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)

2.5, 5, 10, 20 mg tabs (1)

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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None · 100% (IV) · ~100% from subcutaneous depot · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' · 70–90% (oral) · ~100% (oral)'"`UNIQ--ref-0000001C-QINU`"' · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' · ~95% · '''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' · 10-20% (oral; reduced by food, calcium, antacids, PPIs, tea/coffee; enhanced by ascorbate) · 100% (IV); essentially complete (oral) · 100% (IV); rapidly neutralized by gastric acid (oral) · 16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"' · 25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' · 30-40% (oral; increases with repeated dosing as gastric pH rises)'"`UNIQ--ref-000000DF-QINU`"' · 40-45% (oral; not significantly affected by food)'"`UNIQ--ref-0000025C-QINU`"' · 40-80% (oral); reduced by food, calcium, iron, PPIs, fiber; take fasting with water'"`UNIQ--ref-00000037-QINU`"' · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' · 50-60% (oral; decreased with food, but food given anyway for GI tolerance)'"`UNIQ--ref-00000019-QINU`"' · 60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"'

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Category C (1)

None · [[USLegal:Prescription only|Rx-only]] in US · OTC in US · Rx · Rx-only in US · Rx, Schedule IV (US) · Schedule II · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' · Rx-only · [[USLegal:DEA Schedule I|Schedule I]] (United States) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000022-QINU`"' · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000025-QINU`"' · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' · '''[[USLegal:Behind-the-counter|Behind-the-counter]] in US''' under the Combat Methamphetamine Epidemic Act 2005: purchase restricted to ≤3.6 g/day and ≤9 g/30 days, with photo ID, logbook signature, and quantity logging required. Several states schedule higher than federal · '''[[USLegal:Schedule V|Schedule V controlled substance]] in US (federally)''', distinct from gabapentin which remains federally unscheduled'"`UNIQ--ref-00000028-QINU`"' · 5-MeO-DMT is Schedule I in US (since 2011); the toad itself is protected in several southwestern states · Currently legal in most jurisdictions with thujone limits · Investigational · Leaves legal in Bolivia, Peru, Colombia; cocaine internationally controlled · OTC (1% shampoo) and [[USLegal:Prescription only|Rx-only]] (higher strengths, oral) in US. Oral form carries a '''Boxed Warning''' for hepatotoxicity and is restricted by FDA to refractory fungal infections where no alternatives are available

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