Cerekard - instructions for use, dose, side effects, contraindications

A drug from the group of 3-hydroxypyridines. It is an inhibitor of free-radical processes - membrane-protector, which also has antihypoxic, stress-protective, nootropic, antiepileptic and anxiolytic action. The mechanism of action is due to antioxidant and membrane-protective properties. Suppresses lipid peroxidation, increases the activity of superoxide oxidase, increases the ratio of lipid-protein, 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 facilitates their binding to ligands, preservation of the structural and functional organization of biomembranes, neurotransmitter transport and improvement of synaptic transmission.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 hypoxic conditions with an increase in creatine phosphate and ATP, activates energosinteziruyuschuyu mitochondrial function.

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

It improves the metabolism and blood supply of 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. Has hypolipidemic effect, reduces the content of total cholesterol and low density lipoproteins.

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

In the context of the critical reduction in coronary blood flow helps to preserve the structural and functional organization of the cardiomyocyte membrane, stimulates the activity of membrane enzymes - phosphodiesterase, adenylate cyclase, acetylcholinesterase.It supports the activation of aerobic glycolysis in acute ischemia and promotes the restoration of mitochondrial oxidation-reduction processes under conditions of 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, improves the efficiency of the therapy, accelerates restoration of functional activity of the left ventricle, reduces the incidence of arrhythmias and conduction disorders intracardiac. Normalises metabolic processes in the ischemic myocardium reduces the zone of necrosis, restores and / or improves the electrical activity and contractility of the myocardium and increase coronary blood flow in the ischemic area, improves antianginal activity nitropreparatov, improves the rheological properties of the blood, reduces the consequences of reperfusion syndrome in acute coronary insufficiency.

Pharmacokinetics:

The time to reach maximum concentration when administered intramuscularly - 0,3-0,58 hours.The maximum concentration when administered intramuscularly at a dose of 400-500 mg is 2.5 to 4 μg / ml.

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.

Metabolized in the liver by glucuronation. 5 metabolites were detected: 3-hydroxypyridine phosphate (formed in the liver and decomposed into phosphoric acid and 3-hydroxypyridine with the participation of alkaline phosphatase); The 2-nd metabolite is pharmacologically active and is found in urine on the 1-2 day after administration; 3rd - is excreted in large quantities with urine; The 4th and 5th represent conjugates with glucuronic acid.

It is quickly excreted in the urine mainly in the form of metabolites (50% in 12 hours) and in an insignificant amount - unchanged (0.3% per 12 hours). The most intense withdrawal within the first 4 hours after taking the drug. The indices of excretion in the urine of unchanged drug and metabolites have a significant individual variability.

Indications:

As part of complex therapy:

- anxiety states in neurotic and neurosis-like states;

- vegetative-vascular dystonia;

- encephalopathy;

- acute disorders of cerebral circulation (ischemic stroke);

- mild cognitive impairment of atherosclerotic origin;

- abstinent alcoholic syndrome with a predominance of neurosis-like and vegeto-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 insufficiency;

- age under 18 years (effectiveness and safety not established);

- pregnancy;

- the period of breastfeeding.

Carefully:

Allergic diseases in the anamnesis.

Dosing and Administration:

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

With the infusion method of administration, the drug is previously 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 to obtain a therapeutic effect. The maximum daily dose is 800 mg.

With acute impairment of cerebral circulation injected intravenously drip 200-300 mg once a day for the first 2-4 days, then intramuscularly 100 mg 3 times a day.

When dyscirculatory encephalopathy (decompensation phase) injected intravenously struino or drip on 100 mg 2-3 times a day for 14 days, and then intramuscularly at 100 mg for 14 days.

For the course of prophylaxis of dyscirculatory encephalopathy Assign intramuscularly to 100 mg twice a day for 10-14 days.

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

With abstinent alcohol syndrome administered intramuscularly for 100-200 mg 2-3 times a day or intravenously drip on 100-200 mg 1-2 times a day for 5-7 days.

In acute intoxication with antipsychotic drugs administered intravenously at 50-300 mg per day for 7-14 days.

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

Acute myocardial infarction: in the first 5 days, the drug is administered intravenously infusion for 30-90 minutes (100-150 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose) or intravenously strumed 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, single dose - 2-3 mg / kg. The maximum daily dose should not exceed 800 mg, a single dose of 250 mg.

Side effects:

It is possible to develop (especially with intravenous jet injection) dryness in the mouth, a "metallic" taste in the mouth, a sensation of "spilling heat" throughout the body, an unpleasant odor, a sore throat and chest discomfort, a feeling of lack of air (which, as a rule, is associated with an excessively high rate of administration and is of a short-term nature), allergic reactions.

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

Overdose:

Symptoms of overdose: sleep disorders (insomnia, in some cases - drowsiness), with intravenous administration - a slight and short-term (up to 1.5-2 h) 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, insomnia is recommended the appointment of hypnotics from the group of benzodiazepine derivatives (nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg).

With a marked increase in blood pressure, it is necessary to prescribe antihypertensive drugs under the control of blood pressure and / or supplement therapynitro preparations.

Interaction:

The drug enhances the action of anxiolytics from the benzodiazepine group, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates.

Reduces toxic effects of ethanol.

Effect on the ability to drive transp. cf. and fur:

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

Form release / dosage:Solution for intravenous and intramuscular injection, 50 mg / ml.

Packaging:

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

5 ampoules in a contour acrylic package made of polyvinyl chloride film and aluminum foil. It is allowed to package the preparation in a contour mesh package without foil.

For 1 or 2 contour packs together with instructions for medical use in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003013/09

Date of registration:16.04.2009

The owner of the registration certificate:EKOFARMPLUS, CJSC EKOFARMPLUS, CJSC Russia

Manufacturer: & nbsp

EKOFARMPLUS, CJSC Russia

Information update date: & nbsp10.10.2015

Illustrated instructions

Instructions

Cerekard (Cerecard)