Tablets - 1 tablet:
- Active substance: trimetazidine dihydrochloride 35 mg.
- Excipients: hypromellose - 93 mg, microcrystalline cellulose - 178.9 mg, colloidal silicon dioxide - 1.55 mg, magnesium stearate - 1.55 mg.
- Film shell composition: opadry II 85F240012 Pink (polyvinyl alcohol - 4 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).
10 pieces. - contour cell packaging (6) - cardboard boxes.
20 pcs. - contour cell packaging (3) - cardboard packs.
30 pcs. - contour cell packaging (2) - cardboard packs.
60 pcs. - polymer containers (1) - cardboard packs.
Description of the dosage form
Extended-release tablets, film-coated, creamy pink, biconvex; On a cross section, two layers are visible, the inner layer (core) is white or white with a yellowish tint.
pharmachologic effect
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 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 CK from cells and the severity of ischemic damage to the myocardium.
Trimetazidine reduces the frequency of angina attacks, reduces the need for nitrates, after 2 weeks of use it increases exercise tolerance, and sharp fluctuations in blood pressure are reduced. Reduces dizziness and tinnitus of ischemic etiology. In case of vascular pathology of the eye, it restores the functional activity of the retina.
Pharmacokinetics
Suction and distribution
After taking the drug orally, trimetazidine is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability - 90%. The time to reach Cmax in blood plasma is 3-5 hours. The equilibrium state is reached after 60 hours. Vd is 4.8 l/kg. Plasma protein binding - 16%. Easily penetrates histohematic barriers.
breeding
Trimetazidine is excreted from the body mainly by the kidneys (about 60% unchanged). T1/2 - about 7 hours.
Pharmacokinetics in special clinical situations
T1/2 in patients over 65 years of age is about 12 hours. The renal clearance of trimetazidine directly correlates with CC, hepatic clearance decreases with age.
Antisten MV: Indications
- IHD: prevention of angina attacks (in complex therapy);
- cochleovestibular disorders of ischemic nature, such as dizziness, tinnitus, hearing impairment;
- choreoretinal vascular disorders.
Antisten MV: Contraindications
- Hypersensitivity to any component of the drug;
- renal failure (creatinine clearance less than 15 ml/min);
- severe liver dysfunction;
- age under 18 years (efficacy and safety have not been established).
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. Use during pregnancy is contraindicated.
It is not known whether Antisten MV 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
Contraindication: age under 18 years (efficacy and safety have not been established).
Antisten MV: Side effects
Frequency: very often - more than 1/10; often - more than 1/100 and less than 1/10; uncommon - more than 1/1000 and less than 1/100; rarely - more than 1/10000 and less than 1/1000; very rarely - less than 1/100000, including individual messages.
From the digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting.
From the cardiovascular system: rarely - orthostatic hypotension, flushing of the facial skin.
From the side of the central nervous system: often - dizziness, headache; very rarely - extrapyramidal disorders (tremor, rigidity, akinesia), reversible after discontinuation of the drug.
Dermatological reactions: often - skin rash, itching, urticaria.
Other: often - asthenia.
Overdose
Currently, cases of drug overdose have not been reported.
Every year, cardiovascular diseases claim the lives of thousands of people. These pathologies require complex treatment, which necessarily includes antianginal and antihypoxic drugs. These drug groups include Antisten. Consider what this remedy is, when it is prescribed and how it is taken.
Antisten is an antianginal drug that normalizes cellular energy metabolism under conditions of ischemia or hypoxia. The international non-proprietary name of the drug is Trimetazidine. Belongs to the pharmacological group of drugs prescribed for cardiovascular pathologies and used to correct metabolism. This is a long-acting prescription drug available in tablet form.
Release form and cost
The tablets are biconvex, creamy pink, containing 20 and 35 mg of the active substance. The drug is sold in cardboard boxes and packs of 60 tablets. Depending on the dosage, the cost of the drug also differs. Average prices are presented in the table (Table 1).
Table 1 - Cost of Antisten
Compound
One tablet of Antisten contains 20 or 35 mg of trimetazidine dihydrochloride. Auxiliary substances include:
- hypromellose;
- microcrystalline cellulose;
- polysorb;
- magnesium stearate.
The film shell consists of:
- polyvinyl alcohol;
- macrogol;
- iron oxide (Iron Oxides);
- talc;
- titanium dioxide.
Indications and contraindications
Antisten is prescribed for a pathological condition characterized by partial or absolute disruption of myocardial blood circulation due to damage to the coronary arteries. The drug is used both for the prevention of angina pectoris and in complex treatment.
For lesions of the inner ear and auditory nerve against the background of cardiovascular pathology, therapy allows you to get rid of severe symptoms:
- dizziness;
- hearing impairment;
- ear noise.
Also, this medicinal product is effective for hearing loss and other vestibular disorders. In addition, it is used for degenerative changes in the choroid of the visual organs in ophthalmology.
Antisten is not prescribed for:
- hypersensitivity to the components of the drug;
- severe liver dysfunction;
- under 18 years of age (since the safety and effectiveness of the drug has not been established for this age category of patients);
- renal failure.
No disruption of embryonic development under the influence of this medication was detected in animal studies. But due to the lack of clinical data on the harmlessness of using Antisten when carrying a child, it is not recommended to take it. The risk of pathologies of intrauterine development is not excluded.
It is not known whether the active substance passes into breast milk, so this medication should not be used during breastfeeding. If treatment requires the inclusion of Antisten in the treatment protocol, then breastfeeding is stopped.
Pharmacodynamics and pharmacokinetics
Antianginal medication Antisten is used in cardiology for:
Antisten belongs to the pharmacological group of antihypoxants. Its active components direct cellular metabolism in the energetically correct direction. Instead of oxidizing fatty acids, the drug promotes the oxidation of glucose.
Inhibition of fatty acid blocking occurs by blocking 3-ketoacyl-CoA thiolase. As a result, the concentration of ATB and creatine phosphoric acid in structures during hypoxia is normalized and the heart rate is maintained at normal levels.
When the acid-base balance of the body shifts towards increasing acidity, Antisten helps regulate the electrolyte balance of the muscle cells of the heart and neurosensory tissues, preventing the accumulation of calcium and sodium, and normalizing the potassium content.
As a result, a change in the membrane potential in a negative direction contributes to the lengthening of the excitation wave moving along the cell membrane in the form of a short-term change in the membrane potential in a small area of the excitable cardiomyocyte.
The drug minimizes the negative consequences of restoring blood flow through the coronary arteries after ischemia, which often lead to a deterioration in the patient’s condition, reducing the severity of acidosis.
Thanks to its membrane-stabilizing effect, Antisten promotes the restoration of cell membranes, protecting them from the further negative effects of toxins formed during lipid oxidation. By preventing the migration of neutrophils into intervascular tissues susceptible to ischemia, the active substances of the drug prevent further damage.
For ENT pathologies caused by dysfunction of the inner ear, ear noises and dizziness are eliminated. With stable angina, prolonged use of Antisten reduces the number of attacks, reduces the need for nitrates and increases physical capabilities due to an increase in coronary reserves. Antisten MF tablets help:
The active components are quickly and almost completely (90%) broken down by the intestinal mucosa. The maximum concentration in the blood is reached within 2 hours. 16% bound to plasma proteins. They are excreted naturally (almost 60% unchanged).
Instructions for use Antisten MV (35 mg)
The most commonly used form of the drug in cardiology is one containing 35 mg of the active ingredient - regular and prolonged action. Let's take a closer look at how to use it.
Dosage
The dosage calculation depends on the form of the product:
Antisten is taken during or immediately after meals, since when taken on an empty stomach it has a strong irritant effect on the mucous membranes, which can lead to dyspeptic disorders and worsening the patient's condition.
The therapeutic course is prescribed and determined by the doctor, but it cannot last more than two weeks. If it is necessary to continue treatment with the drug, then a break is taken for a month, and only then therapy is resumed.
special instructions
The drug cannot be prescribed independently to relieve angina attacks. It is not used for unstable angina or to treat myocardial infarction. In addition, the medicine should not be used in conjunction with alcoholic beverages. The active substance trimetazidine and ethanol have opposite effects, which can significantly worsen the patient's condition.
If angina develops, it is necessary to reconsider the treatment protocol. If a dose of the drug is missed for any reason, the next tablet is taken at the appointed time. The dosage cannot be increased in this case.
This medication does not affect the ability to drive vehicles or perform work involving dangerous machinery.
There is no information about the interaction of Antisten with other medications. But to exclude possible interactions between drugs of different groups, it is recommended to take other drugs no earlier than 2-3 hours after Antisten.
Also, cases of drug overdose have not been established. If the patient mistakenly took a double dose instead of the prescribed dose, then it is better to skip the next dose of pills.
Possible side effects
In patients taking Antisten, the following side effects have been identified:
- allergic manifestations (skin rash, itching, redness, swelling);
- tremor, numbness of limbs;
- attacks of dizziness;
- attacks of cephalalgia;
- asthenic manifestations;
- nausea, vomiting;
- indigestion;
- difficult and painful digestion;
- pain in the abdomen and pelvis.
Analogues
The prevention of angina pectoris can be carried out using a huge number of drugs - both completely similar to Antisten in the active substance and in action, but produced on the basis of other active components. The specialist will recommend which one is better to choose, based on the individual characteristics of the patient and his condition.
Structural
Among the structural analogues of Antisten, the following drugs can be noted:
Other similar means
You can also use other medications that have a similar effect:
Efficiency
Experts have a positive attitude towards Antisten. But it is not recommended to prescribe it yourself without consulting a doctor. Most experts note that the influence and effectiveness of the drug should be judged by the patient’s condition over time. It will be suitable for one person and will help eliminate the problem when another patient needs to be prescribed another drug with a similar effect.
Result: positive feedback
Cure for tinnitus
Advantages: Acts quickly and effectively
Disadvantages: None.
After 40 years, I developed tinnitus and it really bothered me, especially before bed, and it intensified many times over. Since I have coronary artery disease, I had to go to an appointment with a cardiologist. The doctor prescribed Antisten MB to improve cell metabolism during ischemia. To be honest, I did not believe the doctor, and was internally confident that the medicine would help me. If anyone has encountered this problem, they know that 99% of opinions claim that the cause of tinnitus is cervical osteochondrosis. I still took the pills. I took 1 tablet 3 times a day. About 3 weeks later, lying in bed before going to bed, unexpectedly for myself, I began to see clearly and realized that nothing was stopping me! Complete silence and comfort!
Result: positive feedback
Improves quality of life!
Benefits: Efficiency
Disadvantages: maybe price
Antisten MV is a domestic drug, an analogue of the French Preductal (the same active substance in the composition), accelerates metabolism, improves the functioning of the cardiovascular system. The price is not very different from Preductal. I was appointed a cardiologist, I can’t stand the off-season badly and I have weather dependence, during such periods I feel dizzy, I want to lie down, a condition that is called “heart aches”, “not enough breathing”. As an emergency medical aid, it will not work, according to the sensation, the effect in the form of an improvement in well-being appears after about a week of admission. In addition to supporting the heart, I felt how headaches decreased - it improves cerebral circulation.
Result: positive feedback
Be patient and you will feel the effect
Advantages: Effective, safe
Disadvantages: The effect appears only after a couple of months of treatment
Antisten MV is a truly safe drug. For more than six months, it did not harm me at all, did not even cause nausea, not to mention anything else. The effect is more difficult. It is wonderful, but to achieve it you need to be treated for at least 3-4 months. At least I felt noticeably better after 3 months. The first thing I noticed was a weakening of the constant buzzing in my head and the “trilling” in my ears. A little later, the headache stopped hurting, and the dizziness became much less frequent. Slowly, by the 5th month, all of the above left me alone. The drug helped my heart only later, but the effect began to be felt somehow sharply and very strongly. It’s just that the heart has stopped seizing so often, and now everything is generally fine - if there is no severe stress, it doesn’t even think about getting sick. Things have also improved with heart rate, and a heart rate of 120 is a thing of the past. Now the maximum is 90, and only if I’m worried. I still haven’t gotten used to it, I continue to drink and live peacefully.
Result: negative feedback
Helps with heart pain. Someone but not me
Benefits: no
Disadvantages: terrible side effects
The hospital prescribed the drug, saying that it would cope well with my problems (heart pain, shortness of breath). At the pharmacy I even managed to buy two packages for the price of one, there was some kind of promotion there. I started drinking according to the instructions and immediately all possible side effects appeared. Nightmarish headaches, nausea, pain and heaviness in the intestines... Maybe it’s just me who was unlucky, or maybe the product is really disgusting, so they sell it on sale in order to somehow sell it to people. I quit it after the second dose, so I can’t say anything about its effectiveness. I seriously doubt that she exists.
pharmachologic effect
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 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 CK from cells and the severity of ischemic damage to the myocardium.
Trimetazidine reduces the frequency of angina attacks, reduces the need for nitrates, after 2 weeks of use it increases exercise tolerance, and sharp fluctuations in blood pressure are reduced. Reduces dizziness and tinnitus of ischemic etiology. In case of vascular pathology of the eye, it restores the functional activity of the retina.
Pharmacokinetics
Suction and distribution
After oral administration, trimetazidine is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability - 90%. The time to reach C max in blood plasma is 3-5 hours. The equilibrium state is reached after 60 hours. V d is 4.8 l / kg. Plasma protein binding - 16%. Easily penetrates histohematic barriers.
breeding
Trimetazidine is excreted from the body mainly by the kidneys (about 60% - unchanged). T 1/2 about 7 hours.
Pharmacokinetics in special clinical situations
T 1/2 in patients over 65 years old is about 12 hours. Renal clearance of trimetazidine directly correlates with CC, hepatic clearance decreases with age.
Indications
— IHD: prevention of angina attacks (in complex therapy);
- cochleovestibular disorders of an ischemic nature, such as dizziness, tinnitus, hearing impairment;
- Choreoretinal vascular disorders.
Dosage regimen
Inside, during meals.
Antisten MV is prescribed 1 tablet. 2 times/day (morning and evening). The course of treatment is determined by the doctor individually.
Side effect
Frequency: very often - more than 1/10; often - more than 1/100 and less than 1/10; uncommon - more than 1/1000 and less than 1/100; rarely - more than 1/10000 and less than 1/1000; very rarely - less than 1/100000, including individual messages.
From the digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting.
From the cardiovascular system: rarely - orthostatic hypotension, flushing of the facial skin.
From the side of the central nervous system: often - dizziness, headache; very rarely - extrapyramidal disorders (tremor, rigidity, akinesia), reversible after discontinuation of the drug.
Dermatological reactions: often - skin rash, itching, urticaria.
Other: often - asthenia.
Contraindications for use
- hypersensitivity to any component of the drug;
- renal failure (creatinine clearance less than 15 ml/min);
- severe liver dysfunction;
- age under 18 years (efficacy and safety have not been established).
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. Use during pregnancy is contraindicated.
It is not known whether Antisten MV 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
Contraindication: age under 18 years (efficacy and safety have not been established).
Overdose
Currently, cases of drug overdose have not been reported.
Drug interactions
There is no information about drug interactions between the drug.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
List B. The drug should be stored in a dry place, protected from light, out of reach of children, at a temperature not exceeding 25°C. Shelf life - 3 years. Do not use after expiration date.
Use for liver dysfunction
Contraindication: severe liver dysfunction.
Use for renal impairment
Contraindication: renal failure (creatinine clearance less than 15 ml/min).
Use in elderly patients
T1/2 in patients over 65 years of age - about 12 hours.
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 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.
Registration number: LSR-008140/10-160810
Trade name of the drug: Antisten MB
International Nonproprietary Name (INN): trimetazidine
Dosage form: extended-release, film-coated tablets.
Compound: for 1 tablet:
Active substance: trimetazidine dihydrochloride - 35 mg;
Excipients (core): hypromellose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate.
Excipients (shell): hypromellose, macrogol, red iron oxide, titanium dioxide.
Description: Biconvex, film-coated tablets of creamy pink 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 code S01EB15
PHARMACOLOGICAL PROPERTIES
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 damage to the myocardium.
Trimetazidine reduces the frequency of angina attacks, reduces the need for nitrates, after 2 weeks of use it increases exercise tolerance, and sharp fluctuations in blood pressure (BP) are reduced. 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, trimetazidine 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. Connection with blood plasma proteins -16%. Trimetazidine 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 for use
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 under 18 years (efficacy and safety have not been established).
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 the drug during pregnancy is contraindicated.
It is unknown whether ANTISTEN MB 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.
Dosage and administration
Inside, during meals.
Antisten MB is prescribed 1 tablet 2 times a day (morning and evening).
The course of treatment is as recommended by a doctor.
Side effect
Frequency: very often - more than 1/10; often - more than 1/100 and less than 1/10; uncommon - 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 digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting.
From the cardiovascular 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 side of the skin and subcutaneous fat: often - skin rash, itching, urticaria.
Others: often - asthenia.
Overdose
Currently, cases of drug overdose have not been reported.
Interaction with other drugs
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! A"
Impact on the ability to drive vehicles and operate machinery
The drug ANTISTEN MB 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
Extended-release film-coated tablets 35 mg.
10, 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 are 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.
Storage conditions
List B.
Store in a dry place, protected from light, at a temperature not exceeding 25°C.
Keep out of the reach of children.
Best before date
3 years.
Do not use after expiration date.
Conditions for dispensing from pharmacies
On prescription.
Manufacturer
Ozon LLC
Legal address:
445351, Russia, Zhigulevsk, Samara region, st. Pesochnaya, 11
Address for correspondence (actual address, including for receiving claims):
445351, Russia, Zhigulevsk, Samara region, st. Hydrostroiteley, 6.
