FangSanhuaAnti-parasitedrugsHumanparasite•Protozoa(原虫):孢子虫-疟原虫鞭毛虫-阴道毛滴虫叶足虫-阿米巴原虫纤毛虫-结肠小袋纤毛虫•Helminth(蠕虫):吸虫-血吸虫绦虫-链状带绦虫线虫-蛔虫、丝虫•Arthropod(节肢动物):蛛形纲-蜱、螨昆虫纲-蚊、蝇、虱AntimalarialdrugsAntimalarialdrugs•Themalarialparasite,Plasmodium,isaverysmall,Themalarialparasite,Plasmodium,isaverysmall,single-cellorganism.single-cellorganism.•Itlivesasaparasiteinotherorganisms,namelyItlivesasaparasiteinotherorganisms,namelymanmanandmosquitoandmosquito..•TheparasiteisthecauseofthetropicalorsubtropicalTheparasiteisthecauseofthetropicalorsubtropicaldiseasediseasemalaria.malaria.AntimalarialdrugsAntimalarialdrugs-Malarialparasite-MalarialparasiteFourspeciesofplasmodiumcanproducethediseaseiFourspeciesofplasmodiumcanproducethediseaseinitsvariousforms:nitsvariousforms:•PlasmodiumfalciparumPlasmodiumfalciparum((恶性疟原虫)恶性疟原虫)•PlasmodiumvivaxPlasmodiumvivax((间日疟原虫)间日疟原虫)•PlasmodiumovalePlasmodiumovale((卵形疟原虫)卵形疟原虫)•PlasmodiummalariaPlasmodiummalaria((三日疟原虫)三日疟原虫)AntimalarialdrugsAntimalarialdrugs--ParasiteLifeCycleParasiteLifeCycle红细胞外期红细胞内期按蚊-有性繁殖人体-无性繁殖•NooneavailableagentcanreliablyeffectaradicalcuNooneavailableagentcanreliablyeffectaradicalcure,ie,eliminatebothexo-re,ie,eliminatebothexo-erythrocyticerythrocyticanderythrocyticsanderythrocyticstages.tages.•Fewavailableagentsarecausalprophylacticdrugs,iFewavailableagentsarecausalprophylacticdrugs,ie,capableofpreventingerythrocyticinfection.e,capableofpreventingerythrocyticinfection.AntimalarialdrugsAntimalarialdrugs控制复发Primaquine(伯氨喹)迟发病因预防Pyrimethamine(乙胺嘧啶)速发控制症状Chloroquine(氯喹)Quinine(奎宁)Mefloquine(甲氟喹)Artemisinin(青蒿素)阻止传播Pyrimethamine(乙胺嘧啶)阻止传播Primaquine(伯氨喹)Chloroquine(氯喹)Quinine(奎宁)(恶性疟无效)红细胞外期红细胞内期按蚊-有性繁殖AntimalarialdrugsAntimalarialdrugs––ChloroquineChloroquine(氯喹)(氯喹)•Chloroquineisasynthetic4-aminoquinolinederivateChloroquineisasynthetic4-aminoquinolinederivate控制症状Chloroquine氯喹Quinine奎宁Mefloquine甲氟喹Artemisinin青蒿素红细胞内期PharmacologicaleffectsPharmacologicaleffects1.Antimalarialeffects1.Antimalarialeffects•RapidschizonticidalactivityRapidschizonticidalactivity((裂殖体杀灭剂)裂殖体杀灭剂)aagainstallinfectionsofmalariaspeciesgainstallinfectionsofmalariaspecies..•AlsogametocytocidalAlsogametocytocidal((杀配子体)杀配子体)againstP.vivaagainstP.vivax,P.malariaeandP.ovale.x,P.malariaeandP.ovale.•Itisnotactiveagainstexo-erythrocyticform,andshoItisnotactiveagainstexo-erythrocyticform,andshouldthereforebeusedwithprimaquineuldthereforebeusedwithprimaquine((伯氨喹)伯氨喹)totoeffectradicalcureofP.vivax.effectradicalcureofP.vivax.AntimalarialdrugsAntimalarialdrugs--ChloroquineChloroquinePharmacologicaleffectsPharmacologicaleffects2.Immuneinhibition2.Immuneinhibition•Treatmentofrheumatoidarthritis,lupuserTreatmentofrheumatoidarthritis,lupuserythematosusythematosus3.3.ExtraintestinalamebiasisExtraintestinalamebiasis•AmoebatrophozoiteamebicliverabscessAmoebatrophozoiteamebicliverabscessAntimalarialdrugsAntimalarialdrugs--ChloroquineChloroquineMechanismofactionsMechanismofactions•Accumulationinerythrocyte→pH↑→malarialpigAccumulationinerythr...