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Glutethimide
Glutethimide is a member of the piperidine chemical class1 with sedative and hypnotic effects.2 It promotes sleep and is used to treat insomnia.3 It was introduced in 1954 as a supposedly safer alternative to barbiturates,4 but was subsequently found to be just as likely to cause addiction and withdrawal symptoms. Its medical use has largely been superseded by other drugs.2
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Glutethimide enhances GABA-A receptor activity through positive allosteric modulation5, contributing to its sedative action. It also appears to act as an agonist at the receptor's alpha-1 subunit.5 In animal models, the (R) isomer has greater anticonvulsant activity than the (S) isomer.
Pharmacokinetics
Glutethimide absorption is variable6 and is unaffected by food. It is inactivated by conjugation.6 Metabolites are excreted in urine,6 with only 2% of the parent substance excreted unchanged in urine6 and up to 2% of the dose reported in feces.6 Its elimination half-life is 10-12 hours.6 Glutethimide induces CYP2D6.3 Computational predictions suggest intestinal absorption, blood-brain barrier penetration, and substrate activity at P-glycoprotein and CYP3A4.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
Addiction & Dependence
Psychological
Glutethimide is habit-forming,7 with addiction potential comparable to barbiturates.8
Physical
Glutethimide can cause withdrawal symptoms,9 with a propensity comparable to barbiturates. Abrupt discontinuation can produce rebound effects resembling withdrawal from other GABAergic substances.
Toxicity
History & Culture
Glutethimide was developed by Ciba Specialty Chemicals in 1954 and introduced as an alternative to barbiturates that was intended to be safer for treating insomnia. Patent US2673205A lists Hoffmann Karl and Tagmann Eugen as its inventors.10 The U.S. Food and Drug…
Legality
International
Regulatory groupings include approved and illicit.
References
Citations
Article Status
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