A benzoxazine derivative.
Pharmacological action - anxiolytic .
In in vitro and in vivo studies on rats and mice, it was shown that the anxiolytic activity of etifoxine is due to a dual mechanism of action on GABA A receptors, which improves GABAergic impulse transmission. Under direct exposure, etifoxine binds mainly to the β 2 or β 3 subunits of the GABA A receptor (studies have shown that binding occurs at sites other than the binding sites of benzodiazepines) and causes allosteric modulation of GABA A-receptor. Indirect action is provided by increasing the synthesis of neurosteroids (as a result of activation of the mitochondrial translocator protein), such as allopregnanolone, which is also a positive allosteric modulator of the GABA A receptor.
Etifoxine is rapidly absorbed from the gastrointestinal tract , rapidly metabolized in the liver to the formation of several metabolites. One of the metabolites (diethylethifoxine) is active, and its T 1/2 is about 20 hours.
Penetrates through GPB.
T max in the blood is 2-3 hours, T 1/2 - 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 the bile.
Application of Etifoxine
- Treatment of psychosomatic manifestations of anxiety
- Eliminating anxiety,
- increased irritability,
- internal stresses,
- decreased mood (including against the background of somatic diseases, especially of a cardiovascular nature).
Hypersensitivity; shock conditions; myasthenia gravis; severe impairment of liver and / or kidney function; age up to 18 years.
Application during pregnancy and lactation
It is not recommended to use etifoxine during pregnancy. If pregnancy is detected while taking etifoxine, you should consult your doctor about continuing treatment.
It is not recommended to use etifoxine during breastfeeding.
Side effects of Etifoxin
Listed below are the undesirable effects observed when taking etifoxine, by systemic organ classes and frequency of occurrence: rarely (≥1 / 10000, <1/1000); very rare (<1/10000), in decreasing order of frequency.
From the nervous system: rarely - slight drowsiness that appears in the first days of admission and usually disappears on its own in the course of treatment.
On the part of the skin and subcutaneous tissue: rarely - skin reactions (maculopapular rash, erythema multiforme, itching, facial edema).
From the liver and biliary tract: the frequency has not been established - hepatitis, cytolytic hepatitis.
On the part of the genitals and breast: the frequency has not been established - metrorrhagia in women taking oral contraceptives.
From the gastrointestinal tract : the frequency has not been established - lymphocytic colitis.
Allergic reactions: very rarely - allergic reactions (urticaria, Quincke's edema); frequency not established - anaphylactic shock, drug-induced hypersensitivity syndrome with eosinophilia, Stevens-Johnson syndrome, leukocytoclastic vasculitis.
It potentiates the action of drugs that depress the central nervous system , such as opioid analgesics, barbiturates, hypnotics, antihistamines, antipsychotics. Enhances the effect of alcohol.
Symptoms: lethargy, excessive sleepiness.
Treatment: if necessary, symptomatic treatment is performed. There is no specific antidote.
Route of administration
The dose of the drug is determined by the doctor, individually, depending on the patient's condition.
Usually 1 capsule is prescribed 3 times a day, or 2 capsules 2 times a day. (150-200 mg / day)
Precautions of Etifoxine
If skin or allergic reactions occur, as well as complications from the liver, etifoxine should be discontinued.
If you skip taking etifoxine, you should not double the dose the next time you take it.
Due to the risk of drowsiness, during treatment, you should avoid driving vehicles and activities requiring increased attention, for example, controlling various mechanisms.
It is not recommended to take etifoxine together with alcoholic beverages and exceed the dose prescribed by your doctor.