Drilldown: Medicines

None (3) · Bisoprolol (1) · Bromazolam (1) · Nebivolol (1) · Vardenafil (1)

(none, never marketed) (1) · Belsomra (1) · Bystolic (1) · Dayvigo (1) · Levitra, Staxyn (1) · Quviviq (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · Designer benzodiazepine (1) · Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · Research material (1) · Sedative-Hypnotic (1) · the first approved (1) · Triazolobenzodiazepine (1)

None (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) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (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) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (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) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (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) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 5 mg daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

2.5, 5, 10, 20 mg tabs (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) · 5, 10 mg tabs (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)

10 mg/d (1) · 20 mg/d (3) · 40 mg/d (1) · 50 mg/d (1) · N/A (never approved) (1)

intranasal; rectal and IV reported. (1) · Oral (7) · sublingual (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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24 h (2) · 4–5 h (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · ~7-8 hours (3)

4–5 h (1) · 9–12 h (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

Not formally characterized in humans. (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~62% (1) · ~82% (1) · ~90% (low first-pass) (1)

Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Category B (1) · Category C (2) · Limited data; avoid (3)

None (1) · Rx, Schedule IV (US) (3) · Rx-only in US (3)