Drilldown: Medicines

None (2) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1)

Dual orexin receptor antagonist (DORA) (2) · PDE5 Inhibitor (1) · the first approved (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) · '"`UNIQ--vote-00000669-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1)

2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

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Oral (3)

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

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4–5 h (1) · ~7-8 hours (2)

4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1)

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

Category B (1) · Limited data; avoid (2)

Rx, Schedule IV (US) (2) · Rx-only in US (1)