Etizolam is a thienodiazepine derivative, with high affinity for the benzodiazepine site in GABAA receptors. It was developed in the 1980’s as an alternative to known benzodiazepines. Also, it is readily absorbed and it has a shorter half-life than benzodiazepines.
However,it is sold commercially as a medicine to control generalized anxiety and other psychiatric pathologies in some countries. It is also sold in the internet by several companies for research purposes.
There have been a few studies comparing the differential pharmacological profile of etizolam compared to benzodiazepines. A major difference with benzodiazepines is its shorter half-life. It also differs from benzodiazepines as it has lower sedative effects. It has been proposed that this could be due to a lower affinity for GABAA receptors containing alpha1-subunits.
A. Routes of administration and dosage
Etizolam is administered orally. The usual clinical dose is 0.5 to 2.0 mg/day.
Etizolam is readily metabolized in humans and animals by microsomal oxidation at its methyl and ethyl groups. The hydroxylated derivatives of etizolam are conjugated
and excreted. Etizolam has a half-life of about 6 hrs. Thus, as stated by Fracasso et al, 1991, it should be considered as a short acting benzodiazepine. It has been shown that etizolam metabolism is affected by CYP2C19 polymorphism.
Etizolam has similar pharmacological profile than benzodiazepines. It acts by allosterically potentiating chloride currents induced by GABA in GABA-A receptors.
However, it has been shown some differences in its actions.
Etizolam is used, in some countries, for generalized anxiety disorder, panic disorder and to reduce anxiety. There is evidence that together with
being useful to treat generalized anxiety disorder, it produce significant improve of depressive symptoms.There is also a study showing that etizolam is useful to treat psychiatric symptoms in children and adolescents without or with minimal adverse effects.