Pharmacology Chapter8 胆碱受体阻断药课件.ppt

第8章抗胆碱酯酶药

Chapter8AnticholinesteraseDrugs复旦大学上海医学院姚明辉徐昕红PharmacologyChapter8胆碱受体阻断药

第一节胆碱酯酶PharmacologyChapter8胆碱受体阻断药

胆碱酯酶(cholinesterase，ChE)乙酰胆碱酯酶(acetylcholinesterase，AChE)relativelyspecificforacetylcholinerapidacetylcholinehydrolysisatcholinergicsynapsesPharmacologyChapter8胆碱受体阻断药

胆碱酯酶(cholinesterase，ChE)假性胆碱酯酶(pseudocholinesterase)relativelylowspecificityforacetylcholineacetylcholinehydrolysisinplasmaandmanyothertissuesPharmacologyChapter8胆碱受体阻断药

AChE分布分子组成同聚体异聚体PharmacologyChapter8胆碱受体阻断药

AChE水解过程结合裂解水解PharmacologyChapter8胆碱受体阻断药

AcetateAc-serinehydrolysedAcetyl-grouptransferredtoserine-OHAcetylcholinebindsEsteraticsiteAnionicsitePharmacologyChapter8胆碱受体阻断药

第二节抗胆碱酯酶药(anticholinesteraseagents)PharmacologyChapter8胆碱受体阻断药

Fig.8-1TheinteractionsofAChEwithacetylcholine(A),reversibleanticholinesterasedrugs(B)andirreversibleanticholinesteraseagents(C).PharmacologyChapter8胆碱受体阻断药

anticholinesteraseagents非共价结合的抑制药氨甲酰类抑制药有机磷化合物易逆性抗AChE药难逆性抗AChE药PharmacologyChapter8胆碱受体阻断药

anticholinesteraseagents非共价结合的抑制药依酚氯铵（edrophonium）他克林（tacrine）多奈哌齐（donepezil）PharmacologyChapter8胆碱受体阻断药

anticholinesteraseagents氨甲酰类抑制药新斯的明（neostigmine）吡斯的明（pyridostigmine）地美溴铵（demecarium）利凡斯的明（rivastigmine）PharmacologyChapter8胆碱受体阻断药

易逆性抗AChE药PharmacologyChapter8胆碱受体阻断药

一般特性药理作用体内过程临床应用不良反应PharmacologyChapter8胆碱受体阻断药

药理作用眼缩瞳调节痉挛降低眼内压PharmacologyChapter8胆碱受体阻断药

药理作用胃肠道胃收缩?，胃酸分泌?食管蠕动?，张力增加?小肠、大肠(尤其结肠)活动?，肠内容排出?PharmacologyChapter8胆碱受体阻断药

TherapeuticusesanddurationsofactionofcholinesteraseinhibitorsdrugsusesapproximateDurationofactionedrophoniummyastheniagravis5-15minneostigminemyastheniagravis0.5~2hpyridostigminemyastheniagravis3~6hphysostigmineglaucogma0.5~2hambenoniummyastheniagravis4~8hDemecariumglaucogma4~6hPharmacologyChapter8胆