Drilldown: Medicines

Bisoprolol (1) · Estradiol (17β-estradiol) (1) · Linagliptin (1) · Nebivolol (1) · Sitagliptin (1)

Bystolic (1) · Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol) (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:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Estrogens|Estrogen]] (1) · [[:Category:Hormone_replacement_therapy|Hormone replacement therapy]] (1) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2) · [[:Category:Sex_hormones|Sex hormone]] (1)

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-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-000003B5-QINU`"', '"`UNIQ--vote-000003B6-QINU`"', '"`UNIQ--vote-000003B7-QINU`"', '"`UNIQ--vote-000003B8-QINU`"', '"`UNIQ--vote-000003B9-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-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) · Oral 1-2 mg daily; transdermal patch 0.025-0.05 mg/d twice weekly; transdermal gel 0.5-1 g/d; vaginal 10 mcg tablet twice weekly for GSM. Always combine with a progestogen in patients with an intact uterus. (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) · Oral 0.5, 1, 2 mg tablets; transdermal patches (twice-weekly and once-weekly); 0.06% gel; 1.53 mg/spray topical; vaginal ring (Estring); vaginal tablet (Vagifem/Yuvafem); vaginal cream (1)

100 mg/d (1) · 20 mg/d (1) · 40 mg/d (1) · 5 mg/d (1) · Indication-specific; lowest effective dose for shortest duration is the WHI-era standard (1)

cypionate) (1) · IM (estradiol valerate (1) · Oral (5) · transdermal (1) · vaginal (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) · Route- and formulation-dependent (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) · ~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing'"`UNIQ--ref-000003BA-QINU`"' (1)

Oral ~5% (extensive first-pass to estrone and conjugates); transdermal bypasses first-pass, giving more physiologic estradiol:estrone ratio'"`UNIQ--ref-000003BB-QINU`"' (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1) · ~90% (low first-pass) (1)

Category C (2) · Contraindicated in pregnancy (use is not appropriate during gestation; class label X). Lactation considerations vary by indication.<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)