Overview

Risperidone is a second-generation antipsychotic (SGA) medication used in the treatment of a number of mood and mental health conditions including schizophrenia and bipolar disorder. It is one of the most widely used SGAs. Paliperidone, another commonly used SGA, is the primary active metabolite of risperidone (i.e. 9-hydroxyrisperidone). Schizophrenia and various mood disorders are thought to be caused by an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively. Risperidone is thought to reduce this overactivity through inhibition of dopaminergic D2 receptors and serotonergic 5-HT2A receptors in the brain. Risperidone binds with a very high affinity to 5-HT2A receptors, approximately 10-20 fold greater than the drug's binding affinity to D2 receptors, and carries lesser activity at several off-targets which may responsible for some of its undesirable effects.

Indication

Risperidone is indicated for the treatment of schizophrenia and irritability associated with autistic disorder. It is also indicated as monotherapy, or adjunctly with lithium or valproic acid, for the treatment of acute mania or mixed episodes associated with bipolar I disorder. Risperidone is additionally indicated in Canada for the short-term symptomatic management of aggression or psychotic symptoms in patients with severe dementia of the Alzheimer type unresponsive to nonpharmacological approaches. Risperidone is also used off-label for a number of conditions including as an adjunct to antidepressants in treatment-resistant depression.

Associated Conditions

Acute Mania
Irritability
Mixed manic depressive episode
Psychosis
Schizophrenia
Acute Manic episode
Agitated psychotic state

Research Report

Published: Jul 14, 2025

A Comprehensive Monograph on Risperidone: Pharmacology, Clinical Efficacy, and Safety

Executive Summary

Risperidone (DrugBank ID: DB00734) is a foundational second-generation, or atypical, antipsychotic agent that has played a pivotal role in psychiatric pharmacotherapy since its initial approval. As a small molecule benzisoxazole derivative, its pharmacological signature is defined by a potent, high-affinity antagonism of serotonin type 2A (5−HT2A) receptors combined with a moderate-affinity antagonism of dopamine type 2 (D2) receptors. This distinct receptor binding profile differentiates it from first-generation antipsychotics and is believed to underpin its efficacy against both the positive and negative symptoms of schizophrenia while carrying a reduced, though not eliminated, risk of extrapyramidal symptoms at therapeutic doses.

The clinical utility of risperidone is well-established across a range of psychiatric disorders. It holds regulatory approval for the treatment of schizophrenia in adults and adolescents, as monotherapy or adjunctive therapy for acute manic or mixed episodes associated with Bipolar I Disorder in adults and children, and for the management of irritability associated with autistic disorder in pediatric patients. Its application has also extended to numerous off-label uses, including as an adjunctive therapy in treatment-resistant depression.

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Clinical Trials

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Title	Posted	Study ID	Phase	Status	Sponsor
Risperidone Treatment in Schizophrenia Patients Who Are Currently Taking Clozapine	2003/03/17	NCT00056498	Phase 4	Completed	University of Maryland, Baltimore
Treatment of Early Onset Schizophrenia Spectrum Disorders (TEOSS)	2003/02/05	NCT00053703	Phase 4	Completed	University of North Carolina, Chapel Hill
Schizophrenia Study In Adults	2002/11/18	NCT00049946	Phase 2	Completed	GlaxoSmithKline
Treatment and Outcome of Early Onset Bipolar Disorder	2002/11/13	NCT00048802	Phase 4	Completed	Northwell Health
Switching Medication to Treat Schizophrenia	2002/09/05	NCT00044655	Phase 4	Completed	Icahn School of Medicine at Mount Sinai
A Study of the Effectiveness and Safety of Risperidone to Augment SSRI Therapy in Patients With Treatment-resistant Depression	2002/09/05	NCT00044681	Phase 3	Completed	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
Efficacy and Safety of Risperidone Compared With Placebo in the Treatment of Psychotic Symptoms in Patients With Alzheimer's Disease	2002/05/03	NCT00034762	Phase 3	Completed	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
A Study to Assess Safety and Tolerabiltiy Associated With a Switch From Oral Antipsychotic Medications to Long-acting Injectable Risperidone in Patients With Schizophrenia.	2002/05/03	NCT00034775	Phase 3	Completed	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
The Efficacy and Safety of Risperidone in the Treatment of Adolescents With Schizophrenia	2002/05/03	NCT00034749	Phase 3	Completed	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.
CAFE Comparison of Atypicals in First Episode of Psychosis	2002/05/03	NCT00034892	Phase 3	Completed	AstraZeneca

FDA Drug Approvals

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Approved Product	Manufacturer	NDC Code	Route	Strength	Effective Date
No FDA approvals found for this drug.

EMA Drug Approvals

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Approved Product	Authorization Holder	Status	Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

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NMPA Drug Approvals

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PPB Drug Approvals

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TGA Drug Approvals

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Health Canada Drug Approvals

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CIMA AEMPS Drug Approvals

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No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

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No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

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No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

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No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

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Medicine Name	MA Holder	MA Number	Pharmaceutical Form	Active Ingredient	Authorization Date
No UK EMC drug information found for this drug.