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Medicines > duration : 6-8 hours or 8-12 hours or Daily dosing

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classes:
[[:Category:Antibacterials|Antibacterial]] (3) · [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]] (3) · Atypical antipsychotic (2)
mechanism:
None (15) · Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) · Selective NET inhibitor (no significant DAT activity, distinguishes from amphetamine/methylphenidate). Also: 5HT1A receptor partial agonism, 5HT2B and 5HT7 receptor antagonism. The serotonergic actions may underlie better tolerability and possibly different efficacy spectrum than atomoxetine. (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-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-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-00001284-QINU`"' Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both'"`UNIQ--ref-00001285-QINU`"'. (1)
uses:
ADHD in children (6+), adolescents, and adults (FDA-approved 2021 for pediatric, 2022 for adult) (1) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · Investigational for major depressive disorder; trials underway (phase 3 mixed results) (1) · Major depressive disorder in adults (FDA-approved 2011) (1) · Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) · Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1) · Schizophrenia (FDA-approved Dec 2019). Bipolar depression as monotherapy or adjunct to lithium/valproate (FDA-approved Dec 2021). (1) · '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"' (1) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (1) · '"`UNIQ--vote-00000050-QINU`"' (1) · '"`UNIQ--vote-000004ED-QINU`"', '"`UNIQ--vote-000004EE-QINU`"', '"`UNIQ--vote-000004EF-QINU`"', '"`UNIQ--vote-000004F0-QINU`"', '"`UNIQ--vote-000004F1-QINU`"' (1) · '"`UNIQ--vote-00000932-QINU`"', '"`UNIQ--vote-00000933-QINU`"', '"`UNIQ--vote-00000934-QINU`"', '"`UNIQ--vote-00000935-QINU`"', '"`UNIQ--vote-00000936-QINU`"', '"`UNIQ--vote-00000937-QINU`"' (1) · '"`UNIQ--vote-00000B42-QINU`"', '"`UNIQ--vote-00000B43-QINU`"', '"`UNIQ--vote-00000B44-QINU`"', '"`UNIQ--vote-00000B45-QINU`"' (1) · '"`UNIQ--vote-00000BE3-QINU`"', '"`UNIQ--vote-00000BE4-QINU`"', '"`UNIQ--vote-00000BE5-QINU`"', '"`UNIQ--vote-00000BE6-QINU`"', '"`UNIQ--vote-00000BE7-QINU`"', '"`UNIQ--vote-00000BE8-QINU`"', '"`UNIQ--vote-00000BE9-QINU`"', '"`UNIQ--vote-00000BEA-QINU`"' (1) · '"`UNIQ--vote-00000D38-QINU`"', '"`UNIQ--vote-00000D39-QINU`"', '"`UNIQ--vote-00000D3A-QINU`"', '"`UNIQ--vote-00000D3B-QINU`"', '"`UNIQ--vote-00000D3C-QINU`"', '"`UNIQ--vote-00000D3D-QINU`"' (1) · '"`UNIQ--vote-00000E71-QINU`"', '"`UNIQ--vote-00000E72-QINU`"', '"`UNIQ--vote-00000E73-QINU`"', '"`UNIQ--vote-00000E74-QINU`"', '"`UNIQ--vote-00000E75-QINU`"' (1) · '"`UNIQ--vote-00000FB3-QINU`"', '''adjunctive only''' (does not treat the underlying infection) (1) · '"`UNIQ--vote-00000FCF-QINU`"', '"`UNIQ--vote-00000FD0-QINU`"', '"`UNIQ--vote-00000FD1-QINU`"' (1) · '"`UNIQ--vote-00000FF3-QINU`"', '"`UNIQ--vote-00000FF4-QINU`"', '"`UNIQ--vote-00000FF5-QINU`"', '"`UNIQ--vote-00000FF6-QINU`"', '"`UNIQ--vote-00000FF7-QINU`"', '"`UNIQ--vote-00000FF8-QINU`"' (1) · '"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1) · '"`UNIQ--vote-0000143C-QINU`"', '"`UNIQ--vote-0000143D-QINU`"', '"`UNIQ--vote-0000143E-QINU`"', '"`UNIQ--vote-0000143F-QINU`"', '"`UNIQ--vote-00001440-QINU`"', '"`UNIQ--vote-00001441-QINU`"' (1)
starting dose:
10 mg PO once daily × 7 days, then 20 mg × 7 days, then 40 mg as target dose (take with food) (1) · 10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (1) · 10-20 mg PO/IV once daily; titrate by clinical response. 1:1 IV to PO conversion (unlike furosemide's 1:2) (1) · 100-200 mg PO TID after meals × no more than 2 days when used with concurrent antibiotic (1) · 250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections (1) · 250-500 mg PO every 6-8 hours (1) · 250-500 mg PO QID; 7.5-12.5 mg/kg IV q6h; topical and ophthalmic per formulation (1) · 34 mg PO once daily (1) · 4 g PO daily (as 4 x 1 g capsules once daily, or 2 capsules BID) (1) · 4 mg PO initially, then 2 mg after each loose stool, '''not to exceed 16 mg/d''' (8 mg OTC); chronic-use lower (1) · 42 mg PO once daily with food (no titration) (1) · 500 mg PO every 6 hours, or 250 mg every 6 hours for mild infections (1) · 500 mg PO TID × 7-10 days (most indications); 2 g single dose for trichomoniasis; 500 mg IV q8h for severe anaerobic infection; rectal 1 g BID (1) · 500-750 mg PO BID; 400 mg IV q8-12h (1) · Allergy: 4 mg PO TID. Serotonin syndrome: 12 mg loading dose PO or by nasogastric tube, then 2 mg every 2 hours until clinical improvement. Appetite stimulation: 2-4 mg PO TID-QID (1) · Anxiety: 0.5-1 mg PO BID-TID. Insomnia: 1-2 mg PO at bedtime. Status epilepticus: 4 mg IV (adult), repeat after 5-10 minutes if needed. Acute agitation: 1-2 mg IM (1) · Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1) · Ophthalmic 1 drop in each eye every 8-12 hours (1) · Oral 300-450 mg PO QID; IV 600-900 mg q8h; topical 1% solution/gel BID; vaginal 100 mg ovule × 3 days or 2% cream × 7 days (1) · Pediatric 6-11: 100 mg PO daily, titrate weekly to max 400 mg. Adolescent 12-17: 200 mg, max 400 mg. Adult: 200 mg, max 600 mg. (1) · Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1) · Trials use 25 mg or 50 mg PO daily (1)
preparations:
0.025%, 0.035% ophthalmic solutions (1) · 0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (1) · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 1 g soft gelatin capsules containing ~465 mg EPA + ~375 mg DHA as ethyl esters (1) · 10 mg, 20 mg, 40 mg tablets (1) · 10 mg, 34 mg capsules/tablets (1) · 100 mg, 150 mg, 200 mg extended-release capsules (can be sprinkled on food) (1) · 125, 250, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension; 750 mg, 1.5 g IV vials (1) · 2 mg capsules and tablets; 1 mg/5 mL oral solution; combined with simethicone (Imodium Multi-Symptom) (1) · 250 mg, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension (1) · 250 mg, 500 mg, 750 mg capsules; 250 mg/5 mL, 125 mg/5 mL suspension; tablets (1) · 250, 500 mg base or stearate tablets; ER tablets; ethyl succinate 200 mg/5 mL suspension; 500 mg, 1 g IV (lactobionate); 2% topical solution/gel; 0.5% ophthalmic ointment (1) · 250, 500 mg tablets; 750 mg ER; 500 mg/100 mL IV; 0.75-1% topical gel/cream; 0.75% vaginal gel; suppository (1) · 250, 500, 750 mg IR tablets; 500, 1000 mg ER tablets (XR); 250, 500 mg/5 mL oral suspension; 200, 400 mg IV; 0.3% ophthalmic solution and ointment; 0.2% otic (1) · 42 mg capsules (1) · 5 mg, 10 mg, 20 mg tablets (1) · 5, 10, 20, 100 mg tablets; 10 mg/mL IV (1) · 75, 150, 300 mg capsules; 75 mg/5 mL solution; 150 mg/mL IV; 1% topical; 2% vaginal cream (1) · 95 mg (OTC), 99.5 mg, 100 mg, 200 mg tablets (1) · Investigational oral capsule (1) · Tablets 0.5, 1, 2 mg; oral concentrate 2 mg/mL; injection 2 mg/mL and 4 mg/mL; Loreev XR capsules 1, 2, 3 mg (1) · Tablets 4 mg; oral syrup 2 mg/5 mL (1)
duration: (Click arrow to add another value)
bioavailability:
90% (oral; food delays but does not reduce absorption)'"`UNIQ--ref-000004F3-QINU`"' (1) · Adequate oral bioavailability with extended-release formulation (1) · High (oral)'"`UNIQ--ref-00000FB5-QINU`"' (1) · Improved with food'"`UNIQ--ref-00000052-QINU`"' (1) · Limited but adequate; take with food (1) · Not characterized; oral dosing once daily (1) · Oral bioavailability suitable for daily dosing (1) · Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) · Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) · ~0.3% (oral; extensive first-pass via CYP3A4 and P-glycoprotein-mediated efflux at the intestinal and blood-brain barriers limit systemic and CNS exposure at therapeutic doses)'"`UNIQ--ref-00000FD3-QINU`"' (1) · ~30-65% (oral; acid-labile, hence enteric-coated formulations; food affects absorption variably)'"`UNIQ--ref-00000D3F-QINU`"' (1) · ~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-QINU`"' (1) · ~60% (oral; phenoxymethyl modification makes it acid-stable, unlike penicillin G which is destroyed by gastric acid)'"`UNIQ--ref-00000E77-QINU`"' (1) · ~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"' (1) · ~72% (with food); much lower fasting (~36%) (1) · ~75% (1) · ~80% (oral)'"`UNIQ--ref-00000BEC-QINU`"' (1) · ~80% (oral; predictable absorption — a substantive practical advantage over furosemide whose oral absorption is 10-100% variable)'"`UNIQ--ref-00000B47-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000024-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00001443-QINU`"' (1) · ~95% (1) · ~95% (oral)'"`UNIQ--ref-0000001F-QINU`"' (1)
pregnancy:
'''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern); use only when benefit clearly outweighs.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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> (1) · Generally considered acceptable when needed.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe (minimal systemic exposure).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe after the first trimester; first-trimester use weighed against indication.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Generally considered safe; commonly used in pregnancy.<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.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Investigational (1) · Limited data (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; avoid (1) · Limited data; National Pregnancy Registry available (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (1) · Limited data; not first-line in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; weigh benefits/risks (2) · Limited human data; older agent with substantial use experience.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft lip/palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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