Drug intelligence / Profile preview

heptabarbital

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Heptabarbital is a barbiturate drug that was primarily used as a sedative and hypnotic for the treatment of insomnia. It is classified as an intermediate or short-acting barbiturate. Heptabarbital acts by binding to the GABAA receptor at either the alpha or beta subunit—sites distinct from those of GABA itself and benzodiazepines—potentiating the inhibitory effects of GABA in the central nervous system. This results in decreased neuronal excitability through increased chloride influx into neurons, leading to sedation and hypnosis. In addition to its action on GABAA receptors, heptabarbital also blocks AMPA-type glutamate receptors (reducing excitatory neurotransmission) and appears to bind neuronal nicotinic acetylcholine receptors. The drug undergoes hepatic metabolism and has an elimination half-life ranging from 6.1 to 11.2 hours; it is excreted renally[1][2][4][5].

Brand names
EudanMedapanMedominNoctyn
Other names
heptabarbitoneheptabarb
02

Targets

AMPAR (AMPA receptor)GABRR (GABA-A receptor subunit rho)Nicotinic Acetylcholine Receptor

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