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

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generic:
None (2)
brand:
None (43) · DXM (1) · DXO (1) · Nuplazid (1) · Spravato (1)
classes: (Click arrow to add another value)
mechanism:
None (1) · 5-HT2A agonist (15) · 5-HT2A agonist; 5-HT3 antagonist (1) · 5-HT2A agonist; minor psilocybin mushroom alkaloid (1) · 5-HT2A agonist; primarily auditory effects (1) · 5-HT2A agonist; sigma-1 agonist (1) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · Monoamine releasing agent; 5-HT2A agonist; MAO inhibitor (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; sigma-1 agonist (1) · Prodrug of 4-HO-DET; 5-HT2A agonist (1) · Prodrug of 4-HO-DiPT; 5-HT2A agonist (1) · Prodrug of 4-HO-MET; 5-HT2A agonist (1) · Prodrug of 4-HO-MiPT; 5-HT2A agonist (1) · Prodrug of psilocin; 5-HT2A agonist (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)
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 (45) · Intranasal (under direct medical supervision) (1) · Oral (1)
onset:
None (45) · Benefit over weeks of dosing (1) · Within hours of first administration (1)
duration:
None (45) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Daily dosing (1)
halflife:
None (45) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~7-12 hours (1)
bioavailability:
None (45) · Not characterized; oral dosing once daily (1) · ~48% intranasal (1)
pregnancy:
None (45) · Avoid; may cause fetal harm (1) · Limited data; avoid (1)
legal:
None (45) · 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)

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