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Glutethimide![]() |
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indicationFor the treatment of insomnia.pharmacologyGlutethimide is a hypnotic sedative that was introduced in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms.mechanism of actionGlutethimide seems to be a GABA agonist which helps induced sedation. It also induces CYP 2D6. When taken with codeine, it enables the body to convert higher amounts of the codeine (higher than the average 5 - 10%) to morphine. The general sedative effect also adds to the power of the combination.toxicityIn 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.biotransformationHepatic. Glutethimide is almost completely metabolized.absorptionVariablehalf life10-12 hoursroute of eliminationglutethimide 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.drug interactionsAcenocoumarol: Glutethimide may decrease the anticoagulant effect of acenocoumarol.Anisindione: Glutethimide may decrease the anticoagulant effect of anisindione. Dicumarol: Glutethimide may decrease the anticoagulant effect of dicumarol. Donepezil: Possible antagonism of action Galantamine: Possible antagonism of action Rivastigmine: Possible antagonism of action Triprolidine: The CNS depressants, Triprolidine and Glutethimide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. Warfarin: Glutethimide may decrease the serum concentration of warfarin by increasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if glutethimide is initiated, discontinued or dose changed. |