Drilldown: Medicines

Bupropion / Naltrexone (1) · Irbesartan (1) · Linagliptin (1) · Sitagliptin (1) · Telmisartan (1)

Avapro (1) · Contrave (US), Mysimba (EU) (1) · Januvia; with metformin Janumet/Janumet XR (1) · Micardis (1) · Tradjenta; with metformin Jentadueto (1)

atypical)]] (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (2) · [[:Category:Anorectics|Anorectic (weight-loss agent)]] (1) · [[:Category:Antidepressants|Antidepressant (bupropion (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:Antihypertensives|Antihypertensive]] (2) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Fixed-dose_combinations|Fixed-dose combination]] (1) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2) · [[:Category:Opioid_antagonists|Opioid antagonist (naltrexone)]] (1)

None (2) · '"`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-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'. (1) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'. (1)

'"`UNIQ--vote-00000764-QINU`"' (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1) · '"`UNIQ--vote-0000117B-QINU`"' (1) · '"`UNIQ--vote-00001567-QINU`"' (1)

100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 40 mg PO once daily; titrate to 80 mg (1) · 5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1) · Week 1: 1 tablet (8/90 mg) PO morning; week 2: 1 tablet AM + 1 PM; week 3: 2 AM + 1 PM; week 4 onward: 2 AM + 2 PM (32 mg naltrexone / 360 mg bupropion/d) (1)

20, 40, 80 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 5 mg tablets; combination with metformin (1) · 75, 150, 300 mg tablets (1) · 8 mg naltrexone / 90 mg bupropion ER tablets (titration-pack design) (1)

100 mg/d (1) · 300 mg/d (1) · 32 mg naltrexone / 360 mg bupropion per day (1) · 5 mg/d (1) · 80 mg/d (1)

Oral (5)

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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12 hours (BID dosing required) (1) · 24 hours (4)

11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · Naltrexone ~4 hours (6β-naltrexol metabolite ~13 hours); bupropion ~21 hours'"`UNIQ--ref-00001568-QINU`"' (1) · ~12 hours (effective); terminal much longer'"`UNIQ--ref-0000117C-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1)

42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · Naltrexone ~5% (oral, extensive first-pass to 6β-naltrexol); bupropion ER ~87%'"`UNIQ--ref-00001569-QINU`"' (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · Contraindicated in pregnancy (FDA label).<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)

None (1) · [[USLegal:Prescription only|Rx-only]] in US (4)