Lemborexant: Difference between revisions
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| intro = '''Lemborexant''' (brand name Dayvigo) is a dual orexin receptor antagonist (DORA) FDA-approved in December 2019 for insomnia in adults. Among DORAs, lemborexant has faster receptor association/dissociation kinetics than suvorexant | | intro = '''Lemborexant''' (brand name Dayvigo) is a dual orexin receptor antagonist (DORA) FDA-approved in December 2019 for insomnia in adults. Among DORAs, lemborexant has faster receptor association/dissociation kinetics than suvorexant, which is hypothesized to facilitate sleep onset while still maintaining adequate duration of antagonism for sleep maintenance. The 17-19 hour half-life can produce some next-day residual sedation in sensitive individuals. | ||
DORAs broadly produce sleep that more closely resembles physiologic sleep architecture than GABAergic hypnotics, with reduced REM suppression. Side effect profile favorable compared to benzodiazepines, but sleep paralysis, sleep-related hallucinations, and complex sleep behaviors have been reported. | DORAs broadly produce sleep that more closely resembles physiologic sleep architecture than GABAergic hypnotics, with reduced REM suppression. Side effect profile favorable compared to benzodiazepines, but sleep paralysis, sleep-related hallucinations, and complex sleep behaviors have been reported. | ||
Revision as of 03:16, 19 May 2026
Dual orexin receptor antagonist (DORA)
Lemborexant
Dayvigo
Lemborexant (brand name Dayvigo) is a dual orexin receptor antagonist (DORA) FDA-approved in December 2019 for insomnia in adults. Among DORAs, lemborexant has faster receptor association/dissociation kinetics than suvorexant, which is hypothesized to facilitate sleep onset while still maintaining adequate duration of antagonism for sleep maintenance. The 17-19 hour half-life can produce some next-day residual sedation in sensitive individuals.
DORAs broadly produce sleep that more closely resembles physiologic sleep architecture than GABAergic hypnotics, with reduced REM suppression. Side effect profile favorable compared to benzodiazepines, but sleep paralysis, sleep-related hallucinations, and complex sleep behaviors have been reported.
Competitive antagonism at OX1R (Ki ~6 nM) and OX2R (Ki ~3 nM). No clinically significant activity at other receptors.
Experience
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Problems
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Effects
Somnolence (next-day), headache, nightmares, abnormal dreams, sleep paralysis, hallucinations near sleep onset. Complex sleep behaviors class warning.
Pharmacodynamics
Interactions
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Summary
Classes
Dual orexin receptor antagonist (DORA)
Pharmacy
Starting dose
5 mg PO at bedtime; may increase to 10 mg if inadequate
Preparations
5 mg, 10 mg tablets
US FDA Max
10 mg/d
Pharmacology
Routes
Oral
Onset
~30 min
Duration
~7-8 hours
Half-life
~17-19 hours (longer than daridorexant)
Bioavailability
~44%
Pregnancy
Limited data; avoid
Legal status
Rx, Schedule IV (US)
Purported mechanism
Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance.