Receptor occupancy and clinical response for antipsychotic agents

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Presentation transcript:

Receptor occupancy and clinical response for antipsychotic agents Receptor occupancy and clinical response for antipsychotic agents. Typically, in D2 receptor occupancy by the drug more than 60% provides antipsychotic effects, receptor occupancy greater than 80% causes EPSs. Atypical agents combine weak D2 receptor blockade with more potent 5HT2A antagonism/inverse agonism. Inverse agonism at 5HT2 receptor subtypes may contribute to the reduced EPS risk of olanzapine (A) and risperidone (B) and efficacy at lower D2 receptor occupancy (olanzapine, A). Aripiprazole is a partial D2 agonist that can achieve only 75% functional blockade (see Figure 16–2). Source: Pharmacotherapy of Psychosis and Mania, Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 13e Citation: Brunton LL, Hilal-Dandan R, Knollmann BC. Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 13e; 2017 Available at: http://accesspharmacy.mhmedical.com/DownloadImage.aspx?image=/data/books/2189/goodman13_ch16_f003.png&sec=170290202&BookID=2189&ChapterSecID=170290136&imagename= Accessed: October 21, 2017 Copyright © 2017 McGraw-Hill Education. All rights reserved

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