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Drilldown: Medicines

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

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mechanism:
None (7) · 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-00001302-QINU`"' Renally cleared; accumulation in advanced CKD can produce neuromuscular and cardiac depression. Hypomagnesemia frequently co-exists with hypokalemia and is often the reason refractory potassium loss does not correct until magnesium is repleted. (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-00000050-QINU`"' (1) · '"`UNIQ--vote-0000108C-QINU`"', '"`UNIQ--vote-0000108D-QINU`"', '"`UNIQ--vote-0000108E-QINU`"', '"`UNIQ--vote-0000108F-QINU`"', '"`UNIQ--vote-00001090-QINU`"', '"`UNIQ--vote-00001091-QINU`"' (1) · '"`UNIQ--vote-000012B7-QINU`"', '"`UNIQ--vote-000012B8-QINU`"', '"`UNIQ--vote-000012B9-QINU`"', '"`UNIQ--vote-000012BA-QINU`"', '"`UNIQ--vote-000012BB-QINU`"' (1) · '"`UNIQ--vote-00001303-QINU`"', '"`UNIQ--vote-00001304-QINU`"', '"`UNIQ--vote-00001305-QINU`"', '"`UNIQ--vote-00001306-QINU`"', '"`UNIQ--vote-00001307-QINU`"', '"`UNIQ--vote-00001308-QINU`"', '"`UNIQ--vote-00001309-QINU`"' (1)
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