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Medicines > classes : Atypical antipsychotic or Botanical or Research material

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generic:
None (3)
brand:
None (153) · (none, never marketed) (1) · Caplyta (1) · O-DSMT (1) · Rexulti (1) · Vraylar (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin/norepinephrine/dopamine releasing agent (3) · None (2) · Cathinone analogue; monoamine reuptake inhibitor (2) · Contains LSA (2) · Contains mescaline (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (154) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · 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) · 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)
starting dose:
None (154) · 42 mg PO once daily with food (no titration) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (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) · 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 (154) · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 42 mg capsules (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (154) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) · 42 mg/d (1) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) · N/A (never approved) (1)
routes:
None (154) · intranasal; rectal and IV reported. (1) · Oral (4) · sublingual (1)
onset:
None (154) · Antipsychotic effect over weeks (1) · Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1) · Weeks for psychosis/mood efficacy (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (154) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Daily dosing (2) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1)
halflife:
None (154) · 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) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~18 hours (terminal) (1) · ~91 hours (1)
bioavailability:
None (154) · Adequate oral bioavailability (1) · Limited but adequate; take with food (1) · Not formally characterized in humans. (1) · ~95% (1)
pregnancy:
None (154) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Limited data (1) · Limited data; National Pregnancy Registry available (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (1)
legal:
None (155) · Rx (3)

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