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Medicines > duration : 12-24 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) · 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 COX-2)]] (1) · Selective norepinephrine reuptake inhibitor (NRI) with 5HT1A partial agonism (1) · Serotonin partial agonist reuptake inhibitor (SPARI) (1) · [[:Category:ACE_inhibitors|ACE inhibitor]] (1) · [[:Category:Analgesics|Analgesic]] (1) · [[:Category:Antibacterials|Antibacterial]] (1) · [[:Category:Antifungals|Antifungal (imidazole)]] (1) · [[:Category:Antifungals|Antifungal]] (2) · [[:Category:Antihistamines|Antihistamine]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]] (1) · [[:Category:Cephalosporins|Cephalosporin (third-generation)]] (1) · [[:Category:Corticosteroids|Corticosteroid]] (1) · [[:Category:Depigmenting_agents|Depigmenting agent]] (1) · [[:Category:Glucocorticoids|Glucocorticoid]] (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (1) · [[:Category:Hydroxypyridones|Hydroxypyridone]] (1) · [[:Category:Inhaled_corticosteroids|Inhaled corticosteroid (ICS)]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) · [[:Category:NSAIDs|Non-steroidal anti-inflammatory (NSAID (1) · [[:Category:Omega-3_fatty_acids|Omega-3 fatty acid]] (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 (10) · 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-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (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)
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-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"' (1) · '"`UNIQ--vote-00000050-QINU`"' (1) · '"`UNIQ--vote-0000099F-QINU`"', '"`UNIQ--vote-000009A0-QINU`"', '"`UNIQ--vote-000009A1-QINU`"', '"`UNIQ--vote-000009A2-QINU`"', '"`UNIQ--vote-000009A3-QINU`"', '"`UNIQ--vote-000009A4-QINU`"' (1) · '"`UNIQ--vote-000009DF-QINU`"', '"`UNIQ--vote-000009E0-QINU`"', '"`UNIQ--vote-000009E1-QINU`"', '"`UNIQ--vote-000009E2-QINU`"', '"`UNIQ--vote-000009E3-QINU`"' (1) · '"`UNIQ--vote-000009FF-QINU`"', '"`UNIQ--vote-00000A00-QINU`"', '"`UNIQ--vote-00000A01-QINU`"' (1) · '"`UNIQ--vote-00000B81-QINU`"', '"`UNIQ--vote-00000B82-QINU`"', '"`UNIQ--vote-00000B83-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-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-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)
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) · 300 mg PO BID, or 600 mg PO once daily, ×5-10 days; pediatric 14 mg/kg/d (1) · 34 mg PO once daily (1) · 4 g PO daily (as 4 x 1 g capsules once daily, or 2 capsules BID) (1) · 42 mg PO once daily with food (no titration) (1) · 5-10 mg PO once daily (2.5 mg if on diuretic or in heart failure); titrate to 10-20 mg BID for HFrEF (1) · 60 mg PO BID or 180 mg PO once daily (1) · Apply thin layer to hyperpigmented areas BID; limit to 4-6 month courses to avoid ochronosis (1) · ICS Pulmicort Flexhaler 180-360 mcg BID; intranasal Rhinocort 64 mcg/spray, 1-2 sprays/nostril daily; Entocort EC 9 mg PO daily for active Crohn's; Symbicort 80/4.5 or 160/4.5 mcg, 2 puffs BID (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) · Osteoarthritis: 200 mg PO once daily or 100 mg BID. Rheumatoid arthritis: 100-200 mg PO BID. Acute pain: 400 mg loading, then 200 mg every 12 hours (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)
duration: (Click arrow to add another value)
bioavailability:
16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"' (1) · 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: minimal systemic; troche: ~3% systemic'"`UNIQ--ref-00000F46-QINU`"' (1) · Topical; minimal systemic absorption'"`UNIQ--ref-00000A03-QINU`"' (1) · ~33% (oral; fruit juices including grapefruit, orange, and apple reduce absorption substantially via OATP1A2 inhibition — distinctive interaction not seen with most other H1s)'"`UNIQ--ref-00000CCD-QINU`"' (1) · ~6-13% inhaled lung deposition; ~10% oral (Entocort EC; extensive first-pass via CYP3A4 — this is the basis of the favorable hepatic-targeted local-effect profile in IBD)'"`UNIQ--ref-000009A6-QINU`"' (1) · ~60% (oral; food does not affect absorption)'"`UNIQ--ref-00000B85-QINU`"' (1) · ~72% (with food); much lower fasting (~36%) (1) · ~75% (1) · ~95% (1) · ~99% (oral)'"`UNIQ--ref-0000002A-QINU`"' (1)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000B86-QINU`"' (1) · Avoid from 20 weeks gestation onward per FDA's 2020 expanded NSAID warning (fetal renal dysfunction, oligohydramnios); contraindicated from 30 weeks (risk of premature ductus arteriosus closure)'"`UNIQ--ref-0000002B-QINU`"' (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 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 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; loratadine and cetirizine have more pregnancy data and are typically preferred.<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; 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) · Long the preferred ICS in pregnancy (Pulmicort) due to the most pregnancy data among the class.<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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