Pharmacology
DrugBankDescription
Glutethimide is a hypnotic and sedative. Its use has been largely superseded by other drugs.
Mechanism of Action
Glutethimide seems to be a GABA agonist which helps induce sedation. It also induces CYP 2D6. When taken with codeine, it enables the body to convert higher amounts of codeine (higher than the average 5 - 10%) to morphine. This combination of effects enhances sedation.
Pharmacodynamics
Glutethimide, like the barbiturates, is a hypnotic sedative. It was introduced in 1954 as a safer alternative to barbiturates but was soon determined to be just as likely to cause addiction and withdrawal symptoms.
Metabolism
Hepatic. Glutethimide is almost completely metabolized.
Toxicity
In adults, death has been reported after 5 g. The usual lethal dose is 10 to 20g, although survival after a dose of 28 g has been reported.
Indication
For the treatment of insomnia.
Elimination
glutethimide is inactivated by conjugation and the metabolites are excreted in urine, only 2% of the parent substance is excreted in urine, up to 2% of the dose has been reported to be found in the faeces.
Effect Profile
CuratedStrong euphoria with mild sedation and itching/nausea