Mexidol Forte tablets p / o 250mg, No. 40

• consequences of acute disorders of cerebral circulation, including after transient ischemic attacks, in the phase of subcompensation as preventive courses;

• slight traumatic brain injury, the consequences of traumatic brain injury;

• encephalopathy of various origins (dyscirculatory, dysmetabolic, post-traumatic, mixed);

• vegetative dystonia syndrome;

• mild cognitive disorders of atherosclerotic genesis;

• anxiety disorders in neurotic and neurosis-like states;

• ischemic heart disease as part of complex therapy;

• relief of withdrawal symptoms in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, post-withdrawal disorders;

• conditions after acute intoxication with antipsychotic drugs;

• asthenic conditions, as well as for the prevention of the development of somatic diseases under the influence of extreme factors and loads;

• exposure to extreme (stress) factors.

Inside, 250 mg 3 times a day.
The initial dose is 250 mg (1 tablet) 1-2 times a day with a gradual increase to a therapeutic effect. The maximum daily dose is 750 mg (3 tablets).
Duration of treatment is 2-6 weeks; for relief of alcohol withdrawal - 5-7 days. The duration of the course of therapy in patients with ischemic heart disease is at least 1.5Ц2 months.
Repeated courses (on the recommendation of a doctor), preferably in the spring and autumn periods.

Active ingredient: ethylmethylhydroxypyridine succinate in terms of 100% substance - 250.0 mg.
Excipients: lactose monohydrate, povidone K-30, magnesium stearate.
Film casing: opadry II pink 33G240018 (hypromellose, titanium dioxide, lactose monohydrate, macrogol 4000, triacetin, iron dye red oxide, iron dye yellow oxide).

- Acute violations of liver and / or kidney function;

- increased individual sensitivity to the drug and its components;

- children's age (due to insufficient knowledge of the effect of the drug);

- pregnancy, breastfeeding (due to insufficient knowledge of the effect of the drug);

- lactose intolerance, lactase deficiency, glucose-galactose mapabsorption.

Trade name:

MexidolЃ FORTE 250

International non-proprietary or group name:

ethylmethylhydroxypyridine succinate

Chemical name:

2-ethyl-6-methyl-3-hydroxypyridine succinate

Dosage form:

film-coated tablets

Composition for 1 tablet:

Active ingredient: ethylmethylhydroxypyridine succinate in terms of 100% substance - 250.0 mg.
Excipients: lactose monohydrate, povidone K-30, magnesium stearate.
Film casing: opadry II pink 33G240018 (hypromellose, titanium dioxide, lactose monohydrate, macrogol 4000, triacetin, iron dye red oxide, iron dye yellow oxide).

Description:

round biconvex film-coated tablets of light pink color. In cross section, the core is almost white.

Pharmacotherapeutic group:

antioxidant agent.

ATX code:

N07XX.

Pharmacological properties:

Pharmacodynamics:
MexidolЃ FORTE 250 is an inhibitor of free radical processes, membrane protector with antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic effects. Belongs to the class of 3-hydroxypyridines.
The mechanism of action of MexidolЃ FORTE 250 is due to its antioxidant, antihypoxant and membrane-protective action. It inhibits lipid peroxidation, increases the activity of superoxide dismutase, increases the lipid-protein ratio, improves the structure and function of the cell membrane. The drug modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, gamma-aminobutyric acid (GABA), acetylcholine), which enhances their ability to bind to ligand-functional, helps to preserve the organization of biomembrane transport of neurotransmitters and improve synaptic transmission. MexidolЃ FORTE 250 increases the content of dopamine in the brain.It causes an increase in the compensatory activation of aerobic glycolysis and a decrease in the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in the content of adenosine triphosphate (ATP) and creatine phosphate, activation of the energy-synthesizing functions of mitochondria.
Increases the body's resistance to the effects of various damaging factors in pathological conditions (hypoxia and ischemia, impaired cerebral circulation, intoxication with ethanol and antipsychotics).
In conditions of a critical decrease in coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes - phosphodiesterase, adenylate cyclase, acetylcholinesterase. Supports the activation of aerobic glycolysis that develops during acute ischemia and promotes the restoration of mitochondrial redox processes under conditions of hypoxia, increases the synthesis of ATP and creatine phosphate. Provides the integrity of the morphological structures and physiological functions of the ischemic myocardium. Improves the clinical course of myocardial infarction, increases the effectiveness of therapy, reduces the incidence of arrhythmias and intracardiac conduction disorders. Normalizes metabolic processes in the ischemic myocardium, increases the antianginal activity of nitrates,improves the rheological properties of blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency.
Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.
Improves metabolism and blood supply to the brain, improves microcirculation and rheological properties of blood, reduces platelet aggregation. It stabilizes the membrane structures of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis. It has a hypolipidemic effect, reduces the content of total cholesterol and low density lipoproteins.
The antistress effect is manifested in the normalization of post-stress behavior, somatovegetative disorders, restoration of sleep-wakefulness cycles, impaired learning and memory processes, reduction of dystrophic and morphological changes in various structures of the brain.
MexidolЃ FORTE 250 has a pronounced antitoxic effect in case of withdrawal symptoms. It eliminates the neurological and neurotoxic manifestations of acute alcohol intoxication, restores behavioral disorders, autonomic functions, and is also able to relieve cognitive impairment caused by long-term ethanol intake and its cancellation. Under the influence of the drug, the effect of tranquilizing, neuroleptic, antidepressant, hypnotics and anticonvulsants is enhanced, which makes it possible to reduce their doses and reduce side effects.
MexidolЃ FORTE 250 improves the functional state of the ischemic myocardium. In conditions of coronary insufficiency, it increases collateral blood supply to the ischemic myocardium, contributes to the preservation of the integrity of cardiomyocytes and the maintenance of their functional activity. Effectively restores myocardial contractility in reversible cardiac dysfunction.

Pharmacokinetics:
It is rapidly absorbed when taken orally. The maximum concentration (Cmax) at doses of 400-500 mg is 3.5-4.0 ?g / ml. It is quickly distributed in organs and tissues. The average retention time (MRT) of the drug in the body when taken orally is 4.9-5.2 hours. It is metabolized in the liver by glucuron conjugation. 5 metabolites have been identified: 3-hydroxypyridine phosphate is formed in the liver, with the participation of alkaline phosphatase it breaks down into phosphoric acid and 3-hydroxypyridine; The 2nd metabolite is pharmacologically active, is formed in large quantities and is found in the urine for 1-2 days. after the introduction; 3rd - excreted in large quantities in the urine; 4th and 5th - glucuron conjugates. The half-life (T1 / 2) for oral administration is 2.0Ц2.6 hours. It is quickly excreted in the urine, mainly in the form of metabolites and in small quantities - unchanged.It is most intensively excreted during the first 4 hours after taking the drug. The indicators of excretion in the urine of unchanged drug and metabolites have individual variability.

Indications for use:

• consequences of acute disorders of cerebral circulation, including after transient ischemic attacks, in the phase of subcompensation as preventive courses;

• slight traumatic brain injury, the consequences of traumatic brain injury;

• encephalopathy of various origins (dyscirculatory, dysmetabolic, post-traumatic, mixed);

• vegetative dystonia syndrome;

• mild cognitive disorders of atherosclerotic genesis;

• anxiety disorders in neurotic and neurosis-like states;

• ischemic heart disease as part of complex therapy;

• relief of withdrawal symptoms in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders, post-withdrawal disorders;

• conditions after acute intoxication with antipsychotic drugs;

• asthenic conditions, as well as for the prevention of the development of somatic diseases under the influence of extreme factors and loads;

• exposure to extreme (stress) factors.

Contraindications:

- Acute violations of liver and / or kidney function;

- increased individual sensitivity to the drug and its components;

- children's age (due to insufficient knowledge of the effect of the drug);

- pregnancy, breastfeeding (due to insufficient knowledge of the effect of the drug);

- lactose intolerance, lactase deficiency, glucose-galactose mapabsorption.

Application during pregnancy and during breastfeeding:

MexidolЃ FORTE 250 is contraindicated during pregnancy and during breastfeeding.

Method of administration and dosage:

Inside, 250 mg 3 times a day.
The initial dose is 250 mg (1 tablet) 1-2 times a day with a gradual increase to a therapeutic effect. The maximum daily dose is 750 mg (3 tablets).
Duration of treatment is 2-6 weeks; for relief of alcohol withdrawal - 5-7 days. The duration of the course of therapy in patients with ischemic heart disease is at least 1.5Ц2 months.
Repeated courses (on the recommendation of a doctor), preferably in the spring and autumn periods.

Side effect:

The incidence of side effects was determined in accordance with the classification of the World Health Organization (WHO): very common (> 10%); often (> 1%, but <10%); infrequently (> 0.1%, but <1%); rarely (> 0.01%, but <0.1%); very rare (<0.01%); the frequency is unknown (the frequency cannot be determined from the available data).
Immune system disorders: very rarely angioedema, urticaria.
Mental disorders: very rarely - drowsiness. Nervous system disorders:
very rarely - headache.

Gastrointestinal disorders: very rarely - dry mouth, nausea, pain, burning sensation and discomfort in the epigastric region, heartburn, flatulence, diarrhea. Violations of the skin and subcutaneous tissues: very rarely - rash, itching, hyperemia.

Overdose:

Symptoms: drowsiness, insomnia.
Treatment: due to low toxicity, overdose is unlikely. Treatment, as a rule, is not required - the symptoms disappear on their own within 24 hours. With pronounced manifestations, supportive and symptomatic treatment is carried out.

Interaction with other medicinal products:

MexidolЃ FORTE 250 is compatible with all drugs used to treat somatic diseases.
Strengthens the effect of benzodiazepine drugs, antidepressants, anxiolytics, antiepileptic drugs (carbamazepine) and antiparkinsonian drugs (levodopa), nitrates. Reduces the toxic effect of ethanol.

The effect of the drug on the ability to drive vehicles or work with mechanisms:

during the period of taking the drug, care should be taken when working that requires the speed of psychophysical reactions (driving vehicles, mechanisms, etc.).

Release form:

film-coated tablets, 250 mg. 10 tablets, film-coated, in a blister strip made of polyvinyl chloride film and aluminum foil. 1, 2, 3, 4, 5, 6 blisters, together with instructions for use in a cardboard box.

Storage conditions:

store in a dark place at a temperature not exceeding 25 ? C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Vacation conditions:

dispensed by prescription.