Risperidone: Difference between revisions
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MDElliottMD (talk | contribs) home-claude: fix CPIC citation hard errors (CPIC scope does not cover these medicines; correct to PharmGKB/DPWG/FDA label where applicable) |
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{{MedTemplate | {{MedTemplate | ||
| generic | | generic = Risperidone | ||
| brand | | brand = Risperdal (oral), Risperdal M-Tab (ODT), Risperdal Consta (biweekly IM LAI), Perseris (monthly SC LAI), Uzedy (monthly/bimonthly SC LAI), Rykindo (biweekly IM LAI) | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:Neuroleptics|Neuroleptic]], [[:Category:Atypical neuroleptics|Atypical neuroleptic (second-generation)]], [[:Category:Benzisoxazoles|Benzisoxazole]], [[:Category:Mood stabilizers|Mood stabilizer]] | ||
| | | uses = <vote slug="schizophrenia-use">Schizophrenia (FDA)</vote>, <vote slug="bipolar-mania-mixed-use">Bipolar I mania and mixed episodes (FDA)</vote>, <vote slug="autism-irritability-pediatric-use">Autism spectrum disorder-associated irritability (FDA, pediatric ages 5+)</vote>, <vote slug="schizoaffective-disorder-use">Schizoaffective disorder (off-label)</vote>, <vote slug="severe-agitation-dementia-use">Severe agitation in dementia (off-label; with mortality-warning caveats)</vote> | ||
| | | starting_dose = 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 | ||
| | | preparations = 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 | ||
| | | fda_max = 16 mg/day (schizophrenia, adult); 6 mg/day (bipolar maintenance, autism irritability) | ||
| | | pill_id = | ||
| routes | | routes = Oral, intramuscular (LAI), subcutaneous (LAI) | ||
| onset | | onset = Neuroleptic effect emerges over days to weeks | ||
| duration | | duration = 24 hours (oral); 2-4 weeks (LAI formulations) | ||
| halflife | | halflife = 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)<ref name="risperdal-label">FDA Prescribing Information, Risperdal (risperidone), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020272s068,020588s053,021444s041lbl.pdf</ref> | ||
| bioavailability = ~70% (oral)<ref name="risperdal-label" /> | |||
| pregnancy = Signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.{{citation needed}} | |||
| legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the atypical-neuroleptic '''Boxed Warning''' for increased mortality in elderly patients with dementia-related psychosis<ref name="risperdal-label" /> | |||
| | | mechanism = <vote slug="risperidone-mech-claim">'''D2 dopamine receptor antagonist plus 5-HT2A serotonin receptor antagonist''', the classical atypical-neuroleptic signature originally derived from clozapine but with a more dopamine-tilted occupancy profile than olanzapine or quetiapine. The high D2 occupancy at therapeutic doses produces the highest rates of '''hyperprolactinemia''' among second-generation neuroleptics (galactorrhea, amenorrhea, sexual dysfunction, and bone density loss with chronic use), along with dose-dependent extrapyramidal symptoms above ~6 mg/day.</vote> CYP2D6 substrate; CYP2D6 oxidation produces 9-hydroxy-risperidone (paliperidone). CYP2D6 poor metabolizers have higher risperidone exposure, but the active-moiety sum (risperidone plus paliperidone) is relatively preserved across CYP2D6 phenotypes.<ref name="risperdal-label" /> PharmGKB clinical annotations for risperidone-CYP2D6 apply (Level 2A) and the Dutch Pharmacogenetics Working Group (DPWG) has issued CYP2D6 dosing guidance for risperidone.<!-- citation needed: PharmGKB risperidone CYP2D6 annotation Level 2A; DPWG risperidone CYP2D6 dosing guidance. Search: pharmgkb.org risperidone; dpwg risperidone cyp2d6 --> No formal CPIC guideline for neuroleptic CYP2D6 dosing has been published. | ||
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== References == | |||
<references /> | |||
[[Category:Neuroleptics]] | [[Category:Neuroleptics]] | ||
[[Category:Atypical neuroleptics]] | |||
[[Category:Benzisoxazoles]] | |||
[[Category:Mood stabilizers]] | |||