Drug intelligence / Profile preview

thiamylal

Development stage
Unknown
Modality
Small Molecules
Administration
Intravenous
01

Overview

Thiamylal is a barbiturate derivative developed in the 1950s and primarily used as a short-acting intravenous anesthetic and sedative-hypnotic. It is indicated for the induction of general anesthesia, production of complete anesthesia of short duration, or to induce a hypnotic state. Thiamylal acts as a nonselective central nervous system depressant with sedative, anticonvulsant, and hypnotic effects. Its mechanism involves binding to distinct sites on the GABAA receptor complex (specifically at the chloride ionophore), increasing the duration that chloride channels remain open in response to GABA. This potentiates inhibitory neurotransmission in the CNS, especially within the thalamus[2][3][6][7]. Thiamylal is metabolized mainly by hepatic pathways and has rapid onset due to high lipid solubility; its clinical use includes induction for surgical anesthesia and as an anticonvulsant during certain anesthetic procedures[3][5]. Thiamylal is more potent than thiopental and has faster onset but shorter duration due to increased lipophilicity from sulfur substitution on its barbiturate backbone[5][6]. It remains in veterinary use (notably under Surital) for induction of anesthesia in animals such as horses and cattle[4][5]. In humans it may be combined with other agents for tension headaches or pain management but is less commonly used today due to availability of safer alternatives.

Brand names
Surital
Other names
Thioseconalthiamylal sodium
02

Targets

KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)GABRR (GABA-A receptor subunit rho)KCNJ8 (ATP-sensitive potassium channel subunit Kir6.1)

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