Drilldown: Medicines

Azelastine (1) · Bisoprolol (1) · Nebivolol (1)

Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista (1) · Bystolic (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Intranasal_antihistamines|Intranasal antihistamine]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (1)

Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (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)

'"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-QINU`"' (1)

2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (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 (1) · 5, 10 mg tabs (1)

2 sprays/nostril BID (1) · 20 mg/d (1) · 40 mg/d (1)

Intranasal (1) · Oral (2) · 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 h (2)

9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~22 hours; longer 54 hours (desmethylazelastine, active metabolite)'"`UNIQ--ref-000013B6-QINU`"' (1)

Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~90% (low first-pass) (1)

Category C (2) · 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-only in US (2)