Risperidone

Identification

Summary

Risperidone is a second-generation antipsychotic medication used to treat a number of mental health disorders including schizophrenia, bipolar mania, psychosis, or as an adjunct in severe depression.

Brand Names
Perseris, Risperdal, Rykindo, Uzedy
Generic Name
Risperidone
DrugBank Accession Number
DB00734
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.16 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).16

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.16

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.16

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 410.4845
Monoisotopic: 410.211804333
Chemical Formula
C23H27FN4O2
Synonyms
  • Risperidona
  • Rispéridone
  • Risperidone
  • Risperidonum
External IDs
  • R-64,766
  • R-64766
  • RCN-3028
  • RCN3028

Pharmacology

Indication

Risperidone is indicated for the treatment of schizophrenia 16,20,21 and irritability associated with autistic disorder.16 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.16,20

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.19

Risperidone is also used off-label for a number of conditions including as an adjunct to antidepressants in treatment-resistant depression.11

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofAcute mania••••••••••••
Adjunct therapy in treatment ofAcute mania••••••••••••
Adjunct therapy in treatment ofAcute mania••••••••••••
Treatment ofIrritability••••••••••••••••••••• ••••••• ••••••• •••••• ••••••••••••••
Treatment ofMixed manic depressive episode••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

The primary action of risperidone is to decrease dopaminergic and serotonergic pathway activity in the brain, therefore decreasing symptoms of schizophrenia and mood disorders.3,4

Risperidone has a high binding affinity for serotonergic 5-HT2A receptors when compared to dopaminergic D2 receptors in the brain.2,3 Risperidone binds to D2 receptors with a lower affinity than first-generation antipsychotic drugs, which bind with very high affinity. A reduction in extrapyramidal symptoms with risperidone, when compared to its predecessors, is likely a result of its moderate affinity for dopaminergic D2 receptors.7,5

Mechanism of action

Though its precise mechanism of action is not fully understood, current focus is on the ability of risperidone to inhibit the D2 dopaminergic receptors and 5-HT2A serotonergic receptors in the brain. Schizophrenia is thought to result from an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively.3,4,5

D2 dopaminergic receptors are transiently inhibited by risperidone, reducing dopaminergic neurotransmission, therefore decreasing positive symptoms of schizophrenia, such as delusions and hallucinations.14 Risperidone binds transiently and with loose affinity to the dopaminergic D2 receptor, with an ideal receptor occupancy of 60-70% for optimal effect.7,10 Rapid dissociation of risperidone from the D2 receptors contributes to decreased risk of extrapyramidal symptoms (EPS), which occur with permanent and high occupancy blockade of D2 dopaminergic receptors.6,7 Low-affinity binding and rapid dissociation from the D2 receptor distinguish risperidone from the traditional antipsychotic drugs. A higher occupancy rate of D2 receptors is said to increase the risk of extrapyramidal symptoms and is therefore to be avoided.6,7,8

Increased serotonergic mesocortical activity in schizophrenia results in negative symptoms, such as depression and decreased motivation. The high-affinity binding of risperidone to 5-HT2A receptors leads to a decrease in serotonergic activity. In addition, 5-HT2A receptor blockade results in decreased risk of extrapyramidal symptoms, likely by increasing dopamine release from the frontal cortex, and not the nigrostriatal tract. Dopamine level is therefore not completely inhibited.5,7 Through the above mechanisms, both serotonergic and D2 blockade by risperidone are thought to synergistically work to decrease the risk of extrapyramidal symptoms.

Risperidone has also been said to be an antagonist of alpha-1 (α1), alpha-2 (α2), and histamine (H1) receptors.13 Blockade of these receptors is thought to improve symptoms of schizophrenia, however the exact mechanism of action on these receptors is not fully understood at this time.16

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Humans
ADopamine D2 receptor
antagonist
Humans
UAlpha-1B adrenergic receptor
antagonist
Humans
UAlpha-2B adrenergic receptor
antagonist
Humans
UAlpha-1A adrenergic receptor
antagonist
Humans
UAlpha-2C adrenergic receptor
antagonist
Humans
UHistamine H1 receptor
antagonist
Humans
U5-hydroxytryptamine receptor 2C
antagonist
Humans
U5-hydroxytryptamine receptor 1D
antagonist
Humans
U5-hydroxytryptamine receptor 1A
antagonist
Humans
U5-hydroxytryptamine receptor 7
antagonist
Humans
UD(2L) dopamine receptor
antagonist
Humans
UDopamine D1 receptor
antagonist
Humans
Absorption

Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.16

Volume of distribution

The volume of distribution of risperidone is approximately 1 to 2 L/kg.16

Protein binding

Risperidone and its active metabolite, 9-hydroxyrisperidone, are ~88% and ~77% protein-bound in human plasma, respectively.9,16 They each bind to both serum albumin and alpha-1-acid glycoprotein.16

Metabolism

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone (i.e. paliperidone), which has approximately the same receptor binding affinity as risperidone.6,9 Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase.7,9 Risperidone also undergoes N-dealkylation to a lesser extent.7,9

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Route of elimination

Risperidone is extensively metabolized in the liver. In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives are prolonged compared to young healthy subjects.9,15

Half-life

3 hours in extensive metabolizers9 Up to 20 hours in poor metabolizers9

Clearance

Risperidone is cleared by the kidneys. Clearance is decreased in the elderly and those with a creatinine clearance (ClCr) between 15-59 mL/min, in whom clearance is decreased by approximately 60%.15

Adverse Effects
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Toxicity

Symptoms of overdose include lethargy, dystonia/spasm, tachycardia, bradycardia, and seizures. LD50=57.7 mg/kg (rat, oral) and 34 mg/kg (rat, intravenous).5,6,7

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Risperidone is combined with 1,2-Benzodiazepine.
AbaloparatideAbaloparatide may increase the hypotensive activities of Risperidone.
AbametapirThe serum concentration of Risperidone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Risperidone can be increased when combined with Abatacept.
AbirateroneThe metabolism of Risperidone can be decreased when combined with Abiraterone.
Food Interactions
  • Take with or without food. Food does not affect the rate or extent of absorption.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Risperidone tartrate0S6B72E3LK666179-92-6KSWIOGDSXUFKOC-LREBCSMRSA-N
Product Images
International/Other Brands
Risperidal M-Tab (Janssen) / Risperin (Gador) / Rispolept / Rispolin / Sequinan
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act RisperidoneTablet3 mgOralActavis Pharma Company2006-07-052018-06-26Canada flag
Act RisperidoneTablet0.5 mgOralActavis Pharma Company2006-07-052018-06-26Canada flag
Act RisperidoneTablet0.25 mgOralActavis Pharma Company2006-07-052018-06-26Canada flag
Act RisperidoneTablet2 mgOralActavis Pharma Company2006-07-052018-06-26Canada flag
Act RisperidoneTablet4 mgOralActavis Pharma Company2006-07-052018-06-26Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ag-risperidoneTablet3 mgOralAngita Pharma Inc.2018-09-06Not applicableCanada flag
Ag-risperidoneTablet0.5 mgOralAngita Pharma Inc.2018-09-06Not applicableCanada flag
Ag-risperidoneTablet2 mgOralAngita Pharma Inc.2018-09-06Not applicableCanada flag
Ag-risperidoneTablet0.25 mgOralAngita Pharma Inc.2018-09-06Not applicableCanada flag
Ag-risperidoneTablet4 mgOralAngita Pharma Inc.2018-09-06Not applicableCanada flag

Categories

ATC Codes
N05AX08 — Risperidone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyridopyrimidines. These are compounds containing a pyridopyrimidine, which consists of a pyridine fused to a pyrimidine. Pyridine is 6-membered ring consisting of five carbon atoms and a nitrogen atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridopyrimidines
Sub Class
Not Available
Direct Parent
Pyridopyrimidines
Alternative Parents
Benzisoxazoles / Pyrimidones / Aralkylamines / Pyridines and derivatives / Piperidines / Aryl fluorides / Benzenoids / Heteroaromatic compounds / Isoxazoles / Trialkylamines
show 8 more
Substituents
Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle / Azole / Benzenoid / Benzisoxazole / Heteroaromatic compound
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, pyridopyrimidine, 1,2-benzoxazoles, heteroarylpiperidine (CHEBI:8871)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
L6UH7ZF8HC
CAS number
106266-06-2
InChI Key
RAPZEAPATHNIPO-UHFFFAOYSA-N
InChI
InChI=1S/C23H27FN4O2/c1-15-18(23(29)28-10-3-2-4-21(28)25-15)9-13-27-11-7-16(8-12-27)22-19-6-5-17(24)14-20(19)30-26-22/h5-6,14,16H,2-4,7-13H2,1H3
IUPAC Name
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-one
SMILES
CC1=C(CCN2CCC(CC2)C2=NOC3=C2C=CC(F)=C3)C(=O)N2CCCCC2=N1

References

Synthesis Reference
US4804663
General References
  1. Altschuler EL, Kast RE: The atypical antipsychotic agents ziprasidone [correction of zisprasidone], risperdone and olanzapine as treatment for and prophylaxis against progressive multifocal leukoencephalopathy. Med Hypotheses. 2005;65(3):585-6. [Article]
  2. Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. doi: 10.1592/phco.29.1.64. [Article]
  3. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [Article]
  4. Kemp DE, Canan F, Goldstein BI, McIntyre RS: Long-acting risperidone: a review of its role in the treatment of bipolar disorder. Adv Ther. 2009 Jun;26(6):588-99. doi: 10.1007/s12325-009-0039-0. Epub 2009 Jun 26. [Article]
  5. Szarfman A, Tonning JM, Levine JG, Doraiswamy PM: Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy. 2006 Jun;26(6):748-58. [Article]
  6. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
  7. Yamanouchi Y, Iwata N, Suzuki T, Kitajima T, Ikeda M, Ozaki N: Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone. Pharmacogenomics J. 2003;3(6):356-61. [Article]
  8. Acri AA, Henretig FM: Effects of risperidone in overdose. Am J Emerg Med. 1998 Sep;16(5):498-501. [Article]
  9. Mannens G, Meuldermans W, Snoeck E, Heykants J: Plasma protein binding of risperidone and its distribution in blood. Psychopharmacology (Berl). 1994 May;114(4):566-72. [Article]
  10. Hall H, Halldin C, Nyberg S, Farde L, Sedvall G: Effect of clozapine and risperidone on 5-HT2 and D2-dopamine receptor binding in the post-mortem human brain. An autoradiographic study. Eur Neuropsychopharmacol. 1995 Mar;5(1):19-25. [Article]
  11. Kennedy SH, Lam RW, McIntyre RS, Tourjman SV, Bhat V, Blier P, Hasnain M, Jollant F, Levitt AJ, MacQueen GM, McInerney SJ, McIntosh D, Milev RV, Muller DJ, Parikh SV, Pearson NL, Ravindran AV, Uher R: Canadian Network for Mood and Anxiety Treatments (CANMAT) 2016 Clinical Guidelines for the Management of Adults with Major Depressive Disorder: Section 3. Pharmacological Treatments. Can J Psychiatry. 2016 Sep;61(9):540-60. doi: 10.1177/0706743716659417. Epub 2016 Aug 2. [Article]
  12. Ejsing TB, Pedersen AD, Linnet K: P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments. Hum Psychopharmacol. 2005 Oct;20(7):493-500. doi: 10.1002/hup.720. [Article]
  13. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  14. McEvoy JP: Efficacy of risperidone on positive features of schizophrenia. J Clin Psychiatry. 1994 May;55 Suppl:18-21. [Article]
  15. Pharmacokinetics of Risperidone: Clinical Summary [Link]
  16. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
  17. FDA Approved Drug Products: Risperdal Consta (risperidone) long-acting intramuscular injection [Link]
  18. FDA Approved Drug Products: Perseris (risperidone) extended-release suspension for subcutaneous injection [Link]
  19. Health Canada Product Monograph: Risperdal (risperidone) oral tablets [Link]
  20. FDA Approved Drug Products: RYKINDO (risperidone) for extended-release injectable suspension, for intramuscular use [Link]
  21. FDA Approved Drug Products: UZEDY (risperidone) extended-release injectable suspension, for subcutaneous use [Link]
  22. FDA Label - Risperidone [File]
  23. Health Canada Monograph - Risperidone [File]
Human Metabolome Database
HMDB0005020
KEGG Drug
D00426
PubChem Compound
5073
PubChem Substance
46505850
ChemSpider
4895
BindingDB
50001885
RxNav
35636
ChEBI
8871
ChEMBL
CHEMBL85
ZINC
ZINC000000538312
Therapeutic Targets Database
DAP000003
PharmGKB
PA451257
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Risperidone
FDA label
Download (2.54 MB)
MSDS
Download (25.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentSchizophrenia1
4CompletedNot AvailableSchizoaffective Disorders / Schizophrenia1
4CompletedNot AvailableSchizophrenia1
4CompletedBasic ScienceHealthy Volunteers (HV) / Schizophrenia1
4CompletedBasic ScienceSchizophrenia Spectrum and Other Psychotic Disorders1

Pharmacoeconomics

Manufacturers
  • Ortho mcneil janssen pharmaceuticals inc
  • Ortho mcneil janssen pharmaceutical inc
  • Apotex inc richmond hill
  • Aurobindo pharma ltd
  • Dr reddys laboratories ltd
  • Precision dose inc
  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Wockhardt ltd
  • Par pharmaceutical inc
  • Ranbaxy laboratories inc
  • Sandoz inc
  • Zydus pharmaceuticals usa inc
  • Actavis totowa llc
  • Apotex inc
  • Cadista pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Pliva hrvatska doo
  • Ratiopharm
  • Synthon pharmaceuticals inc
  • Torrent pharmaceuticals ltd
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
  • West ward pharmaceuticals corp
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • Apotheca Inc.
  • Atlantic Biologicals Corporation
  • Aurobindo Pharma Ltd.
  • Barr Pharmaceuticals
  • Cadila Healthcare Ltd.
  • Cardinal Health
  • Cobalt Pharmaceuticals Inc.
  • Comprehensive Consultant Services Inc.
  • Core Pharmaceuticals
  • Dept Health Central Pharmacy
  • DispenseXpress Inc.
  • Doctor Reddys Laboratories Ltd.
  • Greenstone LLC
  • Hikma Pharmaceuticals
  • Janssen-Ortho Inc.
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • Nutritional Research Association Inc.
  • Ortho Mcneil Janssen Pharmaceutical Inc.
  • Par Pharmaceuticals
  • Patriot Pharmaceuticals
  • PD-Rx Pharmaceuticals Inc.
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Pliva Inc.
  • Prepak Systems Inc.
  • Qualitest
  • Quality Care
  • Ratiopharm Inc.
  • Rebel Distributors Corp.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Sandoz
  • Southwood Pharmaceuticals
  • Stat Rx Usa
  • Sun Pharmaceutical Industries Ltd.
  • Teva Pharmaceutical Industries Ltd.
  • Torrent Pharmaceuticals
  • UDL Laboratories
  • Va Cmop Dallas
  • Vangard Labs Inc.
  • Vintage Pharmaceuticals Inc.
  • West-Ward Pharmaceuticals
  • Wockhardt Ltd.
  • Zydus Pharmaceuticals
Dosage Forms
FormRouteStrength
TabletOral0.50 mg
SolutionOral1.0 mg/ml
Solution / dropsOral
Tablet, coatedOral4 mg
Tablet, solubleOral0.5 mg
Tablet, solubleOral2 mg
TabletOral3.000 mg
TabletOral1.000 mg
Tablet, delayed releaseOral1 mg
Tablet, delayed releaseOral2 mg
Tablet, effervescent
SolutionOral
Tablet, film coatedOral
Tablet, orally disintegratingOral
Tablet
Injection, powder, for suspension, extended releaseIntramuscular100 mg
Injection, powder, for suspension, extended releaseIntramuscular75 mg
Injection, powder, for suspension, extended release; kitSubcutaneous120 mg / syr
Injection, powder, for suspension, extended release; kitSubcutaneous90 mg / syr
KitSubcutaneous120 mg/0.8mL
KitSubcutaneous90 mg/0.6mL
TabletOral1.0 mg
TabletOral2.0 mg
TabletOral3.0 mg
TabletOral4.0 mg
Tablet, orally disintegratingOral3 mg
Tablet, orally disintegratingOral4 mg
SolutionOral0.100 g
TabletOral2.000 mg
SyrupOral
Tablet, film coatedOral0.50 mg
TabletOral1 MG
Tablet, film coatedOral2.00 mg
Injection, powder, for suspension, extended releaseParenteral25 MG/2ML
Injection, powder, for suspension, extended releaseParenteral37.5 MG/2ML
Injection, powder, for suspension, extended releaseParenteral50 MG/2ML
SolutionOral100.000 mg
Solution / dropsOral1 MG/ML
TabletOral0.25 mg
TabletOral0.5 mg
TabletOral3 mg
TabletOral4 mg
TabletOral5 mg
SolutionOral100 mg
Injection, powder, for solutionIntramuscular
Injection, powder, for suspension, extended release; kitIntramuscular12.5 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular12.5 mg/2mL
Injection, powder, for suspension, extended release; kitIntramuscular25 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular25 mg/2mL
Injection, powder, for suspension, extended release; kitIntramuscular37.5 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular37.5 mg/2mL
Injection, powder, for suspension, extended release; kitIntramuscular50 mg / vial
Injection, powder, for suspension, extended release; kitIntramuscular50 mg/2mL
SuspensionIntramuscular25.000 mg
Injection, suspension, extended releaseIntramuscular25 mg
Injection, powder, for suspension, extended releaseParenteral25 mg
Injection, powder, for suspension, extended releaseIntramuscular
InjectionIntramuscular
Injection, suspension, extended releaseIntramuscular37.5 mg
Injection, powder, for suspension, extended releaseParenteral37.5 mg
Injection, suspension, extended releaseIntramuscular50 mg
Injection, powder, for suspension, extended releaseParenteral50 mg
Injection, powder, for solutionIntramuscular25 mg
Injection, powder, for solutionIntramuscular37.5 mg
Injection, powder, for suspensionIntramuscular37.5 mg
SolutionOral1 mg / mL
SolutionOral1 mg/ml
Tablet, orally disintegratingOral0.5 mg
Tablet, orally disintegratingOral1 mg
Tablet, orally disintegratingOral2 mg
Tablet, solubleOral4 mg
TabletBuccal; Oral0.5 mg
TabletOral2 mg
Tablet, film coatedOral3 mg
Injection, powder, for suspensionIntramuscular25 mg
Tablet, solubleBuccal1 mg
Tablet, film coatedOral0.5 MG
Tablet, film coatedOral1.0 MG
Tablet, film coatedOral2.0 MG
Tablet, film coatedOral4.0 MG
Tablet, film coatedOral6 MG
Tablet, film coatedOral0.25 MG
Injection, powder, for suspensionParenteral25 mg
Tablet, film coatedOral3.0 MG
Injection, powder, for suspensionParenteral37.5 mg
Injection, powder, for suspensionParenteral50 mg
Tablet, film coatedOral8 MG
Film, solubleOral
Tablet, coatedOral3 mg
Tablet, solubleOral1 mg
SolutionOral1 mg/1mL
TabletOral
TabletOral.25 mg/1
TabletOral.5 mg/1
TabletOral0.25 mg/1
TabletOral0.5 mg/1
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral3 mg/1
TabletOral4 mg/1
Tablet, coatedOral.25 mg/1
Tablet, coatedOral.5 mg/1
Tablet, coatedOral1 mg/1
Tablet, coatedOral2 mg/1
Tablet, coatedOral3 mg/1
Tablet, coatedOral4 mg/1
Tablet, film coatedOral0.25 mg/1
Tablet, film coatedOral0.5 mg/1
Tablet, film coatedOral0.50 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral3 mg/1
Tablet, film coatedOral4 mg/1
Tablet, orally disintegratingOral0.25 mg/1
Tablet, orally disintegratingOral0.5 mg/1
Tablet, orally disintegratingOral1 mg/1
Tablet, orally disintegratingOral2 mg/1
Tablet, orally disintegratingOral3 mg/1
Tablet, orally disintegratingOral4 mg/1
Tablet, film coatedOral1 mg
Tablet, film coatedOral2 MG
Tablet, film coatedOral4 MG
Injection, powder, for suspension, extended release25 MG
Injection, powder, for suspension, extended release37.5 MG
Injection, powder, for suspension, extended release50 MG
Injection, powder, lyophilized, for suspension, extended release; kitIntramuscular12.5 mg/2mL
Injection, powder, lyophilized, for suspension, extended release; kitIntramuscular25 mg/2mL
Injection, powder, lyophilized, for suspension, extended release; kitIntramuscular37.5 mg/2mL
Injection, powder, lyophilized, for suspension, extended release; kitIntramuscular50 mg/2mL
SolutionOral0.1 g
SolutionOral1 mg
SolutionOral100000 mg
Injection, suspension, extended releaseSubcutaneous100 mg/0.28mL
Injection, suspension, extended releaseSubcutaneous125 mg/0.35mL
Injection, suspension, extended releaseSubcutaneous150 mg/0.42mL
Injection, suspension, extended releaseSubcutaneous200 mg/0.56mL
Injection, suspension, extended releaseSubcutaneous250 mg/0.7mL
Injection, suspension, extended releaseSubcutaneous50 mg/0.14mL
Injection, suspension, extended releaseSubcutaneous75 mg/0.21mL
TabletOral2.00 mg
Capsule, delayed releaseOral3 mg
Tablet, coatedOral1 mg
Tablet, coatedOral2 mg
Prices
Unit descriptionCostUnit
Risperdal consta 50 mg syr592.93USD syringe
Risperdal consta 37.5 mg syr444.68USD syringe
Risperdal consta 25 mg syr296.46USD syringe
Risperdal 1 mg/ml Solution 30ml Bottle204.42USD bottle
Risperdal M-TAB 28 1 mg Dispersible Tablet Box196.08USD box
Risperdal M-TAB 28 0.5 mg Dispersible Tablet Bottle167.82USD bottle
Risperidone 1 mg/ml Solution 30ml Bottle158.66USD bottle
Risperdal consta 12.5 mg syr148.22USD syringe
Risperdal m-tab 4 mg odt18.55USD tablet
Risperdal 4 mg tablet16.47USD tablet
Risperidone m-tab 4 mg odt15.16USD tablet
Risperdal m-tab 3 mg odt13.81USD tablet
Risperdal 3 mg tablet11.45USD tablet
Risperidone m-tab 3 mg odt11.29USD tablet
Risperdal m-tab 2 mg odt10.95USD tablet
Risperidone 4 mg tablet9.0USD tablet
Risperidone m-tab 2 mg odt8.95USD tablet
Risperdal 2 mg tablet6.94USD tablet
Risperdal m-tab 1 mg odt6.73USD tablet
Risperidone 3 mg tablet6.63USD tablet
Risperdal 1 mg tablet6.12USD tablet
Risperdal m-tab 0.5 mg odt5.76USD tablet
Risperidone 2 mg tablet5.59USD tablet
Risperidone m-tab 1 mg odt5.5USD tablet
Risperidone M-TAB 0.5 mg Dispersible Tablet4.9USD dispersible tablet
Risperidone m-tab 0.5 mg odt4.71USD tablet
Risperdal M-Tab 4 mg Disintegrating Tablet4.6USD tablet
Risperdal 0.25 mg tablet4.56USD tablet
Risperidone 0.25 mg odt4.48USD tablet
Risperdal 0.5 mg tablet3.62USD tablet
Risperdal M-Tab 3 mg Disintegrating Tablet3.44USD tablet
Risperidone 1 mg tablet3.27USD tablet
Risperidone 0.5 mg tablet3.03USD tablet
Apo-Risperidone 4 mg Tablet2.53USD tablet
Co Risperidone 4 mg Tablet2.53USD tablet
Mylan-Risperidone 4 mg Tablet2.53USD tablet
Novo-Risperidone 4 mg Tablet2.53USD tablet
Phl-Risperidone 4 mg Tablet2.53USD tablet
Pms-Risperidone 4 mg Tablet2.53USD tablet
Ran-Risperidone 4 mg Tablet2.53USD tablet
Ratio-Risperidone 4 mg Tablet2.53USD tablet
Rbx-Risperidone 4 mg Tablet2.53USD tablet
Sandoz Risperidone 4 mg Tablet2.53USD tablet
Risperdal M-Tab 2 mg Disintegrating Tablet2.29USD tablet
Apo-Risperidone 3 mg Tablet1.9USD tablet
Co Risperidone 3 mg Tablet1.9USD tablet
Mylan-Risperidone 3 mg Tablet1.9USD tablet
Novo-Risperidone 3 mg Tablet1.9USD tablet
Phl-Risperidone 3 mg Tablet1.9USD tablet
Pms-Risperidone 3 mg Tablet1.9USD tablet
Ran-Risperidone 3 mg Tablet1.9USD tablet
Ratio-Risperidone 3 mg Tablet1.9USD tablet
Rbx-Risperidone 3 mg Tablet1.9USD tablet
Sandoz Risperidone 3 mg Tablet1.9USD tablet
Risperidone 0.25 mg tablet1.88USD tablet
Apo-Risperidone 2 mg Tablet1.26USD tablet
Co Risperidone 2 mg Tablet1.26USD tablet
Mylan-Risperidone 2 mg Tablet1.26USD tablet
Novo-Risperidone 2 mg Tablet1.26USD tablet
Phl-Risperidone 2 mg Tablet1.26USD tablet
Pms-Risperidone 2 mg Tablet1.26USD tablet
Ran-Risperidone 2 mg Tablet1.26USD tablet
Ratio-Risperidone 2 mg Tablet1.26USD tablet
Rbx-Risperidone 2 mg Tablet1.26USD tablet
Sandoz Risperidone 2 mg Tablet1.26USD tablet
Risperdal M-Tab 1 mg Disintegrating Tablet1.16USD tablet
Risperdal M-Tab 0.5 mg Disintegrating Tablet0.84USD tablet
Apo-Risperidone 1 mg Tablet0.63USD tablet
Co Risperidone 1 mg Tablet0.63USD tablet
Mylan-Risperidone 1 mg Tablet0.63USD tablet
Novo-Risperidone 1 mg Tablet0.63USD tablet
Phl-Risperidone 1 mg Tablet0.63USD tablet
Pms-Risperidone 1 mg Tablet0.63USD tablet
Ran-Risperidone 1 mg Tablet0.63USD tablet
Ratio-Risperidone 1 mg Tablet0.63USD tablet
Rbx-Risperidone 1 mg Tablet0.63USD tablet
Sandoz Risperidone 1 mg Tablet0.63USD tablet
Apo-Risperidone 0.5 mg Tablet0.46USD tablet
Co Risperidone 0.5 mg Tablet0.46USD tablet
Mylan-Risperidone 0.5 mg Tablet0.46USD tablet
Novo-Risperidone 0.5 mg Tablet0.46USD tablet
Phl-Risperidone 0.5 mg Tablet0.46USD tablet
Pms-Risperidone 0.5 mg Tablet0.46USD tablet
Ran-Risperidone 0.5 mg Tablet0.46USD tablet
Ratio-Risperidone 0.5 mg Tablet0.46USD tablet
Rbx-Risperidone 0.5 mg Tablet0.46USD tablet
Sandoz Risperidone 0.5 mg Tablet0.46USD tablet
Apo-Risperidone 0.25 mg Tablet0.27USD tablet
Co Risperidone 0.25 mg Tablet0.27USD tablet
Mylan-Risperidone 0.25 mg Tablet0.27USD tablet
Novo-Risperidone 0.25 mg Tablet0.27USD tablet
Phl-Risperidone 0.25 mg Tablet0.27USD tablet
Pms-Risperidone 0.25 mg Tablet0.27USD tablet
Ran-Risperidone 0.25 mg Tablet0.27USD tablet
Ratio-Risperidone 0.25 mg Tablet0.27USD tablet
Rbx-Risperidone 0.25 mg Tablet0.27USD tablet
Sandoz Risperidone 0.25 mg Tablet0.27USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6110921No2000-08-292013-11-19US flag
CA2406536No2009-12-222021-04-19Canada flag
CA2194564No1998-01-272015-07-04Canada flag
US6667061Yes2003-12-232020-11-25US flag
US5792477Yes1998-08-112017-11-02US flag
US5916598Yes1999-06-292017-11-02US flag
US6379703Yes2002-04-302019-06-30US flag
US6403114Yes2002-06-112017-11-02US flag
US6596316Yes2003-07-222019-06-30US flag
US6194006Yes2001-02-272019-06-30US flag
US6224905Yes2001-05-012017-12-10US flag
US9186413No2015-11-172028-02-13US flag
US10010612No2018-07-032028-02-13US flag
US9180197No2015-11-102028-02-13US flag
US9597402No2017-03-212026-09-26US flag
US10058554No2018-08-282026-09-26US flag
US10406160No2019-09-102026-06-26US flag
US10376590No2019-08-132028-02-13US flag
US11013809No2021-05-252028-02-13US flag
US11110093No2021-09-072026-11-05US flag
US10406161No2019-09-102032-04-10US flag
US10098882No2018-10-162032-04-10US flag
US9532991No2017-01-032032-04-10US flag
US9446135No2016-09-202032-04-10US flag
US11110094No2021-09-072032-04-10US flag
US9439905No2016-09-132025-01-12US flag
US8221778No2012-07-172027-11-12US flag
US8741327No2014-06-032027-11-12US flag
US9925268No2018-03-272025-01-12US flag
US10736965No2020-08-112025-01-12US flag
US8802127No2014-08-122025-01-12US flag
US9717799No2017-08-012025-01-12US flag
US9023897No2015-05-052033-04-05US flag
US9895447No2018-02-202025-01-12US flag
US11712475No2008-02-132028-02-13US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)170PhysProp
boiling point (°C)442Not Available
water solubility2.33 mg/mLNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.171 mg/mLALOGPS
logP3.27ALOGPS
logP2.63Chemaxon
logS-3.4ALOGPS
pKa (Strongest Basic)8.76Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area61.94 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity114.55 m3·mol-1Chemaxon
Polarizability45.28 Å3Chemaxon
Number of Rings5Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9925
Caco-2 permeable-0.5057
P-glycoprotein substrateSubstrate0.6163
P-glycoprotein inhibitor IInhibitor0.8564
P-glycoprotein inhibitor IIInhibitor0.9361
Renal organic cation transporterInhibitor0.6491
CYP450 2C9 substrateNon-substrate0.8235
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.82
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8459
Ames testNon AMES toxic0.5302
CarcinogenicityNon-carcinogens0.8204
BiodegradationNot ready biodegradable0.99
Rat acute toxicity3.8290 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.65
hERG inhibition (predictor II)Inhibitor0.8062
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-003r-3943000000-ac9dc593f66de665b41f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-0000900000-b0fe7f692a00657a0970
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03dl-0800900000-4e0f5ed855c5bb92c98f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01ox-0900600000-8473cdb789508bd753a4
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-3d06f3ad1210b9482139
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0900000000-d0dcf9d7f61a2c2bc652
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-03di-0000900000-dde599ea867efca2809b
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0900300000-9a423e6e6775ee918924
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0900000000-b3a1059a8514321aac84
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0900000000-3160d58bf1d154a8d21c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-2900000000-530259828e362c7f2a3c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-02u3-8900000000-c5ae8612478a7ea315c0
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-066r-9200000000-466435c830554a2d51ea
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-066r-9100000000-352e00f2fbc78e81df2c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-066r-9000000000-de0b42c9894812c69015
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03dl-1901800000-c9a45676bc3a1d1829b7
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-2980000000-3574e0025348c64db6fc
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03dl-0900800000-6edaf8e46040d5648f3f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0790000000-e0be2a4dba2d14313d6c
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-2900000000-81e94f588db0cd3c9ea8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0006-0900300000-2ca53f2d737c37046831
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0000900000-aa40d008fd13cce6ef59
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0ap0-0394700000-984852bdb5fc5c28d349
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-01ox-0900400000-7609f5d1d9baaf61709d
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-1228900000-1615e4ed8cf9941637b6
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-1900100000-ffd9b2d17c8e234a673c
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0670-0948100000-d506d47dd432990ecb6c
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-210.5043733
predicted
DarkChem Lite v0.1.0
[M-H]-198.82178
predicted
DeepCCS 1.0 (2019)
[M+H]+210.9869733
predicted
DarkChem Lite v0.1.0
[M+H]+201.1798
predicted
DeepCCS 1.0 (2019)
[M+Na]+211.7954733
predicted
DarkChem Lite v0.1.0
[M+Na]+208.26259
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1B
Uniprot ID
P35368
Uniprot Name
Alpha-1B adrenergic receptor
Molecular Weight
56835.375 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...
Gene Name
ADRA1A
Uniprot ID
P35348
Uniprot Name
Alpha-1A adrenergic receptor
Molecular Weight
51486.005 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
  2. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
12. D(2L) dopamine receptor
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
References
  1. Corena-McLeod M: Comparative Pharmacology of Risperidone and Paliperidone. Drugs R D. 2015 Jun;15(2):163-74. doi: 10.1007/s40268-015-0092-x. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Fang J, Bourin M, Baker GB: Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn Schmiedebergs Arch Pharmacol. 1999 Feb;359(2):147-51. [Article]
  2. Hendset M, Molden E, Refsum H, Hermann M: Impact of CYP2D6 genotype on steady-state serum concentrations of risperidone and 9-hydroxyrisperidone in patients using long-acting injectable risperidone. J Clin Psychopharmacol. 2009 Dec;29(6):537-41. doi: 10.1097/JCP.0b013e3181c17df0. [Article]
  3. Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: part II. Clin Pharmacokinet. 2009;48(12):761-804. doi: 10.2165/11318070-000000000-00000. [Article]
  4. Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I. Clin Pharmacokinet. 2009;48(11):689-723. doi: 10.2165/11318030-000000000-00000. [Article]
  5. Yasui-Furukori N, Hidestrand M, Spina E, Facciola G, Scordo MG, Tybring G: Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001 Oct;29(10):1263-8. [Article]
  6. Flockhart Table of Drug Interactions [Link]
  7. Source [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Fang J, Bourin M, Baker GB: Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn Schmiedebergs Arch Pharmacol. 1999 Feb;359(2):147-51. [Article]
  2. Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8. [Article]
  3. Prior TI, Baker GB: Interactions between the cytochrome P450 system and the second-generation antipsychotics. J Psychiatry Neurosci. 2003 Mar;28(2):99-112. [Article]
  4. Flockhart Table of Drug Interactions [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. FDA Approved Drug Products: Risperdal (risperidone) for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Saikachi H, Nakamura S: [Synthesis of the furan derivatives. XLIX. Wittig reaction of organosulfurphosphoranes with some aromatic aldehydes]. Yakugaku Zasshi. 1969 Oct;89(10):1446-56. [Article]
  2. Ejsing TB, Pedersen AD, Linnet K: P-glycoprotein interaction with risperidone and 9-OH-risperidone studied in vitro, in knock-out mice and in drug-drug interaction experiments. Hum Psychopharmacol. 2005 Oct;20(7):493-500. doi: 10.1002/hup.720. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48