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Drilldown: Medicines

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

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classes:
Atypical antipsychotic (2) · [[:Category:Antibacterials|Antibacterial]] (2) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (2) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (2) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (2) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (2) · [[:Category:Omega-3_fatty_acids|Omega-3 fatty acid]] (2)
mechanism:
None (13) · 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-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-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-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-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) · '"`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-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:
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-00000050-QINU`"' (1) · '"`UNIQ--vote-000001F8-QINU`"', '"`UNIQ--vote-000001F9-QINU`"', '"`UNIQ--vote-000001FA-QINU`"' (1) · '"`UNIQ--vote-00000475-QINU`"', '"`UNIQ--vote-00000476-QINU`"', '"`UNIQ--vote-00000477-QINU`"', '"`UNIQ--vote-00000478-QINU`"', '"`UNIQ--vote-00000479-QINU`"', '"`UNIQ--vote-0000047A-QINU`"', '"`UNIQ--vote-0000047B-QINU`"', '"`UNIQ--vote-0000047C-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-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-00000C8F-QINU`"', '"`UNIQ--vote-00000C90-QINU`"', '"`UNIQ--vote-00000C91-QINU`"' (1) · '"`UNIQ--vote-00000E91-QINU`"', '"`UNIQ--vote-00000E92-QINU`"', '"`UNIQ--vote-00000E93-QINU`"' (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-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-QINU`"' (1) · '"`UNIQ--vote-00001286-QINU`"' (1) · '"`UNIQ--vote-000013B3-QINU`"', '"`UNIQ--vote-000013B4-QINU`"', '"`UNIQ--vote-000013B5-QINU`"' (1) · '"`UNIQ--vote-000013CF-QINU`"', '"`UNIQ--vote-000013D0-QINU`"' (1) · '"`UNIQ--vote-000014BE-QINU`"', '"`UNIQ--vote-000014BF-QINU`"', '"`UNIQ--vote-000014C0-QINU`"', '"`UNIQ--vote-000014C1-QINU`"', '"`UNIQ--vote-000014C2-QINU`"' (1) · '"`UNIQ--vote-00001582-QINU`"' (1)
starting dose:
1 capsule (20/10 mg dextromethorphan/quinidine) PO once daily × 7 days, then 1 capsule BID (1) · 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) · 100 mg PO BID; rickettsial 200 mg/d; doxy-PEP 200 mg within 72 hours after condomless sex (1) · 2 g PO BID with meals (4 g/d total) (1) · 250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections (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) · 50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (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) · ACS/PCI: 180 mg PO loading dose, then 90 mg PO BID for 12 months; long-term post-MI: 60 mg BID (1) · Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID (1) · NVAF: 5 mg PO BID (2.5 mg BID if 2 of 3: age ≥80, weight ≤60 kg, serum creatinine ≥1.5 mg/dL); acute VTE: 10 mg BID for 7 days, then 5 mg BID (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 200-400 mg BID; ophthalmic 1-2 drops in affected eye(s) q2-4h initially, then taper; otic 5-10 drops in affected ear BID (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) · Treatment: 75 mg PO BID × 5 days (adult); pediatric weight-based; prophylaxis: 75 mg PO once daily × 7-10 days (1) · Trials use 25 mg or 50 mg PO daily (1)
preparations:
0.025%, 0.035% ophthalmic solutions (1) · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) (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) · 0.5 g, 1 g capsules (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) · 2.5 mg, 5 mg tablets (1) · 20 mg dextromethorphan HBr / 10 mg quinidine sulfate capsules (1) · 200, 300, 400 mg tablets (mostly generic now); 0.3% ophthalmic solution; 0.3% otic solution (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) · 30, 45, 75 mg capsules; 6 mg/mL oral suspension (1) · 42 mg capsules (1) · 5 mg, 10 mg, 20 mg tablets (1) · 50 mg, 75 mg, 100 mg, 150 mg tablets and capsules; delayed-release; suspension; IV (1) · 50, 100, 150 mg tablets (1) · 60, 90 mg tablets (1) · Investigational oral capsule (1)
duration: (Click arrow to add another value)
bioavailability:
Adequate oral bioavailability with extended-release formulation (1) · Improved with food'"`UNIQ--ref-00000052-QINU`"' (1) · Increased substantially via CYP2D6 inhibition'"`UNIQ--ref-00001584-QINU`"' (1) · Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"' (1) · Limited but adequate; take with food (1) · Not characterized; oral dosing once daily (1) · Oral bioavailability suitable for daily dosing (1) · Substantially improved with high-fat meal; take with food'"`UNIQ--ref-000013D2-QINU`"' (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) · ~36% (oral)'"`UNIQ--ref-00000C93-QINU`"' (1) · ~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-QINU`"' (1) · ~50% (oral; not significantly affected by food)'"`UNIQ--ref-000001FC-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) · ~75% (oral, as the active carboxylate after hepatic esterase activation)'"`UNIQ--ref-00000E95-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000BEC-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00001140-QINU`"' (1) · ~95% (1) · ~95% (oral)'"`UNIQ--ref-000014C4-QINU`"' (1) · ~95% (oral; reduced by dairy, antacids, iron via divalent-cation chelation, though less than for tetracycline itself)'"`UNIQ--ref-0000047E-QINU`"' (1)
pregnancy:
None (2) · '''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) · '''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) · 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 used when influenza treatment is indicated; pregnancy is a recognized risk factor for severe influenza.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · 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> (2) · Limited data; avoid (1) · Limited data; National Pregnancy Registry available (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (1) · Limited data; quinidine has been used in pregnancy as antiarrhythmic.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; second-line to intranasal corticosteroids or PO loratadine/cetirizine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; weigh against alternatives.<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<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use in fetal SVT (transplacental antiarrhythmic therapy) is established; otherwise weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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