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Drilldown: Medicines

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Medicines > duration : 12 hours or 24 hours or Variable

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generic:
brand:
classes:
[[:Category:Antihypertensives|Antihypertensive]] (11) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (7) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (6) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (5) · [[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (4) · [[:Category:ACE_inhibitors|ACE inhibitor]] (3) · [[:Category:Antibacterials|Antibacterial]] (3) · [[:Category:Antihistamines|Antihistamine]] (3) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (3) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (3) · [[:Category:Statins|Statin]] (3)
mechanism:
None (30) · '"`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-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-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-00000391-QINU`"' Minimal CYP metabolism; mostly renally cleared unchanged. Cetirizine is the active racemate; levocetirizine is the active R-enantiomer marketed separately'"`UNIQ--ref-00000392-QINU`"'. (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-0000061E-QINU`"' Less reliably anticholinergic than first-generation H1s; minimal antiemetic effect. Desloratadine (Clarinex) is the active enantiomer-of-metabolite version marketed as a Rx alternative. (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-00000950-QINU`"' Mostly renally cleared unchanged; dose-reduce in renal impairment. Like cetirizine, retains slightly more sedation than fexofenadine in some users'"`UNIQ--ref-00000951-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-00000D7A-QINU`"' Substantial QT-interval prolongation — the most QT-prolonging fluoroquinolone — limits use in patients on other QT-prolonging agents or with electrolyte abnormalities'"`UNIQ--ref-00000D7B-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-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) · '"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-QINU`"'. (1) · '"`UNIQ--vote-00001197-QINU`"' Extracellular cGMP separately activates submucosal sensory afferents in a way that reduces visceral pain perception, distinguishing linaclotide from purely osmotic laxatives in IBS-C. Diarrhea is the dose-limiting effect'"`UNIQ--ref-00001198-QINU`"'. (1) · '"`UNIQ--vote-000011F4-QINU`"' Like all NSAIDs, raises CV thrombotic risk modestly (FDA 2014/2015 advisory) and produces GI, renal, hypertensive, and platelet-inhibitory effects characteristic of the class'"`UNIQ--ref-000011F5-QINU`"'. (1) · '"`UNIQ--vote-00001302-QINU`"' Renally cleared; accumulation in advanced CKD can produce neuromuscular and cardiac depression. Hypomagnesemia frequently co-exists with hypokalemia and is often the reason refractory potassium loss does not correct until magnesium is repleted. (1) · '"`UNIQ--vote-000013B1-QINU`"' Topical application minimizes systemic antihistaminic burden; the characteristic bitter taste with nasal use (drainage to oropharynx) is the main tolerability issue'"`UNIQ--ref-000013B2-QINU`"'. (1) · '"`UNIQ--vote-000014BC-QINU`"' Topical ophthalmic and otic formulations remain widely used in ENT and ophthalmology. Subject to all fluoroquinolone-class restrictions (tendinitis/rupture, peripheral neuropathy, QT prolongation)'"`UNIQ--ref-000014BD-QINU`"'. (1) · '"`UNIQ--vote-00001549-QINU`"' Metabolic effects (weight gain, dyslipidemia, glucose dysregulation) dominate the long-term tolerability profile; routine metabolic monitoring is standard'"`UNIQ--ref-0000154A-QINU`"'. (1) · '"`UNIQ--vote-00001580-QINU`"' First FDA-approved treatment for PBA. The 10 mg quinidine daily dose is far below antiarrhythmic levels but sufficient to nearly fully inhibit CYP2D6, the basis of the combination's pharmacokinetic rationale'"`UNIQ--ref-00001581-QINU`"'. (1)
uses:
starting dose:
preparations:
5, 10 mg tablets (2) · 5, 10, 20, 40 mg tablets (2)
fda max:
80 mg/d (4) · 10 mg/d (3) · 10 mg/d (adults) (3) · 100 mg/d (2) · 400 mg/d (2) · 5 mg/d (2)
onset:
Hours (4) · 30-60 minutes (2) · BP and symptomatic LUTS improvement within 1-2 weeks (2) · BP effect within 1-2 weeks (2) · LDL lowering at 2 weeks, max by 4 weeks (2) · Postprandial glucose effect within days; HbA1c by 12 weeks (2)
duration: (Click arrow to add another value)
halflife:
bioavailability:
pregnancy:
None (4) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (4) · 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> (3) · '''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · 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) · Limited data; weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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> (2)
legal:
OTC (Astepro 0.15%) and [[USLegal:Prescription only|Rx-only]] (other intranasal, ophthalmic, Dymista) in US (1) · OTC (low-dose, dietary supplement) and [[USLegal:Prescription only|Rx-only]] (Niaspan ER) in US (1) · OTC (Nasonex 24HR) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · OTC (oral salts) and [[USLegal:Prescription only|Rx-only]] (IV) in US (1) · OTC (oral supplements) and [[USLegal:Prescription only|Rx-only]] (IV) in US (1) · OTC (topical) and [[USLegal:Prescription only|Rx-only]] (oral) in US (1) · OTC in US (3) · [[USLegal:Prescription only|Rx-only]] in US (36) · [[USLegal:Prescription only|Rx-only]] in US (the veterinary preparations are not for human use) (1) · [[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated in structural heart disease''' — CAST trial (1989) showed increased mortality from class IC agents in patients with prior MI; modern use is limited to structurally normal hearts'"`UNIQ--ref-00001141-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. '''FDA Boxed Warning (2020):''' neuropsychiatric events including agitation, depression, sleep disturbance, and suicidal thoughts; benefit-risk should be reassessed regularly'"`UNIQ--ref-00000160-QINU`"'. (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' contraindicating use in children <2 years (lethal dehydration in animal studies)'"`UNIQ--ref-0000119E-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for bleeding risk and against aspirin maintenance doses above 100 mg/d (reduces ticagrelor efficacy, per PLATO subgroup analysis)'"`UNIQ--ref-00000C94-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' for heart failure (do not initiate in NYHA III/IV; can precipitate or worsen HF in any patient)'"`UNIQ--ref-00000826-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the '''antidepressant Boxed Warning''' for suicidality in children/adolescents/young adults and the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly dementia patients'"`UNIQ--ref-0000154F-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-0000001C-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the NSAID-class '''Boxed Warning''' for cardiovascular thrombotic events and serious GI bleeding'"`UNIQ--ref-000011FB-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-00000D84-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin/levofloxacin'"`UNIQ--ref-000014C5-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the same fluoroquinolone-class '''Boxed Warnings''' as ciprofloxacin: tendinitis/tendon rupture (especially elderly, corticosteroid co-use), peripheral neuropathy, CNS effects, worsening of myasthenia gravis'"`UNIQ--ref-00000CF7-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Caution with QT-prolonging medicines (quinidine itself is class IA antiarrhythmic, and the dose here, though sub-antiarrhythmic, still contributes to QT)'"`UNIQ--ref-00001585-QINU`"' (1)

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