Risperidone
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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)
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Summary
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
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
- ↑ 1.0 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