Drilldown: Medicines

Bisoprolol (1) · Losartan (1) · Lovastatin (1) · Nebivolol (1) · Pravastatin (1) · Simvastatin (1)

Altoprev (ER), Mevacor (discontinued US); mostly generic (1) · Bystolic (1) · Cozaar (1) · Pravachol (1) · Zebeta (1) · Zocor (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (3) · [[:Category:Statins|Statin]] (3)

None (2) · 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-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'. (1) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1)

'"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) · '"`UNIQ--vote-00000178-QINU`"', '"`UNIQ--vote-00000179-QINU`"' (1) · '"`UNIQ--vote-000003D3-QINU`"', '"`UNIQ--vote-000003D4-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000805-QINU`"', '"`UNIQ--vote-00000806-QINU`"' (1)

10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk) (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 20 mg PO once daily with the evening meal; titrate to 40-80 mg/d (1) · 40 mg PO once daily (10-20 mg in elderly, hepatic impairment, or strong drug interactions) (1) · 5 mg daily (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)

10 mg, 20 mg, 40 mg, 80 mg tablets (1) · 10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets (1) · 2.5, 5, 10, 20 mg tabs (1) · 25 mg, 50 mg, 100 mg tablets (1) · 5, 10 mg tabs (1) · 5, 10, 20, 40, 80 mg tablets; 4 mg/mL oral suspension (1)

100 mg/d (1) · 20 mg/d (1) · 40 mg/d (1) · 40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction) (1) · 80 mg/d (1) · 80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions) (1)

Oral (6)

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:

Search

24 h (2) · 24 hours (3) · 24 hours (evening dosing aligns with overnight HMG-CoA reductase peak) (1)

2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · 9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover'"`UNIQ--ref-0000017A-QINU`"' (1) · ~2-3 hours (parent); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-000003D5-QINU`"' (1) · ~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-00000807-QINU`"' (1)

<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"' (1) · <5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"' (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~90% (low first-pass) (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · Category C (2) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (3)

Rx-only in US (2) · [[USLegal:Prescription only|Rx-only]] in US (4)