Routes of
administration Oral Bioavailability 90% | ATC code N05BX03 (WHO) Molar mass 300.7827 g/mol | |
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AHFS/Drugs.com International Drug Names Pregnancy
category Not recommended. Crosses the placental barrier Legal status US: Unscheduled and not FDA approved | ||
Etifoxine (INN, also known as etafenoxine; trade name Stresam) is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. It is used in some countries for anxiety disorders. It has similar effects to benzodiazepine drugs, but is structurally distinct and does not bind to the benzodiazepine receptor. It is more effective than lorazepam as an anxiolytic, and has fewer side effects. Etifoxine is not approved by the U.S. Food and Drug Administration or the European Medicines Agency.
Contents
Side effects
The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines Etifoxine for Pain Patients with Anxiety
Mechanism of action
Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines. This difference in binding means that etifoxine can be used alongside benzodiazepines to potentiate their effects without competing for binding sites; however, it also means that the effects of etifoxine are not reversed by the benzodiazepine antagonist flumazenil.
Etifoxine has been shown to stimulate the biosynthesis of endogenous neurosteroids, namely 17-hydroxypregnenolone, dehydroepiandrosterone, progesterone and tetrahydroprogesterone. This is likely to contribute to the drug's effects, to what extent however, is unclear.