Drilldown: Medicines

None (3) · Sodium Oxybate (1) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Quviviq (1) · Xyrem; Xywav (lower-sodium formulation with Ca/Mg/K salts) (1)

Dual orexin receptor antagonist (DORA) (3) · GABAB Agonist; Endogenous GHB receptor agonist (1) · PDE5 Inhibitor (1) · the first approved (1)

None (1) · Agonist at the metabotropic GABAB receptor and the endogenous γ-hydroxybutyrate (GHB) receptor. Produces deep sleep with increased slow-wave architecture, suppression of REM intrusion, and cataplexy reduction. (1) · 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) · Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses). (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) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000717-QINU`"', '"`UNIQ--vote-00000718-QINU`"', '"`UNIQ--vote-00000719-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 2.25 g at bedtime + 2.25 g 2.5–4 h later; titrate weekly to 6–9 g/night total (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)

0.5 g/mL oral solution (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (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 (2) · 50 mg/d (1) · 9 g/night (1)

Oral (4) · Oral (must be taken in bed; effects within minutes) (1)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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4–5 h (1) · ~3 h per dose (twice-nightly schedule required) (1) · ~7-8 hours (3)

30–60 min (1) · 4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~15% (extensive hepatic first-pass) (1) · ~25% (high first-pass) (1) · ~44% (1) · ~62% (1) · ~82% (1)

Category B (1) · Category C (1) · Limited data; avoid (3)

Rx, Schedule IV (US) (3) · Rx-only in US (1) · Schedule III; REMS-restricted (Schedule I if outside the pharmaceutical channel, same molecule as illicit GHB) (1)