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Medicines > duration : 12 hours or 12-24 hours or Daily dosing

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classes:
Atypical antipsychotic (2) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (2) · [[:Category:Omega-3_fatty_acids|Omega-3 fatty acid]] (2)
mechanism:
None (12) · 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-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (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-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-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-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-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-00000B81-QINU`"', '"`UNIQ--vote-00000B82-QINU`"', '"`UNIQ--vote-00000B83-QINU`"' (1) · '"`UNIQ--vote-00000C8F-QINU`"', '"`UNIQ--vote-00000C90-QINU`"', '"`UNIQ--vote-00000C91-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-QINU`"' (1) · '"`UNIQ--vote-00000E91-QINU`"', '"`UNIQ--vote-00000E92-QINU`"', '"`UNIQ--vote-00000E93-QINU`"' (1) · '"`UNIQ--vote-0000113C-QINU`"', '"`UNIQ--vote-0000113D-QINU`"', '"`UNIQ--vote-0000113E-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) · 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) · 50 mg PO BID; titrate to 100-200 mg BID; pill-in-pocket 200-300 mg PO single dose for AF conversion (1) · 60 mg PO BID or 180 mg PO once daily (1) · ACS/PCI: 180 mg PO loading dose, then 90 mg PO BID for 12 months; long-term post-MI: 60 mg BID (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) · 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) · 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) · 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) · 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)
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) · 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) · ~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) · ~36% (oral)'"`UNIQ--ref-00000C93-QINU`"' (1) · ~50% (oral; not significantly affected by food)'"`UNIQ--ref-000001FC-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) · ~75% (oral, as the active carboxylate after hepatic esterase activation)'"`UNIQ--ref-00000E95-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) · ~99% (oral)'"`UNIQ--ref-0000002A-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) · '''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 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 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> (1) · 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) · 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) · 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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