Drug intelligence / Profile preview

Risperdal CONSTA (risperidone)

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

Overview

Risperdal CONSTA is a long-acting injectable (LAI) formulation of the atypical antipsychotic risperidone, developed by Janssen (a Johnson & Johnson company) and Alkermes. It utilizes Alkermes' proprietary Medisorb® microsphere technology, where risperidone is encapsulated in a biodegradable polylactide-co-glycolide (PLG) polymer. This formulation allows for the sustained release of the drug over a two-week period following intramuscular injection, overcoming the need for daily oral dosing and improving treatment adherence. Risperidone acts primarily as a potent antagonist at dopamine D2 and serotonin 5-HT2A receptors. Risperdal CONSTA was the first long-acting atypical antipsychotic to receive FDA approval, initially for the treatment of schizophrenia in 2003 and subsequently for the maintenance treatment of bipolar I disorder as both monotherapy and adjunctive therapy to lithium or valproate.

Brand names
Risperdal CONSTA
Other names
risperidone long-acting injectionrisperidone LAIRLAIrisperidone microspheres
02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2C (5-hydroxytryptamine 2C receptor)HTR1D (5-hydroxytryptamine receptor 1D)HTR2A (Serotonin receptor 5-HT2A)DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)ADRA2A (α2A)

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