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Drilldown: Medicines

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Medicines > duration : 8-12 hours or Daily dosing or Hours per application

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classes:
5HT1A activity than aripiprazole (1) · 5HT2A (1) · 5HT2A/D2 antagonist with proposed differential pre/post-synaptic D2 activity (1) · Atypical antipsychotic (2) · D2/5HT1A partial agonist with stronger α1A (1) · gut-restricted)]] (1) · low-trapping) (1) · Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) · NMDA receptor antagonist (uncompetitive (1) · non-stimulant ADHD agent (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · Selective norepinephrine reuptake inhibitor (NRI) with 5HT1A partial agonism (1) · Serotonin partial agonist reuptake inhibitor (SPARI) (1) · [[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) · [[:Category:Antibacterials|Antibacterial (anaerobic)]] (1) · [[:Category:Antibacterials|Antibacterial]] (2) · [[:Category:Antidiarrheals|Antidiarrheal]] (1) · [[:Category:Antifungals|Antifungal (imidazole)]] (1) · [[:Category:Antifungals|Antifungal]] (2) · [[:Category:Antiprotozoals|Antiprotozoal]] (1) · [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]] (1) · [[:Category:Cephalosporins|Cephalosporin (second-generation)]] (1) · [[:Category:Depigmenting_agents|Depigmenting agent]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1) · [[:Category:Glaucoma_medications|Glaucoma medication]] (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (1) · [[:Category:Hydroxypyridones|Hydroxypyridone]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) · [[:Category:Mast_cell_stabilizers|Mast cell stabilizer]] (1) · [[:Category:Nitroimidazoles|Nitroimidazole antibiotic]] (1) · [[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (1) · [[:Category:Omega-3_fatty_acids|Omega-3 fatty acid]] (1) · [[:Category:Ophthalmic_antihistamines|Ophthalmic antihistamine]] (1) · [[:Category:Opioid_receptor_agonists|Peripheral opioid receptor agonist (μ-selective (1) · [[:Category:Polyene_antifungals|Polyene antifungal]] (1) · [[:Category:Skin_lightening_agents|Skin-lightening agent]] (1) · [[:Category:Topical_antibiotics|Topical antibiotic]] (1) · [[:Category:Topical_antifungals|Topical antifungal]] (2)
mechanism:
None (11) · 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-000009FD-QINU`"' Active against gram-positive cocci including MRSA; the unique target underlies the absence of cross-resistance with other antibiotic classes. High-level resistance (plasmid-mediated mupA) is rising and limits prolonged or repeated use'"`UNIQ--ref-000009FE-QINU`"'. (1) · '"`UNIQ--vote-00000D11-QINU`"' Same mechanistic family as amphotericin B but with prohibitive systemic toxicity at therapeutic doses, hence restriction to topical and luminal-gut indications. No clinically meaningful resistance after decades of use'"`UNIQ--ref-00000D12-QINU`"'. (1) · '"`UNIQ--vote-00001233-QINU`"' Onychomycosis cure rates with nail lacquer are modest (mycologic cure ~30-50%, complete cure ~5-12% at 48 weeks); oral terbinafine remains substantially more effective when systemic therapy is acceptable'"`UNIQ--ref-00001234-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-00000050-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-000009FF-QINU`"', '"`UNIQ--vote-00000A00-QINU`"', '"`UNIQ--vote-00000A01-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-00000D13-QINU`"', '"`UNIQ--vote-00000D14-QINU`"', '"`UNIQ--vote-00000D15-QINU`"', '"`UNIQ--vote-00000D16-QINU`"' (1) · '"`UNIQ--vote-00000F40-QINU`"', '"`UNIQ--vote-00000F41-QINU`"', '"`UNIQ--vote-00000F42-QINU`"', '"`UNIQ--vote-00000F43-QINU`"', '"`UNIQ--vote-00000F44-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-00001215-QINU`"', '"`UNIQ--vote-00001216-QINU`"', '"`UNIQ--vote-00001217-QINU`"' (1) · '"`UNIQ--vote-00001235-QINU`"', '"`UNIQ--vote-00001236-QINU`"', '"`UNIQ--vote-00001237-QINU`"', '"`UNIQ--vote-00001238-QINU`"' (1) · '"`UNIQ--vote-00001286-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) · 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) · 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) · Apply thin layer to hyperpigmented areas BID; limit to 4-6 month courses to avoid ochronosis (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: 4-6 mL (400,000-600,000 units) suspension QID swish-and-swallow; topical: BID-QID; vaginal tablet 1 daily for 2 weeks (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) · Topical cream/lotion BID; shampoo twice weekly; nail lacquer (Penlac) once daily for up to 48 weeks (1) · Topical: 1% cream BID × 2-4 weeks; vaginal: 1% or 2% cream nightly × 7 days, or 100/200/500 mg vaginal tablet single or 3-day regimens; troche: 10 mg PO five times daily × 2 weeks for thrush (1) · Topical: apply small amount to affected area TID × 5-10 days; nasal: apply half the contents of a single-use tube into each nostril BID × 5 days (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) · 0.77% topical cream, lotion, suspension; 1% shampoo; 8% nail lacquer (Penlac) (1) · 1 g soft gelatin capsules containing ~465 mg EPA + ~375 mg DHA as ethyl esters (1) · 1% topical cream, lotion, solution; 1%, 2% vaginal cream; 100, 200, 500 mg vaginal tablets; 10 mg oral troches; combination with betamethasone (Lotrisone, Rx) (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) · 100,000 units/mL oral suspension; 500,000 unit tablets; 100,000 units/g cream, ointment, powder; vaginal tablets (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% ointment; 2% cream; 2% nasal ointment (Bactroban Nasal) (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) · 4% prescription cream/lotion; OTC 2% withdrawn in US (2020 CARES Act); compounded higher strengths available (1) · 42 mg capsules (1) · 5 mg, 10 mg, 20 mg tablets (1) · Investigational oral capsule (1)
duration: (Click arrow to add another value)
bioavailability:
Adequate oral bioavailability with extended-release formulation (1) · Essentially zero systemic absorption from oral or topical routes — the topical-action-only profile is the basis of its safety'"`UNIQ--ref-00000D18-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 limited but measurable systemic absorption'"`UNIQ--ref-00001219-QINU`"' (1) · Topical with minimal systemic absorption'"`UNIQ--ref-0000123A-QINU`"' (1) · Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) · Topical: minimal systemic; troche: ~3% systemic'"`UNIQ--ref-00000F46-QINU`"' (1) · Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) · Topical; minimal systemic absorption'"`UNIQ--ref-00000A03-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) · ~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-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) · ~95% (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) · Generally avoided in pregnancy.<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 absorption).<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 (no systemic absorption).<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; minimal systemic exposure.<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> (1) · Limited data; avoid (1) · Limited data; National Pregnancy Registry available (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (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) · Topical and vaginal generally considered safe; widely used.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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