3-hydroxy-6-methyl-2-ethylpyridine succinate

acute myocardial infarction — as part of complex therapy (from the first day of the disease)

ischemic stroke (as part of complex therapy)

dyscirculatory encephalopathy (including atherosclerotic origin)

mild and moderate cognitive disorders of various origins.

anxiety states in neurotic and neurosis-like states

vegetative-vascular dystonia

dyscirculatory encephalopathy

mild cognitive disorders of atherosclerotic origin

acute disorders of cerebral circulation (as part of combination therapy)

withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders

acute intoxication with antipsychotic drugs (as part of complex therapy).

acute disorders of cerebral circulation

dyscirculatory encephalopathy

vegetative-vascular dystonia

atherosclerotic disorders of the brain

neurotic and neurosis-like disorders with the manifestation of anxiety

relief of withdrawal syndrome in alcoholism with the presence of neurosis-like and vegetative-vascular disorders in the clinical picture, as well as acute intoxication with neuroleptics

in the complex treatment of acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis).

I / m or I / v (jet or drip).

In the treatment of acute myocardial infarction, I/v or I/m is administered for 14 days, against the background of traditional therapy for myocardial infarction, including nitrates, beta-blockers, ACE inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic agents as indicated.

In the first 5 days, to achieve maximum effect, the drug should be administered intravenously, in the next 9 days-intravenously.

Intravenous administration of the drug is carried out by drip infusion, slowly (to avoid side effects), on a saline solution or 5% dextrose (glucose) solution in a volume of 100-150 ml for 30-90 minutes. If necessary, a slow jet injection of the drug is possible, lasting at least 5 minutes.

Administration of the drug (intravenous or intravenous) is carried out 3 times a day, every 8 hours. The daily therapeutic dose is 6-9 mg/kg / day, a single dose is 2-3 mg/kg. The maximum daily dose should not exceed 800 mg, a single dose-250 mg.

In acute disorders of cerebral circulation (ischemic stroke) 3-hydroxy-6-methyl-2-ethylpyridine succinate® is used in complex therapy in the first 2-4 days of IV, drip 200-300 mg 2-3 times a day, then-in / m 100 mg 3 times a day. The duration of treatment is 10-14 days. In the future, the drug is prescribed in capsules of 100 mg 2 times a day for 14 days and 100 mg 3 times a day for the next 7 days. The frequency and duration of repeated courses of therapy is determined by the doctor.

In dyscirculatory encephalopathy in the decompensation phase of 3-hydroxy-6-methyl-2-ethylpyridine succinate® should be administered intravenously or drip at a dose of 100 mg 2-3 times a day for 14 days. Then the drug is administered in / m at 100 mg per day for the next 2 weeks. In the future, the drug is prescribed in capsules of 100 mg 2-4 times a day (on the recommendation of a doctor), the frequency and duration of therapy courses is determined by the doctor.

For the course prevention of dyscirculatory encephalopathy, the drug is administered in / m at a dose of 100 mg 2 times a day for 10-14 days.

For the treatment of mild to moderate cognitive disorders, 3-hydroxy-6-methyl-2-ethylpyridine succinate® is prescribed in/m at a dose of 100-300 mg per day for 14 days. If necessary, in the future, the drug is prescribed in capsules of 100 mg 2-4 times a day (on the recommendation of a doctor), the frequency and duration of therapy courses is determined by the doctor.

Inside 125-250 mg 3 times a day. The initial dose is 125-250 mg (1-2 tablets) 1-2 times a day with a gradual increase until a therapeutic effect is obtained. The maximum daily dose is 750 mg (6 tablets). The duration of treatment is 2-6 weeks.

Treatment of withdrawal syndrome (complex therapy) — по 250–500 мг 3 раза в сутки.

Treatment is stopped gradually, reducing the dose for 2-3 days.

Solution for intravenous and intramuscular administration

V / m, v / v (струйно или капельно). Дозы подбирают индивидуально. При инфузионном способе введения препарат следует разводить в физиологическом растворе натрия хлорида. Начинают лечение с дозы 50–100 мг 1–3 раза в сутки, постепенно повышая дозу до получения терапевтического эффекта. Струйно препарат 3-hydroxy-6-methyl-2-ethylpyridine succinate^® вводят медленно в течение 5–7 мин, капельно — со скоростью 40–60 капель в минуту. Максимальная суточная доза не превышает 800 мг.

In acute disorders of cerebral circulation (в комплексной терапии): в первые 2–4 дня — в/в капельно по 200–300 мг/сут, затем — в/м по 100 мг 3 раза в сутки. Продолжительность лечения — 10–14 сут.

In case of dyscirculatory encephalopathy in the decompensation phase: в/в струйно или капельно в дозе 100 мг 2–3 раза в сутки на протяжении 14 дней. Затем препарат вводят в/м по 100 мг/сут на протяжении последующих 2 нед. Для курсовой профилактики дисциркуляторной энцефалопатии препарат вводят в/м в дозе 100 мг 2 раза в сутки на протяжении 10–14 дней.

In mild cognitive impairment in elderly patients and in anxiety disorders: препарат применяют в/м в суточной дозе 100–300 мг на протяжении 14–30 дней.

With alcohol withdrawal syndrome: в/м в дозе 100–200 мг 2–3 раза в сутки или в/в капельно 1–2 раза в сутки в течение 5–7 дней.

In acute intoxication with antipsychotic drugs: в/в в дозе 50–300 мг/сут на протяжении 7–14 дней.

Film-coated tablets

Inside. Применяемые терапевтические дозы и продолжительность лечения определяются чувствительностью больных к препарату. Начинают лечение с дозы 0,25–0,5 г; средняя суточная доза составляет 0,25–0,5 г, максимальная — 0,8 г. Суточную дозу препарата распределяют на 2–3 приема в течение дня.

For the treatment of patients with anxiety disorders, autonomic vascular dysfunction and cognitive impairment препарат 3-hydroxy-6-methyl-2-ethylpyridine succinate^® применяют в течение 2–6 нед.

When relief of alcohol withdrawal syndrome препарат 3-hydroxy-6-methyl-2-ethylpyridine succinate^® применяют в течение 5–7 дней.

Course therapy with 3-hydroxy-6-methyl-2-ethylpyridine succinate® is completed gradually, reducing the dose over 2-3 days.

I / m or I / v (jet or drip). For intravenous administration, water for injection is used as a solvent. Jet mexidol is administered for 5-7 minutes, drip-at a rate of 60 drops per minute. The doses are selected individually.

Start treatment with a dose of 0.05-0.1 g 1-3 times a day, gradually increasing the dose until a therapeutic effect is obtained. The duration of treatment and the choice of individual dose depends on the severity of the patient's condition and the effectiveness of treatment. The maximum daily dose should not exceed 0.8 g.

For the treatment of atherosclerotic dementia in elderly patients, mexidol is prescribed in / m at a dose of 0.1–0.3 g/day.

In acute intoxication with neuroleptics, the drug is injected into the vein at a dose of 0.5–0.3 g/day.

In the complex treatment of acute purulent-inflammatory processes of the abdominal cavity (acute destructive pancreatitis, peritonitis), mexidol is prescribed in a single dose of 200 mg 3 times a day. In severe cases, the drug is diluted in 200 ml of a physiological 0.9% sodium chloride solution and administered at a rate of 40-60 drops per minute. With a lighter course of the disease, mexidol is administered in/m. The course of treatment is 3-10 days.

hypersensitivity to the drug

acute disorders of liver and kidney function

pregnancy

breastfeeding period

age under 18 (efficacy and safety not established).

hypersensitivity to the drug

acute liver failure

acute renal failure

lactose intolerance, lactase deficiency, and glucose-galactose malabsorption syndrome

children's age.

hypersensitivity or intolerance to the drug

acute disorders of liver and kidney function.

At/in the introduction, especially inkjet, it may cause dry mouth and metallic taste, the feeling of warmth spreading throughout the body, sore throat and discomfort in the chest, feeling of shortage of air. As a rule, these phenomena are associated with an excessively fast rate of administration of the drug and are transient in nature.

Against the background of prolonged administration of the drug, the following side effects may occur:

From the gastrointestinal tract: тошнота, метеоризм.

From the central nervous system: нарушения сна (сонливость или нарушение засыпания).

From the digestive system: nausea, dryness of the oral mucosa, diarrhea.

Other: аллергические реакции, сонливость.

Nausea and dry mouth may occur.

Due to the low toxicity of the drug, an overdose is unlikely.

Symptoms: нарушение сна (бессонница), в редких случаях — незначительное и кратковременное (до 1,5–2 ч) повышение АД.

Treatment: развитие симптомов передозировки, как правило, не требует применения купирующих средств, указанные симптомы нарушения сна исчезают самостоятельно в течение суток. В особо тяжелых случаях рекомендуется применение одного из снотворных и анксиолитических средств для приема внутрь (нитразепам 10 мг, оксазепам 10 мг или диазепам 5 мг). При чрезмерном повышении АД — назначение гипотензивных средств (под контролем АД).

Symptoms: with an overdose, sleep disorders are possible (insomnia, in some cases — drowsiness).

Treatment: как правило, не требуется — симптомы исчезают самостоятельно в течение суток. В тяжелых случаях при бессоннице — назначение нитразепама в дозе 10 мг, оксазепама — 10 мг или диазепама — 5 мг. При чрезмерном повышении АД — назначение гипотензивных ЛС под контролем АД.

3-hydroxy-6-methyl-2-ethylpyridine succinate ® improves the functional state of the ischemic myocardium in myocardial infarction, improves the contractile function of the heart, and reduces the manifestations of systolic and diastolic dysfunction of the left ventricle. The action of the drug is based on its antioxidant activity, the ability to inhibit free radical processes (pronounced intensification of which is observed in ischemia and myocardial necrosis, especially during reperfusion) and reduce the damaging effect of free radicals on cardiomyocytes. Under conditions of critical decrease in coronary blood flow, 3-hydroxy-6-methyl-2-ethylpyridine succinate® helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes — PDE, adenylate cyclase, acetylcholinesterase. The drug supports the activation of aerobic glycolysis that develops in acute ischemia and promotes the restoration of mitochondrial redox processes in hypoxia, increases the synthesis of ATP and creatine phosphate. These mechanisms ensure the integrity of the morphological structures and physiological functions of the ischemic myocardium.

3-hydroxy-6-methyl-2-ethylpyridine succinate ® improves the clinical course of myocardial infarction, increases the effectiveness of therapy, accelerates the restoration of the functional activity of the left ventricular myocardium, reduces the frequency of arrhythmic complications and disorders of intracardiac conduction. The drug normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and / or improves the electrical activity and contractility of the myocardium, as well as increases coronary blood flow in the ischemic zone, increases the antianginal activity of nitropreparations, improves the rheological properties of blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency

3-hydroxy-6-methyl-2-ethylpyridine succinate® has a neuroprotective effect, increases the stability of blood circulation in the brain under hypoperfusion, prevents a decrease in blood flow to the brain in the reperfusion period after ischemia. The drug helps to adapt to the damaging effect of ischemia, inhibiting the depletion of carbohydrate reserves, blocking the postischemic drop in the utilization of glucose and oxygen by the brain and preventing the progressive accumulation of lactate.

3-hydroxy-6-methyl-2-ethylpyridine succinate® improves and stabilizes brain metabolism and blood supply to the brain, improves blood rheological properties and microcirculation. The drug supports the functional activity of the brain, both during ischemia and in the post-ischemic period. 3-hydroxy-6-methyl-2-ethylpyridine succinate® has a selective, not accompanied by sedation and muscle relaxation, anxiolytic effect, eliminates anxiety, fear, tension, anxiety.

3-hydroxy-6-methyl-2-ethylpyridine succinate® has nootropic properties, prevents and reduces learning and memory disorders that occur in vascular diseases of the brain (ischemic stroke, dyscirculatory encephalopathy), in mild and moderate cognitive disorders, has an antihypoxic effect, increases concentration and performance.

The inclusion of the drug 3-hydroxy-6-methyl-2-ethylpyridine succinate® in the complex therapy of patients with acute circulatory disorders of the brain reduces the severity of clinical manifestations of stroke and improves the course of the rehabilitation period.

3-hydroxy-6-methyl-2-ethylpyridine succinate® is an inhibitor of free radical processes, a membrane protector. It also has antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic effects. It belongs to the class of 3-oxypyridines.

Mechanism of action of 3-hydroxy-6-methyl-2-ethylpyridine succinate® is due to its antioxidant and membrane-protective effects. The drug inhibits lipid peroxidation, increases the activity of superoxidase, increases the lipid-protein ratio, improves the structure and function of the cell membrane.

3-hydroxy-6-methyl-2-ethylpyridine succinate® modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ability to bind to ligands, contributes to the preservation of the structural and functional organization of biomembranes, the transport of neurotransmitters and the improvement of synaptic transmission. 3-hydroxy-6-methyl-2-ethylpyridine succinate® 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 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, disorders of cerebral circulation, intoxication with ethanol and antipsychotic drugs).

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 in acute ischemia and promotes the restoration of mitochondrial redox processes in hypoxia, increases the synthesis of ATP and creatine phosphate. Ensures 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 frequency of arrhythmias and disorders of intracardiac conduction. 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 the metabolism and blood supply to the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. It stabilizes the membranes of blood cells (red blood cells and platelets), reducing the likelihood of hemolysis.

It has a hypolipidemic effect, reduces the content of total cholesterol and LDL.

Mexidol is an antioxidant - inhibitor of free radical processes, which has antihypoxic, stress-protective, antiamnestic, and anxiolytic effects. The drug increases the body's resistance to the effects of extreme factors and oxygen-dependent pathological conditions (shock, hypoxia, disorders of cerebral circulation), prevents and reduces the toxic effects of ethyl alcohol.

With intravenous administration, the drug quickly (within 0.5–1.5 hours) passes from the bloodstream to organs and tissues, and therefore its concentration in unchanged form quickly decreases. With intravenous administration in therapeutic doses, the Cmax of the drug in the blood plasma is reached in 30-40 minutes and is 2.5-3 mcg/ml, while its metabolites are determined in the blood plasma for 7-9 hours.

The drug is excreted from the body in the urine in glucuronoconjugated form, as well as in small amounts in unchanged form.

Suction and distribution. It is rapidly absorbed when taken orally (the half-absorption period is about 1 h). Tmax when taken orally is 0.5 h. Cmax when taken orally is 50-100 ng / ml. It is rapidly distributed in organs and tissues. The average retention time of ethylmethylhydroxypyridine succinate in the body when taken orally is about 5 hours.

Metabolism. Метаболизируется в печени путем глюкуронирования. Идентифицировано 5 метаболитов: 3-оксипиридина фосфат — образуется в печени и при участии ЩФ распадается на фосфорную кислоту и 3-оксипиридин; 2-й метаболит — фармакологически активный, образуется в больших количествах и обнаруживается в моче на 1–2-е сут после введения; 3-й — выводится в больших количествах с мочой; 4-й и 5-й — глюкуронконъюгаты.

Output. T1/2 when taken orally-4-5 hours. It is rapidly excreted in the urine mainly in the form of metabolites (50% in 12 hours) and in a small amount (0.3% in 12 hours) - in an unchanged form. It is most intensively excreted during the first 4 hours after taking the drug. Indicators of urinary excretion of unchanged drug and metabolites have individual variability.

Increases the effect of anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa) and benzodiazepine anxiolytics.

Increases the antianginal activity of nitropreparations.

When combined with 3-hydroxy-6-methyl-2-ethylpyridine succinate ® increases the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. 3-hydroxy-6-methyl-2-ethylpyridine succinate® reduces the toxic effects of ethanol.