Cerecard (Solution) Instructions for Use

ATC Code

N07XX (Other drugs for the treatment of nervous system diseases)

Active Substance

Ethylmethylhydroxypyridine succinate (Grouping name)

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

An inhibitor of free radical processes – a membrane protector that also has antihypoxic, stress-protective, nootropic, anticonvulsant, and anxiolytic effects. It belongs to the class of 3-oxypyridines.

The mechanism of action is due to its antioxidant and membrane-protective properties. It suppresses lipid peroxidation, increases superoxide dismutase activity, improves the lipid-protein ratio, and enhances the structure and function of cell membranes.

It modulates the activity of membrane-bound enzymes (Ca²⁺-independent PDE, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, GABA, acetylcholine), which promotes their binding to ligands, preserves the structural and functional organization of biomembranes, neurotransmitter transport, and improves synaptic transmission. It 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 ATP and creatine phosphate, and activates the energy-synthesizing function of mitochondria.

It increases the body’s resistance to the effects of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebrovascular accidents, ethanol intoxication, and antipsychotic drug intoxication).

It improves metabolism and blood supply to the brain, microcirculation and rheological properties of blood, and reduces platelet aggregation. It stabilizes the membranes of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis.

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

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

Under conditions of critical reduction in coronary blood flow, it helps preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes – PDE, adenylate cyclase, acetylcholinesterase. It maintains the developing activation of aerobic glycolysis during acute ischemia and promotes the restoration of mitochondrial redox processes under hypoxia, increasing the synthesis of ATP and creatine phosphate. It ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium.

It improves the clinical course of myocardial infarction, increases the effectiveness of the therapy, accelerates the recovery of the functional activity of the left ventricular myocardium, reduces the frequency of arrhythmias and intracardiac conduction disturbances. It normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and/or improves the electrical activity and contractility of the myocardium, increases coronary blood flow in the ischemic zone, enhances the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency.

It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Pharmacokinetics

It is rapidly absorbed after oral administration (half-absorption period – 0.08-1 h). T_max after IM administration – 0.3-0.58 h, after oral administration – 0.46-0.5 h. C_max after IM administration at a dose of 400-500 mg – 2.5-4 µg/ml, after oral administration – 50-100 ng/ml.

It is rapidly distributed in organs and tissues. The mean residence time of the drug in the body after IM administration is 0.7-1.3 h, after oral administration – 4.9-5.2 h.

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

T_1/2 after oral administration – 4.7-5 h. It is rapidly excreted in the urine mainly as metabolites (50% within 12 h) and in small amounts – unchanged (0.3% within 12 h). It is most intensively excreted within the first 4 hours after drug administration. The indicators of excretion of the unchanged drug and metabolites in the urine have significant individual variability.

Indications

Anxiety disorders in neurotic and neurosis-like conditions; vegetative-vascular dystonia; dyscirculatory encephalopathy; mild cognitive disorders of atherosclerotic origin.

Acute cerebrovascular accidents (as part of combination therapy).

Withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders; acute intoxication with antipsychotic drugs.

Acute purulent-inflammatory processes in the abdominal cavity (including acute necrotizing pancreatitis, peritonitis (as part of complex therapy)).

Acute myocardial infarction from the first days (parenterally); coronary artery disease; complex therapy of ischemic stroke (orally) – as part of complex therapy.

ICD codes

Dosage Regimen

Determine the dose, frequency, and duration of treatment individually based on the indication and clinical situation.

For oral administration, administer a total daily dose of 250-500 mg divided into 2-3 doses.

Do not exceed the maximum daily oral dose of 600-800 mg.

For intramuscular or intravenous administration (bolus or infusion), administer a single dose of 50-400 mg.

Do not exceed the maximum daily parenteral dose of 1200 mg.

For acute myocardial infarction, initiate parenteral therapy from the first days.

For acute cerebrovascular accidents and acute necrotizing pancreatitis, use as part of combination therapy.

For withdrawal syndrome in alcoholism with neurosis-like and vegetative-vascular disorders, adjust the dose based on symptom severity.

For anxiety disorders, dyscirculatory encephalopathy, and mild cognitive disorders, use oral administration.

Administer intravenous bolus injections slowly to avoid adverse effects like dryness, metallic taste, or sensations of warmth.

Adjust the infusion rate for intravenous administration to minimize the risk of shortness of breath or throat discomfort.

Monitor patients for drowsiness, especially when initiating therapy or operating vehicles.

Adverse Reactions

When taken orally nausea, dry mouth, diarrhea, drowsiness, allergic reactions.

With parenteral administration (especially IV bolus) dryness, “metallic” taste in the mouth, sensations of “spreading warmth” throughout the body, unpleasant odor, sore throat and discomfort in the chest, feeling of shortness of breath (usually associated with an excessively high rate of administration and are short-term in nature); with prolonged use – nausea, flatulence; sleep disorders (drowsiness or difficulty falling asleep).

Contraindications

Hypersensitivity; acute hepatic and/or renal failure; pregnancy; lactation period; childhood.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindication: acute hepatic failure.

Use in Renal Impairment

Contraindication: acute renal failure.

Pediatric Use

The drug is contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

Use with caution in patients with a history of allergic diseases.

During treatment, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

It enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian (levodopa) drugs, and nitrates.

It reduces the toxic effects of ethanol.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.