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Medicines > duration : 12-24 hours or Daily dosing or ~7-8 hours

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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) · Dual orexin receptor antagonist (DORA) (3) · 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) · the first approved (1) · [[:Category:ACE_inhibitors|ACE inhibitor]] (1) · [[:Category:Analgesics|Analgesic]] (1) · [[: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:Glucocorticoids|Glucocorticoid]] (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist (second-generation)]] (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)
mechanism:
None (9) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · 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-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction). (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) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (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-00000B81-QINU`"', '"`UNIQ--vote-00000B82-QINU`"', '"`UNIQ--vote-00000B83-QINU`"' (1) · '"`UNIQ--vote-00000CCA-QINU`"', '"`UNIQ--vote-00000CCB-QINU`"' (1)
starting dose:
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (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) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (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 mg PO at bedtime; may increase to 10 mg if inadequate (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) · 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) · 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) · Trials use 25 mg or 50 mg PO daily (1)
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