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
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.
Clinical Trials
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Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2007/02/14 | Phase 3 | Completed | |||
2007/02/09 | Phase 4 | Completed | |||
2007/01/18 | Phase 4 | Completed | |||
2007/01/05 | Phase 4 | Terminated | |||
2007/01/01 | Phase 4 | Completed | |||
2006/11/15 | Phase 3 | Completed | |||
2006/11/03 | N/A | Completed | |||
2006/10/23 | Phase 3 | Completed | Janssen Pharmaceutica N.V., Belgium | ||
2006/10/18 | Not Applicable | Completed | |||
2006/10/11 | Phase 2 | Completed |
FDA Drug Approvals
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Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Jubilant Cadista Pharmaceuticals Inc. | 59746-050 | ORAL | 4 mg in 1 1 | 2/24/2023 | |
| Chartwell RX, LLC | 62135-603 | ORAL | 2 mg in 1 1 | 4/2/2024 | |
| State of Florida DOH Central Pharmacy | 53808-0909 | ORAL | 2 mg in 1 1 | 9/30/2014 | |
| Teva Pharmaceuticals USA, Inc. | 51759-740 | SUBCUTANEOUS | 150 mg in 0.42 mL | 5/8/2023 | |
| Preferred Pharmaceuticals Inc. | 68788-7211 | ORAL | 2 mg in 1 1 | 9/9/2021 | |
| Janssen Pharmaceuticals, Inc. | 50458-395 | ORAL | 0.5 mg in 1 1 | 8/31/2022 | |
| Solco Healthcare US, LLC | 43547-344 | ORAL | 4 mg in 1 1 | 7/27/2023 | |
| Solco Healthcare US, LLC | 43547-341 | ORAL | 1 mg in 1 1 | 7/27/2023 | |
| Amneal Pharmaceuticals NY LLC | 69238-2112 | ORAL | 3 mg in 1 1 | 12/30/2023 | |
| Janssen Pharmaceutical, Inc. | 50458-605 | ORAL | 4 mg in 1 1 | 9/14/2022 |
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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Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
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Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
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Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
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Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
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