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首页> 外文期刊>CNS spectrums >D2 receptor occupancy following lurasidone treatment in patients with schizophrenia or schizoaffective disorder
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D2 receptor occupancy following lurasidone treatment in patients with schizophrenia or schizoaffective disorder

机译：精神分裂症或精神分裂症患者接受卢拉西酮治疗后的D2受体占有率

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Objective/Introduction Lurasidone is an atypical antipsychotic medication approved for the treatment of schizophrenia over a dose range of 40-160 mg/day. This study examined D2 receptor occupancy and its association with clinical improvement and side effects in patients with schizophrenia or schizoaffective disorder following repeated doses of 80, 120, or 160 mg/day of lurasidone. Methods Twenty-five patients with The Diagnostic and Statistical Manual of Mental Disorders, 4th ed. (DSM-IV) diagnoses of schizophrenia or schizoaffective disorder were washed out of their antipsychotic medications (5 half-lives) and randomly assigned to 80, 120, or 160 mg/day of lurasidone. Subjects were imaged with 18F-fallypride at baseline and at steady-state lurasidone treatment to determine D2 receptor occupancy. Results Blood lurasidone concentration (plus major metabolite), but not dose, significantly correlated with D2 receptor occupancy. D2 receptor occupancy in several subcortical structures is associated with positive but not negative symptom improvement or the presence of movement symptoms. Discussion Blood concentrations greater than 70 ng/mL may be required to achieve a 65% occupancy level in subcortical areas. Intersubject blood concentrations at fixed dose were highly variable and may account for the lack of dose correlations. Conclusions Positron emission tomography (PET) occupancy data suggest that greater than 65% occupancy can be achieved across the dose range of 80-160 mg/day and that some patients require higher doses to achieve antipsychotic efficacy; this finding supports prior randomized clinical trial results.
机译：目的/简介卢拉西酮是一种非典型的抗精神病药物，已被批准用于治疗40-160 mg / day的精神分裂症。这项研究检查了反复服用80、120或160 mg /天的卢拉西酮后，精神分裂症或精神分裂症患者的D2受体占有率及其与临床改善和副作用的关系。方法25例《精神疾病诊断和统计手册》第4版。 （DSM-IV）诊断为精神分裂症或精神分裂症的患者从抗精神病药物中清除（5个半衰期），并随机分配为80、120或160毫克/天的卢拉西酮。在基线和稳态卢拉西酮治疗下，对受试者进行18F-氟吡脲成像，以确定D2受体的占有率。结果血液中卢拉西酮的浓度（加上主要代谢物）而不是剂量与D2受体的占有率显着相关。 D2受体在几个皮层下结构中的占据与阳性症状改善或阴性症状改善或运动症状的出现无关。讨论在皮层下区域可能需要大于70 ng / mL的血液浓度才能达到65％的占用水平。固定剂量的受试者间血液浓度变化很大，可能解释了缺乏剂量相关性。结论正电子发射断层扫描（PET）占用率数据表明，在80-160 mg / day的剂量范围内可达到65％以上的占用率，并且某些患者需要更高的剂量才能获得抗精神病功效。这一发现支持了先前的随机临床试验结果。

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