Etoxidol, 100 mg 50 pcs.

Antioxidant drug

ATX code: C01EB

Pharmacological properties

Pharmacodynamics

Tethoxidol^® is an inhibitor of free radical processes, has membranoprotective, antihypoxic, nootropic, anticonvulsant, anxiolytic action, increases resistance to stress. Ethoxidol^® has anti-ischemic properties, improves blood flow in ischemic area, limits the zone of ischemic injury, shows hypolipidemic action, reduces the total cholesterol and low-density lipoproteins.

The drug increases resistance of the body to various damaging factors, to oxygen-dependent pathological states (shock, hypoxia and ischemia, cerebral circulatory disorders, intoxication with alcohol and antipsychotic drugs (neuroleptics).

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

The mechanism of action of the drug is caused by its antioxidant, antihypoxant and membrane-protective actions. It inhibits lipid peroxidation, increases superoxidase activity, increases lipid-protein ratio, decreases membrane viscosity and increases its fluidity.

Modulates the activity of membrane-bound enzymes (calcium independent phosphodiesterase, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which increases their ability to bind to ligands, helps to maintain the structural and functional organization of biomembranes, neurotransport and improve synaptic transmission.

Pharmacokinetics

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract at an average rate of 0.569±0.086 h^-1. In healthy volunteers, oral administration of Ethoxidol^® tablets at a dose of 100 mg found that the maximum concentration (C_max) in plasma reaches 0.28±0.08 hours and is 487.0±72.4 ng/ml followed by rapid drug elimination, with half-life (T_1/2) = 1.46±0.13 hours.

Ethoxidol^® is rapidly distributed throughout the organs and tissues of the body. It is determined in blood plasma for 7-10 hours.

The drug is extensively metabolized in the liver with the formation of phosphate-3-oxypyridine, glucuron-conjugated products.

Indications

– Coronary heart disease (as part of complex therapy);

– Complex therapy for ischemic stroke;

– Dyscirculatory encephalopathy;

– Mild to moderate cognitive impairment.

Active ingredient

Composition

One tablet contains:

The active ingredient:

ethylmethylhydroxypyridine malate (ethoxidol) – 100 mg.

Excipients:

acetylglutamic acid (N-acetyl-L-glutamic acid) – 68 mg,

deanol (2-dimethylaminoethanol) – 32 mg,

glycine – 20 mg,

microcrystalline cellulose – 260.1 mg,

povidone (collidone 90F) – 1.6 mg,

lactose monohydrate (milk sugar) – 36 mg,

pregelatinized starch (starch 1500) – 30 mg,

colloidal silica (aerosil) – 9.5 mg,

magnesium stearate – 6 mg,

croscarmellose sodium (primellose) – 12.8 mg,

sodium cyclamate – 18 mg,

orange flavoring (Orange food flavoring) – 6 mg.

How to take, the dosage

For complex therapy of ischemic heart disease and therapy of ischemic stroke, 100 mg (1 tablet) 3 times daily, gradually increasing the dose until therapeutic effect is achieved.

The maximum single dose is 200 mg; the daily dose is 800 mg.

The course is at least 2 months, repeated courses – on the doctor’s recommendation. The duration of treatment and the choice of the individual dose depend on the severity of the patient’s condition and the effectiveness of the treatment.

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

Interaction

It enhances the effect of antiepileptic drugs (carbamazepine), anti-Parkinsonian drugs (levodopa) and benzodiazepine anxiolytics. Increases antianginal activity of nitropreparations and hypotensive activity of ACE inhibitors and beta-adrenoblockers. Reduces toxic effects of ethyl alcohol.

Special Instructions

Synopsis

The tablets are white or white with a creamy tint, flat-cylindrical shape, beveled and rimmed; “marbling”, specks and some surface roughness are allowed.

Contraindications

Hypersensitivity to the components of the drug, lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Acute hepatic and/or renal failure, pregnancy, lactation, age under 18 years (efficacy and safety have not been established).

Side effects

The drug is usually well tolerated. In rare cases, allergic reactions, dyspeptic disorders, nausea and dry mouth, diarrhea may occur, which quickly disappear on their own or with discontinuation of the drug.

Long-term use may cause flatulence, sleep disturbances (drowsiness or disturbance in falling asleep).

Overdose

The treatment is symptomatic.

Pregnancy use

Itoxidol is contraindicated in pregnancy and during breastfeeding because strictly controlled clinical studies of the safety of the drug in pregnancy and lactation have not been conducted.