Drilldown: Medicines

None (3) · Coffee (1) · Dexmethylphenidate (1) · Sildenafil (1) · Vardenafil (1)

''Coffea arabica'', ''Coffea canephora'' (robusta) (1) · Belsomra (1) · Dayvigo (1) · Focalin, Focalin XR (1) · Levitra, Staxyn (1) · Quviviq (1) · Viagra, Revatio (1)

Caffeine plant (1) · CNS stimulant (1) · Dual orexin receptor antagonist (DORA) (3) · Excitantia (1) · NDRI (1) · PDE5 Inhibitor (2) · Plant Medicine (1) · Psychostimulant (1) · the first approved (1) · Xanthine (1)

None (1) · Caffeine is a non-selective adenosine A1/A2A receptor antagonist; also weak PDE inhibition. Beans contain theobromine (3,7-DMX) and theophylline (1,3-DMX) in smaller amounts. (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) · Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate (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) · Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation. (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-000000CF-QINU`"', '"`UNIQ--vote-000000D0-QINU`"', '"`UNIQ--vote-000000D1-QINU`"' (1) · '"`UNIQ--vote-00000150-QINU`"', '"`UNIQ--vote-00000151-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1)

None (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (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) · 50 mg ~1 h before sexual activity (ED); 20 mg TID (PAH) (1) · One cup (~80–145 mg caffeine for brewed; 60–100 mg for instant) (1)

None (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg tablets (1) · 25, 50, 100 mg tabs (Viagra); 20 mg tabs and 10 mg/mL oral suspension (Revatio) (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · Roasted beans, ground; brewed (drip, French press, espresso, cold brew, percolated) (1)

None (2) · 10 mg/d (1) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 20 mg/d (2) · 50 mg/d (1)

IV (Revatio) (1) · Oral (7)

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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3–5 h (subjective) (1) · 4–5 h (1) · IR 4–6 h; XR 8–12 h (1) · ~4 h (1) · ~7-8 hours (3)

2.2 h (IR parent); ~3 h (XR parent) (1) · 4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~4 h (1) · ~5 h (caffeine) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~15% (extensive hepatic first-pass) (1) · ~22–25% (1) · ~40% (1) · ~44% (1) · ~62% (1) · ~82% (1) · ~99% (caffeine) (1)

Category B (2) · Category C (1) · Limit to <200 mg/d (~2 cups brewed) (1) · Limited data; avoid (3)

Rx, Schedule IV (US) (3) · Rx-only in US (2) · Schedule II (1) · Unrestricted (food) (1)