Venocor

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT VENOCOR (VENOCOR)

Composition:

Active substance: ethylmethylhydroxypyridine succinate;

1 ml of solution contains ethylmethylhydroxypyridine succinate 50 mg;

Excipients: sodium metabisulfite (E 223), water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: colorless or slightly yellowish clear liquid.

Pharmacotherapeutic group. Agents affecting the nervous system.

ATC code N07 X X.

Pharmacological Properties

Pharmacodynamics

Venocor is an inhibitor of free radical processes and a membrane protector, exerting antioxidant, anti-hypoxic, stress-protective, nootropic, anticonvulsant, and anxiolytic effects. The drug enhances the body's resistance to various harmful factors, particularly oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebral circulation disorders, alcohol intoxication, and intoxication with antipsychotic agents (neuroleptics)).

Venocor improves cerebral metabolism and cerebral blood supply, enhances microcirculation and blood rheological properties, and reduces platelet aggregation. It stabilizes blood cell membrane structures (erythrocytes and platelets) during hemolysis. The drug exerts a hypolipidemic effect, reducing total cholesterol and low-density lipoprotein (LDL) levels. It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action of the drug is determined by its antioxidant and membrane-protective effects. It inhibits lipid peroxidation, increases superoxide dismutase activity, improves the lipid-to-protein ratio, reduces membrane viscosity, and increases membrane fluidity. Venocor modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, gamma-aminobutyric acid (GABA), acetylcholine), thereby enhancing their ability to bind ligands, promoting preservation of the structural and functional organization of biomembranes, neurotransmitter transport, and improving synaptic transmission. Venocor increases dopamine levels in the brain. It enhances compensatory activation of aerobic glycolysis and reduces the degree of suppression of oxidative processes in the Krebs cycle under hypoxic conditions, increasing adenosine triphosphate (ATP) and creatine phosphate levels, activating mitochondrial energy-synthesizing functions, and stabilizing cellular membranes.

Venocor normalizes metabolic processes in ischemic myocardium, reduces the area of necrosis, restores and improves myocardial electrical activity and contractility, increases coronary blood flow in the ischemic area, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency. It enhances the antianginal activity of nitrate drugs. Venocor promotes preservation of retinal ganglion cells and optic nerve fibers in progressive neuropathy caused by chronic ischemia and hypoxia. It improves functional activity of the retina and optic nerve and increases visual acuity.

Pharmacokinetics

After intramuscular administration, the drug is detectable in blood plasma for up to 4 hours post-administration. Time to reach maximum concentration is 0.45–0.5 hours. Maximum concentration at doses of 400–500 mg is 3.5–4.0 μg/mL. Venocor rapidly transfers from the bloodstream into organs and tissues and is quickly eliminated from the body. The drug is excreted in urine, primarily in glucuronide-conjugated form, and in minor amounts unchanged.

Clinical characteristics.

Indications.

Acute cerebrovascular disorders;

head trauma, consequences of head injuries;

dyscirculatory encephalopathy;

vegetative dystonia syndrome;

mild cognitive impairments of atherosclerotic origin;

anxiety disorders in neurotic and neuropathy-like conditions;

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

primary open-angle glaucoma at various stages, as part of complex therapy;

alcohol withdrawal syndrome with predominant neuropathy-like and vegetative-vascular disorders;

acute intoxication with antipsychotic agents;

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

Contraindications.

Acute hepatic or renal failure, increased individual sensitivity to the drug, childhood, pregnancy, breastfeeding.

Interaction with other medicinal products and other types of interactions.

Venocor enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa). Reduces the toxic effect of ethanol.

Special precautions for use.

In individual cases, especially in predisposed patients or in patients with bronchial asthma with increased sensitivity to sulfites, severe hypersensitivity reactions may occur. The medicinal product contains sodium metabisulfite, which may cause bronchospasm.

Use with caution in patients with diabetic retinopathy (the course should not exceed 7–10 days) due to its potential to enhance proliferative processes.

After completion of parenteral administration, to maintain the achieved therapeutic effect, continuation of treatment with the drug orally in tablet form is recommended.

Use during pregnancy or breastfeeding.

Venocor is contraindicated during pregnancy and breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

During treatment, caution is required when driving or operating complex machinery, due to possible adverse effects that may affect reaction speed and the ability to concentrate.

Method of Administration and Dosage

Venocor is administered intramuscularly or intravenously (bolus or infusion). Dosages are individually adjusted. When administered by infusion, the drug should be diluted in 200 ml of physiological saline (sodium chloride solution). Treatment in adults is initiated at a dose of 50–100 mg once to three times daily, gradually increasing the dose until the desired therapeutic effect is achieved. Intravenous bolus administration should be performed slowly over 5–7 minutes; infusion should be given at a rate of 40–60 drops per minute. The maximum daily dose should not exceed 1200 mg.

In acute cerebral circulation disorders, Venocor is used in adults as part of combination therapy. During the first 2–4 days, it is administered intravenously as a bolus or infusion at 200–500 mg once daily, followed by intramuscular administration of 200–500 mg two to three times daily. The total treatment duration is 14 days.

In traumatic brain injury and its sequelae, Venocor is administered intravenously by infusion at 200–500 mg two to four times daily for 10–15 days.

In decompensated phase of dyscirculatory encephalopathy, Venocor should be administered intravenously as a bolus or infusion at 200–500 mg once or twice daily for 14 days. This is followed by intramuscular administration of 100–250 mg daily for the subsequent 2 weeks.

For course prophylaxis of dyscirculatory encephalopathy, the drug is administered intramuscularly to adults at 200–250 mg twice daily for 10–14 days.

In mild cognitive disorders in elderly patients and in anxiety states, the drug is administered intramuscularly at 100–300 mg daily for 14–30 days.

In acute myocardial infarction, Venocor is administered intravenously or intramuscularly for 14 days, in addition to standard myocardial infarction therapy, including nitrates, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulant and antiplatelet agents, as well as symptomatic treatments as indicated. Intravenous administration of Venocor is recommended during the first 5 days to achieve maximum effect; intramuscular administration may be used during the subsequent 9 days. Intravenous infusion of Venocor should be performed slowly (to avoid adverse effects) by drip infusion over 30–90 minutes in 100–150 ml of 0.9% sodium chloride solution or 5% dextrose (glucose) solution. If necessary, slow intravenous bolus injection of Venocor may be performed over no less than 5 minutes.

Venocor administration (intravenous or intramuscular) should be performed three times daily, every 8 hours. The daily therapeutic dose is 6–9 mg per kg of body weight; the single dose is 2–3 mg/kg. The maximum daily dose should not exceed 800 mg; the maximum single dose should not exceed 250 mg.

In various stages of open-angle glaucoma, Venocor is used as part of combination therapy, administered intramuscularly at 100–300 mg daily, once to three times daily, for 14 days.

In alcohol withdrawal syndrome, Venocor is administered at 200–500 mg intravenously or intramuscularly two to three times daily for 5–7 days.

In acute intoxication with antipsychotic agents, the drug is administered intravenously to adults at 200–500 mg daily for 7–14 days.

In acute purulent-inflammatory conditions of the abdominal cavity (acute necrotizing pancreatitis, peritonitis), the drug is prescribed on the first day both in the preoperative and postoperative periods. Dosages depend on the form and severity of the disease, extent of the process, and clinical course. Discontinuation of the drug should be gradual and only after a stable positive clinical and laboratory response.

In acute edematous (interstitial) pancreatitis, Venocor is prescribed to adults at 200–500 mg three times daily intravenously by infusion (with isotonic sodium chloride solution) and intramuscularly. Mild severity: 100–200 mg three times daily intravenously by infusion (with isotonic sodium chloride solution) and intramuscularly. Moderate severity: 200 mg three times daily intravenously by infusion (with isotonic sodium chloride solution) in adults. Severe course: pulse-dose regimen of 800 mg on the first day administered twice, followed by 200–500 mg twice daily with gradual reduction of the daily dose. Very severe course: initial dose of 800 mg daily until stable control of pancreatogenic shock is achieved; after stabilization of the patient’s condition, 300–500 mg twice daily intravenously by infusion (with isotonic sodium chloride solution), with gradual reduction of the daily dose.

Children.

Well-controlled clinical studies on the safety of Venocor in children have not been conducted; therefore, Venocor is contraindicated in this patient population.

Overdose.

Symptoms: drowsiness, insomnia.

Treatment: due to the low toxicity of the drug, overdose is unlikely. Treatment is generally not required; symptoms resolve spontaneously within 24 hours. In cases of pronounced symptoms, supportive and symptomatic therapy is administered.

Adverse reactions.

To avoid the occurrence of adverse effects, it is recommended to adhere to the recommended dosage regimen and rate of administration of the drug. The frequency of adverse effects was determined according to the World Health Organization (WHO) classification: very common (≥ 10%); common (≥ 1% but ≤ 10%); uncommon (≥ 0.1% but ≤ 1%); rare (≥ 0.01% but ≤ 0.1%); very rare (≤ 0.01%); frequency not known (frequency cannot be determined based on available data).

Immune system disorders: very rare – anaphylactic shock, angioneurotic edema, urticaria; frequency not known – allergic reactions, hyperemia, possible severe hypersensitivity reactions.

Psychiatric disorders: very rare – drowsiness; frequency not known – sleep disturbances, anxiety, emotional reactivity.

Cardiac disorders: frequency not known – palpitations, tachycardia.

Nervous system disorders: very rare – headache, dizziness (may be related to excessively rapid administration and may be transient); frequency not known – coordination disturbances, tremor.

Vascular disorders: very rare – hypotension, hypertension (may be related to excessively rapid administration and may be transient).

Respiratory, thoracic and mediastinal disorders: very rare – dry cough, throat irritation, chest discomfort, dyspnea (may be related to excessively rapid administration and may be transient); frequency not known – bronchospasm.

Gastrointestinal disorders: very rare – dry mouth, nausea, unpleasant taste sensation, metallic taste in the mouth; frequency not known – dyspeptic disorders, diarrhea.

Skin and subcutaneous tissue disorders: very rare – pruritus, rash, facial hyperemia; frequency not known – distal hyperhidrosis.

General disorders and administration site conditions: very rare – sensation of warmth; frequency not known – changes at the injection site.

During prolonged administration of the drug, the following adverse effects may occur: flatulence, weakness, peripheral edema.

Shelf life.

2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Incompatibility.

The drug should not be mixed with other medicinal products. Use only solvents specified in the instructions.

Packaging. 2 mL in an ampoule; 10 or 100 ampoules in a pack, or 5 ampoules in a blister, 2 blisters in a pack; 5 mL in an ampoule, 5 or 100 ampoules in a pack, or 5 ampoules in a blister, 1 blister in a pack.

Prescription status.

Prescription only.

Manufacturer.

Private Joint-Stock Company "Lekhim-Kharkiv".

Manufacturer's address and location of its business activities.

36 Severina Pototskogo Street, Kharkiv, Kharkiv Oblast, 61115, Ukraine.