Strеsam® [Etifoxine] Instruction

International Non-Proprietary Name (INN): etifoxine
Dosage form: capsules (50 mg)
Structure
In 1 capsule:
Active ingredient: etifoxine hydrochloride 50 mg;
Excipients: lactose monohydrate, talc, microcrystalline cellulose, anhydrous colloidal silicon dioxide, magnesium stearate;
Capsule shell composition: titanium dioxide, gelatin, indigo carmine.
Description
Smooth, shiny gelatin capsules with a white body and a blue cap. The content is a powder of white or white with a slight yellowish tint color.
Pharmacological classification: anxiolytic (tranquilizer)
ATC code: N05BX03
Pharmacological action: anxiolytic


Pharmacodynamics

Etifoxine hydrochloride is a benzoxazine derivative. As an anxiolytic, etifoxine has an autonomous controlling effect. In vitro and in vivo studies of rats and mice have shown that anxiolytic activity of etifoxine is driven by the dual mechanism of its action (direct and indirect) on GABA-A receptors, which improves GABAergic impulse transmission. When there is a direct effect on the GABA-A receptor by allosteric modulation, etifoxine binds predominantly with β2 or β3 receptor subunits; studies have shown that etifoxine binds with the GABA-A receptor at a binding site other than benzodiazepines. The indirect effect is provided by increasing the synthesis of neurosteroids (by activation of mitochondrial translocator protein), such as allopregnanolone, which is also a positive allosteric modulator of the GABA-A receptor.

Pharmacokinetics

Absorption: Strеsam is quickly absorbed from the gastrointestinal tract. The maximum concentration in blood is reached within 2-3 hours.

Distribution: Strеsam penetrates through the placental barrier.

Metabolism: Strеsam metabolizes quickly in the liver until it forms several metabolites. One of the metabolites – diethyl-etifoxine – is active.

Excretion: Etifoxine’s half-life is around 6 hours; the active metabolite’s half-life is 20 hours. It is mainly excreted in the urine in the form of metabolites and in small amounts in the unchanged form. It is also excreted in bile.

Intended uses

Strеsam is used for the treatment of psychosomatic signs of anxiety, fear, inner tension, increased irritability, and decreased mood (including associated with somatic diseases and especially diseases of cardiovascular nature).

Contraindications

Hypersensitivity to the active ingredient or other components of the drug, shock state, myasthenia, and severe disorders of the liver and/or kidney function. Due to the presence of lactose in the drug, it should not be used if the patient suffers from galactosemia, glucose-galactose malabsorption syndrome, and lactase deficiency.

It is not recommended to use the drug at the age below 18 years old as well as during pregnancy or lactation.

Dosage and administration

Ingest orally with a small amount of water. The dosage of the drug is determined by the doctor individually, depending on the patient’s condition. The usual dosage is 1 capsule three times a day, or 2 capsules twice a day (150–200 mg/day). The length of the treatment varies from several days to 4–6 weeks, depending on the patient’s condition.

Side effects

Definition of the frequency of adverse events: rarely (≥ 1/10,000 and < 1/1,000), very rarely (< 1/10,000) in decreasing order of frequency.

Central nervous system disorders
Rare: Insignificant drowsiness during the first days of taking the drug. It usually disappears on its own in the process of treatment.

Skin and subcutaneous tissue disorders
Rare: Maculopapular rash, erythema multiform, itching, facial edema; (very rare) urticaria, Quincke’s edema; (frequency unidentified) anaphylactic shock, drug-induced hypersensitivity syndrome with eosinophilia, Stevens-Johnson syndrome, leukocytoclastic vasculitis.

Hepatobiliary disorders
Frequency unidentified: Hepatitis, cytolytic hepatitis.

Reproductive system and breast disorders
Frequency unidentified: Metrorrhagia among women who take oral contraceptives.

Gastrointestinal tract disorders
Frequency unidentified: Lymphocytic colitis.

Overdose

Symptoms
Torpidity, excessive drowsiness.

Treatment
If necessary, symptomatic treatment is provided. There is no specific antidote.

Interaction with other drugs

Potentiates effects of drugs that inhibit the central nervous system such as opioid analgesics, barbiturates, opiates, antihistamines, neuroleptics, etc. Also potentiates the effects of alcohol.

Special precaution

In case of skin or allergic reactions or liver complications administration of Stresam® should be discontinued.

If you missed taking the drug, do not double the dose at the next intake.

IT IS NOT RECOMMENDED TO TAKE THE DRUG ALONG WITH ALCOHOL.

DO NOT EXCEED THE DOSE PRESCRIBED BY YOUR DOCTOR.

Pregnancy and lactation

It is not recommended to take Strеsam during pregnancy. If pregnancy is detected during the treatment, you should consult your doctor about the continuation of the treatment. It is not recommended to take Strеsam during lactation.

Influence on the ability to drive vehicles and operate mechanisms

Due to the risk of drowsiness, during the treatment, you should avoid driving vehicles or engaging into activity, which requires increased attention such as operating various mechanisms.

Terms of release from pharmacy

On prescription.

Storage conditions

Store at temperatures of 15–25°C. Keep out of reach of children.

Shelf life

3 years. Do not use beyond the expiration date.

Manufacturer

Biocodex, France. https://www.biocodex.com/

Instructions