Drug intelligence / Profile preview

risperidone or paliperidone

Development stage
Approved
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Risperidone and paliperidone are atypical antipsychotics used primarily for schizophrenia and related disorders. Risperidone (Risperdal) is a benzisoxazole derivative, and paliperidone (Invega) is its primary active metabolite (9-hydroxyrisperidone). Both function as potent antagonists of dopamine D2 and serotonin 5-HT2A receptors. They also exhibit affinity for alpha-1 and alpha-2 adrenergic receptors and H1 histaminergic receptors. Developed by Janssen Pharmaceuticals, these agents are available in oral and long-acting injectable (LAI) formulations. While risperidone is metabolized by CYP2D6, paliperidone is largely excreted unchanged, reducing its susceptibility to certain drug-drug interactions.

Brand names
RisperdalInvegaRisperdal ConstaInvega SustennaInvega TrinzaInvega Hafyera
Other names
9-hydroxyrisperidone
02

Targets

HRH1 (Histamine H1 Receptor)ADRA2A (α2A)HTR2A (Serotonin receptor 5-HT2A)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)

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