PMID: 7543969Jan 1, 1995Paper

The D2 dopamine receptor occupancy of risperidone and its relationship to extrapyramidal symptoms: a PET study

Life Sciences
S KapurS Houle

Abstract

Risperidone is a recently introduced neuroleptic distinguished by a decreased incidence of extrapyramidal side effects (EPS). The mechanism of its low EPS is unclear. Since it has been shown that EPS is related to the level of D2 receptor occupancy, we studied nine patients receiving 2-6 mg/day of risperidone using [11C]-raclopride PET scans in order to determine the in vivo D2 receptor binding characteristics of risperidone. The mean level of receptor occupancy was 66% at 2 mg; 73% at 4 mg; and 79% at 6 mg. Three patients, those with the highest receptor occupancies, exhibited mild EPS, though none required anitparkinsonian medications. Our results suggest that at doses of 4-6 mg the in vivo D2 receptor occupancy of risperidone is similar to that of typical neuroleptics and higher than that of clozapine. This would suggest that the EPS benefits of risperidone cannot be explained by a low D2 binding but may be related to its high 5-HT2 affinity. However, the emergence of EPS at higher levels of D2 receptor occupancy, in this study and in previous clinical trials, would suggest that risperidone's high 5-HT2 affinity provides only a relative protection from EPS. And once the D2 occupancy exceeds a certain threshold this 'relative...Continue Reading

References

May 1, 1989·The British Journal of Psychiatry : the Journal of Mental Science·T R Barnes
Apr 1, 1994·Archives of General Psychiatry·S R MarderR P Liberman

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Citations

Sep 2, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Marie-Bernadette AssiéAdrian Newman-Tancredi
Apr 20, 2010·Psychopharmacology·Brooke M RobertsStacy A Castner
Feb 19, 2013·Psychopharmacology·Takefumi SuzukiDavid Mamo
Aug 16, 2005·Current Psychiatry Reports·Thomas W Weickert, Terry E Goldberg
Dec 4, 2003·Progress in Neuro-psychopharmacology & Biological Psychiatry·Shitij Kapur, David Mamo
Nov 28, 2002·Progress in Neuro-psychopharmacology & Biological Psychiatry·Helen Rosengarten, David Quartermain
Dec 7, 2002·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Peter S Talbot, Marc Laruelle
Nov 11, 2009·Journal of the International Neuropsychological Society : JINS·Sophie RémillardHenri Cohen
May 15, 2004·Journal of Child and Adolescent Psychopharmacology·Harpreet S Duggal
Jan 19, 2011·Imaging in Medicine·Judy L ThompsonAnissa Abi-Dargham
Feb 25, 2006·Primary Care Companion to the Journal of Clinical Psychiatry·Andrew Farah
Sep 29, 2004·Psychopharmacology·Richard De La GarzaAri D Kalechstein
Oct 10, 2007·Harvard Review of Psychiatry·W Gordon Frankle
Jul 16, 2010·Journal of Clinical Psychopharmacology·Simon ZhornitskyStéphane Potvin
Jan 1, 2002·Expert Review of Neurotherapeutics·Gary Remington
Jan 10, 2014·Drug Development and Industrial Pharmacy·Wei GongXing-Guo Mei
Mar 17, 2012·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Ken NagataYasuo Terayama
Mar 20, 2010·Progress in Neuro-psychopharmacology & Biological Psychiatry·Ashish AggarwalR C Jiloha
Dec 8, 2009·Journal of Psychiatric Research·Ina GieglingAlessandro Serretti
Sep 1, 2009·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Lieuwe AppelShitij Kapur
Mar 25, 2009·Pharmacology & Therapeutics·Sarah Grimwood, Paul R Hartig
Apr 18, 2013·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Joel T DunnSuzanne J Reeves
Feb 19, 2008·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Giuseppe MainaFilippo Bogetto
Jan 1, 2011·Schizophrenia Research and Treatment·Patrick D McGorryTim Lambert
Jul 30, 2010·Movement Disorders : Official Journal of the Movement Disorder Society·Simon ZhornitskyStéphane Potvin
Dec 22, 2004·Progress in Neuro-psychopharmacology & Biological Psychiatry·Iluminada CorripioEnric Alvarez
Sep 2, 2006·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Trawat AttarbaschiJohannes Tauscher
Sep 20, 2005·Schizophrenia Research·Laurie McCormickNancy Andreasen

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