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Medicines > classes : Research material or [[:Category:Atypical neuroleptics|Atypical neuroleptic (second-generation)]]

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generic:
brand:
None (130) · (none, never marketed) (1) · O-DSMT (1) · Risperdal (oral), Risperdal M-Tab (ODT), Risperdal Consta (biweekly IM LAI), Perseris (monthly SC LAI), Uzedy (monthly/bimonthly SC LAI), Rykindo (biweekly IM LAI) (1) · Zyprexa (oral, IM acute), Zyprexa Zydis (ODT), Zyprexa Relprevv (LAI), Lybalvi (with samidorphan) (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) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (131) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"' (1) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1)
starting dose:
None (131) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Schizophrenia / acute mania: 5-10 mg PO once daily, target 10-15 mg/day. Acute agitation IM: 10 mg, may repeat in 2 hours. Relprevv LAI: 150-300 mg every 4 weeks after oral overlap (1) · Schizophrenia / mania: 1 mg PO BID, titrate to 4-8 mg/day. Pediatric autism irritability: 0.25-0.5 mg/day, weight-titrated. Consta LAI: 25 mg IM every 2 weeks after oral overlap (1)
preparations:
None (131) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablets 0.25, 0.5, 1, 2, 3, 4 mg; M-Tab ODT 0.5, 1, 2, 3, 4 mg; oral solution 1 mg/mL; Consta LAI 12.5, 25, 37.5, 50 mg; Perseris SC LAI 90, 120 mg monthly (1) · Tablets 2.5, 5, 7.5, 10, 15, 20 mg; ODT (Zydis) 5, 10, 15, 20 mg; acute IM injection 10 mg/vial; Relprevv LAI 210, 300, 405 mg vials (1)
fda max:
None (131) · 16 mg/day (schizophrenia, adult); 6 mg/day (bipolar maintenance, autism irritability) (1) · 20 mg/day (oral) (1) · N/A (never approved) (1)
routes:
None (131) · intramuscular (acute and long-acting) (1) · intramuscular (LAI) (1) · intranasal; rectal and IV reported. (1) · Oral (3) · subcutaneous (LAI) (1) · sublingual (1)
onset:
None (131) · Neuroleptic effect emerges over days to weeks (1) · Sedation from first dose; neuroleptic effect emerges over days to weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 24 hours (oral); 2-4 weeks (LAI formulations) (1) · 24 hours (oral); 2-4 weeks (LAI) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)
halflife:
None (131) · 21-54 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Risperidone 3-20 hours; '''9-hydroxy-risperidone (paliperidone) ~20-24 hours''' is the major active metabolite and is separately marketed as a parent compound (Invega)'"`UNIQ--ref-00000021-QINU`"' (1)
bioavailability:
None (131) · Not formally characterized in humans. (1) · ~60% (oral); ~100% (IM)'"`UNIQ--ref-00000027-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-00000022-QINU`"' (1)
pregnancy:
None (131) · 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) · Signal for gestational diabetes and metabolic syndrome with maternal exposure; the metabolic load can be substantial during pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (133) · [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis'"`UNIQ--ref-00000023-QINU`"' (1)

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