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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
From an SAR perspective, the related analog rogletimide (Figure 8.13) generated interest as it had similar selective aromatase inhibition activity to aminoglutethimide but with no significant sedative effect. However, its lower aromatase-inhibitory potency prevented further progression in the clinic. The other related analog, glutethimide, is a hypnotic sedative that was introduced by Ciba in 1954 (marketed as DoridenTM) as a safe alternative to barbiturates for the treatment of insomnia. However, before long it become clear that glutethimide was just as likely to cause addiction and led to similarly severe withdrawal symptoms. Glutethimide is still available today, but is tightly controlled due to its addictive properties and is rarely prescribed.
Alcohol and Sedatives
Published in Frank Lynn Iber, Alcohol and Drug Abuse as Encountered in Office Practice, 2020
Glutethimide is a Schedule III drug with cross-tolerance for this group of agents. It is erratic in absorption, with some people absorbing only half the drug, others hydrolyzing the biliary excreted conjugate once it reaches the gut and reabsorbing it. Its half life is 10 to 12 h with much variation. The lengthy duration leads to increased toxicity. The drug is highly dialyzable in overdose, which is an effective means for removal. For reasons unclear to this author, glutethimide is the most abused of the sedative drugs now that methaqualone is no longer readily available.8
Barbiturates, Alcohol, And Tranquilizers
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
Glutethimide dependence may occur when the drug is taken in doses of 2.5 g over a period of three months. Symptoms of the glutethimide abstinence syndrome are similar to those produced by barbiturate or meprobamate withdrawal. They include vomiting, abdominal cramps, agitation, tremor, sweating, hyperpyrexia, and tachycardia. The major withdrawal manifestations are seizures and a delirium consisting of disorientation, confusion, and hallucinations. Multiple seizures have been precipitated 16 hours after withdrawal of the drug, though the onset of convulsions may be delayed until the sixth day of abstinence.
Time trends in hospitalizations with anxiolytic, sedative, or hypnotic drug use disorder: a 17-year U.S. national study
Published in Journal of Addictive Diseases, 2022
Anxiolytic, sedative, or hypnotic drugs (ASH) are commonly prescribed medications in the United States. These include drugs/drug groups, such as benzodiazepines, benzodiazepine-like substances (e.g., zolpidem, zaleplon, and eszopiclone), barbiturates, melatonin agonists (ramelteon, tasimelteon, and agomelatine), orexin antagonists (suvorexant), chloral hydrate, glutethimide, methaqualone, and meprobamate.