compound:

For 1 tablet:

Active substance: trimetazidine dihydrochloride - 35 mg;

Excipients (core): hypromellose - 93.0 mg, microcrystalline cellulose - 178.9 mg, colloidal silicon dioxide - 1.55 mg, magnesium stearate - 1.55 mg.

Excipients (shell): Opadry II 85F240012 Pink: polyvinyl alcohol - 4.0 mg, macrogol 3350 - 2.438 mg, red iron oxide dye - 0.04 mg, yellow iron oxide dye - 0.022 mg, talc - 1.48 mg, titanium dioxide - 2.02 mg.

Description:

Tablets are biconvex, film-coated, creamy pink in color. On a cross section, two layers are visible, the inner layer (core) is white or white with a yellowish tint.

Pharmacotherapeutic group:Antihypoxic agent ATX:

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

C.01.E.B.15 Trimetazidine

Pharmacodynamics:

Has an antihypoxic effect.

By directly influencing cardiomyocytes and neurons of the brain, the drug optimizes their metabolism and function. The cytoprotective effect is due to an increase in energy potential, activation of oxidative decarboxylation and rationalization of oxygen consumption (increased glycolysis and blockade of fatty acid oxidation).

Trimetazidine maintains myocardial contractility and prevents a decrease in the intracellular content of adenosine triphosphoric acid (ATP) and phosphocreatinine. In conditions of acidosis, it normalizes the functioning of membrane ion channels, prevents the accumulation of calcium and sodium ions in cardiomyocytes, and normalizes the intracellular content of potassium ions.

Reduces intracellular acidosis and increased phosphate levels caused by myocardial ischemia and reperfusion. Prevents the damaging effects of free radicals, preserves the integrity of cell membranes, prevents activation of neutrophils in the ischemic zone, increases the duration of the electrical potential, reduces the release of creatine phosphokinase (CPK) from cells and the severity of ischemic myocardial damage Trimetazidine reduces the frequency of angina attacks, reduces the need for nitrates, after 2 weeks of use it increases exercise tolerance, and sharp fluctuations are reduced blood pressure(HELL). Reduces dizziness and tinnitus of ischemic etiology. In case of vascular pathology of the eye, it restores the functional activity of the retina.

Pharmacokinetics:

After taking the drug orally, it is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability - 90%. The time to reach maximum concentration in blood plasma is 3-5 hours. A stable state is achieved after 60 hours. The volume of distribution is 4.8 l/kg. Communication with blood plasma proteins - 16%. is excreted from the body mainly by the kidneys (about 60% unchanged). The half-life is about 7 hours, in patients over 65 years of age - about 12 hours. The renal clearance of trimetazidine directly correlates with creatinine clearance (CC), hepatic clearance decreases with age. Easily penetrates histohematic barriers.

Indications:

Coronary heart disease: prevention of angina attacks (in complex therapy).

Cochleovestibular disorders of ischemic nature, such as dizziness, tinnitus, hearing impairment.

Chorioretinal vascular disorders.

Contraindications:

-Hypersensitivity to any component of the drug;

Renal failure (creatinine clearance less than 15 ml/min);

Severe liver dysfunction;

Age up to 18 years (efficacy and safety have not been established).

Pregnancy and lactation:

Animal studies have not revealed teratogenicity effect, however, due to Due to the lack of clinical data on the safety of the drug during pregnancy, the risk of fetal malformations cannot be excluded. The use of the drug during pregnancy is contraindicated.

It is not known whether ANTISTEN MV is excreted in breast milk. If it is necessary to use the drug ANTISTEN MB during lactation, the issue of stopping breastfeeding should be decided.

Directions for use and dosage:

Inside, during meals.

Antisten MV is prescribed 1 tablet 2 times a day (morning and evening).

Side effects:

Frequency very often - more than 1/10; often - more than 1/100 and less than 1/10; infrequently - more than 1/1000 and less than 1/100; rarely - more than 1/10000 and less than 1/1000; very rarely - less than 1/10000, including individual messages.

From the outside digestive system : often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting.

From the outside of cardio-vascular system : rarely - orthostatic hypotension, "hot flashes" to the facial skin.

From the central nervous system: often - dizziness, headache; very rarely - extrapyramidal disorders (tremor, rigidity, akinesia), reversible after discontinuation of the drug.

From the skin and subcutaneous fat: often - skin rash, itching, urticaria.

Others: often - asthenia.

Overdose:

Currently, no cases of drug overdose have been reported.

Interaction:

No information available.

Special instructions:

Do not use to relieve angina attacks!

The drug is not indicated for the initial course of treatment of unstable angina or myocardial infarction.

If an attack of angina occurs, treatment should be reviewed and adapted. If you miss one or more doses of the drug, you cannot take a higher dose at the next dose!

Impact on the ability to drive vehicles. Wed and fur.:

The drug ANTISTEN MV does not have a significant effect on the ability to drive vehicles and perform other work that requires a high speed of psychomotor reactions.

Release form/dosage:Extended-release film-coated tablets 35 mg. Package:

10, 20, 30 tablets are placed in a contour cell packaging made of polyvinyl chloride film and printed varnished aluminum foil.

10, 20, 30, 40, 50, 60 or 100 tablets per placed in a polymer container for medicines. One container or 1, 2, 3, 4, 5, 6 or 10 blister packs along with instructions for use are placed in a cardboard pack.

The page contains instructions for use Antistena. It is available in various dosage forms drug (tablets 20 mg, prolonged action MV 35 mg), and also has a number of analogues. This abstract has been verified by experts. Leave your feedback on the use of Antisten, which will help other site visitors. The drug is used for various diseases(coronary heart disease or ischemic heart disease, Meniere's disease, tinnitus and other vascular disorders). The product has a number side effects and features of interaction with other substances. Doses of the drug differ for adults and children. There are restrictions on the use of the medicine during pregnancy and breastfeeding. Treatment with Antisten can only be prescribed by a qualified doctor. The duration of therapy may vary and depends on the specific disease. Composition and interaction of the drug with alcohol.

Instructions for use and dosage regimen

Taken orally at a dose of 40-60 mg per day, dosage frequency 2-3 times a day. The duration of therapy is determined individually, depending on the clinical situation.

MB extended-release tablets

Inside, during meals.

Antisten MV is prescribed 1 tablet 2 times a day (morning and evening). The course of treatment is determined by the doctor individually.

Compound

Trimetazidine dihydrochloride + excipients.

Release forms

Film-coated tablets 20 mg.

Extended-release, film-coated tablets MB 35 mg.

Pharmacokinetics

Antisten is quickly and almost completely absorbed by the intestinal mucosa. Bioavailability is 90%. Plasma protein binding is 16%. It is excreted by the kidneys (about 60% unchanged).

Indications

IHD: prevention of angina attacks (in complex therapy);
cochleovestibular disorders of ischemic nature, such as dizziness, tinnitus, hearing impairment;
chorioretinal vascular disorders.

Contraindications

pregnancy;
lactation period (breastfeeding);
age under 18 years (efficacy and safety have not been established);
renal failure (creatinine clearance less than 15 ml/min);
hypersensitivity to trimetazidine.

special instructions

Do not use to relieve angina attacks!

The drug is not indicated for the initial course of treatment of unstable angina or myocardial infarction.

If an attack of angina occurs, treatment should be reviewed and adapted.

If you miss one or more doses of the drug, you should not take a higher dose at the next dose.

Impact on the ability to drive vehicles and operate machinery

The drug Antisten does not have a significant effect on the ability to drive vehicles and perform other work that requires a high speed of psychomotor reactions.

Side effect

allergic reactions (including skin rash, itching);
extrapyramidal disorders (tremor, rigidity, akinesia);
dizziness;
headache;
asthenia;
nausea, vomiting;
diarrhea;
dyspepsia;
gastralgia.

Drug interactions

There is no information about drug interactions between the drug.

Analogues of the drug Antisten

Structural analogues of the active substance:

Angiosil retard;
Antisten MV;
Deprenorm MV;
Carditrim;
Metaguard;
Predisin;
Preductal;
Preductal MV;
Precard;
Rimecore;
Rimecor MV;
Triducard;
Trimectal;
Trimectal MV;
Trimet;
Trimetazide;
Trimetazidine;
Trimetazidine MB;
Trimetazidine dihydrochloride;
Trimitard MV.

Use in children

Contraindicated in children and adolescents under 18 years of age (efficacy and safety have not been established).

Use during pregnancy and breastfeeding

It is not known whether Antisten is excreted in breast milk. If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

Availability cardiovascular diseases requires periodic or continuous treatment.

For coronary heart disease and some other pathologies, medications that have a short-term effect on the body may be ineffective.

In such cases, patients are prescribed drugs that can accumulate in the body and have a prolonged effect. These drugs include Antisten MV, a prescription drug for the treatment of cardiovascular diseases.

It is contraindicated to use the medicine without consulting a doctor.

pharmachologic effect

Antisten MV is classified as an antihypoxic agent. medicines, designed to improve indicators of metabolic changes in the myocardium and the function of neurosensory (sensorineural) organs in coronary heart disease.

The drug has pronounced antianginal, cytoprotective and antihypoxic effects. Its antianginal effect is to eliminate the symptoms of myocardial ischemia in persons with diagnosed coronary disease hearts.

This effect is achieved due to the ability of trimetazidine to reduce the level of preload on the heart muscle, dilate collateral vessels, block calcium channels and adrenergic receptors, activate potassium channels, improve blood supply to the subendocardial parts of the heart muscle and epicardial coronary vessels.

The result of all this is:

decreased venous blood flow to the heart muscle;
reduction of pain;
decreased oxygen demand of cardiac muscle cells;
decrease in pressure in pulmonary artery and atrium;
decrease in peripheral vascular resistance indicators.

The antihypoxic effect of trimetazidine is manifested in the ability to improve the body's utilization of oxygen, increase resistance to hypoxia, and reduce the oxygen needs of various tissues and organs.

As for the cytoprotective properties, they are due to the ability to correct ionic balance, maintain energy potential, and increase the protective capabilities of the mucous membranes.

Trimetazidine is capable of:

influence the cells that are the main muscle of the heart, as well as the neurons of the brain, improve their functional activity and metabolism;
maintain cardiac muscle contractility within the physiological norm;
prevent a decrease in phosphocreatinine, a substance that improves metabolism muscle tissue and myocardium;
prevent a decrease in the intracellular content of adenosine triphosphate.

In people with pathological conditions, in which the acid-base balance shifts towards increased acidity, trimetazidine:

prevents the accumulation of sodium and calcium in cardiomyocytes – the cells that form the heart muscle;
normalizes the functioning of IR (ion channels) of cell membranes;
normalizes intracellular potassium content.

Also, the active component of the drug contributes to:

reduction of symptoms of intracellular acidosis, reduction of phosphate levels resulting from ischemic heart disease;
maintaining the integrity of cell membranes;
preventing damage to cellular structures and cells by free radicals;
increasing the duration of the electrical potential;
reducing the frequency of angina attacks;
preventing the activation of neutrophil granulocytes in the ischemic area;
reducing the severity of damage to the heart muscle caused by ischemic heart disease;
reducing the body's need for nitrates;
eliminating sudden surges in blood pressure or reducing the frequency of their occurrence;
preventing the release of creatine phosphokinase from cells;
normalization of hearing;
increasing the body's resistance to physical loads ( this effect develops two weeks after the start of therapy);
improving the performance of vestibular tests in people with diseases of the ENT organs;
restoration of normal retinal function in vascular eye diseases;
reducing the severity of symptoms of coronary artery disease, such as tinnitus and dizziness.

Indications for use of Antisten MV

Appointment is possible if:

IHD (composed of complex treatment for the prevention of angina attacks);
choreoretinal vascular disorders;
cochleovestibular disorders of ischemic nature, such as hearing impairment, tinnitus, dizziness.

Mode of application

You need to take Antisten MV twice a day, 1 tablet - during breakfast and dinner. Taking more than 2 tablets per day is prohibited, because 70 mg is the maximum dosage. The duration of therapy is determined by the doctor.

Treatment of elderly people over the age of 75 years is carried out according to a similar scheme. However, such patients should take precautions and be observed by a doctor throughout the entire therapy.

Persons with diagnosed renal failure You should take no more than 1 tablet per day with your first meal.

If one or more doses of the drug are missed, you cannot take multiple doses at the next dose.

Composition, release form

One tablet consists of trimetazidine dihydrochloride (35 mg) and additional components such as microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide, hypromellose.

The film coating covering the tablet consists of macrogol 3350, talc, polyvinyl alcohol, dyes (iron oxide red, opadry, iron oxide yellow), titanium dioxide.

Antisten MV are packages, each of which contains 60 modified-release tablets. They are covered with a creamy film shell with a pink tint.

Inside the tablets there is a white or slightly yellowish core. The tablets have a round, biconvex shape.

Interaction with other drugs

There is no data on how trimetazidine interacts with other medications. To reduce the risk of developing a drug conflict, Antisten MV should be taken two or three hours after taking other medications.

Side effects

The following describes undesirable reactions that can develop when using Antisten MB:

Digestive system	often – abdominal pain, dyspepsia, vomiting, diarrhea, nausea.
Central nervous system	often – headaches, dizziness; extremely rarely - extrapyramidal disorders (tremor, akinesia, rigidity), reversible after stopping the medication.
Heart, blood vessels	rarely – flushing of the face, orthostatic hypotension.
Dermatological reactions	often - itchy skin, urticaria, various types of rashes.
Others	often - asthenia.

Patients who have previously experienced allergies to medications are recommended to test for the likelihood of developing allergic reactions before starting therapy.

To do this, the tablet is broken into 8 parts and 1 of them is placed under the tongue. If 20-30 minutes after dissolving the tablet no adverse reactions are observed (swelling of the mucous membranes, itching and redness of the skin), Antisten MV can be used in a course according to the regimen prescribed by the doctor.

Overdose

There have been no reports of overdose with the active component of the drug.

Contraindications

It is prohibited to use in treatment:

people with individual intolerance to the active or auxiliary components of Antisten MV;
pregnant patients;
persons with Parkinson's disease and a tendency to movement disorders;
children and adolescents under 18 years of age;
patients with frequent tremor, " restless legs»;
nursing women;
people with severe renal failure.

Prescribing the drug to elderly people and patients with elevated creatinine levels is possible, but some caution must be observed.

During pregnancy

Theoretically, the drug can be prescribed to pregnant women, because Animal experiments have demonstrated the absence of teratogenic effects of trimetazidine on the developing fetus. But in practice, the medicine is not prescribed during pregnancy due to the lack of experience in using Antisten MB in such categories of patients (it is not possible to exclude the occurrence of any pathologies in the fetus).

There is also no information about the excretion of trimetazidine in mother's milk. Therefore, the use of Antisten MV during lactation is prohibited.

Conditions, shelf life

To store Antisten MV, it is better to select dark places with a temperature within 10-25 degrees. The use of the medicine is possible within two years from the date of release.

It is prohibited to use a drug that has expired, because this is fraught with a decrease in the expected effectiveness and the development of undesirable reactions from various body systems.

Price

One package of Antisten MV in Russia costs about 400-500 rubles.

A drug called Antisten MV in Ukrainian pharmacies absent.

Analogues

If Antisten MV is not suitable for the patient for some reason, it can be replaced with another drug with a similar effect, for example,

Antisten is an antihypoxic medicinal product, which is intended for the treatment of diseases of the cardiovascular system. Available in the form of film-coated tablets with prolonged action.

Pharmacological action of Antisten

In accordance with the instructions for Antisten, the active ingredient of the drug is trimetazidine dihydrochloride. Excipients are magnesium stearate, colloidal silicon dioxide, microcrystalline cellulose, hypromellose. The film shell contains titanium dioxide, macrogol, polyvinyl alcohol and dyes.

When used, Antisten has an antihypoxic effect, which is due to the effect on neurons and cardiomyocytes of the brain, as a result of which their metabolism improves and functions are normalized.

The cytoprotective effect of the tablets is to increase energy potential, activate oxidative decarboxylation, enhance glycolysis and block the oxidation of fatty acids.

Antisten supports myocardial contractility, inhibits the decrease in intracellular adenosine triphosphate and phosphocreatinine. Against the background of acidosis, the drug normalizes the functioning of membrane ion channels and the intracellular content of calcium ions, inhibits their accumulation in cardiomyocytes.

When used, Antisten reduces intracellular acidosis and increased phosphate levels that occur under conditions of reperfusion and myocardial ischemia. The drug inhibits the damaging effects of free radicals, helps maintain the integrity of cell membranes, prevents the activation of neutrophils in the ischemic zone, increases the duration of the electrical potential, reduces the release of creatine phosphokinase from cells and reduces the severity of ischemic damage to the myocardium.

According to reviews, Antisten reduces the frequency of angina attacks and the need for nitrates. Already 14 days after the start of drug therapy, the body’s tolerance to physical activity, sharp fluctuations in blood pressure are reduced. The product eliminates dizziness and tinnitus of ischemic origin. In case of vascular eye disorders, Antisten restores the functions of the retina.

After oral administration, Antisten is completely and quickly absorbed into gastrointestinal tract. Has high bioavailability. Reaches maximum concentration in blood plasma after 3-5 hours. It binds poorly to blood proteins and easily penetrates histohematic barriers. Excreted from the body through the kidneys. The complete elimination period is 14 hours, in patients over 65 years of age – 24 hours.

Indications for use Antisten

Indications for Antisten according to the instructions are:

Chorioretinal vascular disorders;
Cochleovestibular disorders of ischemic nature, which include hearing impairment, tinnitus and dizziness;
Coronary heart disease (as part of complex therapy for the prevention of angina attacks).

Methods of use and dosage of Antisten

Antisten is intended for oral use along with food intake.

The drug is prescribed in a single dosage of 1 tablet 2 times a day (morning and evening).

The duration of the course of treatment is determined by the attending physician individually for each patient, depending on his condition and severity of the disease.

Side effects of Antisten

In reviews of Antisten it is noted that the medicine can cause adverse reactions from the body:

Digestive system: abdominal pain, dyspepsia, diarrhea, nausea, vomiting;
Cardiovascular system: facial flushes, orthostatic hypotension;
Central nervous system: headaches, dizziness, rarely - akinesia, rigidity and tremor, which disappear after discontinuation of the drug;
Dermatological reactions: urticaria, itching, skin rash;
Other: asthenia.

Contraindications to the use of Antisten

According to the instructions for Antisten, the contraindications are:

Children and adolescents under 18 years of age;
Severe liver dysfunction;
Renal failure (with CC less than 15 ml/min);
Hypersensitivity to its components;
The period of pregnancy and breastfeeding.

Overdose

In the reviews of Antisten there is no data on an overdose of the drug.

Antisten's analogs

By chemical composition Analogues of Antisten are Angiosil retard, Vero-Trimetazidine, Carditrim, Medarum, Metagard, Predizin, Preductal, Rimekor, Trimectal, Trimet.

According to the mechanism of action, analogues of Antisten are Biosint, Vazomag, Dibikor, Ezaphosphina, Idrinol, Camphor, Cardionat, Coronatera, Kudesan, Mexicor, Mildronate, Meldonium, Neoton, Orocamag, Pedea, Riboxin.

Additional Information

Antisten is not intended to relieve angina attacks.

Do not use the medication for the initial course of treatment of unstable angina and myocardial infarction.

If an angina attack develops, it is necessary to reconsider the treatment regimen.

If you miss one or more doses of Antisten, you cannot take an increased dosage at the next dose.

The instructions for Antisten indicate that the tablets should be stored in a dark, dry, cool place out of reach of children.

The drug is dispensed from pharmacies only with a prescription from the attending physician.

Shelf life – 2 years.