Drug intelligence / Profile preview

methohexital

Development stage
Approved
Lead developer
Eli Lilly
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Methohexital is a short-acting barbiturate derivative used primarily as an intravenous anesthetic for the induction of anesthesia and deep sedation in surgical, diagnostic, or therapeutic procedures. It acts by binding to a distinct site on the gamma-aminobutyric acid type A (GABA-A) receptor complex at the chloride ionophore, increasing the duration that the chloride channel remains open. This potentiates GABAergic inhibitory neurotransmission in the central nervous system, resulting in rapid onset of unconsciousness and sedation. Methohexital is notable for its rapid onset (within 30 seconds IV) and short duration of action with quick recovery times compared to other barbiturates. Unlike many other barbiturates, it lowers seizure threshold and is sometimes used during electroconvulsive therapy (ECT). It provides little analgesia; use in painful procedures may cause excitation[1][2][6].

Brand names
BrevitalBrietal
Other names
methohexitonemethohexital sodium
02

Targets

GABRR (GABA-A receptor subunit rho)

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