Drug intelligence / Profile preview

etizolam

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Sublingual, Intranasal
01

Overview

Etizolam is a thienodiazepine derivative chemically related to benzodiazepines. It acts as a central nervous system depressant with anxiolytic, anticonvulsant, sedative-hypnotic, and muscle relaxant effects. Its primary mechanism is as a positive allosteric modulator at the benzodiazepine site of the Gamma-aminobutyric acid type A receptor (GABA-A receptor), enhancing GABAergic transmission and increasing inhibitory signaling in the brain. Etizolam is 6–10 times more potent than diazepam for most effects. It is used clinically for short-term management of anxiety disorders, panic disorder, insomnia, muscle tension/spasms and sometimes seizure prevention or pre-surgical sedation. Unlike classical benzodiazepines, etizolam contains a thiophene ring, altering its potency and duration of action. It has rapid absorption and an elimination half-life around 3.4 hours. Developed by Takeda Pharmaceutical Company, it's approved in some countries like Japan and Italy but has also emerged on illicit markets.

Brand names
EtilaamEtizestDepasEtizola
Other names
thienodiazepinedesigner benzodiazepinestreet benzodiazepine
02

Targets

GABRR (GABA-A receptor subunit rho)PTAFR (Platelet-activating factor receptor)

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