Daridorexant: Difference between revisions
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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 | ||
| Line 18: | Line 18: | ||
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]] | ||
Latest revision as of 00:36, 22 May 2026
Dual orexin receptor antagonist (DORA)
Daridorexant
Quviviq
Daridorexant (brand name Quviviq) is a dual orexin receptor antagonist (DORA) FDA-approved in January 2022 for insomnia. Among the three approved DORAs, daridorexant has the shortest half-life (~8 hours vs lemborexant ~17-19 h and suvorexant ~12 h), which may reduce next-day residual sedation. Mechanism: orexin/hypocretin neurons in the lateral hypothalamus drive arousal; blocking both OX1R and OX2R reduces wake-promoting signaling. The result is sleep that resembles normal physiologic sleep more closely than GABAergic hypnotics (less REM suppression, fewer abnormal sleep behaviors).
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.
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.
Experience
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Problems
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+ Add a problemTitration strategies
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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.
Pharmacodynamics
Interactions
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Summary
Classes
Dual orexin receptor antagonist (DORA)
Common uses
Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022)
Pharmacy
Starting dose
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate
Preparations
25 mg, 50 mg tablets
US FDA Max
50 mg/d
Pharmacology
Routes
Oral
Onset
~30 min
Duration
~7-8 hours
Half-life
~8 hours (shorter than suvorexant and lemborexant)
Bioavailability
~62%
Pregnancy
Limited data; avoid
Legal status
Rx, Schedule IV (US)
Purported 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.