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Identification
NameRisperidone
Accession NumberDB00734  (APRD00187)
Typesmall molecule
Groupsapproved, investigational
Description

Risperidone, a benzisoxazole derivative, is an atypical antipsychotic drug with high affinity for 5-hydrotryptamine (5-HT) and dopamine D2 receptors. It is used primarily in the management of schizophrenia, inappropriate behavior in severe dementia and manic episodes associated with bipolar I disorder. Risperidone is effective for treating the positive and negative symptoms of schizophrenia owing to its affinity for its “loose” binding affinity for dopamine D2 receptors and additional 5-HT antagonism compared to first generation antipsychotics, which are strong, non-specific dopamine D2 receptor antagonists.

Structure
Thumb
Synonyms
SynonymLanguageCode
RisperdalNot AvailableNot Available
risperdoneNot AvailableNot Available
RisperidonaSpanishINN
RisperidonumLatinINN
RisperinNot AvailableNot Available
RispoleptNot AvailableNot Available
RispolinNot AvailableNot Available
SequinanNot AvailableNot Available
SaltsNot Available
Brand names
NameCompany
RisperdalJanssen
Risperdal ConstaJanssen
Risperdal M-TabJanssen
Risperidal M-TabJanssen
RisperinNot Available
RispoleptNot Available
RispolinNot Available
SequinanNot Available
Brand mixturesNot Available
Categories
CAS number106266-06-2
WeightAverage: 410.4845
Monoisotopic: 410.211804333
Chemical FormulaC23H27FN4O2
InChI KeyRAPZEAPATHNIPO-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
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassPyridopyrimidines
SubclassNot Available
Direct parentPyridopyrimidines
Alternative parentsBenzisoxazoles; Pyrimidones; Fluorobenzenes; Pyridines and Derivatives; Aryl Fluorides; Piperidines; Isoxazoles; Tertiary Amines; Polyamines; Organofluorides
Substituentspyrimidone; fluorobenzene; piperidine; aryl halide; benzene; aryl fluoride; pyrimidine; pyridine; isoxazole; azole; tertiary amine; polyamine; organohalogen; amine; organofluoride; organonitrogen compound
Classification descriptionThis compound belongs to the pyridopyrimidines. These are compounds containing a pyridopyrimidine, which consists of a pyridine fused to a pyrimidine.
Pharmacology
IndicationFor the treatment of schizophrenia in adults and in adolescents, ages 13 to 17, and for the short-term treatment of manic or mixed episodes of bipolar I disorder in children and adolescents ages 10 to 17. May also be used to manage symptoms of inappropriate behavior due to aggression and/or psychosis in patients with severe dementia.
PharmacodynamicsRisperidone is an atypical antipsychotic medication. It is most often used to treat delusional psychosis (including schizophrenia), but risperidone is also used to treat some forms of bipolar disorder and psychotic depression. It also has shown some success in treating symptoms of Asperger's Syndrome and autism. Risperidone is now the most commonly prescribed antipsychotic medication in the United States.
Mechanism of actionBlockade of dopaminergic D2 receptors in the limbic system alleviates positive symptoms of schizophrenia such as hallucinations, delusions, and erratic behavior and speech. Blockade of serotonergic 5-HT2 receptors in the mesocortical tract, causes an excess of dopamine and an increase in dopamine transmission, resulting in an increase in dopamine transmission and an elimination of core negative symptoms. Dopamine receptors in the nigrostriatal pathway are not affected by risperidone and extrapyramidal effects are avoided. Like other 5-HT2 antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors.
AbsorptionWell 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 bindingRisperidone, ~88% bound; 9-hydroxyrisperidone, ~77% bound.
Metabolism

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

SubstrateEnzymesProduct
Risperidone
9-hydroxyrisperidoneDetails
Route of eliminationRisperidone is extensively metabolized in the liver.In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives were prolonged compared to young healthy subjects.
Half life20-24 hours
ClearanceNot Available
ToxicitySymptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD50=82.1mg/kg (orally in mice).
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 1.0
Blood Brain Barrier + 0.9925
Caco-2 permeable - 0.5057
P-glycoprotein substrate Substrate 0.6163
P-glycoprotein inhibitor I Inhibitor 0.8564
P-glycoprotein inhibitor II Inhibitor 0.9361
Renal organic cation transporter Inhibitor 0.6491
CYP450 2C9 substrate Non-substrate 0.8235
CYP450 2D6 substrate Substrate 0.8918
CYP450 3A4 substrate Substrate 0.7407
CYP450 1A2 substrate Non-inhibitor 0.9046
CYP450 2C9 substrate Non-inhibitor 0.9071
CYP450 2D6 substrate Inhibitor 0.8931
CYP450 2C19 substrate Non-inhibitor 0.9026
CYP450 3A4 substrate Non-inhibitor 0.82
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8459
Ames test Non AMES toxic 0.5302
Carcinogenicity Non-carcinogens 0.8204
Biodegradation Not ready biodegradable 0.99
Rat acute toxicity 3.8290 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.65
hERG inhibition (predictor II) Inhibitor 0.8062
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
Dosage forms
FormRouteStrength
Injection, powder, for suspensionIntramuscular12.5 mg
Injection, powder, for suspensionIntramuscular25 mg
Injection, powder, for suspensionIntramuscular37.5 mg
Injection, powder, for suspensionIntramuscular50 mg
SolutionOral1 mg/ml
Tablet, film coatedOral0.25 mg
Tablet, film coatedOral0.5 mg
Tablet, film coatedOral1 mg
Tablet, film coatedOral2 mg
Tablet, film coatedOral3 mg
Tablet, film coatedOral4 mg
Tablet, orally disintegratingOral0.5 mg
Tablet, orally disintegratingOral1 mg
Tablet, orally disintegratingOral2 mg
Tablet, orally disintegratingOral3 mg
Tablet, orally disintegratingOral4 mg
Prices
Unit descriptionCostUnit
Risperdal consta 50 mg syr592.93USDsyringe
Risperdal consta 37.5 mg syr444.68USDsyringe
Risperdal consta 25 mg syr296.46USDsyringe
Risperdal 1 mg/ml Solution 30ml Bottle204.42USDbottle
Risperdal M-TAB 28 1 mg Dispersible Tablet Box196.08USDbox
Risperdal M-TAB 28 0.5 mg Dispersible Tablet Bottle167.82USDbottle
Risperidone 1 mg/ml Solution 30ml Bottle158.66USDbottle
Risperdal consta 12.5 mg syr148.22USDsyringe
Risperdal m-tab 4 mg odt18.55USDtablet
Risperdal 4 mg tablet16.47USDtablet
Risperidone m-tab 4 mg odt15.16USDtablet
Risperdal m-tab 3 mg odt13.81USDtablet
Risperdal 3 mg tablet11.45USDtablet
Risperidone m-tab 3 mg odt11.29USDtablet
Risperdal m-tab 2 mg odt10.95USDtablet
Risperidone 4 mg tablet9.0USDtablet
Risperidone m-tab 2 mg odt8.95USDtablet
Risperdal 2 mg tablet6.94USDtablet
Risperdal m-tab 1 mg odt6.73USDtablet
Risperidone 3 mg tablet6.63USDtablet
Risperdal 1 mg tablet6.12USDtablet
Risperdal m-tab 0.5 mg odt5.76USDtablet
Risperidone 2 mg tablet5.59USDtablet
Risperidone m-tab 1 mg odt5.5USDtablet
Risperidone M-TAB 0.5 mg Dispersible Tablet4.9USDdispersible tablet
Risperidone m-tab 0.5 mg odt4.71USDtablet
Risperdal M-Tab 4 mg Disintegrating Tablet4.6USDtablet
Risperdal 0.25 mg tablet4.56USDtablet
Risperidone 0.25 mg odt4.48USDtablet
Risperdal 0.5 mg tablet3.62USDtablet
Risperdal M-Tab 3 mg Disintegrating Tablet3.44USDtablet
Risperidone 1 mg tablet3.27USDtablet
Risperidone 0.5 mg tablet3.03USDtablet
Apo-Risperidone 4 mg Tablet2.53USDtablet
Co Risperidone 4 mg Tablet2.53USDtablet
Mylan-Risperidone 4 mg Tablet2.53USDtablet
Novo-Risperidone 4 mg Tablet2.53USDtablet
Phl-Risperidone 4 mg Tablet2.53USDtablet
Pms-Risperidone 4 mg Tablet2.53USDtablet
Ran-Risperidone 4 mg Tablet2.53USDtablet
Ratio-Risperidone 4 mg Tablet2.53USDtablet
Rbx-Risperidone 4 mg Tablet2.53USDtablet
Sandoz Risperidone 4 mg Tablet2.53USDtablet
Risperdal M-Tab 2 mg Disintegrating Tablet2.29USDtablet
Apo-Risperidone 3 mg Tablet1.9USDtablet
Co Risperidone 3 mg Tablet1.9USDtablet
Mylan-Risperidone 3 mg Tablet1.9USDtablet
Novo-Risperidone 3 mg Tablet1.9USDtablet
Phl-Risperidone 3 mg Tablet1.9USDtablet
Pms-Risperidone 3 mg Tablet1.9USDtablet
Ran-Risperidone 3 mg Tablet1.9USDtablet
Ratio-Risperidone 3 mg Tablet1.9USDtablet
Rbx-Risperidone 3 mg Tablet1.9USDtablet
Sandoz Risperidone 3 mg Tablet1.9USDtablet
Risperidone 0.25 mg tablet1.88USDtablet
Apo-Risperidone 2 mg Tablet1.26USDtablet
Co Risperidone 2 mg Tablet1.26USDtablet
Mylan-Risperidone 2 mg Tablet1.26USDtablet
Novo-Risperidone 2 mg Tablet1.26USDtablet
Phl-Risperidone 2 mg Tablet1.26USDtablet
Pms-Risperidone 2 mg Tablet1.26USDtablet
Ran-Risperidone 2 mg Tablet1.26USDtablet
Ratio-Risperidone 2 mg Tablet1.26USDtablet
Rbx-Risperidone 2 mg Tablet1.26USDtablet
Sandoz Risperidone 2 mg Tablet1.26USDtablet
Risperdal M-Tab 1 mg Disintegrating Tablet1.16USDtablet
Risperdal M-Tab 0.5 mg Disintegrating Tablet0.84USDtablet
Apo-Risperidone 1 mg Tablet0.63USDtablet
Co Risperidone 1 mg Tablet0.63USDtablet
Mylan-Risperidone 1 mg Tablet0.63USDtablet
Novo-Risperidone 1 mg Tablet0.63USDtablet
Phl-Risperidone 1 mg Tablet0.63USDtablet
Pms-Risperidone 1 mg Tablet0.63USDtablet
Ran-Risperidone 1 mg Tablet0.63USDtablet
Ratio-Risperidone 1 mg Tablet0.63USDtablet
Rbx-Risperidone 1 mg Tablet0.63USDtablet
Sandoz Risperidone 1 mg Tablet0.63USDtablet
Apo-Risperidone 0.5 mg Tablet0.46USDtablet
Co Risperidone 0.5 mg Tablet0.46USDtablet
Mylan-Risperidone 0.5 mg Tablet0.46USDtablet
Novo-Risperidone 0.5 mg Tablet0.46USDtablet
Phl-Risperidone 0.5 mg Tablet0.46USDtablet
Pms-Risperidone 0.5 mg Tablet0.46USDtablet
Ran-Risperidone 0.5 mg Tablet0.46USDtablet
Ratio-Risperidone 0.5 mg Tablet0.46USDtablet
Rbx-Risperidone 0.5 mg Tablet0.46USDtablet
Sandoz Risperidone 0.5 mg Tablet0.46USDtablet
Apo-Risperidone 0.25 mg Tablet0.27USDtablet
Co Risperidone 0.25 mg Tablet0.27USDtablet
Mylan-Risperidone 0.25 mg Tablet0.27USDtablet
Novo-Risperidone 0.25 mg Tablet0.27USDtablet
Phl-Risperidone 0.25 mg Tablet0.27USDtablet
Pms-Risperidone 0.25 mg Tablet0.27USDtablet
Ran-Risperidone 0.25 mg Tablet0.27USDtablet
Ratio-Risperidone 0.25 mg Tablet0.27USDtablet
Rbx-Risperidone 0.25 mg Tablet0.27USDtablet
Sandoz Risperidone 0.25 mg Tablet0.27USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States66670612000-11-252020-11-25
United States61109211993-11-192013-11-19
Canada24065362009-12-222021-04-19
Canada21945641998-01-272015-07-04
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point170 °CPhysProp
water solubility2.8mg/LNot Available
logP2.5Not Available
Predicted Properties
PropertyValueSource
water solubility1.71e-01 g/lALOGPS
logP3.27ALOGPS
logP2.63ChemAxon
logS-3.4ALOGPS
pKa (strongest basic)8.76ChemAxon
physiological charge1ChemAxon
hydrogen acceptor count4ChemAxon
hydrogen donor count0ChemAxon
polar surface area61.94ChemAxon
rotatable bond count4ChemAxon
refractivity114.55ChemAxon
polarizability45.27ChemAxon
number of rings5ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4804663
General Reference
  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
  2. Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. Pubmed
  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
  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. Epub 2009 Jun 26. Pubmed
  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
  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
  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
External Links
ResourceLink
KEGG DrugD00426
PubChem Compound5073
PubChem Substance46505850
ChemSpider4895
ChEBI8871
ChEMBLCHEMBL85
Therapeutic Targets DatabaseDAP000003
PharmGKBPA451257
IUPHAR96
Guide to Pharmacology96
Drug Product Database2247705
RxListhttp://www.rxlist.com/cgi/generic/risperid.htm
Drugs.comhttp://www.drugs.com/risperidone.html
PDRhealthhttp://www.pdrhealth.com/drugs/rx/rx-mono.aspx?contentFileName=ris1382.html&contentName=Risperdal&contentId=667
WikipediaRisperidone
ATC CodesN05AX08
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelshow(2.54 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
ArtemetherAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
CarbamazepineDecreases the effect of risperidone
DonepezilPossible antagonism of action
FluoxetineThe SSRI, fluoxetine, increases the effect and toxicity of risperidone.
GalantaminePossible antagonism of action
IndinavirIncreased risk of extrapyramidal symptoms
ItraconazoleIncreases the level of risperidone
LumefantrineAdditive QTc-prolongation may occur. Concomitant therapy should be avoided.
PaliperidonePaliperidone is the active metabolite of risperidone, 9-OH-risperidone. Concomitant therapy may increase the adverse effects of paliperidone due to additive paliperidone exposure. Consider alternate therapy.
ParoxetineThe SSRI, paroxetine, increases the effect and toxicity of risperidone.
TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Risperidone, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
TacrolimusAdditive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
TerbinafineTerbinafine may reduce the metabolism and clearance of Risperidone. Consider alternate therapy or monitor for therapeutic/adverse effects of Risperidone if Terbinafine is initiated, discontinued or dose changed.
TetrabenazineMay cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
ToremifeneAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
TrimethobenzamideTrimethobenzamide and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TrimipramineAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
TriprolidineTriprolidine and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
TrospiumTrospium and Risperidone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
VoriconazoleAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
ZiprasidoneAdditive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
ZuclopenthixolAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Zuclopenthixol acetateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Zuclopenthixol decanoateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Food InteractionsNot Available

Targets

1. 5-hydroxytryptamine receptor 2A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

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
  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
  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
  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

2. D(2) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

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
  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
  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
  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
  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
  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
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

3. D(3) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

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
  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

4. D(4) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(4) dopamine receptor P21917 Details

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
  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

5. Alpha-1A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

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
  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
  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
  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. Epub 2008 Jun 10. Pubmed
  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
  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

6. Alpha-1B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1B adrenergic receptor P35368 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  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
  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
  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
  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
  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

7. 5-hydroxytryptamine receptor 1D

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

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

8. Histamine H1 receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Histamine H1 receptor P35367 Details

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
  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
  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

9. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

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
  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

10. Alpha-2B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist agonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

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
  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

11. Alpha-2C adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

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
  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

12. 5-hydroxytryptamine receptor 2C

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2C P28335 Details

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
  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

13. 5-hydroxytryptamine receptor 1A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

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

14. D(1A) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details

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
  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

Enzymes

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

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
  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. Pubmed
  3. Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: part II. Clin Pharmacokinet. 2009;48(12):761-804. Pubmed
  4. Zhou SF: Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I. Clin Pharmacokinet. 2009;48(11):689-723. Pubmed
  5. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  6. Effexor XR Product Reference Source
  7. 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. Epub 2009 Nov 24. Pubmed
  8. 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

2. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  3. 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. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. Pubmed
  2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:25