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1、ChineseJournalofNewDrugs2009,18(12)综述新型抗精神病药帕利哌酮的研究进展李继涛,司天梅(北京大学精神卫生研究所,卫生部精神卫生学重点实验室(北京大学),北京100191)[摘要]帕利哌酮是非典型抗精神病药利培酮的活性代谢产物9羟利培酮,为苯并异噁唑的衍生物,主要通过阻断5羟色胺2A(5HT2A)受体和多巴胺D2(DA2)受体发挥抗精神病的作用。帕利哌酮缓释片使用了OROS技术(渗透性控释口服给药系统),可平稳升高血药浓度,降低血浆峰谷浓度波动,临床使用不需要剂量滴定过程,并保持稳定的疗效和较少不良反应,主要经肾脏
2、以原形排泄。临床研究提示帕利哌酮-1缓释片3~15mgd可以有效控制精神分裂症阳性症状、改善阴性和认知损害、提高患者的耐受性和依从性,起效较快,并能改善对其他非典型抗精神病药治疗无效患者的临床疗效。患者可能出现泌乳素水平增高,但较少引起体重增加等代谢性以及其他不良反应,为精神分裂症患者的全面康复提供了一种新的治疗选择。[关键词]帕利哌酮;作用机制;药动学;临床疗效[中图分类号]R971.41[文献标识码]A[文章编号]1003-3734(2009)12-1095-05Advanceinresearchofpaliperidone,anewantipsy
3、choticLIJitao,SITianmei(InstituteofMentalHealth,KeyLaboratoryofMentalHealth,MinistryofHealth,PekingUniversity,Beijing100191,China)[Abstract]Paliperidone,abenzisoxazolederivative,isthemajoractivemetaboliteofrisperidone.Likerisperidoneandotheratypicalantipsychotics,paliperidoneposse
4、ssesahigheraffinityforblockingserotoninreceptortype2A(5HT2A)anddopaminereceptortype2(DA2).Paliperidoneextendedreleasetablet(paliperidoneER)employstheosmoticcontrolledreleaseoraldeliverysystem(OROS);itresultsinrelativelysmoothdiurnalplasmapaliperidoneconcentrationswithlowpeaktotro
5、ughfluctuationsatsteadystate,allowsfortheavoidanceofdosageadjustmentwheninitiatingtherapy,andmayobtainsteadytherapeuticeffectandlesssideeffects.Paliperidonediffersfromrisperidoneandmostotherantipsychoticsastheextentofitsenzymaticmetabolismisrelativelylow.Renalexcretionisthemajorroute
6、ofitselimination.ClinicaltrialshavedemonstratedthatpaliperidoneER(3~15mg-1d)iseffectiveinreducingthepositiveandnegativesymptomsofschizophrenia,improvingcognitiveimpairmen,tandincreasingthetolerabilityandcomplianceascomparedwithplacebo.Comparedwithplacebo,paliperidoneERcansignificantl
7、yimproveclinicalsymptomsinpatientspreviouslytreatedwithrisperidone.Moreover,paliperidoneappearstohaveafewadverseeffects,exceptforanincreasedrateofhyperprolactinemia.Therefore,paliperidoneERmayprovideavaluablenewtreatmentoptionforpatientswithschizophrenia.[Keywords]paliperidone;mechan
8、ism;p
