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Risperidone: Difference between revisions

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Category taxonomy (#23): retag to house-compliant neuroleptic categories
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{{MedTemplate
{{MedTemplate
| generic           = Risperidone
| generic           = Risperidone
| brand             = Risperdal
| 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           = Antipsychotic, Neuroleptic
| classes           = [[:Category:Neuroleptics|Neuroleptic]], [[:Category:Atypical neuroleptics|Atypical neuroleptic (second-generation)]], [[:Category:Benzisoxazoles|Benzisoxazole]], [[:Category:Mood stabilizers|Mood stabilizer]]
| mechanism          = D2/5-HT2A antagonist
| 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>
| uses              =  
| 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
| starting_dose     =  
| 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
| preparations      =  
| fda_max          = 16 mg/day (schizophrenia, adult); 6 mg/day (bipolar maintenance, autism irritability)
| fda_max           =  
| 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    =
| bioavailability   = ~70% (oral)<ref name="risperdal-label" />
| pregnancy         =  
| pregnancy        = Signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.{{citation needed}}
| legal              =  
| 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" />
| intro              =
| 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.
| pharmacokinetics   =  
| pharmacodynamics  =  
| indications        =  
| dosing             =  
| effects            =  
| interactions      = <pharmaInteractions/>
| pregnancy_details  =
| monitoring         =  
| counseling        =  
| anecdotes          =
| seealso            =
| references        =  
}}
}}


[[Category:Second-generation neuroleptics]]
== References ==
<references />
 
[[Category:Neuroleptics]]
[[Category:Neuroleptics]]
[[Category:Atypical neuroleptics]]
[[Category:Benzisoxazoles]]
[[Category:Mood stabilizers]]

Latest revision as of 02:23, 27 May 2026

Neuroleptic, Atypical neuroleptic (second-generation), Benzisoxazole, Mood stabilizer
Risperidone
Risperdal (oral), Risperdal M-Tab (ODT), Risperdal Consta (biweekly IM LAI), Perseris (monthly SC LAI), Uzedy (monthly/bimonthly SC LAI), Rykindo (biweekly IM LAI)

Experience

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Problems

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Titration strategies

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Effects

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Summary
Classes
Neuroleptic, Atypical neuroleptic (second-generation), Benzisoxazole, Mood stabilizer
Common uses
Schizophrenia (FDA)0, Bipolar I mania and mixed episodes (FDA)0, Autism spectrum disorder-associated irritability (FDA, pediatric ages 5+)0, Schizoaffective disorder (off-label)0, Severe agitation in dementia (off-label; with mortality-warning caveats)0
Pharmacy
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
US FDA Max
16 mg/day (schizophrenia, adult); 6 mg/day (bipolar maintenance, autism irritability)
Pharmacology
Routes
Oral, intramuscular (LAI), subcutaneous (LAI)
Onset
Neuroleptic effect emerges over days to weeks
Duration
24 hours (oral); 2-4 weeks (LAI formulations)
Half-life
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)[1]
Bioavailability
~70% (oral)[1]
Pregnancy
Signal for neonatal extrapyramidal symptoms and withdrawal with third-trimester exposure.[citation needed]
Legal status
Rx-only in US. Carries the atypical-neuroleptic Boxed Warning for increased mortality in elderly patients with dementia-related psychosis[1]
Purported mechanism
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.0 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.[1] PharmGKB clinical annotations for risperidone-CYP2D6 apply (Level 2A) and the Dutch Pharmacogenetics Working Group (DPWG) has issued CYP2D6 dosing guidance for risperidone. No formal CPIC guideline for neuroleptic CYP2D6 dosing has been published.

References

  1. ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Risperdal (risperidone), Janssen, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020272s068,020588s053,021444s041lbl.pdf
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