Drug intelligence / Profile preview

chloral betaine

Development stage
Discontinued
Lead developer
Mead Johnson Nutrition
Modality
Small Molecules
Administration
Oral, Rectal
01

Overview

Chloral betaine is a sedative-hypnotic agent consisting of a chemical complex of chloral hydrate and betaine. It was developed to provide a stable, solid dosage form of chloral hydrate, which is otherwise a volatile solid with an unpleasant taste and irritant properties. Upon ingestion, the complex dissociates into its constituent parts; the chloral hydrate is then rapidly metabolized by alcohol dehydrogenase into trichloroethanol, the active metabolite responsible for the drug's pharmacological effects. Trichloroethanol acts as a positive allosteric modulator of the GABA-A receptor, enhancing inhibitory neurotransmission in the central nervous system. Historically, chloral betaine was used for the short-term treatment of insomnia and as a preoperative sedative, particularly in elderly or mentally disturbed patients, though it has largely been replaced by safer alternatives such as benzodiazepines.

Brand names
Beta-Chlor
Other names
BetachlorChloral betaine complexBetaine chloral hydrate
02

Targets

GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)

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