Daridorexant: Difference between revisions
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MDElliottMD (talk | contribs) Category taxonomy ship: retag Sedative-Hypnotics -> Sedative-hypnotics |
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| brand = Quviviq | | brand = Quviviq | ||
| classes = Dual orexin receptor antagonist (DORA) | | classes = Dual orexin receptor antagonist (DORA) | ||
| mechanism = Selective antagonist at both orexin (OX1R, OX2R) receptors. Orexin/hypocretin from lateral hypothalamus is a key wake-promoting neuropeptide; antagonizing its receptors reduces arousal and promotes sleep. Unlike GABAergic hypnotics (benzos, Z-medicines), DORAs do not enhance inhibitory tone | | mechanism = Selective antagonist at both orexin (OX1R, OX2R) receptors. Orexin/hypocretin from lateral hypothalamus is a key wake-promoting neuropeptide; antagonizing its receptors reduces arousal and promotes sleep. Unlike GABAergic hypnotics (benzos, Z-medicines), DORAs do not enhance inhibitory tone, they reduce excitatory tone. Less effect on sleep architecture and possibly lower next-day impairment. | ||
| uses = Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) | | uses = Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) | ||
| starting_dose = 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate | | starting_dose = 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate | ||
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DORAs may be particularly useful when sleep maintenance (rather than just sleep onset) is the problem, since they reduce arousal across the night without enhancing GABA-mediated inhibition. | DORAs may be particularly useful when sleep maintenance (rather than just sleep onset) is the problem, since they reduce arousal across the night without enhancing GABA-mediated inhibition. | ||
| pharmacodynamics= Selective dual antagonist at OX1R (Ki ~0.5 nM) and OX2R (Ki ~0.9 nM). No significant binding at other receptors. Minimal effect on REM/NREM sleep architecture. | | pharmacodynamics= Selective dual antagonist at OX1R (Ki ~0.5 nM) and OX2R (Ki ~0.9 nM). No significant binding at other receptors. Minimal effect on REM/NREM sleep architecture. | ||
| effects = Headache, somnolence (next-day), fatigue, dizziness, nausea. Sleep paralysis, hallucinations near sleep onset reported. Complex sleep behaviors (sleep-driving, etc.) | | effects = Headache, somnolence (next-day), fatigue, dizziness, nausea. Sleep paralysis, hallucinations near sleep onset reported. Complex sleep behaviors (sleep-driving, etc.), class warning. Lower next-day impairment than benzos/Z-medicines in trials. | ||
| interactions = <pharmaInteractions/> | | interactions = <pharmaInteractions/> | ||
}} | }} | ||
[[Category:Hypnotics]] | [[Category:Hypnotics]] | ||
[[Category:Orexin Antagonists]] | [[Category:Orexin Receptor Antagonists]] | ||
[[Category: | [[Category:Sedative-hypnotics]] | ||
[[Category:GABAergics]] | [[Category:GABAergics]] | ||