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.
Background
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
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
---|---|---|---|---|---|
2025/05/14 | Phase 4 | Not yet recruiting | |||
2024/07/22 | Phase 2 | Recruiting | |||
2024/07/01 | Phase 3 | Recruiting | Louisiana State University Health Sciences Center Shreveport | ||
2024/04/16 | Phase 1 | ENROLLING_BY_INVITATION | Spanish Foundation for Neurometrics Development | ||
2024/02/01 | Phase 4 | Recruiting | All India Institute of Medical Sciences, Bhubaneswar | ||
2024/01/23 | Phase 1 | Completed | |||
2024/01/11 | Not Applicable | Completed | Dr Rabia Arshad | ||
2023/06/06 | Phase 4 | Withdrawn | |||
2023/03/22 | Phase 3 | Completed | Lyndra Inc. | ||
2023/02/02 | Phase 2 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
---|---|---|---|---|---|
Janssen Pharmaceutical, Inc. | 50458-602 | ORAL | 1 mg in 1 1 | 9/14/2022 | |
Major Pharmaceuticals | 0904-7363 | ORAL | 2 mg in 1 1 | 10/29/2023 | |
State of Florida DOH Central Pharmacy | 53808-1022 | ORAL | 3 mg in 1 1 | 1/18/2015 | |
MSM Repackaging | 42495-004 | ORAL | 2 mg in 1 1 | 10/13/2015 | |
NuCare Pharmaceuticals,Inc. | 68071-4618 | ORAL | 2 mg in 1 1 | 2/22/2021 | |
Teva Pharmaceuticals USA, Inc. | 51759-960 | SUBCUTANEOUS | 250 mg in 0.7 mL | 5/8/2023 | |
Teva Pharmaceuticals USA, Inc. | 51759-630 | SUBCUTANEOUS | 125 mg in 0.35 mL | 5/8/2023 | |
REMEDYREPACK INC. | 70518-2130 | ORAL | 1 mg in 1 1 | 2/27/2024 | |
Ajanta Pharma USA Inc. | 27241-005 | ORAL | 3 mg in 1 1 | 3/18/2024 | |
TYA Pharmaceuticals | 64725-0321 | ORAL | 4 mg in 1 1 | 8/14/2012 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
---|---|---|---|
Authorised | 2/14/2022 | ||
Authorised | 2/14/2022 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
---|---|---|---|---|---|
RISPERDAL CONSTA FOR INJECTION 37.5 mg/vial | SIN12354P | INJECTION, POWDER, FOR SOLUTION | 37.5 mg/vial | 7/21/2003 | |
RISPERIDONE-CHANELLE ORAL SOLUTION 1 MG/ML | SIN15227P | SOLUTION | 1mg/ml | 4/26/2017 | |
Apo-Risperidone 2mg Tablet | SIN13577P | TABLET, FILM COATED | 2mg | 12/1/2008 | |
RISPERIDEX TABLET 4MG | SIN14416P | TABLET, FILM COATED | 4.0MG | 10/22/2013 | |
RISPERDAL TABLET 1 mg | SIN08061P | TABLET, FILM COATED | 1 mg | 3/9/1995 | |
RISPERIDEX TABLET 1MG | SIN14418P | TABLET, FILM COATED | 1.0MG | 10/22/2013 | |
Apo-Risperidone 1mg Tablet | SIN13578P | TABLET, FILM COATED | 1mg | 12/1/2008 | |
RISPERDAL ORAL SOLUTION 1 mg/ml | SIN09905P | SOLUTION | 1 mg/ml | 7/27/1998 | |
EPERON FILM COATED TABLETS 2MG | SIN14774P | TABLET, FILM COATED | 2.0 mg | 4/10/2015 | |
EPERON FILM COATED TABLETS 1MG | SIN14773P | TABLET, FILM COATED | 1.0 mg | 4/10/2015 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
---|---|---|---|---|---|
Risperidone Tablets | 国药准字H20050160 | 化学药品 | 片剂 | 7/14/2020 | |
Risperidone Tablets | 国药准字H20253707 | 化学药品 | 片剂 | 3/25/2025 | |
Risperidone Tablets | 国药准字H20253706 | 化学药品 | 片剂 | 3/25/2025 | |
Risperidone Tablets | 国药准字H20050042 | 化学药品 | 片剂 | 9/10/2019 | |
Risperidone Tablets | 国药准字H20052330 | 化学药品 | 片剂 | 8/23/2024 | |
Risperidone Tablets | 国药准字H20050776 | 化学药品 | 片剂 | 3/27/2020 | |
Risperidone Tablets | 国药准字H20050410 | 化学药品 | 片剂 | 7/22/2020 | |
Risperidone Tablets | 国药准字H20010310 | 化学药品 | 片剂 | 5/28/2020 | |
Risperidone Tablets | 国药准字H20061072 | 化学药品 | 片剂 | 9/4/2020 | |
Risperidone Tablets | 国药准字H20051731 | 化学药品 | 片剂 | 7/22/2020 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
---|---|---|---|---|---|
RISPONS TAB 1MG | N/A | N/A | N/A | 6/28/2010 | |
RISPONS TAB 4MG | N/A | N/A | N/A | 6/28/2010 | |
JMP-RISPERIDONE TABLET 3MG | N/A | N/A | N/A | 7/14/2014 | |
RISPER TAB 4MG | N/A | N/A | N/A | 2/29/2012 | |
PMS-RISPERIDONE TAB 2MG | N/A | N/A | N/A | 9/11/2006 |
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
---|---|---|---|---|---|
GENRX RISPERIDONE risperidone 3mg tablets blister pack | 127574 | Medicine | A | 8/3/2007 | |
RISPERNIA risperidone 0.5mg tablets bottle | 127918 | Medicine | A | 6/26/2006 | |
RISPERNIA risperidone 1mg tablets bottle | 127920 | Medicine | A | 6/26/2006 | |
RIXADONE risperidone 2 mg film coated tablet blister pack | 199180 | Medicine | A | 9/3/2013 | |
NOUMED RISPERIDONE risperidone 2 mg film-coated tablet blister pack | 284371 | Medicine | A | 6/6/2017 | |
RISPERIDONE RBX risperidone 3mg tablet blister pack | 191540 | Medicine | A | 6/14/2012 | |
RISPERIDONE KXP risperidone 0.5 mg film-coated tablet blister pack | 303376 | Medicine | A | 8/21/2018 | |
RISPERIDONE LAPL risperidone 1 mg/mL oral liquid solution bottle | 389692 | Medicine | A | 9/26/2023 | |
RISPERIDONE RBX risperidone 1mg tablet blister pack | 191538 | Medicine | A | 6/14/2012 | |
RISPERIDONE RAN risperidone 4mg tablet blister pack | 191529 | Medicine | A | 6/14/2012 |