The D2 receptor occupancy profile of loxapine determined using PET

Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology
S KapurS Houle

Abstract

Positron emission tomography (PET) studies of typical neuroleptics suggest that 60% to 80% of striatal D2 occupancy may be sufficient for optimal clinical treatment of psychosis. Therefore, striatal D2 occupancy may be used as an index to determine the optimal dose range. Toward this end, we determined the in vivo D2 profile of loxapine, using [11C]-raclopride and PET. Seven patients selected from a clinical population were scanned while taking steady-state oral loxapine from 10 to 100 mg/day. Their D2 receptor occupancy was estimated by comparing them to age-matched data from neuroleptic-naive patients. The D2 receptor occupancy ranged from 52% to 90%, and there was a very strong relationship between dose and D2 occupancy, suggesting that 15 to 30 mg/day of loxapine would produce, the putatively optimal, 60% to 80% striatal D2 blockade. This dose range is much lower than that used in most clinical settings and points to the potential efficacy of loxapine at lower doses.

Citations

Feb 19, 2013·Psychopharmacology·Takefumi SuzukiDavid Mamo
Aug 16, 2005·Current Psychiatry Reports·Thomas W Weickert, Terry E Goldberg
Apr 20, 2007·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·David MamoDavid McDonnell
Aug 21, 2013·Journal of Clinical Psychopharmacology·Irene M LakoKatja Taxis
Mar 3, 2015·Journal of Molecular Graphics & Modelling·Xinli DuanMing Lei
Jun 18, 2004·Thérapie·Nhan NguyenOlivier Blin
Jan 15, 2015·Journal of Psychopharmacology·Oliver HowesJames Stone

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