Drug intelligence / Profile preview

chlorhexadol

Development stage
Discontinued
Lead developer
Wallace Laboratories
Modality
Small Molecules
Administration
Oral
01

Overview

Chlorhexadol is a hypnotic and sedative agent that was developed and evaluated in the early 1960s. Chemically, it is a hemiacetal derivative of chloral hydrate, specifically formed by the reaction of chloral with 2-methyl-2,4-pentanediol. Like other chloral derivatives, chlorhexadol functions as a prodrug that is rapidly metabolized in the body to trichloroethanol. Trichloroethanol is the active moiety responsible for the drug's central nervous system depressant effects, which it exerts by modulating GABA-A receptors. During its clinical evaluation, chlorhexadol was primarily investigated for the treatment of insomnia and was noted for its hypnotic efficacy. However, it has since been largely superseded by newer classes of sedative-hypnotics, such as benzodiazepines and non-benzodiazepine Z-drugs, and is no longer in common clinical use.

Brand names
LoraMeduane
Other names
chlorhexadolchlorhexadolum2-methyl-4-(2,2,2-trichloro-1-hydroxyethoxy)-2-pentanol
02

Targets

GABAA (Gamma-aminobutyric acid receptor)

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