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单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,Drugs Affecting Gastrointestinal Function,Gao Fen-Fei,OUTLINE,Peptic Ulcer,Digestion,Vomiting,Diarrhea,Bile,Review-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H,2,受体。1976年,第一代H,2,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)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,Epidemiology,incidence of a disease:,10%-12%,Europe and America:,DU, GU; Japan:,GU, DU,Etiology,General consideration:,No Acid No Ulcer,Main Destroy Factors:,HCl, Pepsin, Hp,Protective Barrier:,Mucus-HCO3,-,Pathogenesis of 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,HCl,Mucus,Hp,Anti-ulcer Classification,Antacids-,Neutralize,HCl,Gastric,Antisecretory,Drugs,HCl,secretion,Antagonize,Rs,. on,Parietal Cell,- H,2,M,3, G,Inhibitor of,H,+,-Pump,Protectors of,Mucosa,Agents kill,HP,. Antacids,Mechanism:,AlkalizersTo Neutralize HCl,Agents:,Mg(OH),2,Al(OH),3,CaCO,3,NaHCO,3,Adverse Effect:,Systemic alkalosis, Diarrhea , CO,2,Constituent,Neutralizing Capacity,Salt Formed in Stomach,Solubility of Salt,Adverse Effects,NaHCO,3,High,NaCl,High,Systemic alkalosis, fluid retention,CaCO,3,Moderate,CaCl,2,Moderate,Hypercalcemia, nephrolithiasis, milk-alkali syndrome,Al(OH),3,High,AlCl,3,Low,Constipation, hypophosphatemia; drug adsorption reduces bio-availability,Mg(OH),2,High,MgCl,2,Low,Diarrhea, hypermagnesemia (in patients with renal insufficiency),Major constituents of antacids,.1. H,2,-R Antagonists,Mechanism:,Pharmacologic Effects:,Basal gastric acid,nocturnal secretion,Agents:,Cimetidine, Ranitidine, Famotidine,Adverse Effect:,Gynecomastia, prolactin , CYP450 , headache,.1. Antimuscarinic Agents,Mechanism:,Blocking M,3,-R on Parietal Cell, M-R on ECL cell and G cell,Pharmacologic Effects:,HCl,spasmolysis,Agents:,Atropine ,Probanthine,Pirenzepine,-,M,1,M,2,-R selection,Adverse Effect:,.1. Antagonist of G-R,Mechanism:,Competing Gastrin-R on Parietal Cell,Pharmacologic Effects:,HCl,Mucosal,Agents:,Proglumide,Adverse Effect:,.2. Proton Pump Inhibitors,Mechanism:,H,+,K,+,-ATPase H,+,K,+,Pharmacologic Effects:,HCl,&,Hp,Agents:,Omeprazole(losec),Lansoprazole,Pantoprazole,Rabeprazole,Adverse Effect:,. Mucosal Protective Agents,Derivative,s of Prostaglandin:,Misoprostol,(PGE,1,),Enprostil,Mechanism:,HCl,; Pepsin,Mucus-HCO3,-,;,Cytoprotective,effect,Pharmacologic Effects:,Prevention of ulcers,iduced,by,NSAIDs,Contraindication,:,Women with childbearing,2.,Sucralfate,Mechanism:,Polymerization &,gelatine,barrier,PGE,2,Mucus-HCO3,-,Hp,Pharmacologic Effects:,Effective in Duodenal Ulcers,Notice:,Acid pH,Empty stomach,3.,CBS,Mechanism:,Pepsin,PGE,1,Mucus-HCO3,-,Coating,Hp,(,disputed,),4.,Teprenone,5.,Marzulene,. Anti-Hp Drugs,90%,DU,70% GU -,Helicobacter pylori,(G,-,),Anti-Ulcer Agents:,Bismuth Compounds,Proton Pump Inhibitors,sucralfate,Antibacterial Drugs:,Amoxicillin,Gentamicin,Metronidazole,Combination Therapy,Therapy of triad,Oversea,PPI + two,Antibacterial Drugs,Domestic,CBS + PPI or H,2,-R Antagonist + Antibacterial Drug,Digestion Aids,Contents of Digestive Juice:,Pepsin,Pancreatin,Helpful,Bacterias,in Bowel:,biofermin,Antiemetic Drugs and Drugs Promoting Gastrointestinal Motility,Medulla Oblongata,Vomiting Center,Stimuli,Chemoreceptor Trigger Zone,Stomach and Abdomminal Musculature,Pathogenesis of Vomiting,延髓呕吐中枢,高级中枢,催吐化学感受区,(5-HT,3, D,2, M,1,),孤束核,(5-HT,3, D,2, M, H,1,),咽喉,胃肠道,(5-HT,3,),迷走神经,H,1, M,小脑,内耳前庭,前庭神经,刺激,刺激,化学刺激物,晃动,Antagonists of Receptors of,H,1,:,Nucleus of,tractus,solitarius,vestibulocerebellar,pathway,Diphenhydramine,Dimenhydrinate,M,:,Nucleus of,tractus,solitarius, CTZ,Scopolamine,D,2,:,CTZ, Nucleus of,tractus,solitarius, Stomach, Small intestine,Thiethylperazine,,,Metoclopramide,5-HT,3,:,Stomach, Small intestine, CTZ, Nucleus of,tractus,solitarius,Ondansetron,,,Granisetron,Prokinetics,:,Metoclopramide,Blocking,Gastrointestinal,Domperidone,D,2,-R,Cisapride,:,Ach release,Antidiarrheal Drugs and,Adsorbents,Opium preparation and,Derivative,s,Opiate receptors in Gastrointestinal tract ,tonemotility,(,),,secretion,(,),,Ach release ,Loperamide,:,Derivative,s of Haloperidol,Astringents,Tannalbin,Bismuth subsalicylate, Bismuth,subcarbonate,Adsorbants,Medicinal Charcoal,Kaolin,Laxatives,Contact cathartics,Irritant or stimulant intestinal motility,Phenolphthalein, Rhubarb,Senna, Castor oil,Osmotic laxatives,nonabsorbable, distending peristalsis,MgSO,4,Na,2,SO,4,Lactulose,Celluloses,Surface-active agents,Lubricating,Stool soften,Liquid paraffin,Choleretic drug,Cholic,Acid,HMG-,CoA,reductase,(rate limiting enzyme) bile salt,,,cholesterol ,Chenodiol,(,Chenodeoxycholic,acid),MgSO,4,cholecystokinin,Cinametic,acid,Anethol,trithione,Review-Questions,The classification of drugs used in the treatment of peptic ulceration.,the mechanisms and the agents of each.,Good Bye!,
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