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Medicines > routes: oral & duration : 24 hours or 4 hours (IR); 12 hours (ER)

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generic:
brand:
classes:
[[:Category:Antihypertensives|Antihypertensive]] (11) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (6) · [[:Category:Lipid-lowering_agents|Lipid-lowering 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:Antihistamines|Antihistamine]] (3) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (3) · [[:Category:Statins|Statin]] (3) · [[:Category:Alpha-1_blockers|Alpha-1 adrenergic blocker (non-selective)]] (2) · [[:Category:Antibacterials|Antibacterial]] (2) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (2) · [[:Category:Heart_failure_medications|Heart failure medication]] (2) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2) · [[:Category:Overactive_bladder_medications|Overactive bladder medication]] (2) · [[:Category:SGLT2_inhibitors|SGLT2 inhibitor]] (2)
mechanism:
None (21) · '"`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-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-0000104D-QINU`"' Adequate hydration is at least as important as the drug in producing the expectorant effect clinically. Used in combination with dextromethorphan, decongestants, or antihistamines in many proprietary OTC cold preparations. (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-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-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)
uses:
starting dose:
preparations:
5, 10 mg tablets (2) · 5, 10, 20, 40 mg tablets (2)
routes: (Click arrow to add another value)
onset:
1-2 hours (1) · 1-3 hours (slower onset than cetirizine; symptom relief somewhat less) (1) · 30 minutes (1) · 30-60 minutes (2) · Analgesia within hours; anti-inflammatory effect over days (1) · Antidepressant effect emerges over 1-2 weeks (1) · Biochemical improvement within 2-4 weeks; full euthyroid state 6-12 weeks (1) · Bowel movement within 1 week; abdominal pain improvement over weeks (1) · BP and symptomatic LUTS improvement within 1-2 weeks (2) · BP effect 1-2 hours; max at 6 hours (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 1-2 weeks; max at 2-3 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1) · BP effect within 1-2 weeks (2) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · BP lowering within 1 hour; max at 6 hours (1) · BP lowering within 1 hour; max effect at 6 hours (1) · BPH symptom improvement at 3-6 months; prostate volume reduction over 6-12 months; hair regrowth at 6-12 months (1) · Bronchodilation within 1-2 hours; full controller effect 1-2 weeks (1) · Clinical and mycologic cure follows the full course; nail clearance over months of regrowth (1) · Clinical improvement within 24-72 hours (1) · Estrogen suppression within days; clinical effect over months (1) · Glycosuria within hours; HbA1c effect at 12 weeks; cardiovascular and renal benefits over months (1) · Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) · HbA1c effect at 12-16 weeks (slower than other classes) (1) · Hours (2) · LDL lowering at 1 week, max by 4 weeks (1) · LDL lowering at 2 weeks, max by 4 weeks (2) · LDL lowering within 2 weeks (1) · Lipid changes 4-8 weeks (1) · Mood improvement at 1-3 weeks; full effect 4-6 weeks (1) · Peak anticoagulant effect 2-4 hours (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (2) · Serum urate falls gradually over days to weeks; acute flare prevention requires colchicine cover during initiation (1) · Symptom improvement within 1 week; peak effect at 4-6 weeks (1) · Symptom improvement within 1-2 weeks (1) · Symptom improvement within weeks (1) · Triglyceride lowering at 4-8 weeks (1)
duration: (Click arrow to add another value)
halflife:
bioavailability:
pregnancy:
None (2) · '''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · '''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> (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000004CF-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-0000056E-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''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-0000005B-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000A24-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension'"`UNIQ--ref-00000C34-QINU`"' (1) · '''Pregnant individuals should not handle crushed/broken tablets''' (skin absorption risk); can cause hypospadias in male fetus. Not used in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid after 20 weeks (NSAID-class FDA 2020 advisory on fetal renal injury and oligohydramnios with second/third-trimester use).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid in pregnancy; switch to LMWH. Crosses placenta; warfarin-class concerns about fetal hemorrhage and teratogenicity make heparins the preferred class.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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; switch to insulin. Neonatal hypoglycemia reported.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Contraindicated in pregnancy (only used in postmenopausal women); D class historically.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered acceptable.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; pregnancy registries do not show increased major malformation risk.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used. Cetirizine and loratadine remain the more-studied alternatives.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used. Levocetirizine (the R-enantiomer) is an alternative with similar safety.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; widely used. Loratadine and cetirizine are the most-recommended 2nd-gen H1s in pregnancy and lactation.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (3) · Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; fluoxetine has reassuring data but olanzapine carries metabolic-syndrome and gestational diabetes signals.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; generally avoided in pregnancy for the cosmetic indication of onychomycosis.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; generally avoided particularly in combination with statin.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; generally avoided unless triglyceride pancreatitis risk is high.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; minimal systemic absorption likely renders fetal risk low.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; rarely indicated in pregnancy.<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> (3) · Limited safety data; weigh benefit individually.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Not applicable (male indication); historical Category B if used in unrelated female cases.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Observational signal for neonatal adaptation syndrome with late-pregnancy exposure (SNRI class effect).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Pharmacologic doses generally avoided in pregnancy; vitamin doses fine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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 (low-dose, dietary supplement) and [[USLegal:Prescription only|Rx-only]] (Niaspan ER) in US (1) · OTC (topical) and [[USLegal:Prescription only|Rx-only]] (oral) in US (1) · OTC in US (4) · [[USLegal:Prescription only|Rx-only]] in US (30) · [[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 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: tendinitis/tendon rupture (especially elderly, corticosteroid co-use), peripheral neuropathy, CNS effects, worsening of myasthenia gravis'"`UNIQ--ref-00000CF7-QINU`"' (1)

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