老年科原发性骨质疏松症诊治指南.ppt

不同类型骨质疏松治疗方案第96页,共97页，2024年2月25日，星期天感谢大家观看第97页,共97页，2024年2月25日，星期天**FunctionalDomainsofBisphosphonatesBisphosphonateshaveseveralfunctionaldomainsanddifferentmolecularstructures.Asaclass,allbisphosphonatesworkbybindingtheirphosphonategroupstohydroxyapatite.AllapprovedbisphosphonateshaveandOHgroupinR1;thiscreatesatriplehookandenhancesbindingtobone.VaryingtheR2substituentscanresultindifferencesinantiresorptivepotencyofseveralordersofmagnitude.PamidronateandalendronatehaveanR2sidechainthatcontainsabasicprimarynitrogenatominanalkylchainandhavegreaterantiresorptivepotencythaneitheretidronateorclodronate.IbandronatehasamorehighlysubstitutednitrogenmoietyinR2andshowsgreaterantiresorptivepotencythanpamidronateoralendronate.Themostpotentantiresorptivebisphosphonatesarerisedronateandzoledronicacid,whichbothcontainanitrogenatomwithinaheterocyclicringintheR2position.EnhancementsinantiresorptivepotencyresultingfromdifferencesintheR2groupsappeartobeparticularlylinkedtoinhibitionofthefarnesylpyrophosphatesynthaseenzymewithinthemevalonatepathwayinosteoclasts.ReferenceNancollasGH,TangR,PhippsRJ,etal.Novelinsightsintoactionsofbisphosphonatesonbone:differencesininteractionswithhydroxyapatite.Bone.2006;38:617-627.**唑来膦酸在骨组织的微循环使其具有更长久的疗效与骨组织的结合力对于不同的双膦酸盐的不同临床疗效，包括作用强度，药代特点以及持久疗效。唑来膦酸进入体内后被骨组织迅速吸收，由于强大的吸附力，药物的脱落率很低，并且少量脱落出来的药物可以通过强大的再吸附作用而重被骨组织吸收。因此，唑来膦酸具有更长的作用周期。ReferenceNancollasGH,TangR,PhippsRJ,etal.Novelinsightsintoactionsofbisphosphonatesonbone:differencesininteractionswithhydroxyapatite.Bone.2006;38:617-627.**ConceptofaSERMSelectiveestrogenreceptormodulators(SERMs)arenon-hormonalagentsthatbindtoestrogenreceptors,butproduceestrogenagonisteffectsinsometissueswhileblockingtheeffectofestrogeninothertissues.注意事项第64页,共9