Molecular imaging of dopamine partial agonists in humans

• Verfasst von: Hart, Xenia Marlene [VerfasserIn]
• Verfasst von: Schmitz, Christian N. [VerfasserIn]
• Verfasst von: Gründer, Gerhard [VerfasserIn]
• Titel: Molecular imaging of dopamine partial agonists in humans
• Titelzusatz: implications for clinical practice
• Verf.angabe: Xenia M. Hart, Christian N. Schmitz and Gerhard Gründer
• E-Jahr: 2022
• Jahr: 06 April 2022
• Umfang: 11 S.
• Fussnoten: Gesehen am 18.03.2024
• Titel Quelle: Enthalten in: Frontiers in psychiatry
• Ort Quelle: Lausanne : Frontiers Research Foundation, 2007
• Jahr Quelle: 2022
• Band/Heft Quelle: 13(2022) vom: Apr., Artikel-ID 832209, Seite 1-11
• ISSN Quelle: 1664-0640
• DOI: doi:10.3389/fpsyt.2022.832209
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: aripiprazole
• Sach-SW: Brexpiprazole
• Sach-SW: Cariprazine
• Sach-SW: Dopamine partial agonists
• Sach-SW: molecular neuroimaging
• Sach-SW: positron emission tomography
• K10plus-PPN: 1883714249

Abstract

Positron emission tomography (PET) has been used since the late 1980s for the assessment of relationships between occupancy of D2/3 receptors by antipsychotic drugs in the human brain and the clinical effects and side effects of these compounds in patients. It is now well established for most D 2/3 antagonists, both of the first and the second generation, that the ideal occupancy of their target receptors is between approximately 65 and 80%. If the occupancy is below 65%, the probability of treatment response is reduced, if the occupancy is higher than 80%, the risk for extrapyramidal side-effects increases substantially. However, partial agonist antipsychotics behave different from these rules. It has been shown for all three available drugs of this class (aripiprazole, brexpiprazole, cariprazine) that, due to their special pharmacology, a very high target engagement (90%) not only is not harmful but represents a prerequisite for antipsychotic efficacy. The available PET studies for these drugs are reviewed in this work. It is demonstrated that optimal plasma levels for partial agonist antipsychotics can be derived from these studies, which can guide individual treatment in routine patient care.