OX2 antagonist
Orexin-2 receptor antagonist
- Blocks the dominant wake-promoting orexin-2 (OX2) pathway → sleep
- ↑ REM sleep
- possible cataplexy
- MDD
- agitation in dementia
- Next-day somnolence, vivid dreams, sleep paralysis
Drugs with this mechanism (4)
- Daridorexant — Dual orexin antagonist hypnotic with a short half-life for less next-day effect.
- Lemborexant — Dual orexin antagonist hypnotic.
- Seltorexant — Investigational selective orexin-2 antagonist for insomnia and depression.
- Suvorexant — Dual orexin antagonist for sleep-onset and sleep-maintenance insomnia.
Self-check
- Which sleep stage increases with OX2 blockade?
REM sleep. - Which next-day effect can follow OX2 blockade?
Somnolence.
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