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Medicines > duration : 24 hours (once-daily dosing) or 8-12 hours or Daily dosing

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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:Acetylcholinesterase inhibitors|Acetylcholinesterase inhibitor]] (1) · [[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) · [[:Category:Anti-dementia medicines|Anti-dementia medicine]] (1) · [[:Category:Antibacterials|Antibacterial (anaerobic)]] (1) · [[:Category:Antibacterials|Antibacterial]] (1) · [[:Category:Antidepressants|Antidepressant]] (3) · [[:Category:Antidiarrheals|Antidiarrheal]] (1) · [[:Category:Antiprotozoals|Antiprotozoal]] (1) · [[:Category:Anxiolytics|Anxiolytic]] (2) · [[:Category:Beta-lactam_antibiotics|β-lactam antibiotic]] (1) · [[:Category:Cephalosporins|Cephalosporin (second-generation)]] (1) · [[:Category:Fluoroquinolones|Fluoroquinolone antibiotic]] (1) · [[:Category:Glaucoma_medications|Glaucoma medication]] (1) · [[:Category:H1_receptor_antagonists|Histamine H1 receptor antagonist]] (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:SSRIs|Selective serotonin reuptake inhibitor (SSRI)]] (3)
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-0000001D-QINU`"' CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response'"`UNIQ--ref-0000001E-QINU`"'. (2) · '"`UNIQ--vote-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-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-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (2) · '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"', '"`UNIQ--vote-00000029-QINU`"', '"`UNIQ--vote-0000002A-QINU`"' (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-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-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-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) · 10 mg PO once daily; titrate to 20 mg/day after 1-2 weeks if needed (1) · 20 mg PO once daily; titrate to 40 mg/day after 1 week if tolerated. Elderly (>60) and hepatic impairment: 20 mg/day ceiling (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) · 5 mg PO once daily at bedtime; titrate to 10 mg/day after 4-6 weeks. Severe Alzheimer disease: may escalate to 23 mg/day. Adlarity patch: 5 or 10 mg/day applied weekly (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) · MDD/GAD: 20 mg PO once daily. Panic disorder: 10 mg titrating to 40 mg. OCD: 20 mg titrating to 40-60 mg. CR: 25 mg/day. Brisdelle: 7.5 mg at bedtime for hot flashes (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) · 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)
duration: (Click arrow to add another value)
pregnancy:
None (1) · '''Among the least preferred SSRIs in pregnancy.''' Observational signal for cardiac malformations (atrial and ventricular septal defects) with first-trimester exposure, and the most severe neonatal adaptation syndrome of any SSRI with third-trimester exposure'"`UNIQ--ref-0000002D-QINU`"' (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) · 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; rarely indicated in pregnancy given the patient population.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Observational signal for persistent pulmonary hypertension of the newborn (small absolute risk) and neonatal adaptation syndrome with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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