Lemborexant: Difference between revisions
From Pharmacopedia
More actions
| [unchecked revision] | [pending revision] |
MDElliottMD (talk | contribs) Auto-created stub |
MDElliottMD (talk | contribs) Category taxonomy ship: retag Sedative-Hypnotics -> Sedative-hypnotics |
||
| (9 intermediate revisions by 3 users not shown) | |||
| Line 1: | Line 1: | ||
{{MedTemplate | {{MedTemplate | ||
| | | brand = Dayvigo | ||
| | | 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. | ||
| | | uses = Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) | ||
| starting_dose = 5 mg PO at bedtime; may increase to 10 mg if inadequate | |||
| preparations = 5 mg, 10 mg tablets | |||
| fda_max = 10 mg/d | |||
| routes = Oral | |||
| onset = ~30 min | |||
| duration = ~7-8 hours | |||
| halflife = ~17-19 hours (longer than daridorexant) | |||
| bioavailability = ~44% | |||
| pregnancy = Limited data; avoid | |||
| legal = Rx, Schedule IV (US) | |||
| 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. | |||
| pharmacodynamics= Competitive antagonism at OX1R (Ki ~6 nM) and OX2R (Ki ~3 nM). No clinically significant activity at other receptors. | |||
| effects = Somnolence (next-day), headache, nightmares, abnormal dreams, sleep paralysis, hallucinations near sleep onset. Complex sleep behaviors class warning. | |||
| interactions = <pharmaInteractions/> | |||
}} | }} | ||
[[Category:Orexin Receptor Antagonists]] | |||
[[Category:Sedative-hypnotics]] | |||
[[Category:Hypnotics]] | |||