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Medicines > classes : Phenethylamine or Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) or dissociative

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generic:
None (2)
brand:
None (42) · DXM (1) · DXO (1) · Nexus, Eroxan (historical, late-1980s through mid-1990s) (1) · Nuplazid (1) · Spravato (1)
classes: (Click arrow to add another value)
mechanism:
None (1) · 5-HT2A agonist (12) · 5-HT2A agonist; long duration (1) · 5-HT2A agonist; MAO inhibitor (1) · 5-HT2A agonist; milder than other 2C-x (1) · 5-HT2A partial agonist (1) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · Extremely potent 5-HT2A agonist; vasoconstrictor (1) · Extremely potent 5-HT2A agonist; very long duration (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · NMDA antagonist (3) · NMDA antagonist; endogenous opioid releaser (1) · NMDA antagonist; fluorinated ketamine analogue (1) · NMDA antagonist; kappa-opioid agonist (1) · NMDA antagonist; ketamine analogue (1) · NMDA antagonist; more stimulating than PCP (1) · NMDA antagonist; opioid agonist (1) · NMDA antagonist; potent opioid agonist (1) · NMDA antagonist; SERT inhibitor; sigma-1 agonist (1) · NMDA antagonist; sigma receptor agonist (2) · NMDA antagonist; sigma receptor agonist; dopaminergic (1) · NMDA antagonist; sigma-1 agonist; serotonin reuptake inhibitor (1) · Potent 5-HT2A agonist (5) · Potent 5-HT2A agonist; no oral activity (1) · Potent 5-HT2A agonist; very long duration (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) · Very potent 5-HT2A agonist; long duration (1)
uses:
None (45) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (1)
starting dose:
None (45) · 34 mg PO once daily (1) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (1)
preparations:
None (45) · 10 mg, 34 mg capsules/tablets (1) · 28 mg/device (each dose uses 2 devices) (1)
fda max:
None (45) · 34 mg/d (1) · 84 mg per session (1)
routes:
None (44) · insufflated (1) · Intranasal (under direct medical supervision) (1) · Oral (2) · PR (1)
onset:
None (44) · 45-75 min (oral) (1) · Benefit over weeks of dosing (1) · Within hours of first administration (1)
duration:
None (44) · 4-8 h (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Daily dosing (1)
halflife:
None (44) · Not well characterized (1) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~7-12 hours (1)
bioavailability:
None (44) · Not characterized; oral dosing once daily (1) · Not well characterized (1) · ~48% intranasal (1)
pregnancy:
None (44) · Avoid; may cause fetal harm (1) · Limited data; avoid (1) · Not established (1)
legal:
None (44) · Rx, Schedule III (US). REMS program required. (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · [[USLegal:DEA Schedule I|Schedule I]] (United States) (1)

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