Suvorexant: Difference between revisions
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| brand = Belsomra | | brand = Belsomra | ||
| classes = Dual orexin receptor antagonist (DORA) | | classes = Dual orexin receptor antagonist (DORA), the first approved | ||
| mechanism = Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. | | mechanism = Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. | ||
| uses = Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. | | uses = Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. | ||
| Line 14: | Line 14: | ||
| pregnancy = Limited data; avoid | | pregnancy = Limited data; avoid | ||
| legal = Rx, Schedule IV (US) | | legal = Rx, Schedule IV (US) | ||
| intro = '''Suvorexant''' (brand name Belsomra) is the first FDA-approved dual orexin receptor antagonist (DORA), approved August 2014 for insomnia. Suvorexant established the DORA class as a treatment paradigm | | intro = '''Suvorexant''' (brand name Belsomra) is the first FDA-approved dual orexin receptor antagonist (DORA), approved August 2014 for insomnia. Suvorexant established the DORA class as a treatment paradigm, reducing arousal via orexin blockade rather than enhancing GABA-mediated inhibition. Subsequent DORAs (lemborexant 2019, daridorexant 2022) have been positioned as iterative improvements with different pharmacokinetics. | ||
Suvorexant has been studied in mild-moderate Alzheimer disease with positive results; trials have suggested potential for reducing sleep-disordered breathing exacerbations and possibly delaying cognitive decline (though the cognitive claim remains controversial). | Suvorexant has been studied in mild-moderate Alzheimer disease with positive results; trials have suggested potential for reducing sleep-disordered breathing exacerbations and possibly delaying cognitive decline (though the cognitive claim remains controversial). | ||
Revision as of 03:16, 19 May 2026
Dual orexin receptor antagonist (DORA), the first approved
Suvorexant
Belsomra
Suvorexant (brand name Belsomra) is the first FDA-approved dual orexin receptor antagonist (DORA), approved August 2014 for insomnia. Suvorexant established the DORA class as a treatment paradigm, reducing arousal via orexin blockade rather than enhancing GABA-mediated inhibition. Subsequent DORAs (lemborexant 2019, daridorexant 2022) have been positioned as iterative improvements with different pharmacokinetics.
Suvorexant has been studied in mild-moderate Alzheimer disease with positive results; trials have suggested potential for reducing sleep-disordered breathing exacerbations and possibly delaying cognitive decline (though the cognitive claim remains controversial).
Competitive antagonist at OX1R (Ki ~0.55 nM) and OX2R (Ki ~0.35 nM). Receptor dissociation slower than lemborexant or daridorexant.
Experience
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Problems
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+ Add a problemTitration strategies
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Effects
Next-day somnolence (more common than with daridorexant due to longer half-life), headache, abnormal dreams, dry mouth, fatigue. Sleep paralysis and hallucinations near sleep onset. Complex sleep behaviors class warning.
Pharmacodynamics
Interactions
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Relevant Literature
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Pharmacy
Starting dose
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned)
Preparations
5 mg, 10 mg, 15 mg, 20 mg tablets
US FDA Max
20 mg/d
Common uses
Classification(s)
Classes
Dual orexin receptor antagonist (DORA), the first approved
Pharmacology
Routes
Oral
Onset
~30 min
Duration
~7-8 hours
Half-life
~12 hours
Bioavailability
~82%
Pregnancy
Limited data; avoid
Legal status
Rx, Schedule IV (US)
Purported mechanism
Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant.