Mildronate in bodybuilding. How to take mildronate and what it is for The drug mildronate indications for use

A drug that improves metabolism.
Preparation: MILDRONAT®

It should be especially noted that Mildronate® has a small number of side effects - this is one of the important factors explaining its wide acceptance among doctors and patients. The safety of Mildronate is confirmed by periodically updated safety reports and the results of published clinical studies.

After Latvia joined the European Union, it became a mandatory requirement for the regulatory authorities to have a Pharmacovigilance system responsible for monitoring and evaluating the use of medicines. Since the beginning of the monitoring (since March 21, 2006), JSC "Grindeks" has received 478 spontaneous reports (messages) about products containing meldonium. A potential significant health risk in these cases has not been identified. There have been no reports of the development of dependence and addiction to Mildronate® after its use. Data about side effects meldonium or reactions from athletes have been reported.

As you can see, the total number of reports of side effects of mildronate is very small. During the evaluation of these reports, no new risks of using meldonium preparations were identified. Based on post-marketing data on the use of Mildronate®, capsules, tablets and injection of Mildronate® can be regarded as medicines with an acceptable safety profile. Given the number of packages sold, which is equal to 868 314 370 g (more than 868 tons) in terms of the active substance (meldonium), the benefit-risk ratio of the use is positive.

The active substance of the drug: meldonium
ATX encoding: C01EB
KFG: A drug that improves metabolism and energy supply of tissues
Registration number: P N016028/01
Date of registration: 03.11.06
The owner of the reg. Award: GRINDEX JSC (Latvia)

Mildronate release form, drug packaging and composition.

Capsules hard gelatin, size №1, white color; the content of the capsules is a white crystalline powder with a slight odor, hygroscopic.
Capsules
1 caps.

250 mg

10 pieces. - blisters (4) - packs of cardboard.

Capsules hard gelatin, size No. 00, white; the content of the capsules is a white crystalline powder with a slight odor, hygroscopic.
Capsules
1 caps.
meldonium (trimethylhydrazinium propionate)
500 mg

Excipients: potato starch, colloidal silicon dioxide, calcium stearate.

The composition of the capsule shell: gelatin, titanium dioxide (E171).

10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (6) - packs of cardboard.

The solution for intravenous administration is clear, colorless.
Solution for intravenous administration
1 ml
1 amp.
meldonium (trimethylhydrazinium propionate)
100 mg
500 mg

Excipients: water d / i.

5 ml - ampoules (5) - plastic cell packaging (2) - cardboard packs.

The description of the drug is based on the officially approved instructions for use.

Pharmacological action Mildronate

A drug that improves metabolism. Meldonium is a structural analogue of gamma-butyrobetaine, a substance found in every cell of the human body.

Under conditions of increased stress, Mildronate restores the balance between the delivery and demand of cells for oxygen, eliminates the accumulation of toxic metabolic products in cells, protecting them from damage; also has a tonic effect. As a result of its use, the body acquires the ability to withstand the load and quickly restore energy reserves. Due to these properties, Mildronate is used to treat various disorders of activity. of cardio-vascular system, blood supply to the brain, as well as increasing physical and mental performance.

As a result of a decrease in the concentration of carnitine, gamma-butyrobetaine, which has vasodilating properties, is intensively synthesized. In acute ischemic myocardial damage, Mildronate slows down the formation of a necrotic zone, shortens rehabilitation period.

In heart failure, the drug increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks.

For acute and chronic ischemic disorders cerebral circulation improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area.

Effective in vascular and dystrophic pathology of the fundus.

The drug eliminates functional disorders nervous system in patients with chronic alcoholism with withdrawal syndrome.

Pharmacokinetics of the drug.

Suction

After oral administration, the drug is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 78%. Cmax in plasma is achieved 1-2 hours after administration.

Metabolism and excretion

Biotransformed in the body with the formation of two main metabolites, which are excreted by the kidneys. T1 / 2 is 3-6 hours and depends on the dose.

Indications for use:

As part of complex therapy IHD (angina pectoris, myocardial infarction), chronic heart failure, dyshormonal cardiomyopathy;

As part of the complex therapy of acute and chronic disorders of cerebral circulation (strokes and cerebrovascular insufficiency);

Reduced performance;

Physical overstrain (including in athletes);

Withdrawal syndrome in chronic alcoholism (in combination with specific alcoholism therapy);

Hemophthalmos, retinal hemorrhages of various etiologies;

Thrombosis of the central retinal vein and its branches;

Retinopathy of various etiologies (diabetic, hypertensive).

Dosage and method of application of the drug.

In connection with the possibility of developing an exciting effect, the drug is recommended to be used in the morning.

At cardiovascular diseases as part of complex therapy, the drug is prescribed at 0.5-1 g per day orally or intravenously (5-10 ml of injection solution with a concentration of 500 mg / 5 ml), the frequency of use is 1-2 times / day. The course of treatment is 4-6 weeks.

With cardialgia against the background of dyshormonal myocardial dystrophy, Mildronate is prescribed orally at 250 mg 2 times / day. The course of treatment with the drug in the form of a syrup is 4-6 weeks, in the form of capsules - 12 days.

In case of violation of cerebral circulation in the acute phase, the drug is prescribed intravenously at 500 mg 1 time / day for 10 days, then they switch to taking the drug orally at 0.5-1 g / day. The general course of therapy is 4-6 weeks.

In chronic disorders of cerebral circulation, the drug is taken orally at 0.5-1 g / day. The general course of therapy is 4-6 weeks. Repeated courses are prescribed individually 2-3 times a year.

At vascular pathology and dystrophic diseases of the retina Mildronate is administered parabulbarno at 0.5 ml of injection with a concentration of 500 mg / 5 ml for 10 days.

With mental and physical exertion, 250 mg 4 times / day or intravenously 0.5 g 1 time / day are prescribed orally. The course of treatment is 10-14 days. If necessary, therapy is repeated after 2-3 weeks.

In chronic alcoholism, the drug is prescribed orally at 500 mg 4 times / day, intravenously - 500 mg 2 times / day. The course of treatment is 7-10 days.

Side effects of Mildronate:

Since the cardiovascular system: rarely - tachycardia, changes in blood pressure.

From the side of the central nervous system: rarely - psychomotor agitation.

From the side digestive system: rarely - dyspeptic phenomena.

Allergic reactions: rarely - itching, redness, rash, swelling.

Contraindications to the drug:

Increased intracranial pressure (including in violation of venous outflow, intracranial tumors);

Children's age up to 12 years (for syrup);

Children's and adolescence up to 18 years (for capsules);

Hypersensitivity to the drug.

Use with caution in diseases of the liver and / or kidneys, especially for a long time.

Use during pregnancy and lactation.

The safety of Mildronate during pregnancy has not been proven. To avoid possible adverse effects on the fetus, the drug should not be administered during pregnancy.

It is not known whether the drug is excreted in breast milk. If it is necessary to use Mildronate during lactation, breastfeeding should be discontinued.

Special instructions for the use of Mildronate.

Use the drug with caution for a long time in patients with chronic diseases liver and kidneys.

Many years of experience in the treatment of acute myocardial infarction and unstable angina in cardiology departments shows that Mildronate is not a first-line drug for acute coronary syndrome.

Pediatric use

In children and adolescents under the age of 18 years, the efficacy and safety of Mildronate in the form of capsules and injection solution has not been established.

Influence on the ability to drive vehicles and control mechanisms

Data on the adverse effects of Mildronate on the speed of the psychomotor reaction are not available.

Drug overdose:

Cases of overdose of Mildronate are not described, the drug is of low toxicity and does not cause side effects dangerous to the health of patients.

Interaction of Mildronate with other drugs.

When used together, Mildronate enhances the effect of antianginal drugs, some antihypertensive drugs, cardiac glycosides.

Mildronate can be combined with antianginal agents, anticoagulants and antiplatelet agents, antiarrhythmic agents, diuretics, bronchodilators.

When combined with Mildronate nitroglycerin, nifedipine, alpha-blockers, antihypertensives and peripheral vasodilators, moderate tachycardia, arterial hypotension may develop (care should be taken when using this combination).

Conditions of sale in pharmacies.

The drug is dispensed by prescription.

Terms of the storage conditions of the drug Mildronate.

Capsules should be stored in a dry place at a temperature not exceeding 25°C. Solution for injection - at a temperature not exceeding 25 ° C; do not freeze. Shelf life - 4 years.

The drug should be stored out of the reach of children.

LS-001115-120511

Tradename:

MILDRONAT ®

International non-proprietary name (INN):

meldonium

Dosage form:

capsules

Compound

1 capsule contains:
active substance: meldonium dihydrate - 500 mg;
Excipients: potato starch - 27.2 mg, colloidal silicon dioxide - 10.8 mg, calcium stearate - 5.4 mg;
capsule(body and cap): titanium dioxide (E 171) - 2%, gelatin - 98%.

Description
No. 00 hard gelatin capsules, white body and cap. The content is a white crystalline powder with a slight odor. The powder is hygroscopic.

Pharmacotherapeutic group:

metabolic agent

ATX code: C01EB

Pharmacological properties

Pharmacodynamics
Meldonium is a synthetic analogue of gamma-butyrobetaine, a substance found in every cell of the human body. Inhibits gamma butyrobetainehydrooxinase, reduces carnitine synthesis and transport of long-chain fatty acids through cell membranes, prevents the accumulation in cells of activated forms of unoxidized fatty acids - derivatives of acylcarnitine and acylcoenzyme A.
Cardioprotective agent that normalizes myocardial metabolism. Under conditions of ischemia, meldonium restores the balance between the processes of oxygen delivery and its consumption in cells, prevents a violation of the transport of adenosine triphosphate (ATP); at the same time, it activates glycolysis, which proceeds without additional oxygen consumption. As a result of a decrease in the concentration of carnitine, gamma-butyrobetaine, which has vasodilating properties, is intensively synthesized. The mechanism of action determines the diversity of its pharmacological effects: increased efficiency, reduced symptoms of mental and physical overstrain, activation of tissue and humoral immunity, cardioprotective effect. In the case of acute ischemic damage to the myocardium, meldonium slows down the formation of a necrotic zone and shortens the rehabilitation period.
In heart failure, it increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation, it improves blood circulation in the focus of ischemia, promotes the redistribution of blood in favor of the ischemic area.
Effective in the case of vascular and degenerative pathology of the vessels of the fundus. Also characteristic is a tonic effect on the central nervous system, elimination functional disorders somatic and autonomic nervous systems in patients with chronic alcoholism with withdrawal syndrome.

Pharmacokinetics
After oral administration, meldonium is rapidly absorbed, bioavailability is 78%. The time to reach maximum plasma concentration is 1-2 hours after ingestion. It is metabolized mainly in the liver with the formation of two main metabolites, which are excreted by the kidneys. The half-life (T 1/2) when taken orally depends on the dose, is 3-6 hours.

Indications for use

In complex therapy coronary disease heart (angina pectoris, myocardial infarction), chronic heart failure and dishormonal cardiomyopathy, as well as in the complex therapy of subacute and chronic disorders of the blood supply to the brain (after a stroke, cerebrovascular insufficiency).
Reduced performance; mental and physical overload (including athletes).
Withdrawal syndrome in chronic alcoholism (in combination with specific therapy).

Contraindications

Hypersensitivity to the active substance and other components of the drug, increased intracranial pressure (in violation of venous outflow, intracranial tumors), age under 18 years (efficacy and safety have not been established), pregnancy, lactation.

Carefully:
with diseases of the liver and / or kidneys.

Dosage and administration

In view of the possible development of an exciting effect, it is recommended to use in the first half of the day and no later than 17.00 when taken several times a day.
1. Ischemic heart disease (angina pectoris, myocardial infarction), chronic heart failure and dishormonal cardiomyopathy
As part of complex therapy, 500 mg - 1 g per day orally, using the entire dose at once or dividing it into 2 times. The course of treatment is 4-6 weeks.
Dishormonal cardiomyopathy - as part of complex therapy, 500 mg orally per day. The course of treatment is 12 days.
2. Subacute and chronic disorders of the blood supply to the brain (after a stroke, cerebrovascular insufficiency)
As part of complex therapy, after the end of the course of injection therapy with Mildronate ® , the drug is continued to be taken orally at 500 mg - 1 g per day, using the entire dose at once or dividing it into 2 times. The course of treatment is 4-6 weeks.
In chronic disorders - as part of complex therapy, 500 mg orally per day. The general course of treatment is 4-6 weeks.
Repeated courses (usually 2-3 times a year) are possible after consultation with a doctor.
3. Reduced performance; mental and physical overload (including athletes)
Adults - inside 500 mg 2 times a day. The course of treatment is 10-14 days. If necessary, the treatment is repeated after 2-3 weeks.
Athletes 500 mg - 1 g orally 2 times a day before training. Duration of the course in the preparatory training period - 14 - 21 days, during the competition - 10 -14 days.
4. Withdrawal syndrome in chronic alcoholism (in combination with specific therapy)
Inside, 500 mg 4 times a day. The course of treatment - 7 - 10 days.

Side effect

Rarely - allergic reactions (redness and itching of the skin, skin rash, urticaria, angioedema), as well as dyspepsia, tachycardia, decrease or increase blood pressure, increased excitability. Very rarely - eosinophilia, general weakness.

Overdose

Symptoms: decrease in blood pressure, accompanied by headache, tachycardia, dizziness and general weakness.
Treatment: symptomatic.

Interaction with other drugs
Enhances the effect of coronary dilating agents, some antihypertensive agents, cardiac glycosides. Can be combined with prolonged forms of nitrates, other antianginal agents, anticoagulants, antiplatelet agents, antiarrhythmic agents, diuretics, bronchodilators.
In view of the possible development of tachycardia and arterial hypotension, caution should be exercised when combined with nitroglycerin (for sublingual use) and antihypertensive drugs (especially alpha-blockers and short-acting forms of nifedipine).

special instructions

Patients with chronic diseases of the liver and kidneys should be careful with prolonged use of the drug.
There are no sufficient data on the use of the drug Mildronate ® in children under 18 years of age.

Pregnancy and lactation

The safety of the drug during pregnancy has not been established. To avoid possible adverse effects on the fetus, the use of Mildronate® during pregnancy is not recommended.
It is not known whether meldonium is excreted in breast milk. If treatment with Mildronate ® is necessary for the mother, then breastfeeding is stopped.

Impact on ability to drive vehicles and mechanisms
There is no data on the adverse effect of the drug Mildronate ® on the ability to drive vehicles and mechanisms.

Release form

Capsules 500 mg. 10 capsules in a blister pack made of polyvinyl chloride film with polyvinylidene chloride coating and aluminum foil.
2 or 6 blister packs together with instructions for use are placed in a cardboard box.

Storage conditions

Store in a dry place at a temperature not exceeding 25 °C.
Keep out of the reach of children.

Best before date

4 years.
Do not use after the expiry date stated on the packaging.

Terms of dispensing from pharmacies

On prescription.

Manufacturer

JSC "Grindeks" st. Krustpils 53, Riga, LV-1057, Latvia

Organization accepting claims: representative office in Moscow
Representative office address: 123242, Moscow, st. B. Gruzinskaya, 14, room. board 2.

  • Instructions for use Mildronate
  • Ingredients of Mildronate
  • Indications for Mildronate
  • Storage conditions of the drug Mildronate
  • Shelf life of the drug Mildronate

Release form, composition and packaging

caps. 250 mg: 40 pcs.
Reg. No: 1352/95/99/2000/05/10 of 06/04/2010 - Valid

Capsules

Excipients:

The composition of the capsule shell:

10 pieces. - blisters (4) - packs.

caps. 500 mg: 20 or 60 pcs.
Reg. No: 7304/05/10 dated 04/27/2010 - Valid

Capsules hard gelatin, white; the content of the capsules is a white crystalline powder with a slight odor, hygroscopic.

Excipients: dried potato starch, silicon dioxide, calcium stearate.

The composition of the capsule shell: titanium dioxide (E171), gelatin.

10 pieces. - blisters (2) - packs.
10 pieces. - blisters (6) - packs.



Injection transparent, colorless.

Excipients: water d / i.

solution for injections. 500 mg/5 ml: amp. 10 pieces.
Reg. No: 7397/95/99/2000/05/09/10 dated 07/29/2010 - Valid

Injection transparent, colorless.

Excipients: water d / i.

5 ml - ampoules (5) - plastic blister packs (2) - cardboard packs.

Description medicinal product MILDRONAT based on officially approved instructions for use of the drug and made in 2009. Date of update: 01/29/2009


pharmachologic effect

A drug that improves metabolism. It is a structural analogue of the carnitine precursor gamma-butyrobetaine (GBB), in which one hydrogen atom is replaced by a nitrogen atom.

It is assumed that there are 2 mechanisms of action of Mildronate on the body

1. Effect on carnitine synthesis

As a result of the inhibition of the activity of butyrobetaine hydroxylase, Mildronate reduces the biosynthesis of carnitine and inhibits the transport of long-chain fatty acids through the cell membrane, preventing the accumulation in cells of activated derivatives of unoxidized fatty acids - acylcarnitine and acylcoenzyme A, which have pronounced detergent properties. Under conditions of ischemia, Mildronate restores the balance between the delivery and consumption of oxygen in cells, eliminates ATP transport disorders, while activating an alternative energy source - glycolysis, which is carried out without additional oxygen consumption.

With an increased load as a result of intensive energy consumption in the cells of a healthy body, a temporary decrease in the content of fatty acids, mainly carnitine, occurs. It is known that the biosynthesis of carnitine is regulated by its level in blood plasma and stress, but does not depend on the concentration of carnitine precursors in the cell. Since Mildronate inhibits the conversion of GBB to carnitine, this leads to a decrease in the level of carnitine in the blood, which in turn activates the synthesis of the carnitine precursor - GBB.

With a decrease in the concentration of Mildronate, the process of carnitine biosynthesis is restored and the concentration of fatty acids in the cell is normalized. Thus, cells undergo regular training, which contributes to their survival in conditions of increased stress, in which the content of fatty acids in them regularly decreases, and when the load decreases, the content of fatty acids is quickly restored. Under conditions of real overload, cells "trained" with Mildronate survive in those conditions when "untrained" cells die.

2. Function of the mediator of the hypothetical GBB-ergic system

It is hypothesized that there is a previously undescribed system of transmission of nerve impulses in the body - the GBB-ergic system, which ensures the transmission of nerve impulses to somatic cells. The mediator of this system is the immediate precursor of carnitine, the GBB ester. As a result of the action of esterase, this neurotransmitter gives up an electron to the cell, thus transferring an electrical impulse, and itself turns into GBB.

Synthesis of GBB is possible in any somatic cell of the body. Its speed is regulated by the intensity of the stimulus and energy expenditure, which in turn depend on the concentration of carnitine. Therefore, with a decrease in the concentration of carnitine, the synthesis of GBB is stimulated. With an increase in the concentration of the mediator (HBB ester) in any place in the body, with the participation of the central nervous system, regulatory mechanisms are activated that are "responsible" for it.

Thus, there is an economical chain of reactions in the body that provides an adequate response to irritation or stress:

  • it starts with receiving a signal from nerve fibers(in the form of an electron), followed by the synthesis of GBB and its ester, which, in turn, transfers the signal to the membranes of somatic cells. Somatic cells, in response to irritation, synthesize new molecules, ensuring signal propagation. After that, the hydrolyzed form of GBB, with the participation of active transport, enters the liver, kidneys and testes, where it turns into carnitine.

As mentioned earlier, Mildronate is a structural analogue of GBB, in which one hydrogen atom is replaced by a nitrogen atom. Since Mildronate can be exposed to the action of GBB-esterase, it can act as a hypothetical "mediator". However, GBB-hydroxylase does not act on mildronate, and therefore, when it is introduced into the body, the concentration of carnitine does not increase, but decreases. Due to the fact that Mildronate itself acts as a "mediator" of stress, and also increases the content of GBB, it contributes to the development of the body's response. As a result, the overall metabolic activity also increases in other systems, such as the central nervous system.

Results of experimental studies

In experiments on anesthetized cats, the effect of mildronate on the performance of the cardiovascular system was studied. It has been established that in a wide range of doses, the drug increases volumetric blood flow, systolic and minute volumes, does not have a significant effect or slightly lowers venous pressure. These data indicate a positive effect of Mildronate on the contractile function of the myocardium.

Mildronate has a protective effect in myocardial hypoxia. In experiments on isolated rabbit atria, it was found that after the cessation of hypoxic exposure, the drug accelerates the restoration of myocardial contractility to a normal level.

In another series of experiments on anesthetized white rats, it was found that the introduction of Mildronate before the start of the experiment eliminates the increase in ischemia (ST segment elevation) after ligation of the left coronary artery, reduces the corresponding focus of infarction and increases the life expectancy of animals. With repeated administration of the drug for 10 days, a pronounced (more than 2 times compared with the control) decrease in the focus of infarction was found.

Mildronate is more effective than nifedipine in preventing the development of disorders heart rate, including ventricular fibrillation, in rats after coronary artery ligation.

In conditions of "facilitated" experimental myocardial infarction (ligation of the left coronary artery for ≤1 h) in dogs, the drug eliminates ischemic ECG changes.

Mildronate protects the myocardium from the damaging effects of catecholamines and alcohol.

In experiments on rats, it was found that the preliminary administration of Mildronate in 50% of animals completely eliminates ECG changes caused by isoproterenol (izadrin) and epinephrine (adrenaline). Histological examination myocardium of rats indicates that in the case of the use of epinephrine, mildronate protects myocardial cells, prevents the development of irreversible changes in cardiomyocytes and helps restore the normal structure of the myocardium.

AT experimental studies It was found that toxic concentrations of ethanol caused by myocardial damage do not differ in principle from those caused by ischemia or stress. It can be assumed that this is due to the similarity of the mechanisms of action of factors affecting myocardial tissues. The data that Mildronate reduces myocardial damage caused by ethyl alcohol justifies the use of the drug for the correction of functional and organic disorders of the body in chronic alcohol intoxication.

It has been experimentally established that Mildronate reduces the stimulating effect of ethyl alcohol by about 5 times. Under conditions of "free choice", mildronate reduces the consumption of ethyl alcohol by 80-100% in experimental animals.

In experiments on animals, an antihypoxic and cerebral blood flow-improving effect of the drug was observed. It has been established that Mildronate has a positive effect in ischemia of the brain tissue. The drug optimizes the distribution of cerebral blood flow in favor of ischemic foci, increases the resistance of neurons to hypoxia. So, in experiments on rats, the drug partially or completely eliminated EEG changes after occlusion. carotid artery. Mildronate has an activating effect on the central nervous system:

  • motor activity and physical performance increase, stimulation of motor reactions was noted, as well as an anti-stress effect, manifested in the stimulation of the sympathetic nervous system, an increase in the content of catecholamines in the brain and adrenal glands, and a protective effect against stress-induced changes in internal organs.

The obtained results of experimental studies indicate the effectiveness of Mildronate and the possibility of its use in cerebrovascular pathology.

Results of clinical studies

Analysis of clinical data on the course treatment of stable angina pectoris with Mildronate indicates that under the influence of the drug the frequency and intensity of attacks are reduced, and the amount of nitroglycerin used is also reduced. The drug has a pronounced antiarrhythmic effect in the presence of coronary artery disease and ventricular extrasystoles and less effective in supraventricular extrasystoles. special attention deserves the ability of the drug to reduce oxygen consumption at rest, which is considered an indicator of the effectiveness of antianginal treatment of coronary artery disease. Mildronate has a beneficial effect on atherosclerotic processes in the coronary and other peripheral vessels as a result of lowering the level of total cholesterol in the blood plasma and the atherogenic index.

The role of Mildronate in the treatment of chronic heart failure due to coronary artery disease has been analyzed on the basis of a fairly large number of clinical studies that indicate that the drug increases exercise tolerance and the amount of work performed by patients suffering from heart failure.

In a separate study of the Latvian and Tomsk Institutes of Cardiology, the effectiveness of Mildronate in heart failure was studied. medium degree severity (II functional class according to NYHA classification). After treatment with Mildronate, 59-78% of patients with an initial diagnosis of heart failure of functional class II were assigned to group I of functional class.

It has been established that Mildronate improves the inotropic function of the myocardium and increases exercise tolerance, improves the quality of life of patients without causing severe side effects. It is noted, however, that Mildronate can cause moderate arterial hypotension, allergic skin reactions, headache, discomfort in the stomach. In severe heart failure, Mildronate should be administered in combination with traditional means used to treat this disease.

Good clinical effect Mildronate appeared in patients with cardialgia, which developed as a result of menopause and alimentary obesity.

In clinical conditions, it has been established that the treatment with Mildronate reduces the frequency of relapses of alcoholism. It is shown that Mildronate allows to stop the alcohol withdrawal syndrome.

Mildronate is effective tool complex treatment acute and chronic disorders of cerebral circulation (ischemic stroke, chronic insufficiency cerebral circulation). It has been established that Mildronate normalizes the tone and resistance of capillaries and arterioles of the brain, restores their reactivity.

The effect of Mildronate on the process of rehabilitation of patients with neurological disorders (after past cerebrovascular diseases, brain surgery, tick-borne encephalitis) was studied.

The results of testing the therapeutic efficacy indicate a positive, dose-dependent effect of the drug on the restoration of physical performance and functional independence of patients during the recovery period. When analyzing changes in individual and integral intellectual functions, it was revealed positive influence Mildronate on the process of restoring intellectual functions during the rehabilitation period. It was found that Mildronate improves the quality of life of convalescents (mainly as a result of the restoration of physical functions), and also contributes to the elimination of mental disorders in patients.

During the rehabilitation period, Mildronate has a positive effect on the regression of disorders of the nervous system in patients with neurological deficits. The general neurological condition of patients improves (reduction of brain damage and pathology of reflexes, regression of paresis, improvement of coordination of movements and autonomic functions).

In the clinic and practice of sports medicine, experimental data have been confirmed on the ability of Mildronate to increase performance and accelerate the recovery of performance after intensive physical activity. These features of the action of the drug are characterized by an improvement in the tolerance of training loads, the elimination of a feeling of fatigue, a surge of vivacity. In addition, the drug reduces emotional and mental stress (the disappearance of apathy and irritability after stress in training and competitions).

Toxicological characterization

Mildronate has low toxicity. When administered to mice and rats active ingredient orally, the LD 50 value exceeded 18,000 mg/kg. Repeated administration of mildronate to rats and dogs for 6 months did not cause adverse changes in body weight, blood composition, biochemical indicators animal blood and urine. In high doses, Mildronate caused hemorrhages in the liver and kidneys in dogs, without affecting the functions of these organs.

When studying the specific toxicity of Mildronate, teratogenic and embryotoxic effects were not observed. The drug has no mutagenic and carcinogenic properties. In experiments on animals, an allergenic effect was not detected.

Pharmacokinetics

Pharmacokinetics studied in experimental animal studies when administered orally, intramuscularly or intravenously active substance labeled with the radioactive isotope 14 C.

Suction

Cmax of the active substance in blood plasma was reached within 1-2 hours after administration. The bioavailability of the drug when administered orally is 78%.

Metabolism

The active substance undergoes biotransformation:

  • 2 metabolites were identified in the urine of experimental animals. The intensity of drug metabolism is evidenced by the fact that most of the 14 C is released with exhaled air in the form of 14 CO 2 . In various tissues of experimental animals, radioactivity (as 14 C ) persisted for a long time (more than 4 weeks). It is possible that this indicates the incorporation of metabolites into animal tissues.

breeding

Renal excretion plays an important role in the elimination of Mildronate and its metabolites.

On the elimination curve of radioactive products, 2 phases can be distinguished: a fast α-phase and a slow β-phase, which, apparently, are associated with different kinetics of the active substance and its metabolites. In rabbits after oral administration drug T 1/2 in the α-phase is 2.1 hours, in the β-phase - 21 hours, after i / v administration - 0.7 and 14.8 hours, respectively. In dogs, after intravenous administration, T 1/2 in the α-phase is 1.3 hours, in the β-phase - 14.3 hours

Indications for use

  • as part of the complex therapy of IHD (angina pectoris, myocardial infarction), chronic heart failure, dyshormonal cardiomyopathy;
  • as part of the complex therapy of acute and chronic disorders of cerebral circulation (strokes and cerebrovascular insufficiency);
  • hemophthalmos, retinal hemorrhages of various etiologies;
  • thrombosis of the central retinal vein and its branches;
  • retinopathy of various etiologies (diabetic, hypertensive);
  • withdrawal syndrome in chronic alcoholism (in combination with specific alcoholism therapy);
  • reduced performance;
  • physical overstrain (including athletes).

Dosing regimen

In connection with the possibility of developing an exciting effect, the drug is recommended to be used in the morning.

At cardiovascular diseases as part of complex therapy, the drug is prescribed at 0.5-1 g / day orally or intravenously (5-10 ml of injection solution with a concentration of 500 mg / 5 ml), the frequency of use is 1-2 times / day. The duration of the course of treatment is from 4 to 6 weeks.

At cardialgia on the background of dyshormonal myocardial dystrophy Mildronate is administered orally at 250 mg 2 times / day. The duration of the course of treatment is 12 days.

At cerebrovascular accident in the acute phase, the drug is prescribed intravenously at 500 mg 1 time / day for 10 days, then they switch to taking the drug orally at 0.5-1 g / day (taking the entire dose at once or dividing into 2 doses). The duration of the general course of therapy is from 4 to 6 weeks.

At chronic disorders cerebral circulation, the drug is taken orally at a dose of 0.5-1 g / day. The duration of the general course of therapy is from 4 to 6 weeks. Repeated courses are prescribed individually after consulting a doctor 2-3 times a year.

At vascular pathology and degenerative diseases of the retina Mildronate is administered parabulbarno in 0.5 ml injection solution at a concentration of 500 mg/5 ml for 10 days.

When Mildronate is administered orally at 250 mg 4 times / day or intravenously at 0.5 g 1 time / day. The duration of the course of treatment is from 10 to 14 days. If necessary, therapy is repeated after 2-3 weeks.

At chronic alcoholism the drug is prescribed orally at 500 mg 4 times / day, in / in - 500 mg 2 times / day. The duration of the course of treatment is from 7 to 10 days.

special instructions

Use with caution for a long time in patients with chronic liver and kidney disease.

Many years of experience in the treatment of acute myocardial infarction and unstable angina in cardiology departments shows that Mildronate is not a first-line drug for acute coronary syndrome.

Pediatric use

Data on the use of Mildronate in children is not enough.

Influence on the ability to drive vehicles and control mechanisms

There are no data on the adverse effects of Mildronate on the speed of psychomotor reactions.

drug interaction

With simultaneous use enhances the effect of coronary dilators, antihypertensive drugs, cardiac glycosides.

Mildronate can be combined with antianginal agents, anticoagulants, antiplatelet agents, antiarrhythmic agents, diuretics, bronchodilators.

In view of the possible development of moderate tachycardia and arterial hypotension, caution should be exercised when combined with nitroglycerin, nifedipine, alpha-blockers, antihypertensives and peripheral vasodilators.

Contacts for appeals

GRINDEX JSC, representative office, (Latvia)

Mildronate 500 is a remedy designed to eliminate many health problems. It mainly has a metabolic effect.

Mildronate 500 is a remedy designed to eliminate many health problems.

Release form and composition

The drug is produced in the form of capsules and tablets. 1 capsule contains 500 mg of meldonium dihydrate and excipients. 1 tablet includes 500 mg of meldonium phosphate and additional elements that contribute to better absorption of the active substance.

Mildronate can also be purchased by the patient in the form of a solution for intramuscular, intravenous and parabulbar administration.

Injections of the drug are used in especially severe clinical cases (for example, with retinal disorders).

pharmachologic effect

The active substance is similar to gamma-butyrobetaine, which is found in every cell of the human body.

The agent has a cardioprotective effect on myocardial metabolism. Due to the activity of the drug, a violation of ATP transport is prevented, glycolysis is activated.

The concentration of carnitine falls, as a result of which gamma-butyrobetaine is intensively produced and vasodilating effects appear. Among others, one can note an increase in working capacity, a decrease in overstrain (both physical and mental). It is useful to take medicine to eliminate problems with blood circulation. It has a tonic effect on the central nervous system.

After the patient takes the medicine inside, it is quickly absorbed, the bioavailability is 78%. The highest concentration in the blood plasma can be fixed 1-2 hours after the tablet has been drunk. The breakdown takes place in the liver. The half-life is 3-6 hours.

Indications for use Mildronate 500

The appointment of the drug will be justified if the patient has a need for treatment of such conditions as:

  • withdrawal syndrome in chronic alcoholism (used as a component of complex therapy);
  • ischemic heart disease (angina pectoris and myocardial infarction);
  • dishormonal cardiomyopathy;
  • chronic heart failure;
  • disorders of the blood supply to the brain, occurring both subacutely and chronically.

The drug can be used during periods of increased physical exertion in athletes and to enhance mental performance.

Contraindications

You can not use the drug for therapeutic purposes if the patient suffers from at least one of the following conditions:

  • enlarged intracranial pressure(intracranial tumors and pathologies of venous outflow);
  • hypersensitivity to one of the components of the drug.

With caution, the appointment should be made if the patient has varicose veins, since this pathology refers to violations of the venous outflow. The same goes for serious illnesses liver or kidneys.

How to take Mildronate 500?

Most often, taking pills is prescribed by a doctor several times a day. It is preferable to drink tablets no later than 17:00, since the development of an exciting effect is likely.

In case of cerebral circulation disorders, therapy begins with injections, then a transition is made to capsules or tablets. The daily dose is 500 mg, treatment can last from 4 to 6 weeks.

In coronary heart disease, the dosage will be identical. It can be divided into 2 doses, if it is convenient for the patient.

In order to increase efficiency, adults are prescribed a remedy in the amount of 2 times a day (500 mg each). Treatment goes from 10 to 14 days. If necessary, therapy can be repeated after 2-3 weeks.

Athletes are shown to take 1 g 2 times a day immediately before the training process.

Withdrawal syndrome is treated by prescribing a dosage of 500 mg 4 times a day. The duration of treatment is 7-10 days.

All dosages indicated may be modified at the discretion of the doctor who is monitoring the patient.

Side effects of Mildronate 500

Adverse reactions become a rare occurrence if the patient takes this medicine in accordance with the dosage, which is recognized as optimal and safe for the body.

In some cases it may appear allergic reaction e.g. urticaria, angioedema, skin rash, itching and redness.

Possible dyspeptic phenomena, tachycardia, excitability, increase or decrease in blood pressure.

The most rare are eosinophilia and weakness in the patient.

Overdose

An increased dose can threaten the patient with a sharp drop blood pressure, which will be combined with a headache. Tachycardia, dizziness and a feeling of weakness in the patient become probable. It is necessary in this case to carry out symptomatic treatment.

special instructions

Required to take into account special instructions when using the medication.

Use during pregnancy and lactation

During childbearing and breastfeeding it is preferable to refrain from using meldonium. It can adversely affect the development of the fetus.

If during lactation the treatment with the remedy is recognized as essential, it is necessary to stop natural feeding and transfer the baby to artificial nutrition.

Use in children

Age up to 18 years becomes a contraindication for the use of the drug.

drug interaction

It is possible to combine the drug with diuretics, anticoagulants, bronchodilators and antiplatelet agents. Combination with nitroglycerin should be given with extra caution.

Terms and conditions of storage

Tablets are stored for 3 years, capsules - 4. The temperature should be at room temperature.

Terms of dispensing from pharmacies

Leave is carried out according to a medical prescription.

Price

The cost of the medicine is about 300 rubles, but may vary in different pharmacies. Capsules are often purchased in the amount of 60 pcs.

The mechanism of action of the drug Mildronate

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Analogues

Cardionate, Meldonium, Idrinol.

Which is better - Mildronate 250 or 500?

It is impossible to distinguish which of these drugs is better. They differ only in dosage. The most optimal dosage for the patient is prescribed at the discretion of the doctor who observes the patient and on this basis can conclude that it is advisable to use one or another remedy.