氟吡汀的药理作用和临床评价.pdfVIP

曼!!!竺!』!!婴!!堕塑!!里翌E!!塑!：!!!：!!型!：!! —’-’··’I，、 2新药述评： ～ll。。l。l。lI一 氟吡汀的药理作用和临床评价 陈瑞玲，赵志刚 (首都医科大学附属北京天坛医院，北京100050) [摘要]氟吡汀是一种中枢性非阿片类镇痛药，为选择性神经元钾离子通道开放剂，具有镇痛、肌肉松 弛和神经保护作用。在健康人群中氟吡汀的口服生物利用度为90％，r。。。为1．6～2h，C…为0．8—2．0 mg·L～，t∽为6．5—9．6h；老年人群中，其药物消除半衰期延长，c…提高；其常见不良反应为疲倦、头晕、头 痛、胃肠反应，偶见神经障碍和过敏反应，罕见肝损害。临床上氟吡汀主要用于治疗急慢性疼痛，如静止和运 动肌的肌紧张增高引起的疼痛、紧张性头痛、肿瘤引起的疼痛、痛经和创伤后疼痛等。 【关键词] 氟吡汀；镇痛药；药理作用；临床评价 [中图分类号】R971．1[文献标识码]A andclinicalevaluationof Pharmacology flupirtine CHEN Rui-ling，ZHAOZhi-gang Tiantan Medical 100050，China) (曰e讲ng HospitalofCapital University，Be彬ng isa onthecentralnervous isa ofSelective [Abstract]Flupirtinenon—opioidanalgesicacting system．Ittype NeuronalPotassiumChannel as relaxationand Opener(SNEPCO)，actingpainrelieving，muscle effect．The ineticsof aftera oraldoseof100～200wasstudiedin volunteers． pharmacokflupirtinesingle mg healthy The was90％．The concentrationwasobtainedat1．6～2 concentrationwas0．8～ bioavailability peak h，maximum 2．0 half-lifewas6．5～9．6 eliminationhalf．1ifeandmaximumconcentrationof mg·L～．Plasma h．However．mean were in thanin sideeffectsincludes flupirtinehigherelderlysubjects youngerSUbjects．The and lesionareoccasionalsideeffects． headache，gastricdisorders．Neurologicaldifforder，allergicresponsehepatic inacuteandchronicassociatedwithmuscletenseness．In showsthe Flupirtine pain clinical，flupirtineanalgesic andmuscletone treatmentofacuteandchronicassociatedwithmus