抗胆碱酯酶药和胆碱酯酶复活药1

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1、Chapter7cholinesteraseinhibitingdrugs&cholinesterasereactivators第七章抗胆碱酯酶药和胆碱酯酶复活药TAISHANmedicaluniversityzhangfengCholinesterase（胆碱酯酶，AChE）acetylcholinesterase（乙酰胆碱酯酶）也称真性胆碱酯酶：主要存在于胆碱能神经末梢突触间隙。Pseudocholinesterase（假性胆碱酯酶）：主要存在于血液及肝脏中。新斯的明抑制胆碱酯酶过程示意图Neostigmine（新斯的

2、明）1.Pharmacologicaleffects①cholinesteraseinhibitor②verystrongeffectonskeletalmuscle--directactivatingN2receptors--releaseAChatthemotornerveendings（运动神经）③strongstimulatingeffectongastrointestinaltract（胃肠道平滑肌）andgallbladdersmoothmuscle（胆囊平滑肌）I.易逆性抗胆碱酯酶药2.ClinicalUses

3、①myastheniagravis（重症肌无力）②Postoperativeileus（术后肠梗阻）andurinaryretention（尿潴留）③Paroxysmalsupraventriculartachycardia（阵发性室上性心动过速）④Overdosageofmusclerelaxants⑤Atropineintoxication3.SideEffectslargedosage----nausea（恶心）,vomiting（呕吐）,abdominalpain（腹痛）,HR,fibrillationofmuscl

4、efibers（肌束颤动）,“cholinergiccrisis”（胆碱能危机）4.Contraindications①Mechanicalintestinalobstruction(ileus)（机械性肠梗阻）②urinaryobstruction（尿路阻塞）③bronchialasthma（支气管哮喘）Pyridostigmine（吡斯的明）1.Similarandweakerthanneostigmine2.Durationislonger3.ClinicalUses①myastheniagravis②postop

5、erativeintestinaldistentionandurinaryretention③lesssideeffectsPhysostigmine(毒扁豆碱，又称Eserine）ClinicalUses①glaucoma（青光眼）②awakeningoftraditionalChineseherbanesthesia（中药麻醉的催醒）③atropineintoxication病例讨论Ⅱ.难逆性抗胆碱酯酶药Organophosphates(有机磷酸酯类，OPs）1.Classification①Organophosphor

6、us--dipterex（敌百虫）,rogor（乐果）,DDVP,Parathion（对硫磷）,Malathion（马拉硫磷）--usedasaninsecticide.--rapidlyabsorbed–skin,respiratory,GIetc.②Nervegases--tabun（塔崩）,sarin（沙林）,soman（梭曼）有机磷酸酯类抑制胆碱酯酶过程示意图2.MechanismofOrganophosphateIntoxication①WithexposuretoOpsanticholinesteraseagen

7、ts,theenzyme(AChE)isphosphorylated（使磷酸化）andbecomesunabletofunction.②Acetylcholinebuild-up,whichcausesinterfer-encewithnerveimpulsetransmissionatnerveendings.3.Acuteintoxication①Muscarinicreceptors--pupil,vision,gland,respiration,gastrointestinaltract,bladder,etc.②N

8、icotinicreceptors--heartrate,bloodpressure--neuromuscularjunction③centralnervoussystem--excitement→inhibitionCholinesteraseAging(Onceagingoccurs,