酒石酸匹莫范色林：一种5-HT2A反向激动剂，具有治疗多种神经精神疾病的潜力。
Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders.
作者信息
Abbas Atheir, Roth Bryan L
机构信息
Case Western Reserve University School of Medicine, Biochemistry, Cleveland, OH 44106, USA.
出版信息
Expert Opin Pharmacother. 2008 Dec;9(18):3251-9. doi: 10.1517/14656560802532707.
BACKGROUND
Pimavanserin tartrate is the first 5-HT(2A) inverse agonist to enter clinical trials as a treatment for L-dopa-induced psychosis in Parkinson's disease and for augmentation of low-dose risperidone treatment in schizophrenia. Pimavanserin is also being evaluated as a possible anti-insomnia drug.
OBJECTIVE
To discuss the potential of pimavanserin to fill multiple therapeutic needs.
METHODS
The problems with currently approved antipsychotics and sleep agents are explored to highlight how pimavanserin might address some longstanding issues in the treatment of psychosis and insomnia.
RESULTS/CONCLUSIONS: In Phase II clinical trials, pimavanserin seemed to be safe, well-tolerated and efficacious in treating L-dopa-induced psychosis without worsening motor symptoms. Pimavanserin also potentiated the therapeutic effects of low-dose risperidone, reduced haloperidol-induced akathisia, and increased slow-wave sleep in older individuals.
背景
酒石酸匹莫范色林是首个进入临床试验的5-HT(2A)反向激动剂，用于治疗帕金森病中左旋多巴诱发的精神病以及增强精神分裂症低剂量利培酮治疗的效果。匹莫范色林也正在作为一种可能的抗失眠药物进行评估。
目的
探讨匹莫范色林满足多种治疗需求的潜力。
方法
探讨目前已批准的抗精神病药物和睡眠药物存在的问题，以突出匹莫范色林如何解决精神病和失眠治疗中的一些长期问题。
结果/结论：在II期临床试验中，匹莫范色林在治疗左旋多巴诱发的精神病方面似乎安全、耐受性良好且有效，且不会加重运动症状。匹莫范色林还增强了低剂量利培酮的治疗效果，减少了氟哌啶醇引起的静坐不能，并增加了老年人的慢波睡眠。
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