Dopamine D2 receptor occupancy with risperidone or olanzapine during maintenance treatment of schizophrenia: A cross-sectional study

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• 作者：Yuya Mizuno^a ; Robert R. Bies^b ; ^c ; ^d ; Gary Remington^e ; ^g ; David C. Mamo^b ; ^f ; ^g ; Takefumi Suzuki^a ; ^h ; Bruce G. Pollock^b ; ^g ; Takashi Tsuboi^a ; Koichiro Watanabe^a ; Masaru Mimura^a ; Hiroyuki Uchida^a ; ^b ; ^{mcn41320@biglobe.ne.jp}
• 关键词：AIMS ; Abnormal Involuntary Movement Scale ; BAS ; Barnes Akathisia Rating Scale ; CATIE ; Clinical Antipsychotic Trials in Intervention Effectiveness ; EPS ; extrapyramidal symptoms ; PANSS ; Positive and Negative Syndrome Scale ; PET ; positron emission tomography
• 刊名：Progress in Neuro-Psychopharmacology and Biological Psychiatry
• 出版年：2012
• 期刊代码：222_02785846
• 类别：med
• 出版时间：27 April, 2012
• 卷：37
• 期：1
• 页码：182-187
• 文件大小：269 K

摘要

In treating schizophrenia, it has been established that 65-80%occupancy of dopamine D2 receptors optimizes therapeutic efficacy while minimizing risks of extrapyramidal symptoms. However, it is unclear as to whether it is necessary to keep D2 receptor occupancy within this therapeutic window to maintain response. In this study, daily peak and trough D2 receptor occupancy levels were estimated in clinically stable patients with schizophrenia (DSM-IV) who were receiving risperidone or olanzapine. Using two collected plasma samples, plasma antipsychotic concentrations at peak and trough were estimated with population pharmacokinetic techniques. Corresponding dopamine D2 receptor occupancy levels were then estimated, using a recently developed model. 35 subjects with stable schizophrenia completed the study (mean 卤 SD age, 48.8 卤 13.8 years; male [N = 14]; Asians [N = 23], Caucasians [N = 12]; risperidone [N = 20] at 3.2 卤 2.3 mg/day, and olanzapine [N = 15] at 9.2 卤 4.9 mg/day) between September and December 2010. 48.6%(N = 17) did not achieve a continuous blockade of 鈮?#xA0;65%. Moreover, 11.4%(N = 4) did not achieve the 65%threshold at estimated peak concentrations. In conclusion, approximately half the subjects with stable schizophrenia did not achieve estimated continuous blockade of D2 receptor occupancy of 鈮?#xA0;65%. The results suggest that sustained D2 receptor occupancy levels of 鈮?#xA0;65%may not always be necessary for the maintenance treatment of schizophrenia.