Drilldown: Medicines

None (1) · Bisoprolol (1) · Nebivolol (1)

Bystolic (1) · Vraylar (1) · Zebeta (1)

Atypical antipsychotic (1) · Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · D2/D3/5HT1A partial agonist (1)

None (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)

Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1)

2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1) · Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1)

1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 2.5, 5, 10, 20 mg tabs (1) · 5, 10 mg tabs (1)

20 mg/d (1) · 40 mg/d (1) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1)

Oral (3)

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) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1)

9–12 h (1) · Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1)

Adequate oral bioavailability (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~90% (low first-pass) (1)

Category C (2) · Limited data (1)

Rx (1) · Rx-only in US (2)