Drug intelligence / Profile preview

glutethimide

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Glutethimide is a non-barbiturate sedative-hypnotic drug introduced by Ciba in 1954 and marketed as Doriden. It was developed as a safer alternative to barbiturates for the treatment of insomnia but was later found to have similar risks of dependence, abuse, and severe withdrawal symptoms. Its primary mechanism of action is as a positive allosteric modulator (agonist) at the GABA(A) receptor, enhancing inhibitory neurotransmission in the central nervous system and producing sedative effects. Glutethimide also induces cytochrome P450 2D6 (CYP2D6), which can increase the conversion of codeine to morphine when co-administered, leading to enhanced sedation and risk of respiratory depression. Due to its high potential for abuse and toxicity, glutethimide has been discontinued or banned in many countries[1][2][5][6].

Brand names
Doriden
Other names
2-ethyl-2-phenylglutarimideGlutetimida
02

Targets

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

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