Lemborexant: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| brand = Dayvigo | |||
| brand | | classes = Dual orexin receptor antagonist (DORA) | ||
| 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. | |||
| classes | | uses = Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) | ||
| mechanism | | starting_dose = 5 mg PO at bedtime; may increase to 10 mg if inadequate | ||
| uses | | preparations = 5 mg, 10 mg tablets | ||
| starting_dose | | fda_max = 10 mg/d | ||
| preparations | | routes = Oral | ||
| fda_max | | onset = ~30 min | ||
| routes | | duration = ~7-8 hours | ||
| onset | | halflife = ~17-19 hours (longer than daridorexant) | ||
| duration | | bioavailability = ~44% | ||
| halflife | | pregnancy = Limited data; avoid | ||
| bioavailability | | legal = Rx, Schedule IV (US) | ||
| pregnancy | | 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. | ||
| legal | |||
| intro | 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. | ||
| pharmacodynamics= Competitive antagonism at OX1R (Ki ~6 nM) and OX2R (Ki ~3 nM). No clinically significant activity at other receptors. | |||
| pharmacodynamics | | effects = Somnolence (next-day), headache, nightmares, abnormal dreams, sleep paralysis, hallucinations near sleep onset. Complex sleep behaviors class warning. | ||
| interactions = <pharmaInteractions/> | |||
| effects | |||
| interactions | |||
}} | }} | ||
[[Category:Anxiolytics & Sedative-Hypnotics]] | [[Category:Anxiolytics & Sedative-Hypnotics]] | ||
[[Category:Orexin Receptor Antagonists]] | [[Category:Orexin Receptor Antagonists]] | ||
[[Category:Sedative-Hypnotics]] | [[Category:Sedative-Hypnotics]] | ||
[[Category:Hypnotics]] | |||
[[Category:Orexin Antagonists]] | |||