Drilldown: Medicines

None (3) · Irbesartan (1) · Telmisartan (1) · Valproate (valproic acid, divalproex sodium, sodium valproate) (1) · Vardenafil (1)

Avapro (1) · Belsomra (1) · Dayvigo (1) · Depakote, Depakote ER, Depakene, Depacon (IV) (1) · Levitra, Staxyn (1) · Micardis (1) · Quviviq (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (2) · [[:Category:Antiepileptics|Antiepileptic]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (2) · [[:Category:Migraine_prophylaxis|Migraine prophylaxis]] (1) · [[:Category:Mood_stabilizers|Mood stabilizer]] (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) · 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) · '"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'. (1) · '"`UNIQ--vote-00000975-QINU`"' Hyperammonemic encephalopathy (consider in any unexplained CNS depression), thrombocytopenia, and polycystic ovary syndrome are characteristic chronic-use adverse effects beyond hepatic and pancreatic risks'"`UNIQ--ref-00000976-QINU`"'. (1) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'. (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-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000977-QINU`"', '"`UNIQ--vote-00000978-QINU`"', '"`UNIQ--vote-00000979-QINU`"', '"`UNIQ--vote-0000097A-QINU`"', '"`UNIQ--vote-0000097B-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 40 mg PO once daily; titrate to 80 mg (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · Seizures: 10-15 mg/kg/d divided BID-TID, titrate to therapeutic level (50-100 mcg/mL); bipolar mania: 750 mg/d divided, titrate (1)

125, 250, 500 mg delayed-release tablets (Depakote); 250, 500 mg ER tablets (Depakote ER); 125, 250 mg sprinkle capsules; 250 mg/5 mL syrup; 500 mg IV (Depacon) (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 20, 40, 80 mg tablets (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 75, 150, 300 mg tablets (1)

10 mg/d (1) · 20 mg/d (2) · 300 mg/d (1) · 50 mg/d (1) · 60 mg/kg/d (typically up to 3000 mg/d) (1) · 80 mg/d (1)

IV (1) · Oral (7) · rectal (off-label use of injection) (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:

Search

12 hours (IR); 24 hours (ER) (1) · 24 hours (2) · 4–5 h (1) · ~7-8 hours (3)

11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 4–5 h (1) · 9-16 hours'"`UNIQ--ref-0000097C-QINU`"' (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · ~100% (oral); highly (~90%) protein-bound, with non-linear binding above therapeutic levels (free fraction matters clinically in hypoalbuminemia)'"`UNIQ--ref-0000097D-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~62% (1) · ~82% (1)

'''Contraindicated for migraine prophylaxis in pregnancy; high teratogenic risk''' (neural tube defects, craniofacial anomalies, cardiac defects, cognitive/IQ impairment); avoid in women of childbearing potential without reliable contraception when alternatives exist'"`UNIQ--ref-0000097E-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · Category B (1) · Limited data; avoid (3)

Rx, Schedule IV (US) (3) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US (2) · [[USLegal:Prescription only|Rx-only]] in US. Carries '''Boxed Warnings''' for hepatotoxicity (especially children <2 with metabolic disorders), teratogenicity, and pancreatitis'"`UNIQ--ref-0000097F-QINU`"' (1)