Stresam, 50 mg capsules 60 pcs

Pharmacotherapeutic group:

Anxiolytic medicine (tranquilizer).

ATX CODE: N05BX03

Pharmacological properties

Ethifoxine hydrochloride belongs to benzoxazine derivatives.

As an anxiolytic agent, ethifoxine has an autonomous regulatory effect. In in vitro and in vivo studies in rats and mice it was shown that the anxiolytic activity of ethifoxine is due to its dual mechanism of action (direct and mediated) on GABA-A receptors, which improves GABAergic impulse transmission.

In direct action on the GABA-A receptor by allosteric modulation, ethifoxine binds predominantly to β2 or β3 receptor subunits; studies have shown that ethifoxine binds to the GABA-A receptor at sites other than the benzodiazepine binding site. Indirect action is provided by increasing the synthesis of neurosteroids (through activation of the mitochondrial translocator protein,) such as allopregnanolone, which is also a positive allosteric modulator of the GABA-A receptor.

PHARMACOKINETICS:

It is rapidly absorbed from the GI tract and is rapidly metabolized in the liver to form several metabolites. One of the metabolites (diethyl etifoxin) is active and has a half-life of about 20 hours.

It penetrates the placental barrier.

The time to reach maximum concentration in the blood is 2-3 hours, the elimination half-life is about 6 hours.

Extracted mainly in the urine as metabolites, and also in unchanged form in small amounts. It is also excreted with bile.

Indications

Eliminate anxiety
increased irritability,
fear,
internal stresses,
decreased mood (including against the background of somatic diseases, especially cardiovascular ones).

Pharmacological effect

PHARMACOTHERAPEUTIC GROUP:

anxiolytic drug (tranquilizer).

ATX CODE: N05BX03

PHARMACOLOGICAL PROPERTIES

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 showed that the anxiolytic activity of etifoxine is due to the dual mechanism of its action (direct and indirect) on GABA-A receptors, which improves GABAergic impulse transmission.

When acting directly on the GABA-A receptor through allosteric modulation, etifoxine binds predominantly to the β2 or β3 subunits of the receptor; Studies have shown that etifoxine binds to the GABA-A receptor at sites different from the binding site of benzodiazepines. The indirect effect is achieved by increasing the synthesis of neurosteroids (via activation of mitochondrial translocator protein), such as allopregnanolone, which is also a positive allosteric modulator of the GABA-A receptor.

PHARMACOKINETICS:

quickly absorbed from the gastrointestinal tract, quickly metabolized in the liver to the formation of several metabolites. One of the metabolites (diethylethifoxine) is active and has a half-life of about 20 hours.

Penetrates through the placental barrier.

The time to reach maximum concentration in the blood is 2-3 hours, the half-life is about 6 hours.

It is excreted mainly in the urine in the form of metabolites, as well as unchanged in small quantities. Also excreted in bile.

Special instructions

If you miss a dose of the drug, you should not double the dose the next time you take it.

The dose prescribed by the doctor should not be exceeded.

It is not recommended to take the drug while drinking alcoholic beverages.

Stresam contains lactose, which should be taken into account when prescribing the drug to patients with galactosemia, glucose and galactose malabsorption syndrome, as well as in cases of lactase deficiency.

Use in pediatrics

It is not recommended to use the drug in children and adolescents under 18 years of age.

Impact on the ability to drive vehicles and operate machinery

Due to the risk of drowsiness, you should avoid driving vehicles and activities that require increased attention, such as operating various mechanisms.

Active ingredient

Etifoxine

Composition

1 capsule contains:

Etifoxine hydrochloride 50 mg

Lactose monohydrate 119 mg

Talc 15 mg

Microcrystalline cellulose 10 mg

Silicon dioxide colloidal anhydrous 3 mg

Magnesium stearate 3 mg

Composition of the capsule shell:

titanium dioxide

gelatin

indigo carmine

DESCRIPTION: smooth shiny gelatin capsules No. 2 with a white body and a blue cap. Contents: white or white powder with a slight yellowish tint.

Pregnancy

The use of the drug during pregnancy and breastfeeding is contraindicated.

If pregnancy is detected during treatment with Stresam, you should consult your doctor about continuing treatment.

Contraindications

Hypersensitivity to the active ingredient or other component of the drug, shock, myasthenia gravis, severe dysfunction of the liver and/or kidneys. Due to the presence of lactose in the drug, the drug should not be used for galactosemia, glucose and galactose malabsorption syndrome, as well as in case of lactase deficiency.

Not recommended for use by people under 18 years of age.

Side Effects

The following are the adverse events (AEs) observed while taking this drug, according to the classification by system-organ classes and frequencies of occurrence (“rare”: ≥1/10,000 and <1/1000, “very rare”:

<1/10,000) in descending order of frequency.

Nervous system disorders

Rare: slight drowsiness that appears in the first days of treatment and usually disappears on its own during treatment.

Skin and subcutaneous tissue disorders

Rarely: skin reactions: maculopapular rash, erythema multiforme, itching, facial swelling.

Very rare: allergic reactions: urticaria, Quincke’s edema.

Frequency not established: anaphylactic shock, drug-induced hypersensitivity syndrome with eosinophilia, Stevens-Johnson syndrome, leukocytoclastic vasculitis.

Disorders of the liver and biliary tract

Frequency not established: hepatitis, cytolytic hepatitis.

Disorders of the genital organs and breast

Frequency not established: metrorrhagia in women taking oral contraceptives.

Gastrointestinal disorders

Frequency not established: lymphocytic colitis.

Interaction

potentiates the effect of drugs that depress the central nervous system, such as opioid analgesics, barbiturates, hypnotics, antihistamines, antipsychotics, etc. Also enhances the effects of alcohol.

Overdose

Symptoms: lethargy, excessive sleepiness.

Treatment: gastric lavage with plenty of water, symptomatic treatment. There is no specific antidote.

Storage conditions

At 15–25 °C

Shelf life

3 years

Manufacturer

Biocode, France