AN OPEN LABEL TRIAL OF RACLOPRIDE IN ACUTE SCHIZOPHRENIA - CONFIRMATION OF D2-DOPAMINE RECEPTOR OCCUPANCY BY PET
AN OPEN LABEL TRIAL OF RACLOPRIDE IN ACUTE SCHIZOPHRENIA - CONFIRMATION OF D2-DOPAMINE RECEPTOR OCCUPANCY BY PET
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DOI：
10.1007/bf00735871
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发表时间：
1988-01-01
影响因子：
3.4
通讯作者：
SEDVALL, G
中科院分区：
文献类型：
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作者：
FARDE, L;WIESEL, FA;SEDVALL, G
在一项为期4周的开放标签非对照研究中，向10名精神分裂症患者给予剂量高达4毫克每日两次的雷氯必利（一种高选择性D2 - 多巴胺受体拮抗剂）。对安全性、耐受性、潜在的抗精神病作用、催乳素反应以及药物对血浆高香草酸的影响进行了评估。通过正电子发射断层扫描（PET）测定中枢D2 - 多巴胺受体占有率。在生化和生理安全参数方面未发现重大偏差。雷氯必利耐受性良好。终点时简明精神病评定量表（BPRS）平均评分降低了55%。在总体评估中，7名患者“非常”或“明显”改善。4名患者出现锥体外系副作用，在减少剂量或单次给予比哌立登后消失。在男女患者中均观察到血浆催乳素短时间升高。治疗4周后血浆高香草酸显著降低。对其中2名患者使用PET测量中枢D2 - 多巴胺受体占有率，分别为68%和72%，与使用常规抗精神病药治疗的患者相同。
Raclopride, a highly selective D2-dopamine receptor antagonist, was administered in doses up to 4 mg b.i.d. to ten schizophrenic patients in an open label non-comparative study lasting 4 weeks. Safety, tolerability, potential antipsychotic effect, prolactin response and drug effect on plasma homovanillic acid were evaluated. Central D2-dopamine receptor occupancy was determined by positron emission tomography (PET). No major deviations were found in biochemical and physiological safety parameters. Raclopride was well tolerated. The mean BPRS score was reduced by 55% at endpoint. In the global evaluation seven patients were "very much" or "much" improved. Extrapyramidal side effects were recorded in four patients and disappeared after dose reduction or single doses of biperiden. An increase in plasma prolactin of short duration was observed in both sexes. A significant decrease of plasma HVA was obtained after 4 weeks of treatment. In two of the patients the central D2-dopamine receptors occupancy was measured using PET. The receptor occupancy was 68 and 72% which is the same as that found in patients treated with conventional neuroleptics.