Drilldown: Medicines

Bisoprolol (1) · Methimazole (thiamazole) (1) · Nebivolol (1)

Bystolic (1) · Tapazole; outside US Mercazole (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · [[:Category:Antithyroid_agents|Antithyroid agent]] (1) · [[:Category:Thionamides|Thionamide]] (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-00000ECD-QINU`"' Agranulocytosis is the most-feared adverse effect (~0.3%, usually first 90 days of treatment; warn patients to seek urgent CBC for fever or severe sore throat). Hepatotoxicity is class-recognized but more often associated with PTU'"`UNIQ--ref-00000ECE-QINU`"'. (1)

'"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000ECF-QINU`"', '"`UNIQ--vote-00000ED0-QINU`"', '"`UNIQ--vote-00000ED1-QINU`"', '"`UNIQ--vote-00000ED2-QINU`"' (1)

10-40 mg PO daily depending on hyperthyroidism severity; titrate by clinical and biochemical response (target TSH/free T4) (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1)

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

20 mg/d (1) · 40 mg/d (1) · 60 mg/d typical (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) · 24 hours (1)

9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~4-6 hours (plasma); intrathyroidal accumulation gives a much longer functional duration'"`UNIQ--ref-00000ED3-QINU`"' (1)

~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~90% (low first-pass) (1) · ~93% (oral)'"`UNIQ--ref-00000ED4-QINU`"' (1)

None (1) · Category C (2)

Rx-only in US (2) · [[USLegal:Prescription only|Rx-only]] in US (1)