Drilldown: Medicines

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

Bystolic (1) · Nuplazid (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1)

Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (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)

Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (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) · 34 mg PO once daily (1) · 5 mg daily (1)

10 mg, 34 mg capsules/tablets (1) · 2.5, 5, 10, 20 mg tabs (1) · 5, 10 mg tabs (1)

20 mg/d (1) · 34 mg/d (1) · 40 mg/d (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 (1)

9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~57 hours (parent), ~200 h (active metabolite) (1)

Not characterized; oral dosing once daily (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~90% (low first-pass) (1)

Category C (2) · Limited data; avoid (1)

Rx-only in US (2) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1)