MedPath

Risperidone

Generic Name
Risperidone
Brand Names
Perseris, Risperdal, Rykindo, Uzedy, Okedi
Drug Type
Small Molecule
Chemical Formula
C23H27FN4O2
CAS Number
106266-06-2
Unique Ingredient Identifier
L6UH7ZF8HC

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

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

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