- Glutethimide is used as a sedative-hypnotic for short-term insomnia management.
- Glutethimide enhances GABAergic activity, inducing sleep with CNS depressant effects.
Chemical Formula:
- C₁₃H₁₅NO₂
Mechanism of Action:
- Depresses CNS via non-specific action on reticular formation.
- Weak GABA-A agonist effects (no specific receptor binding like BZDs).
- CYP450 inducer — may enhance metabolism of other drugs (notably codeine → morphine conversion).
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Therapeutic Uses:
- Historical use as sedative/hypnotic (replaced by safer drugs).
Side Effects:
- Respiratory depression
- Dependence & withdrawal
- Drug interaction risk (enzyme induction)
- Overdose → coma
SAR Notes:
- Imide ring essential for CNS activity.
- Lipophilic substituents enhance hypnotic potency.
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