Expiration date: 07/2025

Release form

The solution for the on/in and/m introduction colorless or slightly yellow, transparent

Packaging

2 ml - ampoules (5) - packing contoured plastic (2) - packs of cardboard

Pharmacological action

Inhibitor of free radical processes - membraneprotective, possesses also antihypoxic, substance revealing a stress protective, nootropic, antiepileptic and anxiolytic action. Refers to the class 3-oksipiridina.

The mechanism of action is due to antioxidant and membrane-protective properties. Suppresses GENDER, increases the activity of superoxidised, increases the ratio of lipid-protein that improves the structure and function of cell membranes.

Modulates the activity of membrane-bound enzymes (Ca2+-independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which contributes to their binding with ligands, the preservation of the structural and functional organization of biological membranes, transport of neurotransmitters and improve synaptic transmission. Increases concentration in the brain of dopamine.

Enhances compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle in hypoxia with an increase in ATP and creatine phosphate activates energosintezirutuyu mitochondrial function.

Increases organism resistance to influence of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebrovascular accident, ethanol intoxication and antipsychotic drugs).

Improves metabolism and blood flow in brain microcirculation and blood rheology, reduces platelet aggregation. It stabilizes the membranes of red blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis.

Has hypolipidemic effect, reduces total cholesterol and LDL.

Improves the functional state of the ischemic myocardium during myocardial infarction, the contractile function of the heart, as well as reduces the manifestations of systolic and diastolic LV dysfunction.

In terms of critical reduction of coronary blood flow promotes the preservation of structural and functional organization of membranes cardiomyocytes stimulates the activity of membrane enzymes PDE, adenylate cyclase, acetylcholinesterase. Supports evolving in acute ischemia the activation of aerobic glycolysis and contributes to hypoxic conditions in the restoration of mitochondrial redox processes and increases the synthesis of ATP and creatine phosphate. Ensures the integrity of the morphological structures and physiological functions of ischemic myocardium.

Improves the clinical course of myocardial infarction increases the effectiveness of the therapy accelerates recovery of functional activity of myocardium of the left ventricle, reduces the incidence of arrhythmias and disorders of intracardiac conduction. Normalizes metabolic processes in ishemizirovanna the myocardium reduces the zone of necrosis, restores and/or improves the electrical activity and contractility of myocardium and increases coronary blood flow in the zone of ischemia, increases antianginal activity nitropreparatov, improves rheological properties of blood, reduces the effects of reperfusion syndrome in acute coronary insufficiency.

Reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Pharmacokinetics

Suction

Quickly absorbed by ingestion (the period of poluabsorbtion - 0.08-1 hour). TCmax when in/m introduction - 0.3-0.58 h, the ingestion - 0.46-0.5 h. Cmax when I/m administration at a dose of 400-500 mg - 2.5-4 µg/ml, the ingestion of 50-100 ng/ml.

Distribution

Rapidly distributed to organs and tissues. The average time of retention of the drug in the body when the/m introduction - 0.7-1.3 h, the ingestion of 4.9-5.2 h

Metabolism

It is metabolized in the liver by glukuronirovania. Identified 5 metabolites: 3-hydroxypyridine phosphate is formed in the liver and involvement of alkaline phosphatase breaks down into phosphoric acid and 3-hydroxypyridine; 2-th metabolite is pharmacologically active, it is formed in large quantities and is found in the urine for 1-2 days after administration; the 3rd is excreted in large quantities in the urine; 4th and 5th - glucuroconjugated.

Excretion

T1/2 the ingestion - 4.7-5 h. is Rapidly excreted in the urine mainly as metabolites (50% in 12 h) and in small quantities - unchanged (0.3% in 12 h). The most intensively excreted during the first 4 h after administration of the drug. Indicators of urine excretion of unchanged drug and metabolites have a significant individual variability.

Testimony

• anxiety in neurotic and neurosis-like States;
  
• vegetative-vascular dystonia;
  
• encephalopathy;
  
• mild cognitive disorder atherosclerotic Genesis;
  
• acute disorders of cerebral circulation (composed of combination therapy);
  
• withdrawal syndrome in alcoholism with the prevalence of neurosis and vegetative-vascular disorders;
  
• acute intoxication antipsychotic medicines;
  
• acute purulent-inflammatory processes in the abdominal cavity (including acute necrotic pancreatitis, peritonitis (in the complex therapy));
  
• acute myocardial infarction from the first day (parenteral);
  
• IBS;
  
• complex therapy of ischemic stroke (oral) - in the complex therapy.
  

Contraindications

• hypersensitivity;
  
• acute liver and/or kidney failure;
  
• pregnancy;
  
• lactation;
  
• the children's age.
  

C caution: in the presence of allergic diseases in anamnesis (for parenteral administration).

Application of pregnancy and breastfeeding

Contraindicated in pregnancy, lactation.

Special instructions

During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and psychomotor speed reactions.

Composition

1 ml 1 ampoule contains:

2 ethyl-6-methyl-3-hydroxypyridine succinate 50 mg 100 mg

Auxiliary substances: water d/and.

Method of application and doses

In/m,/in (struino for 5-7 minutes or drip, with a speed of 60 drops/min).

Infusion route of administration diluted in 200 ml of 0.9% solution of sodium chloride. Initial dose 0.05-0.1 g 1-3 times/day with a gradual increase to produce a therapeutic effect. The maximum daily dose is 0.8 g.

In acute violation of cerebral circulation - in/in the drip, 0.2-0.3 g 1 time/day in the first 2-4 days, then in/m to 0.1 g 3 times/day.

In discirculatory encephalopathy (phase decompensation) in/in struino or drip, 0.1 g 2-3 times/day for 14 days and then in/m to 0.1 g for 14 days. In exchange, the prevention of dyscirculatory encephalopathy - in/m to 0.1 g 2 times/day for 10-14 days.

VSD, neurotic and neurosis-like States - in/m to 0.05-0.4 g/day for 14 days.

When withdrawal syndrome - /m 100-200 mg 2-3 times/day or/drip in 1-2 times/day for 5-7 days.

In acute intoxication antipsychotic means in/in the 0.05-0.3 g/day for 7-14 days.

In mild cognitive disorders - /m 0.1-0.3 g/day for 14-30 days.

When purulent-inflammatory processes in the abdominal cavity (acute necrotizing pancreatitis, peritonitis) - the first day in preoperative and postoperative period. The dosage depends on the type and severity of the disease, the prevalence of, and clinical course.

Removal of the drug is done gradually after sustained clinical and laboratory improvement.

In acute edematous (interstitial) pancreatitis mild - 0.1-0.2 g 3 times/day, in/in drip and/m;

moderate - 0.2 g 3 times/day;

severe - in/in the drip, 0.8 g in the first day (split into 2 injections), and then 0.3 g of 2 times/day with a gradual decrease in daily dose;

extremely difficult for in/drip, 0.8 g/day to a persistent relief of symptoms of pancreatogenic shock;

after you have stabilized - at 0.3-0.4 g 2 times/day with a gradual decrease in daily dose.

Myocardial infarction - in/in (during the first 5 days) and/m (next 9 days) 3 times/day (every 8 hours). Daily dose of 6-9 mg/kg/day, single dose - 2-3 mg/kg the Maximum daily dose should not exceed 800 mg, single - 250 mg./administered by infusion over 30-90 min at 100-150 ml 0.9% sodium chloride solution or 5% dextrose solution or bolus for at least 5 min.

In coronary artery disease: inside, on 100 mg 3 times/day. The course duration not less than 2 months; if necessary, possibly re courses.

Side effects

Nausea, dry mouth, diarrhea, drowsiness, allergic reactions.

For parenteral administration (especially in bolus): a dry, metallic taste in the mouth, the feeling of "spreading the heat" throughout the body, unpleasant smell, throat irritation and discomfort in the chest, feeling short of breath (usually associated with excessive rate of introduction and are of short duration); long-term use - nausea, flatulence; sleep disturbances (drowsiness or sleep onset disorder).

Drug interactions

Enhances the action of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates.

Reduces the toxic effects of ethanol.

Overdose

Symptoms: sleep disorders (insomnia, in some cases, drowsiness); the on/in the introduction - small and short-term (up to 1.5-2 h) increase in blood pressure.

Treatment: usually not required. The symptoms disappear on their own within a day. In severe cases when insomnia, nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. excessive increase in blood pressure - antihypertensive drugs under the control of AD.