Drug intelligence / Profile preview

clotiazepam

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Clotiazepam is a thienodiazepine derivative belonging to the benzodiazepine class, used primarily for the short-term management of anxiety disorders and insomnia. It possesses anxiolytic, sedative, hypnotic, anticonvulsant, amnesic, and skeletal muscle relaxant properties. Its mechanism of action involves binding as a full agonist to the benzodiazepine site on the Gamma aminobutyric acid type A receptor (GABA A receptor) complex in the central nervous system. This enhances GABAergic neurotransmission by increasing chloride ion influx through GABA A receptor channels, leading to neuronal hyperpolarization and reduced excitability. The drug is rapidly absorbed after oral administration and has a relatively short elimination half-life (approximately 4–18 hours), resulting in less accumulation with repeated dosing compared to longer acting benzodiazepines. It is metabolized hepatically via oxidation into hydroxy-clotiazepam and desmethyl-clotiazepam[1][2][3][4].

Brand names
RizeTrecalmoRizenTienorRiseDistensanClozanVeratran
Other names
Clotiazepamum [INN-Latin]ClotiazepamumClotiazepam [INN:JAN]CLOTIAZEPAM [MI]CLOTIAZEPAM [INN]
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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