Drilldown: Medicines

Bisoprolol (1) · Diltiazem (1) · Linagliptin (1) · Nebivolol (1) · Sitagliptin (1)

Bystolic (1) · Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) · Januvia; with metformin Janumet/Janumet XR (1) · Tradjenta; with metformin Jentadueto (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (class IV)]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Calcium_channel_blockers|Calcium channel blocker (non-dihydropyridine)]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2)

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) · '"`UNIQ--vote-0000063C-QINU`"' Avoid in HFrEF (negative inotropy). CYP3A4 substrate AND moderate inhibitor — interacts substantially with statins (especially simvastatin), tacrolimus, cyclosporine, and many other CYP3A4 substrates'"`UNIQ--ref-0000063D-QINU`"'. (1) · '"`UNIQ--vote-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1)

'"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-0000063E-QINU`"', '"`UNIQ--vote-0000063F-QINU`"', '"`UNIQ--vote-00000640-QINU`"', '"`UNIQ--vote-00000641-QINU`"' (1) · '"`UNIQ--vote-00000764-QINU`"' (1) · '"`UNIQ--vote-0000117B-QINU`"' (1)

100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1) · 5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1) · ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1)

2.5, 5, 10, 20 mg tabs (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 5 mg tablets; combination with metformin (1) · 5, 10 mg tabs (1) · IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1)

100 mg/d (1) · 20 mg/d (1) · 40 mg/d (1) · 5 mg/d (1) · ~480 mg/d (oral); IV per protocol (1)

IV (1) · multiple ER formulations) (1) · Oral (4) · Oral (IR (1)

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 (2) · IR: 4-8 hours; ER: 24 hours (1)

3-4.5 hours (IR); 5-7 hours (ER; effective duration 24 hours via formulation)'"`UNIQ--ref-00000642-QINU`"' (1) · 9–12 h (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~12 hours (effective); terminal much longer'"`UNIQ--ref-0000117C-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1)

~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1) · ~90% (low first-pass) (1)

Category C (2) · Limited data; labetalol/nifedipine generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2)

Rx-only in US (2) · [[USLegal:Prescription only|Rx-only]] in US (3)