MetucinVel solution 50mg/ml ampoules 5ml, 5pcs

Composition

Per 1 ml:

Active ingredient: ethylmethylhydroxypyridine succinate-50.0 mg.

Excipients: sodium metabisulfite( sodium disulfite), water for injection.

Pharmacological action

Pharmacotherapeutic group: antioxidant agent.

ATX code: [N07 XX]

Pharmacological properties

Pharmacodynamics

Ethylmethylhydroxypyridine succinate belongs to the class of 3-hydroxypyridines, is an inhibitor of free radical processes, a membrane protector. It also has an antihypoxic effect, increases the body’s resistance to stress.

The mechanism of action of ethylmethylhydroxypyridine succinate is due to its antioxidant and membrane-protective effect. The drug inhibits lipid peroxidation, increases the activity of superoxide oxidase, increases the lipid-protein ratio, improves the structure and function of the cell membrane.

Ethylmethylhydroxypyridine succinate simulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, GABA, and acetylcholine), which enhances their ability to bind to ligands, helps preserve the structural and functional organization of biomembranes, transport neurotransmitters, and improve synaptic transmission. Ethylmethylhydroxypyridine succinate increases the level of dopamine in the brain. Causes an increase in 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 triphosphoric acid (ATP) and creatine phosphate, activation of 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 antipsychotic drugs).

In conditions of critical reduction of coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes-phosphodiesterase, adenylate cyclase, and acetylcholinesterase. Supports the activation of acetylcholinesterase that develops in acute ischemia. It 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 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 arrhythmia 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.

Promotes the preservation of retinal ganglion cells and optic nerve fibers in progressive neuropathy caused by chronic ischemia and hypoxia. Improves the functional activity of the retina and optic nerve, increasing visual acuity.

Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Improves metabolism and blood supply to the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membranes of blood cells (red blood cells and platelets), reducing the likelihood of developing hemolysis. It has a hypolipidemic effect by reducing the content of total cholesterol and low-density lipoproteins.

Pharmacokinetics

Suction

With a single and course use, the maximum concentration (Cmax) in blood plasma is reached after 0.58 hours. When administered at a dose of 400-500 mg (Cmax) in blood plasma-3.5-4 mcg / ml.

Distribution

It is rapidly distributed in organs and tissues. The average retention time of ethylmethylhydroxypyridine succinate in the body is 0.7-1.3 hours.

Metabolism

It is metabolized in the liver by glucuronidation. 5 metabolites were identified: 3-oxypyridine phosphate-is formed in the liver and breaks down into phosphoric acid and 3-oxypyridine with the participation of alkaline phosphatase; the 2nd metabolite is pharmacologically active, is formed in large quantities and is detected in the urine 1-2 days after use; the 3rd – is excreted in large quantities in the urine; the 4th and 5th-glucuronconjugates. Deduction

It is removed from the blood plasma quickly and is practically undetectable after 4 hours in it. It is rapidly excreted in the urine mainly in the form of metabolites (50% in 12 hours) and in a small amount – in unchanged form (0.3% in 12 hours). Urinary excretion rates of unchanged ethylmethylhydroxypyridine succinate and its metabolites are individually variable.

Indications

– acute cerebrovascular disease (in the complex therapy);

– traumatic brain injury, the consequences of traumatic brain injury;

– encephalopathy;

a syndrome of vegetative (neurocirculatory) dystonia;

– mild cognitive dysfunction of atherosclerotic;

– anxiety disorders in neurotic and neurosis-like States;

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

primary open-angle glaucoma different stages in the complex therapy;

– the relief of withdrawal syndrome in chronic alcoholism with the prevalence of neurosis and vegetative-vascular disorders;

acute toxicity of antipsychotic drugs;

acute purulent inflammation of the abdominal cavity (acute necrotic pancreatitis, peritonitis) as part of complex therapy.

Use during pregnancy and lactation

No teratogenic or mutagenic embryotoxic effects were detected in experimental studies. Adequate and strictly controlled clinical studies of pregnancy and breast-feeding have not been conducted. The drug is contraindicated during pregnancy and lactation due to insufficient data on the effectiveness and safety of the drug in these periods.

Contraindications

-increased individual sensitivity to the drug;

– acute hepatic and/or renal failure;

– childhood;

– pregnancy;

– breast – feeding period-due to the lack of data on efficacy and safety.

With caution

A history of allergic diseases and reactions.

Side effects

From the digestive system: nausea, dryness of the oral mucosa or a metallic taste in the mouth, flatulence, diarrhea.

Nervous system disorders: drowsiness, difficulty falling asleep.

From the respiratory system: sore throat, chest discomfort, a feeling of lack of air (usually associated with an excessively high rate of use and is short-term).

From the cardiovascular system: short-term increase in blood pressure.

Other: allergic reactions, a feeling of” spreading heat ” throughout the body, an unpleasant smell.

Interaction

Increases the effect of benzodiazepine anxiolytics, antiepileptic drugs (carbamazepine), antiparkinsonian drugs (levodopa).

Reduces the toxic effect of ethanol.

How to take, course of use and dosage

Intramuscularly or intravenously (jet or drip). With the infusion method of use, the drug should be diluted in 0.9% sodium chloride solution.

Doses are selected individually.

Jet is administered slowly for 5-7 minutes, drip at a rate of 40-60 drops per minute. The maximum daily dose should not exceed 1200 mg.

In acute disorders of cerebral circulation, it is used in complex therapy for the first 10-14 days-intravenously drip 200-500 mg 2-4 times a day, then intramuscularly 200-250 mg 2-3 times a day for 2 weeks.

For craniocerebral trauma and the consequences of craniocerebral injuries, the drug is used for 10-15 days intravenously drip 200-500 mg 2-4 times a day.

When dyscirculatory encephalopathy in the decompensation phase, the drug is used intravenously in a jet or drip at a dose of 200-500 mg 1-2 times a day for 14 days. Then intramuscularly 100-250 mg per day for the next two weeks.

For the course prevention of dyscirculatory encephalopathy, intramuscularly administered at a dose of 200-250 mg 2 times a day for 10-14 days.

For neurocirculatory dystonia, neurotic and neurosis-like conditions

, the drug is administered intramuscularly at 50-400 mg per day for 14 days.

For mild cognitive impairment in elderly patients and anxiety disorders, the drug is used intramuscularly at a dose of 100-300 mg per day for 14-30 days.

In acute myocardial infarction as part of complex therapy, the drug is administered intravenously

or intramuscularly for 14 days, against the background of standard therapy for myocardial infarction (including nitrates, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulants and antiplatelet agents, as well as symptomatic agents according to indications).

In the first 5 days, to achieve maximum effect, the drug is administered intravenously, and in the next 9 days, the drug can be administered intramuscularly.

Intravenous use of the drug is carried out by drip infusion, slowly (to avoid side effects) for 30-90 minutes (in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution), if necessary, slow jet intravenous use of the drug is possible, lasting at least 5 minutes.

The drug is administered (intravenously or intramuscularly) 3 times a day every 8 hours. The daily dose is 6-9 mg / kg of body weight, a single dose is 2-3 mg/kg of body weight. The maximum daily dose should not exceed 800 mg, a single dose-250 mg.

With open-angle glaucoma of various stages, as part of complex therapy,100-300 mg per day is administered intramuscularly,1-3 times a day for 14 days.

In case of alcohol withdrawal syndrome, the drug is administered intramuscularly or intravenously in a dose of 200-500 mg 2-3 times a day for 5-7 days.

In acute intoxication with antipsychotic drugs, the drug is administered intravenously at a dose of 200-500 mg per day for 7-14 days.

In acute purulent-inflammatory processes of the abdominal cavity (acute necrotizing pancreatitis, peritonitis), the drug is prescribed on the first day both in the preoperative and postoperative period. The administered doses depend on the form and severity of the disease, the prevalence of the process, and the clinical course options. Discontinuation of the drug should be carried out gradually only after a sustained positive clinical and laboratory effect.

In acute edematous (interstitial) pancreatitis, the drug is prescribed 200-500 mg 3 times a day, intravenously (in 0.9% sodium chloride solution) and intramuscularly.

Mild severity of necrotizing pancreatitis – 100-200 mg 3 times a day, intravenously drip (in 0.9% sodium chloride solution) and intramuscularly. Moderate severity – 200 mg 3 times a day, intravenously drip (in 0.9% sodium chloride solution). Severe course – in a dosage of 800 mg on the first day, with a double mode of use; then 200-500 mg 2 times a day with a gradual decrease in the daily dose. Extremely severe course – at an initial dosage of 800 mg per day until persistent relief of manifestations of pancreatogenic shock, after stabilization of the condition,300-500 mg 2 times a day intravenously (in 0.9% sodium chloride solution) with a gradual decrease in the daily dosage.

Overdose

Due to its low toxicity, overdose is unlikely.

In case of accidental overdose, sleep disorders (insomnia), in some cases drowsiness and sedation may occur. Intravenous use may increase blood pressure.

Treatment

As a rule, it is not required – the symptoms disappear on their own within a day. In particularly severe cases of insomnia, it is recommended to use one of the sleeping pills and anxiolytics for oral use (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg). With an excessive increase in blood pressure, antihypertensive agents are used under the control of blood pressure.

Description

Clear, colorless or slightly yellowish solution.

Special instructions

The drug is not prescribed to children under 18 years of age due to insufficient knowledge of the drug’s action.

Influence on the ability to drive vehicles and mechanisms

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

In a place protected from light at a temperature of no more than 25 degrees. Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date.

Active ingredient

Ethylmethylhydroxypyridine Succinate

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion