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Glutethimide

This article is a stubmissing:
Subjective Effects
Interactions
Tolerance
Glutethimide molecule structureGlutethimide molecule structure
Chemical Class

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 Its medical use has largely been superseded by other drugs.2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.

Threshold~250 mg
Light250 mg
Moderate500 mg
Strong750+ mg

Duration

Onset30-45 minutes
After Effects1-12 hours
Total2-8 hours

Subjective Effects

Subjective Effects not written up yet

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.

Metabolitesnone documented yet

Interactions

Interactions not written up yet

An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.

Check TripSit

Tolerance

Tolerance not written up yet

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

Lethal Dosage

Death in adults has been reported after 5 g;7 the usual lethal dose is reported as 10–20 g.7 Survival after 28 g has also been reported.9

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.

Article Status

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