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Medicines > classes : D2/D3/5HT1A partial agonist or Dissociative or Tryptamine

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generic:
None (2)
brand:
None (43) · DXM (1) · DXO (1) · Spravato (1) · Vraylar (1)
classes: (Click arrow to add another value)
mechanism:
None (2) · 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)
uses:
None (45) · Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (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) · 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) · Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1)
preparations:
None (45) · 1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 28 mg/device (each dose uses 2 devices) (1)
fda max:
None (45) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) · 84 mg per session (1)
routes:
None (45) · Intranasal (under direct medical supervision) (1) · Oral (1)
onset:
None (45) · Weeks for psychosis/mood efficacy (1) · Within hours of first administration (1)
duration:
None (45) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1)
halflife:
None (45) · Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses (1) · ~7-12 hours (1)
bioavailability:
None (45) · Adequate oral bioavailability (1) · ~48% intranasal (1)
pregnancy:
None (45) · Avoid; may cause fetal harm (1) · Limited data (1)
legal:
None (45) · Rx (1) · Rx, Schedule III (US). REMS program required. (1)

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