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glutethimide

N05CE01

Forms & Strengths

Oral tablets: 250 mg, 500 mg

Adult Dosing

Insomnia: 250 mg to 500 mg orally at bedtime
Severe insomnia: 500 mg, occasionally repeated if necessary (rarely used due to abuse potential)

Pediatric Dosing

Safety and efficacy not established in pediatric patients; generally contraindicated or avoided in children

Indications

Short-term management of insomnia (historical usage; largely superseded by safer hypnotics like benzodiazepines and Z-drugs due to high abuse and overdose liability)

Mechanism of Action

Centrally acting sedative-hypnotic structurally related to barbiturates; depresses the central nervous system via GABA-ergic mechanisms, leading to sedation, hypnosis, and anesthesia in high doses

Contraindications

Known hypersensitivity to glutethimide
Porphyria
Severe respiratory depression
Uncontrolled chronic pain (unless accompanied by suitable analgesia)

Adverse Reactions

Drowsiness, hangover effect, paradoxical excitation, headache
Severe respiratory depression, apnea, hypotension, cardiovascular collapse in overdose
Tolerance, physical dependence, psychological dependence, withdrawal syndrome (similar to barbiturates)
Skin rash (frequently maculopapular, requiring cessation)

Drug Interactions

Central nervous system depressants (alcohol, opioids, barbiturates, benzodiazepines, tricyclic antidepressants): synergistic CNS and respiratory depression
Hepatic enzyme inducers/inhibitors: alters metabolism of concurrent medications (e.g., coumarin anticoagulants)

Curated Content: Needs Vetting Before Put to Clinical Use