Drug intelligence / Profile preview

clomethiazole

Development stage
Phase 2
Lead developer
Lundbeck
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Clomethiazole is a sedative and hypnotic drug structurally related to thiamine (vitamin B1) but pharmacologically distinct from benzodiazepines and barbiturates. It acts as a positive allosteric modulator at the barbiturate/picrotoxin site of the GABAA receptor, enhancing the action of gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system. This results in anxiolytic, anticonvulsant, sedative, and hypnotic effects. Clomethiazole is primarily used for treating and preventing symptoms of acute alcohol withdrawal syndrome, agitation or restlessness in elderly patients (including those with dementia), short-term severe insomnia in elderly patients, and has also been used for neuroprotection in stroke research. The drug is approved under various brand names such as Heminevrin[1][2][3][5].

Brand names
Heminevrin
Other names
clomethiazolechlormethiazole
02

Targets

GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)

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