Drilldown: Medicines

None (4)

Belsomra (1) · Dayvigo (1) · Quviviq (1) · Zulresso (1)

Dual orexin receptor antagonist (DORA) (3) · GABA-A positive allosteric modulator (1) · Neuroactive steroid (1) · the first approved (1)

None (2) · 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. (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) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · Postpartum depression (PPD) in adults (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · Single 60-hour continuous IV infusion: 30 mcg/kg/h × 4h → 60 mcg/kg/h × 20h → 90 mcg/kg/h × 28h → 60 mcg/kg/h × 4h → 30 mcg/kg/h × 4h (1)

100 mg/20 mL vial, single-use (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

10 mg/d (1) · 20 mg/d (1) · 50 mg/d (1) · Single 60-hour course (1)

Intravenous (continuous infusion in a REMS-certified facility) (1) · Oral (3)

Antidepressant effect within hours of infusion start; sustained at 30 days (1) · ~30 min (3)

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

Other values:

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~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1) · ~9 hours (terminal) (1)

100% (IV) (1) · ~44% (1) · ~62% (1) · ~82% (1)

Limited data; avoid (3) · Medicine is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered (1)

Rx, Schedule IV (US) (3) · Rx; REMS program required (excessive sedation/loss of consciousness during infusion) (1)