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Active ingredients
Ethifoxin
Release form
Capsules
Composition
Active ingredient: Etifoxine Concentration of active ingredient (mg): 50 mg
Pharmacological effect
Anxiolytic (tranquilizer). Etifoxine hydrochloride belongs to benzoxazine derivatives. As an anxiolytic agent, etifoxine has an autonomous regulatory effect. In vitro and in vivo studies in rats and mice, it was shown that the etipoxin anxiolytic activity is due to its dual mechanism of action (direct and mediated) on GABA-A receptors, which improves GABA-ergic transmission of the impulse. by allosteric modulation, etifoxine binds predominantly to the β2 or β3 receptor subunits; Studies have shown that etifoxine binds to the GABA-A receptor at sites other than the benzodiazepine binding site. Indirect action is provided by increasing the synthesis of neurosteroids (by activating the mitochondrial protein translocator), such as allopregnanolone, which is also a positive aplosteric modulator of the GABA-A receptor.
Pharmacokinetics
AbsorptionAfter ingestion, the drug is rapidly absorbed from the gastrointestinal tract. Time to reach Cmax in the blood is 2-3 hours. Distribution Penetrates through the placental barrier. Metabolism is rapidly metabolized in the liver to form several metabolites. One of the metabolites, diethylethoxoxin, is active. Excretion of T1 / 2 etipoxin is about 6 hours, T1 / 2 of the active metabolite is 20 hours. It is eliminated mainly with urine as metabolites and in small quantities in unchanged form; also excreted in the bile.
Indications
it is used to eliminate anxiety, fear, internal stress, increased irritability, decrease in mood, including against the background of somatic diseases, especially of cardiovascular nature.
Contraindications
shock, myasthenia gravis, severe disorders of the liver and / or kidneys, hypersensitivity. Not recommended for use under the age of 18 years.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
AbsorptionAfter ingestion, the drug is rapidly absorbed from the gastrointestinal tract.Time to reach Cmax in the blood is 2-3 hours. Distribution Penetrates through the placental barrier. Metabolism is rapidly metabolized in the liver to form several metabolites. One of the metabolites, diethylethoxoxin, is active. Excretion of T1 / 2 etipoxin is about 6 hours, T1 / 2 of the active metabolite is 20 hours. It is eliminated mainly with urine as metabolites and in small quantities in unchanged form; also excreted in the bile.
Dosage and administration
inside, with a little water. The dose of the drug is determined by the doctor, individually, depending on the condition of the patient. Usually it is prescribed 1 capsule 3 times a day, or 2 capsules 2 times a day. (150-200 mg / day) Duration of treatment - from several days to 4-6 weeks, depending on the condition of the patient.
Side effects
slight drowsiness that appears in the first days of admission and usually disappears on its own during treatment; rarely, skin rashes, as well as allergic reactions in the form of urticaria and angioedema.
Overdose
Symptoms: lethargy, excessive drowsiness. Treatment: if necessary, symptomatic therapy is carried out. The specific antidote is absent.
Interaction with other drugs
Stresam potentiates the action of drugs that inhibit the central nervous system (including opioid analgesics, barbiturates, sleeping pills, antihistamines, antipsychotics). Stresam enhances the effects of ethanol.
special instructions
If you experience skin or allergic reactions, as well as complications of the liver, the drug should not be taken. If you miss a drug intake, do not double the dose at the next dose. Do not exceed the prescribed dose. Do not use the drug. Pediatrics It is not recommended to use the drug in children and adolescents under the age of 18. Influence on the ability to drive vehicles and control mechanismsIn connection with the risk of drowsiness should be avoided driving a vehicle and activities requiring increased attention, for example, controlling various mechanisms.