Etifoxine

Anxiolytic drug

Etifoxine
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Etifoxine is an anxiolytic drug used primarily for the treatment of anxiety disorders. It is known for its unique mechanism of action, which differs from that of traditional benzodiazepines.

Pharmacology

Etifoxine acts as a positive allosteric modulator of the GABA_A receptor, enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) in the central nervous system. Unlike benzodiazepines, etifoxine does not bind directly to the benzodiazepine site on the GABA_A receptor. Instead, it is believed to interact with the _2 and _3 subunits of the receptor, leading to increased chloride ion influx and neuronal hyperpolarization.

Additionally, etifoxine stimulates the production of neurosteroids such as allopregnanolone, which further potentiate GABAergic transmission. This dual mechanism contributes to its anxiolytic effects without the sedative and muscle relaxant properties commonly associated with benzodiazepines.

Clinical Use

Etifoxine is prescribed for the management of anxiety disorders, particularly when patients are sensitive to the side effects of benzodiazepines. It is favored for its lower risk of dependence and tolerance development. The drug is typically administered orally, and the dosage is adjusted based on the severity of symptoms and patient response.

Side Effects

Common side effects of etifoxine include drowsiness, dizziness, and gastrointestinal disturbances. Rarely, it may cause allergic reactions or hepatic dysfunction. Patients are advised to avoid alcohol consumption during treatment, as it may potentiate the effects of the drug.

Mechanism of Action

Chemical structure of Etifoxine and Chlordiazepoxide

Etifoxine's mechanism of action involves modulation of the GABA_A receptor and stimulation of neurosteroid synthesis. By enhancing GABAergic transmission, it exerts a calming effect on the nervous system, reducing symptoms of anxiety. The increase in neurosteroid levels also contributes to its anxiolytic properties, providing a broader spectrum of action compared to traditional anxiolytics.

Comparison with Benzodiazepines

Etifoxine offers several advantages over benzodiazepines, including a lower risk of sedation, cognitive impairment, and addiction. It is particularly useful in patients who require long-term management of anxiety without the complications associated with benzodiazepine use.

Related pages

• Anxiolytic
• GABA_A receptor
• Neurosteroid
• Benzodiazepine