Drug intelligence / Profile preview

estazolam

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Estazolam is a triazolobenzodiazepine derivative and oral hypnotic agent used for the short-term management of insomnia. It acts as a benzodiazepine, binding to benzodiazepine receptors that are coupled to gamma-aminobutyric acid-A (GABA-A) receptors in the central nervous system. This enhances GABAergic inhibition by increasing GABA affinity for its receptor, leading to increased chloride influx, hyperpolarization of neurons, and reduced neuronal excitability. Estazolam has anticonvulsant, hypnotic, anxiolytic, and muscle relaxant properties. It is generally prescribed for 7–10 days due to risks of dependence and tolerance.

Brand names
Prosom
Other names
estazolam
02

Targets

BZD site (GABA-A receptor benzodiazepine site)TSPO (Translocator Protein (18 kDa))

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