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Statements

Subject Item
n2:DB00734
rdf:type
n3:Drug
n3: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.
n3:dosage
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n3:generalReferences
# 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":http://www.ncbi.nlm.nih.gov/pubmed/16004936 # Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19113797 # Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15907153 # 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":http://www.ncbi.nlm.nih.gov/pubmed/19562274 # Szarfman A, Tonning JM, Levine JG, Doraiswamy PM: Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy. 2006 Jun;26(6):748-58. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16716128 # 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":http://www.ncbi.nlm.nih.gov/pubmed/18537577 # 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":http://www.ncbi.nlm.nih.gov/pubmed/14610521
n3:group
approved investigational
n3:halfLife
20-24 hours
n3:indication
For 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.
n3:manufacturer
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owl:sameAs
n10:DB00734 n21:DB00734
dcterms:title
Risperidone
adms:identifier
n12:Risperidone n23:4895 n24:DB00734 n25:8871 n26:96 n27:D00426 n28:96 n29:5073 n31:46505850 n32:0904-5973-61 n33:PA451257
n3:mechanismOfAction
Blockade 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-HT<sub>2</sub> 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-HT<sub>2</sub> antagonists, risperidone also binds at alpha(1)-adrenergic receptors and, to a lesser extent, at histamine H1 and alpha(2)-adrenergic receptors.
n3:packager
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n3:patent
n8:2194564 n8:6110921 n8:2406536 n8:6667061
n3:routeOfElimination
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 were prolonged compared to young healthy subjects.
n3:synonym
risperdone Risperdal Sequinan Risperidona Risperidonum Rispolept Rispolin Risperin
n3:toxicity
Symptoms of overdose include drowsiness, sedation, tachycardia, hypotension, and extrapyramidal symptoms. LD<sub>50</sub>=82.1mg/kg (orally in mice).
n3:volumeOfDistribution
* 1 to 2 L/kg
n18:hasAHFSCode
n22:28-16-08-04
n3:proteinBinding
Risperidone, ~88% bound; 9-hydroxyrisperidone, ~77% bound.
n3:synthesisReference
"DrugSyn.org":http://www.drugsyn.org/Risperidone.htm
n6:hasConcept
n7:M0028338
foaf:page
n17:rx-mono.aspx?contentFileName=ris1382.html&contentName=Risperdal&contentId=667 n20:risperid.htm n30:risperidone.html
n3:IUPAC-Name
n13:271B522E-363D-11E5-9242-09173F13E4C5
n3:InChI
n13:271B5234-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n13:271B5233-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n13:271B5230-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n13:271B5231-363D-11E5-9242-09173F13E4C5
n3:SMILES
n13:271B5232-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n13:271B522C-363D-11E5-9242-09173F13E4C5 n13:271B5243-363D-11E5-9242-09173F13E4C5
n3:logP
n13:271B5245-363D-11E5-9242-09173F13E4C5 n13:271B522D-363D-11E5-9242-09173F13E4C5 n13:271B522A-363D-11E5-9242-09173F13E4C5
n3:logS
n13:271B522B-363D-11E5-9242-09173F13E4C5
n18:hasATCCode
n19:N05AX08
n3:H-Bond-Acceptor-Count
n13:271B523A-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n13:271B523B-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n13:271B5235-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n13:271B5236-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n13:271B5238-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n13:271B5237-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n13:271B5239-363D-11E5-9242-09173F13E4C5
n3: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.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
106266-06-2
n3:category
n3:containedIn
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n3:Bioavailability
n13:271B523F-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
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n3:MDDR-Like-Rule
n13:271B5242-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n13:271B5244-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
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n3:Physiological-Charge
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n3:Rule-of-Five
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n3:Traditional-IUPAC-Name
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n3:pKa--strongest-basic-
n13:271B523C-363D-11E5-9242-09173F13E4C5