Description overdue on 08/22/2014

• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications Antistius and Antistius MB
• Contraindications
• Side effects
• Instructions for use: Dosing and dosing regimen
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

One tablet contains Antistius incorporates 20 mg Trimetazidine dihydrochloride   and auxiliary components:

• corn starch;
• magnesium stearate;
• mannitol;
• polyvinylpyrrolidone (povidone);
• colloidal silica;
• lactose;
• hydroxypropylmethylcellulose;
• methylcellulose;
• titanium dioxide;
• Tween 80;
• Castor oil;
• polyethylene glycol-4000;
• Acid Red 2C.

One tablet contains 35 MB Antistius mg Trimetazidine dihydrochloride   and auxiliary substances:

• Valium;
• microcrystalline cellulose;
• colloidal silicon dioxide;
• magnesium stearate.

The composition of the coating tablets Antistius CF coating film includes:

• Opadry II 85F240012 Pink;
• polyvinyl alcohol;
• macrogol 3350;
• iron oxide red dye;
• dye yellow iron oxide;
• talc;
• titanium dioxide.

Product form

The drug has two pharmaceutical forms of production:

• Film-coated tablets Red Antistius (each pack contains 60 tablets of the drug).
• Tablets Antistius MB modified release. Each tablet film-coated cream with pink shades in one pack contains 60 tablets of the drug.

Antistius tablets are round, biconvex, in cross section can be easily seen two layers: the top red and internal (core) - White or slightly yellowish color.

Tablets modified release Antistius CF are round, lenticular, a cross section of a well reviewed two layers: the top cream-colored with a pinkish tinge and internal (core) - White or slightly yellowish color.

Pharmacological action

Antistius and Antistius MW belong to the pharmacotherapeutic group antihypoxic drugs Whose action is aimed at improving the metabolic changes myocardium As well as improving the function of sensorineural (neurosensory) in terms of coronary artery disease .

Pharmacodynamics and pharmacokinetics

Antistius: pharmacodynamics of the drug

The pharmacological action of the drug is aimed at the normalization of energy metabolism of cells and cellular structures affected by   ischemia   or hypoxia . Once in the body, the active substance Antistius trimetazidine :

• prevents a decrease in the cells of adenosine triphosphate - nucleotide, plays a key role in the exchange of energy and matter in the body;
• It stimulates the functional activity of ion channels in the cell membrane;
• It stimulates the transmembrane transport of potassium ions and sodium;
• contributes to the maintenance of cellular self-regulation (homeostasis of the cell);

Because of its ability to selectively inhibit the activity of the long-chain 3-CAT (3-ketoacyl-CoA thiolase) trimetazidine   inhibits oxidation lipids .

As a result of this oxidation are stimulated Glucose Restored therebetween conjugation reactions and oxidative decarboxylation, and also increases the level of protection   infarction   from ischemia .

It is the ability to switch oxidation lipids   Oxidation Glucose   based antianginalnoe   effects of the drug.

Antistius MB: pharmacodynamics of the drug

The drug has a pronounced Antistius CF:

• antianginal ;
• antihypoxic ;
• cytoprotective   effects.

Antianginalnoe   effect of the drug is to eliminate clinical manifestations ischemia infarction   in patients with a diagnosis of " coronary artery disease ".

The mechanism of this action due to the ability trimetazidina   reduce the level of preload heart muscle Stimulate blood flow to her subendocardial departments And blood supply Department of epicardial coronary vessels To expand collateral vessels To block adrenergic receptors   and Calcium channels , Simultaneously activating potassium channel .

As a result, the patient:

• reduced inflow of venous blood to the heart muscle ;
• reduced need for cells heart muscle   oxygen;
• reduced performance peripheral vascular resistance;
• reduced severity of pain;
• reduced pressure indicators atrium   and in pulmonary embolism .

Antihypoxia   effect trimetazidina   determined by the ability of the drug to improve the utilization of oxygen, reduce the need of various organs and tissues of oxygen, as well as increase the level of resistance to hypoxia .

Cytoprotective   the properties resulting in the ability to store energy potential, to correct ionic balance, improve the protective capacity of the mucosa, in particular by promoting development prostaglandins   and epidermal growth factor.

Trimetazidine   It has the ability to:

• have a direct effect on the cells that form the basis heart muscle And brain neurons Improving their metabolism and functional activity;
• maintain contractility indices heart muscle   within the physiological norm;
• prevent decline in intracellular adenosine triphosphate ;
• prevent decline in content phosphocreatine   - Physiologically active substance, which improves metabolism infarction   and   muscle .

Under pathological conditions, which are characterized by displacement of acid-base balance in the direction of increasing acidity, trimetazidine :

• normalizes the functioning ion channels (IR) cell membranes ;
• prevents accumulation of calcium and sodium cardiomyocytes   - Forming cells heart muscle ;
• improves the intracellular potassium.

Furthermore, the substance:

• reduces symptoms of intracellular acidosis   (increase the acidity) and lower high phosphate content, which are a consequence coronary   disease ;
• prevents damage to cells and cellular structures by free radicals;
• It provides safety integrity cell membrane ;
• prevents activation neutrophilic granulocytes   ( neutrophil ) In the zone ischemia ;
• increases the duration of an electrical potential;
• prevents the creatine   of cells;
• reduces the severity of injuries heart muscle Induced coronary artery disease ;
• It helps to reduce the frequency of seizures angina ;
• It reduces the body's need for taking nitrates;
• increases resistance to physical stress (the effect develops after about two weeks of Antistius MW);
• eliminates (or at least reduces the frequency of their occurrence) surges indicators Blood Pressure ;
• reduces the severity of vertigo and tinnitus caused coronary artery disease ;
• contributes to the normalization of hearing;
• It improves the vestibular test in patients with pathologies Otolaryngology ;
• vascular pathology of the eye helps to restore the normal function of the light-sensitive inner shell ( retinal ).

Antistius: pharmacokinetics

Trimetazidine , Getting into the body, quickly absorbed from gastrointestinal tract . Indicator substances bioavailability is 90%. Time for which rate plasma concentration reaches its maximum - 2 hours.

Index higher plasma concentrations after a single oral dose trimetazidina Of 20 mg, 55 ng / ml.

The proportion of drug-related rolling in plasma proteins   form (index binding plasma proteins ), Is 16%. The ratio of the total content of substances in the body to its concentration in serum   (so-called distribution volume) - 4, 8 l / kg.

Trimetazidine   characterized by the ability to easily pass through histiocytic (gistogematicalkie) barriers . Partially substance undergoes biotransformation in the body, while about 60% of the amount excreted unchanged from the body kidney .

The half-life trimetazidina   and its metabolites varies between 4, 5 and 5 hours.

Antistius MB: pharmacokinetics

Trimetazidine , Getting into the body, quickly absorbed from gastrointestinal tract . Indicator substances bioavailability is 90%. Time for which rate plasma concentration reaches its maximum - from 3 to 5 hours.

The equilibrium state of the medication blood   It observed 60 hours after first taking the pill Antistius MB. The ratio of the total content of substances in the body to its concentration in serum   - 4, 8 l / kg.

Indicator binding plasma proteins   16%. The product is characterized by the ability to easily penetrate histiocytic barriers .

Excretion trimetazidina   It performed mainly   kidney While most of the material (about 60%) excreted from the body in its purest form. The half-life is usually about 7 hours.

In elderly patients (over 65 years) the biological half-life trimetazidina It stretched to an average of 12 hours. Renal clearance of substances is characterized by a direct correlation on the performance of clearance creatinine , Hepatic clearance of drugs decreases with age.

Indications Antistius and Antistius MB

Indications for use of VHF and Antistius Antistius are:

• coronary artery disease   (coronary heart disease) - a drug recommended for appointment in the complex therapy to maintain the patient's condition and prevent strokes;
• Pathology of the choroid and retina with ischemic component;
• dizziness Vascular natural origin;
• cochle-vestibular disorders caused ischemia   (eg, ringing in the ears, lesions the inner ear   and auditory nerve   etc.)

Contraindications

Both forms of the drug release Antistius have the same contraindications. These include:

• increased individual sensitivity trimetazidina   or any of the supporting components of the tablet;
• renal failure Which is characterized by a decrease in clearance of endogenous creatinine (QC indicator) to 15 ml / min or less;
• liver disease Wearing pronounced;
• age less than 18 years (for this category of patients the safety of the drug and its efficacy has not been studied).

Side effects

Side effects tablets Antistius

The possible adverse reactions that may develop during treatment Antistenom include:
manifestations allergies , Manifested most often in the form of itching and rashes on the skin;
rarely nausea, vomiting, stomachalgia .

Side effects tablets Antistius MB

The most frequent adverse reactions that may occur after taking Antistius CF include: dyspeptic disorders   (epigastric pain, nausea, vomiting, frustration of a chair); headaches and dizziness; skin rash, itching, symptoms   hives . asthenia .

In rare cases, seizures orthostatic collapse   ( orthostatic hypotension ) And flushing.

Even more rarely can be observed different kinds extrapyramidal disorder That are manifested in the form of tremor , Increased rigidity   (a sharp increase in the tone of the different anatomical structures) akinesia   (inability to perform voluntary movements), etc ..

These phenomena are, however, reversible and completely disappear after drug withdrawal.

Instructions for use: Dosing and dosing regimen

Antistius: instructions for use

Daily dose   trimetazidina   It is 2-3 tablets, equivalent to 40-60 mg trimetazidina   per day. The multiplicity of techniques, respectively, equal to 2-3.

The duration of the therapeutic course is determined by the attending physician and the individual in each case, depending on the efficacy and characteristics of the disease.

Antistius MB: instructions for use

Antistius MB is recommended to take twice a day with meals (optimally - in the morning and evening). A single dose of the drug - one tablet.

The duration of the therapeutic course is determined by the attending physician and the individual in each case, depending on the efficacy and characteristics of the disease.

Overdose

Currently, data on overdose and Antistenom Antistenom MB available.

Cooperation

Drug Interactions trimetazidina   with other drugs has not been described.

Terms of sale

Antistius and Antistius MW belong to the category of prescription drugs a physician.

Storage conditions

The tablets were stored in a dark, dry place at a temperature of from 10 to 25 ° C.

Shelf life

Tablets Antistius Antistius and CF are suitable for use within 2 years.

Cautions

Antistius The drug has no effect on the rate of reaction and does not cause impairment of driving ability and potentially dangerous machinery.

Tablets Antistius CF are not intended to relieve the symptoms of acute attacks angina . Also, it is not indicated in the initial stages of treatment aggravation coronary disease and (CHD) or myocardial infarction .

If the patient developed attack angina It is recommended to review the treatment and to adapt it in accordance with the condition of the patient and the characteristics of the disease.

Omitting one (or more) taking the pill Antistius MB are not allowed to take a higher dose of the drug in the following method.

Analogs Antistius

Analogs of the drug Antistius:

• Angiozyme Retard ;
• Vero Trimetazidine ;
• Karditrim ;
• Metagard ;
• Preductal ;
• Prekard ;
• Rimekor ;
• Trimethyl ;
• Trimetazidine .

Actions similar to the drug Antistius CF have:

• Deprenorm MB ;
• Preductal MB ;
• Trimetazidine-Biocom MB ;
• Rimekor MB ;
• Trimektal MB ;
• Trimetazidine MB .

Pregnancy and lactation

Antistius contraindicated in pregnancy   and between breast-feeding .

Studies conducted on animals have shown that MV Antistius not able to have teratogenic effects on the developing fetus. However, due to lack of data on the safety of drug treatment in the period   pregnancy The probability of occurrence of any defects can not be completely ruled out. For this reason, the drug is not permitted to assign the treatment of pregnant women.

Data on whether the trimetazidine   excreted in breast milk, no, so if you can not avoid the appointment Antistius MW during lactation, for the entire period of treatment should stop breastfeeding.

Reviews Antistene

Reviews and Antistius Antistius MB, which can be found on the Internet, mostly positive. Many patients notice a significant improvement in health after starting these drugs.

However, some doctors agree that the two pharmaceutical forms Antistius are mostly preventive tool that is used not only for treatment, but rather to maintain the patient.

The very same drug by itself can not entirely eliminate the problem Cardiovascular   or nervous system . For this reason, it is recommended to be administered in combination with other drugs intended for treatment abnormalities of the heart and blood vessels .

Price Antistius

Average price Antistius CF is about 380-400 Russian rubles Antistius pills cost about 270 rubles.