Cerecard solution for intravenous and intramuscular administration 50 mg / ml
Dispensed by prescription

Dosage form:

Solution for intravenous and intramuscular administration.

Description:

Colorless or light yellow transparent liquid.

Pharmacotherapeutic group:

Antioxidant.

Release form:


Solution for intravenous and intramuscular administration, 50 mg / ml.

In imported ampoules of the 1st hydrolytic class of colorless or light-protective glass with a ring or a break point, 2 ml or 5 ml each.

5 ampoules in a blister strip made of polyvinyl chloride film and aluminum foil. It is allowed to pack the drug in a blister strip without foil.

1 or 2 blister packs with instructions for medical use in a cardboard box.

Instructions for use
  • Dosage form
  • Structure
  • Description of the dosage form
  • Pharmacological group
  • Pharmacodynamics
  • Pharmacokinetics
  • Indications
  • Contraindications
  • Method of administration and dosage
  • Side effects
  • Overdose
  • Interaction
  • special instructions
  • Release form
  • Storage conditions
  • Shelf life
  • Conditions of dispensing from pharmacies

Dosage form

Solution for intravenous and intramuscular administration

 

Structure

 

Active substance:  
Ethylmethylhydroxypyridine succinate 0.050 g
Excipients:  
Water for injections up to 1 ml
 

 

Description of the dosage form

Colorless or light yellow transparent liquid.

 

Pharmacotherapeutic group

Antioxidant

 

Pharmacodynamics

A drug from the 3-hydroxypyridine group. It is an inhibitor of free radical processes - a membrane protector, which also has antihypoxic, stress protective, nootropic, antiepileptic and anxiolytic effects. The mechanism of action is due to antioxidant and membrane-protective properties. Suppresses lipid peroxidation, increases the activity of superoxide oxidase, increases the lipid-protein ratio, improves the structure and function of the cell membrane. Modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, gamma-aminobutyric acid, acetylcholine), which contributes to their binding to ligands, preservation of the structural and functional transport of biomembrane cells. Increases the concentration of dopamine in the brain.

It enhances the compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under conditions of hypoxia with an increase in ATP and creatine phosphate, activates the energy-synthesizing function of mitochondria.

Increases the body's resistance to the effects of various damaging factors in pathological conditions.

Improves metabolism and blood supply to the brain, microcirculation and rheological properties of blood, reduces platelet aggregation. Stabilizes the membranes 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.

Improves the functional state of ischemic myocardium in myocardial infarction, contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle.

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, accelerates the restoration of the functional activity of the left ventricular myocardium, reduces the incidence of arrhythmias and intracardiac conduction disorders.

It normalizes metabolic processes in the ischemic myocardium, reduces the area of ​​necrosis, restores and / or improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemic area, increases the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency.

 

Pharmacokinetics

The time to reach the maximum concentration for intramuscular administration is 0.3-0.58 hours. The maximum concentration for intramuscular administration at a dose of 400-500 mg is from 2.5 to 4 μg / ml.

It is quickly distributed in organs and tissues. The average retention time of the drug in the body with intramuscular injection is 0.7-1.3 hours.

It is metabolized in the liver by glucuronidation. Found 5 metabolites: 3-hydroxypyridine phosphate (formed in the liver and with the participation of alkaline phosphatase decomposes into phosphoric acid and 3-hydroxypyridine); The 2nd metabolite is pharmacologically active and is found in the urine 1-2 days after administration; 3rd - excreted in large quantities in the urine; 4th and 5th are glucuronic acid conjugates.

It is quickly excreted in the urine, mainly in the form of metabolites (50% in 12 hours) and in a small amount - unchanged (0.3% in 12 hours). It is most intensively excreted during the first 4 hours after taking the drug. The rates of excretion in the urine of unchanged drug and metabolites have significant individual variability.

 

Indications

The drug is used as part of complex therapy for:

      Anxiety in neurotic and neurosis-like states;
      Vegetovascular dystonia;
      Encephalopathy;
      Acute disorders of cerebral circulation (ischemic stroke);
      Mild cognitive impairment of atherosclerotic genesis;
      Withdrawal alcohol syndrome with a predominance of neurosis-like and vegetative-vascular disorders;
      Acute intoxication with antipsychotic drugs;
      Acute myocardial infarction from the first day.

 

Contraindications

    

Increased individual sensitivity to the drug;

      Acute hepatic and / or renal failure;
      Age up to 18 years (efficacy and safety have not been established);
      Pregnancy;
      Breastfeeding period.


Carefully

History of allergic diseases.

 

Method of administration and dosage

The drug is administered intramuscularly or intravenously in a stream (within 5-7 minutes) or drip (at a rate of 60 drops per minute).

When administered by infusion, the drug is preliminarily diluted in 200 ml of 0.9% sodium chloride solution. The initial dose of the drug is 50-100 mg 1-3 times a day with a gradual increase until a therapeutic effect is obtained. The maximum daily dose is 800 mg.

In case of acute cerebrovascular accident, intravenous infusion of 200-300 mg is injected once a day for the first 2-4 days, then 100 mg intramuscularly 3 times a day.

In case of discirculatory encephalopathy (decompensation phase), 100 mg is injected intravenously or by drop infusion 2-3 times a day for 14 days, and then 100 mg intramuscularly for 14 days. For the course of prevention of discirculatory encephalopathy, it is prescribed intramuscularly at 100 mg 2 times a day for 10-14 days.

Vegetovascular dystonia, neurotic and neurosis-like states: the drug is administered intramuscularly at 50-400 mg per day, the course of treatment is 14 days.

In case of alcohol withdrawal syndrome, 100-200 mg is administered intramuscularly 2-3 times a day, or 100-200 mg intravenously, 1-2 times a day for 5-7 days.

In case of acute intoxication with antipsychotic drugs, 50-300 mg per day are administered intravenously for 7-14 days.

Mild cognitive impairment: intramuscularly, 100-300 mg per day for 14-30 days.

Acute myocardial infarction: in the first 5 days, the drug is administered intravenously by infusion for 30-90 minutes (in 100-150 ml of 0.9% sodium chloride solution or 5% dextrose solution) or intravenously in a stream for at least 5 minutes. In the next 9 days, the drug is administered intramuscularly 3 times a day (every 8 hours). The daily 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.

 

Side effects

Perhaps the development (especially with intravenous jet injection) dry mouth, "metallic" taste in the mouth, a feeling of "spreading heat" throughout the body, unpleasant odor, sore throat and discomfort in the chest, feeling of lack of air (which, as a rule, associated with an excessively high rate of administration and is short-term), allergic reactions.

With prolonged use, nausea, flatulence may occur; sleep disturbances (drowsiness or trouble falling asleep).

 

Overdose

Overdose symptoms: sleep disturbances (insomnia, in some cases - drowsiness), with intravenous administration - a slight and short-term (up to 1.5-2 hours) increase in blood pressure.

In cases of overdose, treatment is usually not required, since the symptoms disappear on their own within 24 hours. In severe cases of insomnia, it is recommended to prescribe hypnotics from the group of benzodiazepine derivatives (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg).

With a pronounced increase in blood pressure, it is necessary to prescribe antihypertensive drugs under the control of blood pressure and / or supplement therapy with nitro drugs.

 

Interaction

The drug enhances the effect of anxiolytics from the benzodiazepine group, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates. Reduces the toxic effects of ethanol.

 

special instructions

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

 

Release form

Solution for intravenous and intramuscular administration of 50 mg / ml in imported ampoules of the 1st hydrolytic class of colorless or light-shielding glass with a ring or a break point of 2 ml or 5 ml.

5 ampoules in a blister strip made of polyvinyl chloride film and aluminum foil. It is allowed to pack the drug in a blister strip without foil. 1 or 2 blister packs with instructions for medical use in a cardboard box.

 

Storage conditions

In a dry, 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.

 

Terms of dispensing from pharmacies

On prescription.

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