Drilldown: Medicines

Nebivolol (1)

Bystolic (1)

Beta Blocker (1) · Cardioselective (β1) + vasodilator (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-0000059D-QINU`"' (1)

5 mg daily (1)

None · 10 mg, 20 mg, 40 mg, 80 mg tablets · 2.5, 5, 10, 20 mg tabs · 5 mg, 10 mg tablets · 5, 10 mg tablets · 5, 10, 20, 40 mg tablets · 0.005% ophthalmic solution (50 mcg/mL); typical 2.5 mL bottle · 0.01%, 0.03% ophthalmic solution · 0.025%, 0.035% ophthalmic solutions · 0.1% (Patanol), 0.2% (Pataday once-daily original), 0.7% (Pataday 24-hour) ophthalmic solutions; 0.6% nasal spray · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) · 0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) · 0.225%, 0.45%, 0.9%, 3%, 5% IV solutions; 0.9% nasal spray; 3% and 7% nebulizer solutions; oral tablets (1 g) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets · 0.25, 0.5 mcg oral capsules; 1 mcg/mL oral solution; 1 mcg/mL IV; 3 mcg/g topical ointment · 0.35 mg POP tablets; 5 mg tablets (Aygestin); component of COCs and combination HRT · 0.4 mg capsules · 0.4, 0.8, 1 mg OTC; 1 mg Rx; 5 mg/mL injection · 0.5 g, 1 g capsules

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40 mg/d (1)

Oral (1)

1–2 h (1)

24 h (1)

None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"'

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~12% (extensive metabolizers); ~96% (poor metabolizers) (1)

Category C (1)

Rx-only in US (1)