药物的肝脏毒性消化系统用药(高分飞).ppt

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1、Drugs Affecting Gastrointestinal Function,Gao Fen-Fei,OUTLINE,Peptic UlcerDigestionVomitingDiarrheaBileReview-Questions,Ulcer-Background,20世纪初，与应激、生活、饮食等有关，故主张镇静、休息、饮食治疗。1910年，Schwarz提出”No Acid No Ulcer”1971年，Black等发现H2受体。1976年，第一代H2受体拮抗剂西咪替丁用于临床第一次革命。诺贝尔奖。20世纪80年代中期，质子泵抑制剂（proton pump inhibitor，PPI

2、）奥美拉唑问世。1983年，澳大利亚学者Warren与Marshall分离出Hp，病因观念转变，再一次革命。根治成为可能。2005年，获诺贝尔奖。,Introduction of Ulcer,Epidemiologyincidence of a disease:10%-12%Europe and America:DU GU;Japan:GU DU EtiologyGeneral consideration:No Acid No UlcerMain Destroy Factors:HCl,Pepsin,HpProtective Barrier:Mucus-HCO3-,Pathogenesis o

3、f Peptic Ulcer,Review,How is the secretion of gastric acid adjusted?What is the mechanism of secretion of gastric acid?,How to treat peptic ulcer?,Anti-ulcer Targets,HClMucusHp,Anti-ulcer Classification,Antacids-Neutralize HClGastric Antisecretory Drugs HCl secretionAntagonize Rs.on Parietal Cell-H2

4、,M3,GInhibitor of H+-PumpProtectors of MucosaAgents kill HP,.Antacids,Mechanism:AlkalizersTo Neutralize HClAgents:Mg(OH)2 Al(OH)3 CaCO3 NaHCO3Adverse Effect:Systemic alkalosis,Diarrhea,CO2,Major constituents of antacids,.1.H2-R Antagonists,Mechanism:Pharmacologic Effects:Basal gastric acid nocturnal

5、 secretionAgents:Cimetidine，Ranitidine，FamotidineAdverse Effect:Gynecomastia,prolactin,CYP450,headache,.1.Antimuscarinic Agents,Mechanism:Blocking M3-R on Parietal Cell,M-R on ECL cell and G cellPharmacologic Effects:HCl spasmolysisAgents:Atropine，ProbanthinePirenzepine-M1,M2-R selectionAdverse Effe

6、ct:,.1.Antagonist of G-R,Mechanism:Competing Gastrin-R on Parietal CellPharmacologic Effects:HCl Mucosal Agents:ProglumideAdverse Effect:,.2.Proton Pump Inhibitors,Mechanism:H+,K+-ATPase H+K+Pharmacologic Effects:HCl&Hp Agents:Omeprazole（losec）LansoprazolePantoprazole，RabeprazoleAdverse Effect:,.Muc

7、osal Protective Agents,Derivatives of Prostaglandin:Misoprostol(PGE1),EnprostilMechanism:HCl;PepsinMucus-HCO3-;Cytoprotective effectPharmacologic Effects:Prevention of ulcers iduced by NSAIDsContraindication：Women with childbearing,2.SucralfateMechanism:Polymerization&gelatine barrier PGE2 Mucus-HCO

8、3-HpPharmacologic Effects:Effective in Duodenal UlcersNotice:Acid pHEmpty stomach,3.CBS Mechanism:Pepsin PGE1 Mucus-HCO3-CoatingHp（disputed）4.Teprenone5.Marzulene,.Anti-Hp Drugs,90%DU,70%GU-Helicobacter pylori(G-)Anti-Ulcer Agents:Bismuth CompoundsProton Pump InhibitorssucralfateAntibacterial Drugs:

9、AmoxicillinGentamicinMetronidazole,Combination Therapy,Therapy of triadOverseaPPI+two Antibacterial DrugsDomesticCBS+PPI or H2-R Antagonist+Antibacterial Drug,Digestion Aids,Contents of Digestive Juice:PepsinPancreatinHelpful Bacterias in Bowel:biofermin,Antiemetic Drugs and Drugs Promoting Gastroin

10、testinal Motility,Medulla Oblongata Vomiting Center,Stimuli,Chemoreceptor Trigger Zone,Stomach and Abdomminal Musculature,Pathogenesis of Vomiting,延髓呕吐中枢,刺激,晃动,Antagonists of Receptors of H1:Nucleus of tractus solitarius,vestibulocerebellar pathwayDiphenhydramine,DimenhydrinateM:Nucleus of tractus s

11、olitarius,CTZScopolamineD2:CTZ,Nucleus of tractus solitarius,Stomach,Small intestineThiethylperazine，Metoclopramide 5-HT3:Stomach,Small intestine,CTZ,Nucleus of tractus solitariusOndansetron，Granisetron Prokinetics：Metoclopramide Blocking GastrointestinalDomperidone D2-RCisapride：Ach release,Antidia

12、rrheal Drugs and Adsorbents,Opium preparation and DerivativesOpiate receptors in Gastrointestinal tract tonemotility（），secretion（），Ach release Loperamide：Derivatives of HaloperidolAstringentsTannalbinBismuth subsalicylate,Bismuth subcarbonateAdsorbantsMedicinal CharcoalKaolin,Laxatives,Contact catha

13、rticsIrritant or stimulant intestinal motilityPhenolphthalein,Rhubarb,Senna,Castor oilOsmotic laxativesnonabsorbable distending peristalsisMgSO4,Na2SO4,Lactulose,Celluloses Surface-active agentsLubricating,Stool softenLiquid paraffin,Choleretic drug,Cholic AcidHMG-CoA reductase(rate limiting enzyme)bile salt，cholesterol Chenodiol(Chenodeoxycholic acid)MgSO4cholecystokinin Cinametic acidAnethol trithione,Review-Questions,The classification of drugs used in the treatment of peptic ulceration.the mechanisms and the agents of each.,Good Bye!,