Drilldown: Medicines

None (3) · Azelastine (1) · Irbesartan (1) · Telmisartan (1) · Vardenafil (1)

Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista (1) · Avapro (1) · Belsomra (1) · Dayvigo (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:Antihypertensives|Antihypertensive]] (2) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Intranasal_antihistamines|Intranasal antihistamine]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell 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-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) · '"`UNIQ--vote-000013B1-QINU`"' Topical application minimizes systemic antihistaminic burden; the characteristic bitter taste with nasal use (drainage to oropharynx) is the main tolerability issue'"`UNIQ--ref-000013B2-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-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-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) · Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID (1)

0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) (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) · 2 sprays/nostril BID (1) · 20 mg/d (2) · 300 mg/d (1) · 50 mg/d (1) · 80 mg/d (1)

Intranasal (1) · Oral (6) · topical ophthalmic (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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12 hours (1) · 24 hours (2) · 4–5 h (1) · ~7-8 hours (3)

11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~22 hours; longer 54 hours (desmethylazelastine, active metabolite)'"`UNIQ--ref-000013B6-QINU`"' (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) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~44% (1) · ~62% (1) · ~82% (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) · Limited data; second-line to intranasal corticosteroids or PO loratadine/cetirizine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

OTC (Astepro 0.15%) and [[USLegal:Prescription only|Rx-only]] (other intranasal, ophthalmic, Dymista) in US (1) · Rx, Schedule IV (US) (3) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] in US (2)