Drilldown: Medicines

None (3) · Azelastine (1) · Lovastatin (1) · Pravastatin (1) · Simvastatin (1) · Vardenafil (1)

Altoprev (ER), Mevacor (discontinued US); mostly generic (1) · Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista (1) · Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Pravachol (1) · Quviviq (1) · Zocor (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Intranasal_antihistamines|Intranasal antihistamine]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (3) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (1) · [[:Category:Statins|Statin]] (3)

None (3) · 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-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-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-00000178-QINU`"', '"`UNIQ--vote-00000179-QINU`"' (1) · '"`UNIQ--vote-000003D3-QINU`"', '"`UNIQ--vote-000003D4-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000805-QINU`"', '"`UNIQ--vote-00000806-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) · 10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk) (1) · 20 mg PO once daily with the evening meal; titrate to 40-80 mg/d (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 40 mg PO once daily (10-20 mg in elderly, hepatic impairment, or strong drug interactions) (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) · 10 mg, 20 mg, 40 mg, 80 mg tablets (1) · 10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets (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, 20, 40, 80 mg tablets; 4 mg/mL oral suspension (1)

10 mg/d (1) · 2 sprays/nostril BID (1) · 20 mg/d (2) · 40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction) (1) · 50 mg/d (1) · 80 mg/d (1) · 80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions) (1)

Intranasal (1) · Oral (7) · 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:

Search

12 hours (1) · 24 hours (2) · 24 hours (evening dosing aligns with overnight HMG-CoA reductase peak) (1) · 4–5 h (1) · ~7-8 hours (3)

4–5 h (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover'"`UNIQ--ref-0000017A-QINU`"' (1) · ~2-3 hours (parent); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-000003D5-QINU`"' (1) · ~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-00000807-QINU`"' (1) · ~22 hours; longer 54 hours (desmethylazelastine, active metabolite)'"`UNIQ--ref-000013B6-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"' (1) · <5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"' (1) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"' (1) · ~44% (1) · ~62% (1) · ~82% (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) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (3)

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 (3)