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Medicines > routes : Oral or sublingual & legal: [[USLegal:Prescription only|Rx-only]] in US

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generic:
brand:
classes:
[[:Category:Antihypertensives|Antihypertensive]] (19) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (9) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (7) · [[:Category:Analgesics|Analgesic]] (5) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (5) · [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]] (5) · [[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (5) · [[:Category:Corticosteroids|Corticosteroid]] (5) · [[:Category:Immunosuppressants|Immunosuppressant]] (5) · [[:Category:Statins|Statin]] (5) · [[:Category:ACE_inhibitors|ACE inhibitor]] (4) · [[:Category:Antianginals|Antianginal]] (3) · [[:Category:Anticoagulants|Anticoagulant]] (3) · [[:Category:Antivirals|Antiviral]] (3) · [[:Category:Glucocorticoids|Glucocorticoid (intermediate-acting)]] (3) · [[:Category:Hormone_replacement|Hormone replacement]] (3) · [[:Category:Loop_diuretics|Loop diuretic]] (3) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID (3) · [[:Category:Thyroid_hormones|Thyroid hormone]] (3)
mechanism:
None (64) · Synthetic T4 (thyroxine); peripherally deiodinated to T3 (triiodothyronine), the active hormone. '"`UNIQ--vote-00000031-QINU`"' Narrow therapeutic index; brand-to-generic switches can shift TSH and require re-titration'"`UNIQ--ref-00000032-QINU`"'. (1) · TrkB/BDNF'"`UNIQ--ref-00000040-QINU`"' '"`UNIQ--vote-00000041-QINU`"' (1) · '"`UNIQ--vote-00000013-QINU`"' Does not stimulate insulin secretion; minimal hypoglycemia risk as monotherapy. Cleared renally unchanged; dose-adjust by eGFR'"`UNIQ--ref-00000014-QINU`"'. Rare lactic acidosis primarily in renal failure or acute illness. (1) · '"`UNIQ--vote-00000015-QINU`"' CYP2D6 metabolism produces stereoselective clearance; CYP2D6 poor metabolizers have higher plasma exposure and may need lower doses'"`UNIQ--ref-00000016-QINU`"'. (1) · '"`UNIQ--vote-00000015-QINU`"' The favorable pregnancy safety profile and the dual mechanism support its first-line role in pregnancy-associated hypertension and in hypertensive emergencies where rapid, controllable BP reduction is needed'"`UNIQ--ref-00000016-QINU`"'. (1) · '"`UNIQ--vote-00000017-QINU`"' Anticholinergic and sedating, with the standard first-generation antihistamine Beers-list concerns in elderly patients'"`UNIQ--ref-00000018-QINU`"'. (1) · '"`UNIQ--vote-00000019-QINU`"' Once-daily dosing is a clinical advantage over short-half-life NSAIDs'"`UNIQ--ref-0000001A-QINU`"'. (1) · '"`UNIQ--vote-00000032-QINU`"' Brand-to-brand and lot-to-lot variability in T3:T4 ratio is greater than with synthetic levothyroxine, which is why endocrine guidelines prefer the synthetic'"`UNIQ--ref-00000033-QINU`"'. (1) · '"`UNIQ--vote-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-QINU`"'. (1) · '"`UNIQ--vote-00000053-QINU`"' Also raises bradykinin, contributing to vasodilation and the characteristic dry cough. Renally cleared, unmetabolized; dose-adjust by eGFR'"`UNIQ--ref-00000054-QINU`"'. (1) · '"`UNIQ--vote-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-QINU`"'. (1) · '"`UNIQ--vote-00000093-QINU`"' At higher doses β2 selectivity is lost, producing β1 effects (tachycardia, tremor) and hypokalemia from intracellular potassium shift'"`UNIQ--ref-00000094-QINU`"'. (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-000000F7-QINU`"' Minimal CYP3A4 dependence (CYP2C9 minor) reduces drug-drug interactions; transport in and out of hepatocytes is largely via OATP1B1, making SLCO1B1 PGx genotype the most clinically actionable marker for statin-associated myopathy'"`UNIQ--ref-000000F8-QINU`"'. (1) · '"`UNIQ--vote-00000117-QINU`"' Compared with omeprazole, pantoprazole has a more linear pharmacokinetic profile and is metabolized predominantly via CYP2C19 with CYP3A4 contribution; less CYP2C19-driven drug interaction with clopidogrel than omeprazole'"`UNIQ--ref-00000118-QINU`"'. (1) · '"`UNIQ--vote-00000138-QINU`"' Decreases urinary calcium (used in stone prevention); raises serum uric acid, glucose, and lipids modestly; non-anion-gap hypokalemic metabolic alkalosis is the characteristic electrolyte pattern'"`UNIQ--ref-00000139-QINU`"'. (1) · '"`UNIQ--vote-00000199-QINU`"' Extends ampicillin's spectrum with better oral bioavailability. Susceptible to β-lactamases; clavulanate co-administration restores activity against many resistant organisms'"`UNIQ--ref-0000019A-QINU`"'. (1) · '"`UNIQ--vote-000001F6-QINU`"' CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable'"`UNIQ--ref-000001F7-QINU`"'. (1) · '"`UNIQ--vote-000002D7-QINU`"' Hypoglycemia is the central risk, especially in elderly and renally impaired patients (glipizide has shorter half-life than glyburide, which is one reason it is preferred in older adults). CYP2C9 substrate; weight gain typical. (1) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1) · '"`UNIQ--vote-000004A9-QINU`"' Modest HDL rise; LDL effects mixed. Renally cleared; combination with statin carries elevated myopathy risk (greater for gemfibrozil than fenofibrate, but caution still warranted)'"`UNIQ--ref-000004AA-QINU`"'. (1) · '"`UNIQ--vote-000004C8-QINU`"' Largely hepatically cleared (~80% biliary); no active metabolite. Sacubitril-valsartan (Entresto) combines an ARB with neprilysin inhibition for HFrEF and was a notable advance over the ARB-alone trial (PARADIGM-HF, 2014)'"`UNIQ--ref-000004C9-QINU`"'. (1) · '"`UNIQ--vote-0000050D-QINU`"' CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable'"`UNIQ--ref-0000050E-QINU`"'. (1) · '"`UNIQ--vote-000005D0-QINU`"' Selectivity comes from the viral-kinase-only initial phosphorylation step, which is why uninfected cells generate minimal active drug'"`UNIQ--ref-000005D1-QINU`"'. Dose-adjust by renal function; rare crystalline nephropathy with rapid IV acyclovir. (1) · '"`UNIQ--vote-000006BE-QINU`"' Drug-holiday concept (3-5 years on, 1-2 years off) emerged from FLEX and long-term safety data balancing fracture protection against atypical femoral fracture and osteonecrosis of the jaw signals'"`UNIQ--ref-000006BF-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-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-00000860-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction'"`UNIQ--ref-00000861-QINU`"'. (1) · '"`UNIQ--vote-000008BE-QINU`"' Preferred over prednisone in advanced hepatic dysfunction where hepatic 11β-HSD1 activation is impaired. Liquid formulations are the workhorse pediatric oral corticosteroid for asthma and croup'"`UNIQ--ref-000008BF-QINU`"'. (1) · '"`UNIQ--vote-00000A1D-QINU`"' Like other ACE inhibitors, it raises bradykinin (driving the dry cough and rare angioedema). Renally cleared; dose-adjust in renal impairment'"`UNIQ--ref-00000A1E-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-00000B40-QINU`"' The TRANSFORM-HF trial (2023) found no all-cause mortality difference between torsemide and furosemide in heart failure, although torsemide remains pharmacologically preferred where furosemide oral absorption is unreliable'"`UNIQ--ref-00000B41-QINU`"'. (1) · '"`UNIQ--vote-00000DFA-QINU`"' CYP3A4 substrate; QT-interval prolongation has been reported at higher doses. Like other antimuscarinics, contributes to cumulative anticholinergic burden in older adults'"`UNIQ--ref-00000DFB-QINU`"'. (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-00001014-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. The dipropionate, valerate, and augmented dipropionate ester forms determine topical potency (high to super-high)'"`UNIQ--ref-00001015-QINU`"'. (1) · '"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'. (1)
uses:
'"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (5) · '"`UNIQ--vote-00000013-QINU`"', '"`UNIQ--vote-00000014-QINU`"' (2) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (2) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (2)
starting dose:
preparations:
10 mg, 20 mg, 40 mg, 80 mg tablets (2) · 5, 10 mg tablets (2) · 5, 10, 20, 40 mg tablets (2)
fda max:
80 mg/d (5) · Indication-specific (4) · 10 mg/d (3) · 4 g/d (3) · 40 mg/d (3) · 100 mg/d (2) · 5 mg/d (2) · No fixed maximum; titrated to TSH target (2)
routes: (Click arrow to add another value)
onset:
Hours (10) · LDL lowering at 2 weeks, max by 4 weeks (3) · 30-60 minutes (2) · BP and symptomatic LUTS improvement within 1-2 weeks (2) · BP effect within 1-2 weeks (2) · Clinical improvement within 24-72 hours (2) · Motor improvement over days at therapeutic dose (2) · Postprandial glucose effect within days; HbA1c by 12 weeks (2)
duration:
24 hours (30) · 12 hours (4) · 6-8 hours (4) · 12-24 hours (3) · 4-6 hours (2) · 8-12 hours (2) · Steady-state at 4-6 weeks (2)
halflife:
bioavailability:
~100% (oral)'"`UNIQ--ref-0000001C-QINU`"' (2)
pregnancy:
None (9) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (5) · 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) · Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Avoid where possible; class concerns as for other loop diuretics.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Generally considered safe in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Generally considered safe; widely used.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · 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) · Limited human data; rarely indicated in pregnancy given the patient population.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2)
legal: (Click arrow to add another value)

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