Drilldown: Medicines

None (1)

Belsomra (1)

Dual orexin receptor antagonist (DORA) (1) · the first approved (1)

Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1)

Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1)

5 mg, 10 mg, 15 mg, 20 mg tablets (1)

20 mg/d (1)

Oral (1)

~30 min (1)

None · 24 hours · 4-6 hours · 12 hours · 6-8 hours · Daily dosing · 8-12 hours · 12-24 hours · Hours · Hours per application · 24 hours (HS dosing) · 24 hours (once-daily dosing) · 24 h · N/A · N/A (replacement) · Variable · ~7-8 hours · 3-5 hours · 4-6 hours (IR); 24 hours (ER) · 6-12 hours

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None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"'

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~82% (1)

Limited data; avoid (1)

Rx, Schedule IV (US) (1)