Etoxydol^® (Tablets, Solution) Instructions for Use

ATC Code

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

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

Etoxydol^® is an inhibitor of free radical processes, exerts a membrane-protective, antihypoxic, nootropic, anticonvulsant, anxiolytic effect, and increases the body’s resistance to stress.

Etoxydol^® possesses anti-ischemic properties, improves blood flow in the ischemic area, limits the zone of ischemic damage, exhibits a hypolipidemic effect, and reduces the content of total cholesterol and low-density lipoproteins in blood serum.

The drug increases the body’s resistance to the effects of various damaging factors, to oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebrovascular disorders, intoxication with alcohol and antipsychotic agents (neuroleptics)).

The drug improves cerebral metabolism and blood supply to the brain, improves microcirculation and the rheological properties of blood, and reduces platelet aggregation. It stabilizes the membrane structures of blood cells (erythrocytes and platelets) during hemolysis.

The mechanism of action of the drug is due to its antioxidant, antihypoxic, and membrane-protective effects. It inhibits lipid peroxidation, increases the activity of superoxide oxidase, increases the lipid-protein ratio, reduces membrane viscosity, and increases its fluidity. It modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which enhances their ligand-binding ability, contributes to the preservation of the structural and functional organization of biomembranes, neurotransmitter transport, and improvement of synaptic transmission.

Pharmacokinetics

Absorption

After intramuscular administration, the drug is detected in blood plasma for 4 hours after administration. T_max is 0.25 hours. C_max after administration of a 100 mg dose is 0.3-1.06 µg/ml. Etoxydol^® rapidly passes from the bloodstream into organs and tissues and is rapidly eliminated from the body. The retention time of the drug is 1.84-2.38 hours.

Elimination

T_1/2 is 1.15-1.75 hours. Etoxydol^® is excreted from the body by the kidneys, mainly in the form of glucuronides and in small amounts unchanged.

Indications

• Acute cerebrovascular accidents;
• Dyscirculatory encephalopathy;
• Autonomic dystonia syndrome;
• Mild cognitive disorders of atherosclerotic origin;
• Anxiety disorders in neurotic and neurosis-like states;
• Relief of withdrawal syndrome in alcoholism with a predominance of neurosis-like and autonomic-vascular disorders;
• Acute intoxication with antipsychotic agents.

ICD codes

Dosage Regimen

Solution

Etoxydol^® is administered intramuscularly and intravenously (bolus or drip).

For infusion administration, the drug should be diluted in 0.9% sodium chloride solution.

Doses are selected individually. Therapy is started with a dose of 50-100 mg 1-3 times/day, gradually increasing until a therapeutic effect is obtained.

For intravenous bolus administration, the drug is injected slowly over 5-7 minutes; for drip administration – at a rate of 40-60 drops/minute. The maximum daily dose should not exceed 800 mg.

For acute cerebrovascular accidents, Etoxydol^® is prescribed as part of complex therapy in the first 2-4 days intravenously (drip) at a dose of 200-300 mg, then – intramuscularly at 100 mg 3 times/day. The duration of treatment is 10-14 days.

For dyscirculatory encephalopathy in the decompensation phase – intravenously (bolus or drip) at a dose of 100 mg 2-3 times/day for 14 days, then – intramuscularly at 100 mg 2 times/day for 14 days.

For course prophylaxis of dyscirculatory encephalopathy – intramuscularly at a dose of 100 mg 2 times/day for 10-14 days.

For mild cognitive impairments inelderly patientsand for anxiety disorders – intramuscularly at a daily dose of 100-300 mg/day for 14-30 days.

For alcohol withdrawal syndrome – intramuscularly at a dose of 100-200 mg 2-3 times/day or intravenously drip 1-2 times/day for 5-7 days.

For acute intoxication with antipsychotic agents – intravenously at a dose of 50-300 mg/day for 7-14 days.

Tablets

Etoxydol^® tablets are administered orally. The tablets are chewed and washed down with water.

For complex therapy of coronary heart disease and therapy of ischemic stroke, 100 mg (1 tablet) is prescribed 3 times a day, gradually increasing the dose until a therapeutic effect is obtained. The maximum single dose is 200 mg; the daily dose is 800 mg. The course is at least 2 months; repeated courses are as recommended by a doctor. The duration of treatment and the choice of individual dose depend on the severity of the patient’s condition and the effectiveness of treatment.

For complex therapy of mild and moderate cognitive disorders, the drug is prescribed without limiting the duration of the treatment course at a dose of 100 mg 3-4 times a day.

Adverse Reactions

Possible dryness and a “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

• Pregnancy;
• Lactation period;
• Age under 18 years;
• Hypersensitivity to the drug or its components.

With caution: allergic diseases and reactions in history.

Use in Pregnancy and Lactation

Etoxydol^® is contraindicated during pregnancy and lactation, because strictly controlled clinical studies of the safety of the drug use during pregnancy and lactation have not been conducted.

Pediatric Use

Contraindicated in children under 18 years of age.

Geriatric Use

For mild cognitive impairments inelderly patientsand for anxiety disorders – intramuscularly at a daily dose of 100-300 mg/day for 14-30 days.

Special Precautions

Influence on the ability to drive vehicles and mechanisms

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

Overdose

Symptoms sleep disorders (insomnia, in some cases drowsiness); with intravenous administration – a slight and short-term (up to 1.5-2 hours) increase in blood pressure.

Treatment as a rule, is not required – the symptoms disappear on their own within 24 hours. In severe cases with insomnia – nitrazepam 10 mg, oxazepam 10 mg or diazepam 5 mg. With an excessive increase in blood pressure – antihypertensive agents under blood pressure control.

Drug Interactions

Enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa).

Reduces the toxic effects of ethyl alcohol.

Storage Conditions

The drug should be stored in a dry, light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Do not use after the expiration date.

Dispensing Status

The drug is dispensed by prescription.

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.