PH3.2 | PH3.2 | Sedative and Hypnotic Agents — SDL Guide — Summary & Reflection

KEY TAKEAWAYS

Sedative-hypnotic agents include benzodiazepines (↑frequency of GABA-A Cl⁻ channel opening; reversible with flumazenil; dependence risk), barbiturates (↑duration of GABA-A Cl⁻ channel opening; can open channel directly — no ceiling, no reversal agent; CYP enzyme inducers), and Z-drugs (α₁-selective GABA-A agonists; short-acting; dependence risk; parasomnias). Diazepam is long-acting (active metabolite desmethyldiazepam); lorazepam has no active metabolite (preferred in hepatic impairment/elderly). Newer agents — ramelteon (MT₁/MT₂ agonist, no dependence) and suvorexant (dual orexin antagonist) — offer alternatives with lower dependence liability. Barbiturate overdose has no antidote; BZD overdose is reversed by flumazenil. Use ≤4 weeks; taper to avoid withdrawal seizures.

REFLECT

A 72-year-old woman on diazepam 5 mg nightly for insomnia for the past year asks you if she can 'just stop the tablets' as she wants to avoid medications. What would you tell her, and what pharmacological strategy would you use to manage the cessation safely? How does understanding the mechanism of dependence (GABA-A down-regulation) and the specific active metabolite profile of diazepam in elderly patients influence your approach?