Drilldown: Medicines

None (4) · Dexmethylphenidate (1) · Sildenafil (1) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Focalin, Focalin XR (1) · Levitra, Staxyn (1) · Quviviq (1) · Spravato (1) · Viagra, Revatio (1)

CNS stimulant (1) · dissociative (1) · Dual orexin receptor antagonist (DORA) (3) · NDRI (1) · NMDA receptor antagonist (uncompetitive) (1) · PDE5 Inhibitor (2) · Psychostimulant (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) · 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) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (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) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (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) · 28 mg/device (each dose uses 2 devices) (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

None (1) · 10 mg/d (1) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 20 mg/d (2) · 50 mg/d (1) · 84 mg per session (1)

Intranasal (under direct medical supervision) (1) · IV (Revatio) (1) · Oral (6)

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) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (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) · ~7-12 hours (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~15% (extensive hepatic first-pass) (1) · ~22–25% (1) · ~40% (1) · ~44% (1) · ~48% intranasal (1) · ~62% (1) · ~82% (1)

Avoid; may cause fetal harm (1) · Category B (2) · Category C (1) · Limited data; avoid (3)

Rx, Schedule III (US). REMS program required. (1) · Rx, Schedule IV (US) (3) · Rx-only in US (2) · Schedule II (1)