Drilldown: Medicines

Bisoprolol (1) · Ketotifen (1) · Nebivolol (1)

Bystolic (1) · Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US) (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (1) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (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-00001284-QINU`"' Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both'"`UNIQ--ref-00001285-QINU`"'. (1)

'"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1)

2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1) · Ophthalmic 1 drop in each eye every 8-12 hours (1)

0.025%, 0.035% ophthalmic solutions (1) · 2.5, 5, 10, 20 mg tabs (1) · 5, 10 mg tabs (1)

1 drop per eye q8-12h (1) · 20 mg/d (1) · 40 mg/d (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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24 h (2) · 8-12 hours (1)

9–12 h (1) · Not meaningfully described for ophthalmic use'"`UNIQ--ref-00001287-QINU`"' (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1)

Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~90% (low first-pass) (1)

Category C (2) · Generally considered safe (minimal systemic exposure).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

OTC in US (1) · Rx-only in US (2)