医学课件消化系统药物_2

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1、Chapter5DigestiveSystemAgents1OutlineSection1Anti-ulcerAgents(抗溃疡药)Section2Antiemetics(止吐药)Section3Prokinetics(促动力药)Section4AdjuvantforHepaticandBiliaryDisease(肝胆疾病辅助治疗药物)23Section3Prokinetics(促动力药)456ConceptandclassificationProkineticsClassificationD2receptorantagonistsMetoclopramide(甲氧氯普胺)Peripher

2、yD2receptorantagonistsDomperidone(多潘立酮)AcetylcholineagonistsCisapride(西沙必利)PromoteGIcontenttopushforward,usedinthetreatmentofGIdyskinesis(动力障碍)suchasrefluxesophagitis(返流食道炎),dyspepsia(消化不良),intestinalobstruction(肠梗阻),etc.7CommonProkineticsMetoclopramideDomperidoneCisapride89Prokinetics10Metocloprami

3、de(甲氧氯普胺)procainamidemetoclopramidealsousedasanantiemetic胃复安Structureissimilar,buthasnofunctionforanti-cardiacarrhythmias11MetoclopramideItisanantiemeticandgastroprokineticagent.Totreatnauseaandvomiting,andtofacilitategastricemptyinginpatientswithgastroparesis.Varioustradenames:Maxolon(Shire/Valeant

4、),Reglan(SchwarzPharma),Degan(Lek),Maxeran(SanofiAventis),Primperan(SanofiAventis),andPylomid(Bosnalijek).1213Cisapride14Cisapride(西沙必利)1234512343and4-CarebothchiralC3and4-substituentsonthesamesideofpyridinering4-amino-5-chloro-N-((3S,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl)-2-meth

5、oxybenzamide152-cisisomersinclinic4-isomersofCisapride16MetabolismofCisapride17CisaprideinClinicCisaprideisaparasympathomimeticandgastroprokineticagentthatactsasaserotonin5-HT4receptoragonist.Stimulationoftheserotoninreceptorsincreasesacetylcholinereleaseintheentericnervoussystem.Itissoldunderthetra

6、denamesPrepulsid(Janssen-Ortho)andPropulsid(intheU.S.).ItwasdiscoveredbyJanssenPharmaceuticain1980.18InClinicVariousGIdyskinesis(动力障碍)suchasGastroparesis(胃肌轻瘫)andregurgitation(反胃).Sideeffect：anexceptionallife-threateningventriculararrhythmia(室性心律失常).19CisaprideinClinicIn1995,itwasrecordedinBPandEP.I

7、n1997,itbecametop25of500best-sellingdrugswith1.04billiondollars.In2000,386severeADR,125death.ItwassuspendedinUSAandUKinsameyear.20New“Pride”ProkineticDrugsMuchsafer2122Domperidone(多潘立酮)5-chloro-1-(1-[