Identification

Name
Risperidone
Accession Number
DB00734  (APRD00187)
Type
Small Molecule
Groups
Approved, Investigational
Description

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 [11, 12].

Risperidone inhibits dopaminergic D2 receptors and serotonergic 5-HT2A receptors in the brain. It is also said to block histamine receptors, and other neural receptors which are currently being studied [12, 3].

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 [11, 12, 3].

Structure
Thumb
Synonyms
  • risperdone
  • Risperidona
  • Risperidonum
  • Risperin
  • Rispolept
  • Rispolin
  • Sequinan
External IDs
N05AX08 / R-64,766 / R-64766 / RCN-3028 / RCN3028
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RisperidoneTablet0.25 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Act RisperidoneTablet3 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Act RisperidoneTablet0.5 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Act RisperidoneTablet2 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Act RisperidoneTablet4 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Act RisperidoneTablet1 mgOralActavis Pharma Company2006-07-05Not applicableCanada
Q-risperidoneTablet1 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-risperidoneTablet3 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-risperidoneTablet0.5 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-risperidoneTablet2 mgOralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ag-risperidoneTablet0.25 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-risperidoneTablet4.0 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-risperidoneTablet1.0 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-risperidoneTablet3.0 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-risperidoneTablet0.50 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Ag-risperidoneTablet2.0 mgOralAngita Pharma Inc.Not applicableNot applicableCanada
Apo-risperidoneTablet3.0 mgOralApotex Corporation2006-07-05Not applicableCanada
Apo-risperidoneTablet0.50 mgOralApotex Corporation2006-07-05Not applicableCanada
Apo-risperidoneSolution1 mgOralApotex Corporation2006-07-05Not applicableCanada
Apo-risperidoneTablet2.0 mgOralApotex Corporation2006-07-05Not applicableCanada
International/Other Brands
Risperdal / Risperidal M-Tab (Janssen) / Risperin (Gador) / Rispolept / Rispolin / Sequinan
Categories
UNII
L6UH7ZF8HC
CAS number
106266-06-2
Weight
Average: 410.4845
Monoisotopic: 410.211804333
Chemical Formula
C23H27FN4O2
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

Pharmacology

Indication

Risperidone belongs to the class of medications known as ​second generation atypical antipsychotics [2, 3, 12]. It is widely used in the treatment of schizophrenia and mood disorders, including bipolar disorder and depression with pyschosis [3, 4, 11, 12].

Associated Conditions
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, 11].

Risperidone has high affinity binding to serotonergic 5-HT2A receptors versus dopaminergic D2 receptors in the brain [2, 3]. Risperidone binds the D2 receptors with lower affinity than the traditional, first generation antipsychotic drugs, which bind with very high affinity. A reduction in extrapyramidal symptoms in Risperidone use is attributed to its moderate affinity for dopaminergic D2 receptors [7, 11, 5].

Mechanism of action

Though its mechanism of action is not fully understood at this time, 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 be caused by 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. 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 [11, 12]. 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) receptors, and histamine (H1) receptors [11]. 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 [11, 12].

TargetActionsOrganism
A5-hydroxytryptamine receptor 2A
antagonist
Human
AD(2) dopamine receptor
antagonist
Human
UD(3) dopamine receptor
antagonist
Human
UD(4) dopamine receptor
antagonist
Human
UAlpha-1A adrenergic receptor
antagonist
Human
UAlpha-1B adrenergic receptor
antagonist
Human
U5-hydroxytryptamine receptor 1D
antagonist
Human
UHistamine H1 receptor
antagonist
Human
UAlpha-2A adrenergic receptor
antagonist
Human
UAlpha-2B adrenergic receptor
antagonist
agonist
Human
UAlpha-2C adrenergic receptor
agonist
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
U5-hydroxytryptamine receptor 1A
antagonist
Human
UD(1A) dopamine receptor
antagonist
Human
U5-hydroxytryptamine receptor 7Not AvailableHuman
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.

Volume of distribution

1 to 2 L/kg

Protein binding

Risperidone, ~88% bound in human plasma; 9-hydroxyrisperidone, ~77% bound in human plasma [9].

Metabolism

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone, 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 [9]. Risperidone also undergoes N-dealkylation to a lesser extent [7, 9].

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, 13].

Half life

3 hours in extensive metabolizers [9] Up to 20 hours in poor metabolizers [9]

Clearance

Risperidone is cleared by the kidneys. Clearance is decreased in the elderly and those with renal creatinine clearance of 15 mL/min to 59 mL/min, which decreases clearance by 60% [13].

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].

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Risperidone.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Risperidone.
16-BromoepiandrosteroneThe metabolism of 16-Bromoepiandrosterone can be decreased when combined with Risperidone.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Risperidone.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Risperidone is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of serotonin syndrome can be increased when Risperidone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of serotonin syndrome can be increased when Risperidone is combined with 3,4-Methylenedioxyamphetamine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Risperidone.
3,5-DinitrocatecholThe therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Risperidone.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of serotonin syndrome can be increased when Risperidone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Food Interactions
Not Available

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. [PubMed:16004936]
  2. Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. doi: 10.1592/phco.29.1.64. [PubMed:19113797]
  3. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  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. [PubMed:19562274]
  5. Szarfman A, Tonning JM, Levine JG, Doraiswamy PM: Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy. 2006 Jun;26(6):748-58. [PubMed:16716128]
  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. [PubMed:18537577]
  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. [PubMed:14610521]
  8. Acri AA, Henretig FM: Effects of risperidone in overdose. Am J Emerg Med. 1998 Sep;16(5):498-501. [PubMed:9725965]
  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. [PubMed:7531854]
  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. [PubMed:7542051]
  11. Atypicality of antipsychotics: A concept re-examined and re-defined [Link]
  12. Risperidone in the Treatment of Schizophrenia [Link]
  13. Pharmacokinetics of Risperidone: Clinical Summary [Link]
External Links
Human Metabolome Database
HMDB0005020
KEGG Drug
D00426
PubChem Compound
5073
PubChem Substance
46505850
ChemSpider
4895
BindingDB
50001885
ChEBI
8871
ChEMBL
CHEMBL85
Therapeutic Targets Database
DAP000003
PharmGKB
PA451257
IUPHAR
96
Guide to Pharmacology
GtP Drug Page
HET
8NU
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Risperidone
ATC Codes
N05AX08 — Risperidone
AHFS Codes
  • 28:16.08.04 — Atypical Antipsychotics
FDA label
Download (2.54 MB)
MSDS
Download (25.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers5
1CompletedBasic ScienceBipolar Disorder (BD) / Depressive Disorders / Psychotic Disorder NOS / Schizophrenic Disorders1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedOtherAntipsychotics / Immunoassay1
1CompletedTreatmentBipolar Disorder (BD)1
1CompletedTreatmentChild Development Disorders, Pervasive1
1CompletedTreatmentDyskinesia, Drug-Induced1
1CompletedTreatmentFasting1
1CompletedTreatmentFed1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
1CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders4
1CompletedTreatmentSchizophrenic Disorders7
1TerminatedDiagnosticSchizophrenic Disorders1
1Unknown StatusNot AvailableHealthy Volunteers / Pharmacogenetics1
1Unknown StatusTreatmentCocaine-Related Disorders1
1, 2CompletedBasic ScienceSchizotypal Personality Disorder1
1, 2CompletedOtherCognitive Changes / Memory Losses / Postmenopausal Syndrome1
1, 2CompletedTreatmentAsthma Bronchial1
1, 2CompletedTreatmentAsthma Bronchial / Bronchospasm / Difficulty Breathing / Wheezing1
1, 2CompletedTreatmentChild Development Disorders, Pervasive1
1, 2CompletedTreatmentPost-Traumatic Stress Disorder (PTSD)1
1, 2CompletedTreatmentSubjects Had Unipolar, Non-psychotic Major Depression1
1, 2RecruitingBasic ScienceSchizophrenic Disorders1
1, 2TerminatedTreatmentAsthma Bronchial2
1, 2WithdrawnTreatmentSchizophrenic Disorders1
2CompletedPreventionHealthy Volunteers1
2CompletedTreatmentAlcoholism / Dual Diagnosis / Schizophrenic Disorders1
2CompletedTreatmentAttention Deficit Disorder With Hyperactivity1
2CompletedTreatmentAutism, Early Infantile1
2CompletedTreatmentChronic Schizophrenia / Schizoaffective Disorders1
2CompletedTreatmentCocaine-Related Disorders3
2CompletedTreatmentCocaine-Related Disorders / Substance-Related Disorders2
2CompletedTreatmentDementias1
2CompletedTreatmentDependence, Cocaine1
2CompletedTreatmentEfficacy / Iloperidone / Schizophrenic Disorders1
2CompletedTreatmentGilles de la Tourette's Syndrome1
2CompletedTreatmentPost-Traumatic / Stress Disorders1
2CompletedTreatmentSchizophrenia, Acute Episode1
2CompletedTreatmentSchizophrenic Disorders12
2RecruitingTreatmentMenopausal Hot Flushes / Premenstrual Syndrome1
2RecruitingTreatmentSchizophrenic Disorders1
2RecruitingTreatmentTreatment-resistant Schizophrenia1
2TerminatedTreatmentCocaine-Related Disorders2
2TerminatedTreatmentMajor Depressive Disorder With Panic Attacks / Panic Disorders1
2TerminatedTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
2Unknown StatusTreatmentSchizophrenic Disorders1
2WithdrawnTreatmentSchizophrenic Disorders1
2, 3CompletedTreatmentAutism, Early Infantile1
2, 3CompletedTreatmentPost-Traumatic Stress Disorder (PTSD)1
2, 3CompletedTreatmentSchizophrenic Disorders3
2, 3TerminatedTreatmentCognitive Effect on Schizophrenic Patients / Schizophrenic Disorders1
2, 3TerminatedTreatmentSchizophrenic Disorders1
2, 3WithdrawnTreatmentDiabetes Mellitus (DM)1
3Active Not RecruitingTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
3Active Not RecruitingTreatmentSchizophrenic Disorders1
3CompletedNot AvailableBipolar Disorder (BD)1
3CompletedDiagnosticAdjustment Disorder / Attention Deficit Disorder With Hyperactivity (ADHD) / Bipolar Disorder (BD) / Impulse Control Disorders / Intermittent Explosive Disorder / Oppositional Defiant Disorder / Pervasive Developmental Disorder NOS1
3CompletedPreventionBipolar Disorder (BD)1
3CompletedPreventionSchizophrenic Disorders1
3CompletedTreatmentAlzheimer's Disease (AD) / Dementia, Vascular / Dementias3
3CompletedTreatmentAlzheimer's Disease (AD) / Dementias / Psychiatric Disorder NOS1
3CompletedTreatmentAnxiety Disorders1
3CompletedTreatmentAnxiety Disorders / Bipolar Disorder (BD)1
3CompletedTreatmentAsperger's Syndrome / Autistic Disorder / DCild Development Disorders, Pervasive / Developmental Disability / Rett's Syndrome1
3CompletedTreatmentAsthma Bronchial2
3CompletedTreatmentAttention Deficit and Disruptive Behavior Disorders1
3CompletedTreatmentAutistic Disorder1
3CompletedTreatmentAutistic Disorder in Children and Adolescents1
3CompletedTreatmentBipolar Disorder (BD)6
3CompletedTreatmentBipolar Disorder (BD) / Manic Disorder3
3CompletedTreatmentAcute Manic episode / Bipolar Disorder (BD)2
3CompletedTreatmentBipolar I Disorder1
3CompletedTreatmentCessation, Smoking / Schizophrenic Disorders1
3CompletedTreatmentChild Behavior Disorders / Learning Disorders1
3CompletedTreatmentDepression1
3CompletedTreatmentDepression / Depressive Disorders / Major Depressive Disorder (MDD)1
3CompletedTreatmentDepression / Schizophrenic Disorders1
3CompletedTreatmentDevelopmental Delay Disorders / Mental Retardation1
3CompletedTreatmentMajor Depressive Disorder (MDD)1
3CompletedTreatmentMental Health / Psychiatric Disorder NOS / Psychotic Disorder NOS / Schizophrenic Disorders1
3CompletedTreatmentOppositional Defiant Disorder3
3CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders8
3CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders5
3CompletedTreatmentSchizophrenia and Schizoaffective Disorder1
3CompletedTreatmentSchizophrenic Disorders18
3RecruitingTreatmentAnxiety States1
3RecruitingTreatmentSchizophrenic Disorders2
3TerminatedTreatmentAlzheimer's Disease (AD) / Dementias1
3TerminatedTreatmentAnxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders1
3TerminatedTreatmentBipolar I Disorder / Metabolic Syndromes / Schizoaffective Disorders / Schizophrenic Disorders1
3TerminatedTreatmentMajor Depression With Psychotic Features1
3TerminatedTreatmentSchizophrenic Disorders3
3Unknown StatusNot AvailableSchizoaffective Disorders1
3Unknown StatusTreatmentMajor Depressive Disorder (MDD)1
3Unknown StatusTreatmentPsychosis Nos/Other1
3Unknown StatusTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
3WithdrawnTreatmentSchizophrenic Disorders1
4Active Not RecruitingTreatmentSchizoaffective Disorders / Schizophrenia and Disorders With Psychotic Features / Schizophrenic Disorders1
4Active Not RecruitingTreatmentSchizophrenic Disorders1
4CompletedNot AvailableAntipsychotic Agents / Physiological Effects of Drugs / Psychiatric Disorder NOS / Psychotropic Drugs / Schizophrenic Disorders / Therapeutic Uses / Tranquilizing Agents1
4CompletedNot AvailableSchizoaffective Disorders / Schizophrenic Disorders1
4CompletedNot AvailableSchizophrenic Disorders2
4CompletedBasic ScienceHealthy Volunteers / Schizophrenic Disorders1
4CompletedPreventionPost-Traumatic Stress Disorder (PTSD)1
4CompletedPreventionSchizophrenic Disorders2
4CompletedSupportive CareAutistic Disorder1
4CompletedTreatmentAcute Agitation1
4CompletedTreatmentAcute Agitation / Aggressive Behavior / Alzheimer's Disease (AD) / Psychotic Disorder NOS1
4CompletedTreatmentAcute Agitation / Alzheimer's Disease (AD) / Psychosis1
4CompletedTreatmentAggressive Behavior1
4CompletedTreatmentAggressive Behavior / Attention Deficit Disorder With Hyperactivity (ADHD) / Attention Deficit-Hyperactivity / Bipolar Disorder (BD) / Oppositional Defiant Disorder / PDD / Pervasive Development Disorders1
4CompletedTreatmentAlcohol Abuse / Psychotic Disorder NOS / Schizophrenic Disorders / Substance Abuse1
4CompletedTreatmentAlzheimer's Disease (AD) / Dementia, Alzheimer Type / Dementias / Senile Dementia, Alzheimer Type1
4CompletedTreatmentAlzheimer's Disease (AD) / Dementias / Schizophrenic Disorders1
4CompletedTreatmentAnorexia Nervosa (AN)1
4CompletedTreatmentAnxiety Disorders / Moods Disorders / Schizophrenic Disorders1
4CompletedTreatmentAsperger's Disorder1
4CompletedTreatmentAutism, Early Infantile / Autistic Disorder1
4CompletedTreatmentAutistic Disorder / Bipolar Disorder (BD) / Conduct and Other Disruptive Behavior Disorders / Schizophrenic Disorders1
4CompletedTreatmentBipolar Disorder (BD)6
4CompletedTreatmentBipolar Disorder (BD) / Generalized Anxiety Disorder (GAD) / Panic Disorders1
4CompletedTreatmentBipolar Disorder (BD) / Mania1
4CompletedTreatmentBipolar Spectrum Disorder1
4CompletedTreatmentBorderline Personality Disorder (BPD)1
4CompletedTreatmentCannabis Abuse / Cannabis Dependence / Dual Diagnosis / Schizophrenic Disorders1
4CompletedTreatmentDementias2
4CompletedTreatmentDepression, Bipolar / Substance Abuse1
4CompletedTreatmentDiabetes Mellitus (DM) / Hyperglycemias / Metabolic Syndromes / Schizophrenic Disorders1
4CompletedTreatmentDiabetes Mellitus (DM) / Schizophrenic Disorders1
4CompletedTreatmentEmergency Treatment / Psychotic Disorder NOS / Schizophrenic Disorders1
4CompletedTreatmentExtrapyramidal Syndrome / Schizophrenic Disorders1
4CompletedTreatmentHyperglycemias / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
4CompletedTreatmentMethamphetamine Dependence1
4CompletedTreatmentNegative Symptoms / Schizophrenic Disorders1
4CompletedTreatmentNeuroleptic-Induced Tardive Dyskinesia1
4CompletedTreatmentPsychosis, Schizophrenia1
4CompletedTreatmentPsychosis / Schizophrenic Disorders1
4CompletedTreatmentPsychotic Disorder NOS2
4CompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders2
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders8
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder2
4CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Substance Abuse / Substance Dependence1
4CompletedTreatmentSchizophrenia, Schizoaffective Disorder1
4CompletedTreatmentSchizophrenic Disorders27
4CompletedTreatmentSchizophrenic Disorders / Type 2 Diabetes Mellitus1
4Enrolling by InvitationTreatmentPsychosis / Psychotic Disorder NOS / Schizophrenic Disorders1
4Enrolling by InvitationTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
4Not Yet RecruitingTreatmentDiagnosis and Treatment of Depression1
4Not Yet RecruitingTreatmentSchizophrenic Disorders2
4RecruitingBasic ScienceSchizophrenia Spectrum and Other Psychotic Disorders1
4RecruitingDiagnosticFirst Episode Psychosis / Schizoaffective Disorders / Schizophrenic Disorders1
4RecruitingDiagnosticFragile X Syndrome (FXS) / Velocardiofacial Syndrome / Williams Syndrome1
4RecruitingTreatmentBipolar Disorder (BD)1
4RecruitingTreatmentSchizophrenia (Recent-onset)1
4RecruitingTreatmentSchizophrenic Disorders1
4TerminatedNot AvailableHigh Risk MC4R Genotype / Low Risk MC4R Genotype / One Week or Less Antipsychotic Lifetime Exposure1
4TerminatedNot AvailableSchizophrenic Disorders1
4TerminatedBasic ScienceSchizophrenic Disorders1
4TerminatedPreventionSchizophrenic Disorders1
4TerminatedTreatmentAcute Agitation / Delirium1
4TerminatedTreatmentMajor Depressive Disorder (MDD)1
4TerminatedTreatmentMethamphetamine Dependence1
4TerminatedTreatmentSchizophrenic Disorders7
4Unknown StatusDiagnosticSchizophrenic Disorders1
4Unknown StatusTreatmentAttention Deficit Disorder With Hyperactivity1
4Unknown StatusTreatmentAttention Deficit/Hyperactivity Disorder / Oppositional Defiant Disorder1
4Unknown StatusTreatmentDelirium1
4Unknown StatusTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
4Unknown StatusTreatmentSchizophrenia, First-Episode1
4Unknown StatusTreatmentSchizophrenic Disorders4
4WithdrawnPreventionSchizophrenic Disorders1
4WithdrawnTreatmentTreatment Resistant Depression (TRD)1
Not AvailableActive Not RecruitingTreatmentSchizophrenia Relapse1
Not AvailableCompletedNot AvailableBipolar Disorder (BD)1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Metabolic Syndromes / Psychotic Disorder NOS1
Not AvailableCompletedNot AvailableBipolar Disorder (BD) / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableHealthy Volunteers2
Not AvailableCompletedNot AvailableNormal Volunteers1
Not AvailableCompletedNot AvailablePatients Already Taking Risperidone for Clinical Indications1
Not AvailableCompletedNot AvailableSchizophrenic Disorders1
Not AvailableCompletedBasic ScienceImaging of the Brain and Antipsychotics / Neuronal Network Changes1
Not AvailableCompletedBasic ScienceSchizophrenic Disorders1
Not AvailableCompletedDiagnosticProdromal Schizophrenia / Psychotic Disorder NOS1
Not AvailableCompletedDiagnosticSchizophrenic Disorders1
Not AvailableCompletedHealth Services ResearchPsychomotor Agitation / Sleep Disorders, Circadian Rhythm / Sleeplessness1
Not AvailableCompletedScreeningBMI >30 kg/m2 / Diabetes Mellitus (DM) / Metabolic Syndromes1
Not AvailableCompletedTreatmentAlzheimer's Disease (AD)1
Not AvailableCompletedTreatmentAlzheimer's Disease (AD) / Dementias1
Not AvailableCompletedTreatmentAutistic Disorder1
Not AvailableCompletedTreatmentBipolar Disorder (BD)1
Not AvailableCompletedTreatmentBipolar Disorder (BD) / Bipolar I / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableCompletedTreatmentBipolar Disorder (BD) / Dependence, Cocaine / Methamphetamine Dependence1
Not AvailableCompletedTreatmentCannabis-Related Disorder / Psychotic Disorder NOS / Schizophrenic Disorders / Substance-Related Disorders1
Not AvailableCompletedTreatmentChild Development Disorders, Pervasive1
Not AvailableCompletedTreatmentDelusional Disorder / Psychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableCompletedTreatmentMajor Depression With Panic Attacks / Panic Disorders1
Not AvailableCompletedTreatmentObsessive-Compulsive Disorder (OCD)1
Not AvailableCompletedTreatmentPsychotic Disorder NOS / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorders1
Not AvailableCompletedTreatmentPsychotic Disorder NOS / Schizophrenic Disorders1
Not AvailableCompletedTreatmentSchizophrenic Disorders3
Not AvailableCompletedTreatmentSchizophrenic Disorders / Type 2 Diabetes Mellitus1
Not AvailableCompletedTreatmentSchizotypal Personality Disorder1
Not AvailableEnrolling by InvitationNot AvailableBipolar Disorder (BD)1
Not AvailableNot Yet RecruitingNot AvailableWeight, Body1
Not AvailableRecruitingNot AvailableAcute Bacterial Exacerbation of Chronic Bronchitis (ABECB) / Acute Bacterial Sinusitis (ABS) / Acute Decompensated Heart Failure (ADHF) / Acute Pyelonephritis / Adenovirus / Adjunct to general anesthesia therapy / Adrenal Insufficiency / Airway Swelling / Anaesthesia therapy / Anxiolysis / Arterial Hypotension / Autism, Early Infantile / Autistic Disorder / Bartonellosis / Benzodiazepine Withdrawal / Benzodiazepines / Bipolar Disorder (BD) / Bloodstream Infections / Bone and Joint Infections / Brain Swelling / Bronchospasm / Brucellosis / Cardiac Arrest / Central Nervous System Infections / Cholera / Chronic Bacterial Prostatitis / Community Acquired Pneumonia (CAP) / Complicated Urinary Tract Infections / Convulsions / Cyanide Poisoning / Cytomegalovirus Retinitis / Drug hypersensitivity reaction / Early-onset Schizophrenia Spectrum Disorders / Edema / Epilepsies / Feeling Anxious / Flu caused by Influenza / Gastroparesis / Gynaecological infection / Headaches / Herpes Simplex Virus / High Blood Cholesterol Level / High Blood Pressure (Hypertension) / Hospital-acquired bacterial pneumonia / Hyperlipidemias / Infantile Hemangiomas / Infection NOS / Inflammatory Conditions / Inflammatory Reaction / Influenza Treatment or Prophylaxis / Inhalational Anthrax (Post-Exposure) / Intra-Abdominal Infections / Life-threatening Fungal Infections / Lower Respiratory Tract Infection (LRTI) / Meningitis, Bacterial / Migraines / Muscle Spasms / Nausea / Opioid Addiction / Pain / Plague / Pneumonia / Prophylaxis / Psittacosis / Q Fever / Reflux / Relapsing Fever / Rocky Mountain Spotted Fever / Schizophrenic Disorders / Sedation therapy / Seizures / Sepsis / Skeletal Muscle Spasms / Skin and Subcutaneous Tissue Bacterial Infections / Skin Structures and Soft Tissue Infections / Stable Angina (SA) / Thromboprophylaxis / Thrombosis / Trachoma / Treatment-resistant Schizophrenia / Tularemia / Typhus Fever / Uncomplicated Skin and Skin Structure Infections / Uncomplicated Urinary Tract Infections / Urinary Tract Infections (UTIs) / Vomiting / Withdrawal1
Not AvailableRecruitingNot AvailableAdverse Drug Effect of Antipsychotics and Neuroleptics / Efficacy / Individualed Opitmal Therapy / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailableBipolar Disorder (BD) / First-Episode Psychosis1
Not AvailableRecruitingNot AvailableMental Illnesses / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailableMicrognathia / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailablePsychosis / Schizoaffective Disorders / Schizophrenic Disorders1
Not AvailableRecruitingNot AvailablePsychotic Disorder NOS1
Not AvailableRecruitingNot AvailableSchizophrenic Disorders1
Not AvailableRecruitingTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableRecruitingTreatmentSchizophrenic Disorders1
Not AvailableSuspendedTreatmentPsychotic Disorder Not Otherwise Specified / Schizoaffective Disorders / Schizophrenic Disorders / Severe Bipolar Disorder With Psychotic Features1
Not AvailableTerminatedNot AvailableSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableTerminatedNot AvailableSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorders1
Not AvailableTerminatedBasic ScienceSchizophrenic Disorders1
Not AvailableTerminatedOtherBipolar Disorder (BD)1
Not AvailableTerminatedTreatmentAggressive Behavior / Psychosis1
Not AvailableUnknown StatusNot AvailableSchizophrenic Disorders1
Not AvailableUnknown StatusPreventionPsychotic Disorder NOS1
Not AvailableUnknown StatusTreatmentBorderlone Personality Disorder1
Not AvailableUnknown StatusTreatmentCannabis Dependence / Psychostimulant Dependence1
Not AvailableUnknown StatusTreatmentSchizophrenic Disorders2
Not AvailableUnknown StatusTreatmentSevere Mood Dysregulation1
Not AvailableUnknown StatusTreatmentTreatment Resistant Depression (TRD)1
Not AvailableWithdrawnTreatmentDepression / Impulsivity / Suicidal Ideation Active1
Not AvailableWithdrawnTreatmentPsychosis Not Otherwise Specified (NOS) / Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform1

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
Tablet, orally disintegratingOral0.5 mg
TabletOral1.0 mg
TabletOral2.0 mg
TabletOral3.0 mg
TabletOral4.0 mg
Tablet, orally disintegratingOral1 mg
Tablet, orally disintegratingOral2 mg
Tablet, orally disintegratingOral3 mg
Tablet, orally disintegratingOral4 mg
TabletOral0.25 mg
TabletOral0.5 mg
TabletOral1 mg
TabletOral2 mg
TabletOral3 mg
TabletOral4 mg
TabletOral5 mg
Injection, powder, for suspension, extended release; kitIntramuscular12.5 mg
Injection, powder, for suspension, extended release; kitIntramuscular25 mg
Injection, powder, for suspension, extended release; kitIntramuscular37.5 mg
Injection, powder, for suspension, extended release; kitIntramuscular50 mg
Kit12.5 mg/2mL
Kit25 mg/2mL
Kit37.5 mg/2mL
Kit50 mg/2mL
SolutionOral1 mg
SolutionOral1 mg/1mL
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
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)
US6110921No1993-11-192013-11-19Us
CA2406536No2009-12-222021-04-19Canada
CA2194564No1998-01-272015-07-04Canada
US6667061Yes2000-11-252020-11-25Us
US5792477Yes1997-11-022017-11-02Us
US5916598Yes1997-11-022017-11-02Us
US6379703Yes1999-06-302019-06-30Us
US6403114Yes1997-11-022017-11-02Us
US6596316Yes1999-06-302019-06-30Us
US6194006Yes1999-06-302019-06-30Us
US6224905Yes1997-12-102017-12-10Us
US9186413No2008-02-132028-02-13Us
US10010612No2008-02-132028-02-13Us
US9180197No2008-02-132028-02-13Us
US9597402No2006-09-262026-09-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)170PhysProp
boiling point (°C)442[FDA]
water solubility2.33 mg/mL[FDA]
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
Polarizability45.27 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-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
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

Taxonomy

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
Pyridopyrimidine / Benzisoxazole / Aralkylamine / Pyrimidone / Aryl fluoride / Aryl halide / Piperidine / Pyridine / Benzenoid / Pyrimidine
show 19 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, pyridopyrimidine, 1,2-benzoxazoles, heteroarylpiperidine (CHEBI:8871)

Targets

Kind
Protein
Organism
Human
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. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  2. Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [PubMed:15992090]
  3. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  4. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. [PubMed:17316700]
Details
2. D(2) dopamine receptor
Kind
Protein
Organism
Human
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. Catafau AM, Corripio I, Perez V, Martin JC, Schotte A, Carrio I, Alvarez E: Dopamine D2 receptor occupancy by risperidone: implications for the timing and magnitude of clinical response. Psychiatry Res. 2006 Dec 1;148(2-3):175-83. Epub 2006 Oct 23. [PubMed:17059881]
  2. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  3. Lane HY, Lee CC, Chang YC, Lu CT, Huang CH, Chang WH: Effects of dopamine D2 receptor Ser311Cys polymorphism and clinical factors on risperidone efficacy for positive and negative symptoms and social function. Int J Neuropsychopharmacol. 2004 Dec;7(4):461-70. Epub 2004 May 12. [PubMed:15140279]
  4. Naiker DV, Catts SV, Catts VS, Bedi KS, Bryan-Lluka LJ: Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. Epub 2006 May 11. [PubMed:16730699]
  5. Remington G, Mamo D, Labelle A, Reiss J, Shammi C, Mannaert E, Mann S, Kapur S: A PET study evaluating dopamine D2 receptor occupancy for long-acting injectable risperidone. Am J Psychiatry. 2006 Mar;163(3):396-401. [PubMed:16513859]
  6. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Details
3. D(3) dopamine receptor
Kind
Protein
Organism
Human
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 inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [PubMed:7520908]
  2. Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [PubMed:7531353]
Details
4. D(4) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [PubMed:7520908]
  2. Megens AA, Awouters FH, Schotte A, Meert TF, Dugovic C, Niemegeers CJ, Leysen JE: Survey on the pharmacodynamics of the new antipsychotic risperidone. Psychopharmacology (Berl). 1994 Feb;114(1):9-23. [PubMed:7531353]
Kind
Protein
Organism
Human
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. Eltze M: In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1996 Jan 4;295(1):69-73. [PubMed:8925876]
  2. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  3. Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [PubMed:15992090]
  4. Nourian Z, Mow T, Muftic D, Burek S, Pedersen ML, Matz J, Mulvany MJ: Orthostatic hypotensive effect of antipsychotic drugs in Wistar rats by in vivo and in vitro studies of alpha1-adrenoceptor function. Psychopharmacology (Berl). 2008 Jul;199(1):15-27. doi: 10.1007/s00213-007-1064-9. Epub 2008 Jun 10. [PubMed:18542932]
  5. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  6. Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. [PubMed:7691623]
Kind
Protein
Organism
Human
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Eltze M: In functional experiments, risperidone is selective, not for the B, but for the A subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1996 Jan 4;295(1):69-73. [PubMed:8925876]
  3. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  4. Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [PubMed:15992090]
  5. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  6. Sleight AJ, Koek W, Bigg DC: Binding of antipsychotic drugs at alpha 1A- and alpha 1B-adrenoceptors: risperidone is selective for the alpha 1B-adrenoceptors. Eur J Pharmacol. 1993 Jul 20;238(2-3):407-10. [PubMed:7691623]
Kind
Protein
Organism
Human
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. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Details
8. Histamine H1 receptor
Kind
Protein
Organism
Human
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. Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [PubMed:15992090]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  3. Schreiber S, Backer MM, Weizman R, Pick CG: Augmentation of opioid induced antinociception by the atypical antipsychotic drug risperidone in mice. Neurosci Lett. 1997 May 30;228(1):25-8. [PubMed:9197279]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Thioesterase 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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
Agonist
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. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
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. Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. [PubMed:15907153]
  2. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Kind
Protein
Organism
Human
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. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
  2. Canton H, Verriele L, Millan MJ: Competitive antagonism of serotonin (5-HT)2C and 5-HT2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics. Neurosci Lett. 1994 Nov 7;181(1-2):65-8. [PubMed:7898773]
Kind
Protein
Organism
Human
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. Richelson E, Souder T: Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [PubMed:11132243]
Details
14. D(1A) dopamine receptor
Kind
Protein
Organism
Human
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. Keks NA, Culhane C: Risperidone (Risperdal): clinical experience with a new antipsychosis drug. Expert Opin Investig Drugs. 1999 Apr;8(4):443-52. [PubMed:15992090]
  2. Leysen JE, Janssen PM, Megens AA, Schotte A: Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12. [PubMed:7520908]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Curator comments
Acts as an inactivating antagonist competing for the ligand binding site and producing lasting inactivation of the receptor.
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. Knight JA, Smith C, Toohey N, Klein MT, Teitler M: Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists. Mol Pharmacol. 2009 Feb;75(2):374-80. doi: 10.1124/mol.108.052084. Epub 2008 Nov 7. [PubMed:18996971]
  2. Toohey N, Klein MT, Knight J, Smith C, Teitler M: Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other "inactivating antagonists". Mol Pharmacol. 2009 Sep;76(3):552-9. doi: 10.1124/mol.109.056283. Epub 2009 Jun 9. [PubMed:19509219]
  3. Teitler M, Toohey N, Knight JA, Klein MT, Smith C: Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions. Psychopharmacology (Berl). 2010 Dec;212(4):687-97. doi: 10.1007/s00213-010-2001-x. Epub 2010 Sep 9. [PubMed:20827463]

Enzymes

Kind
Protein
Organism
Human
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. [PubMed:10048600]
  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. [PubMed:19910717]
  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. [PubMed:19902987]
  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. [PubMed:19817501]
  5. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  6. 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. [PubMed:11560868]
  7. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  8. Source [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. [PubMed:10048600]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]

Drug created on June 13, 2005 07:24 / Updated on September 21, 2018 20:42