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Gastrointestinal Drugs

Gastrointestinal Drugs. Hepatic, pacreatic and biliary disorders. Ulcer disorders. Abnormal mobility. Gastrointestinal drugs. Drugs used in the treatment of peptic ulcers Modulators of gastrointestinal functions Drugs used in the hepatic and bile diseases. Gastrointestinal drugs.

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Gastrointestinal Drugs

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  1. Gastrointestinal Drugs

  2. Hepatic, pacreatic and biliary disorders Ulcer disorders Abnormal mobility

  3. Gastrointestinal drugs • Drugs used in the treatment of peptic ulcers • Modulators of gastrointestinal functions • Drugs used in the hepatic and bile diseases

  4. Gastrointestinal drugs Peptic ulcers: gastric and duodenal ulcers

  5. Gastrointestinal drugs Peptic ulcers: endoscopic view

  6. Gastrointestinal drugs Peptic ulcers: Over-production of gastric acid

  7. Gastrointestinal drugs Peptic ulcers: Helicobacter pylori

  8. Gastrointestinal drugs Peptic ulcers: inadequate mucosal defense against gastric acid and pepsin H+; pepsin

  9. Peptic ulcers: development and complications

  10. Gastrointestinal drugs H. pylori Peptic ulcers: imbalance between aggressive and protective factors

  11. Gastrointestinal drugs Peptic ulcers: pathogenesis and treatments Treatment approaches Eradicating Helicobacter pylori infection Reducing secretion of gastric acid or neutralizing the acid Protecting the gastric mucosa from damage Pathogenesis of peptic ulcers Infection with gram-negative Helicobacter pylori Increased gastric acid secretion Inadequate mucosal defense against gastric acid

  12. misoprostol Sucralfate Bismuth, etc Gastric structure related to peptic ulcer

  13. Gastric acid secretion and regulation

  14. A. Drugs used for peptic ulcers • 1. Antacids • 2. Drugs affecting gastric acid secretion • Muscarinic receptor antagonists • H2 receptor antagonists • H+-K+-ATPase inhibitors (proton pump inhibitors) • Gastrin receptor antagonists • 3. Mucosal protective drugs • 4. Antimicrobial drugs (Helicobacter pylori)

  15. A. Drugs used for peptic ulcers • Antacids • Basic substances that reduce gastric acidity by neutralizing HCl • The hydroxide is the most common base but trisilicate, carbonate and bicarbonate ions are also used. • Aluminium, magnesium or sodium • calcium carbonate (碳酸钙) • magnesium oxide (氧化镁) • magnesium hydroxide (氢氧化镁) • magnesium trisilicate (三硅酸镁) • aluminum hydroxide (氢氧化铝) • sodium bicarbonate (碳酸氢钠)

  16. misoprostol Sucralfate Bismuth, etc

  17. A. Drugs used for peptic ulcers • Drugs affecting gastric acid secretion • Muscarinic receptor antagonists Pirenzepine 哌仑西平

  18. A. Drugs used for peptic ulcers • Pirenzepine（哌仑西平） • 1. Pharmacological effects and clinical uses • high affinity for M1- and low affinity for M2-receptors of the smooth muscle of the ileum and urinary bladder. • blocking of M1-muscarinic receptors in autonomic ganglia, inhibiting HCl secretion • 2. Adverse effects • Atropine-like effects, especially at larger doses • Other drugs • Telenzepine（替仑西平） • Atropine: various side effects • Propantheline bromide (溴丙胺太林)

  19. misoprostol Sucralfate Bismuth, etc

  20. A. Drugs used for peptic ulcers • H2 receptor antagonists Cimetidine西咪替丁 cimetidine 西咪替丁 ranitidine 雷尼替丁

  21. A.Drugs used for peptic ulcers • Cimetidine （西咪替丁） • 1. Pharmacological effects • Blocking H2 receptors, decreasing H+ secretion • 2. Clinical uses • Duodenal and gastric ulcer, reflux esophagitis: relieving symptoms,promoting healing of ulcers, and preventing ulcers • Acute stress ulcers, gastroesophageal reflux disease (heartburn)

  22. misoprostol Sucralfate Bismuth, etc

  23. A. Drugs used for peptic ulcers • 3. Adverse effects • (1) Side effects: constipation, diarrhea, tiredness, muscular pain, etc. • (2) CNS effects: headache, dizziness, confusion, hallucination, etc. (elderly, long-term uses) • (3) Endocretion effects: antiandrogen, gynecomastia (男性乳房发育), galactorrhea (溢乳), reduced sperm count, and male sexual dysfunction • 4. Drug interactions • Inhibiting hepatic P450, raising plasma concentrations of warfarin, phenytoin, diazepam, propranolol, quinidine and theophylline

  24. A. Drugs used for peptic ulcers Others Ranitidine 雷尼替丁 Longer acting; 4-10 times more potent Minimal side effects, on antiandrogenic and prolactin-stimulating effects, not inhibiting P450 Famotidine 法莫替丁 Similar to ranitidine, but 7-20 times more potent Nizatidine 尼扎替丁 Bioavailability is near 100%, principally eliminated by kidney

  25. A. Drugs used for peptic ulcers • H+-K+-ATPase inhibitors • ( proton pump inhibitors, PPI ) Omeprazole 奥美拉唑

  26. A. Drugs used for peptic ulcers • 1. Pharmacological effects • (1) Inhibiting gastric acid secretion by various stimuli (histamine, gastrin, aspirin, ethanol, stress) • (2) Inhibiting H. pylori • 2. Clinical uses • (1) Highly effective for duodenal and gastric ulcer, reflux esophagitis: relieving symptoms,promoting healing of ulcers • (2) Used with antimicrobial regimens to eradicate H. pylori

  27. misoprostol Sucralfate Bismuth, etc

  28. A. Drugs used for peptic ulcers • 3. Adverse effects • (1) Side effects: nausea, headache, diarrhoea, constipation and rash occur but are uncommon • (2) Increase of gastric carcinoid tumor: prolonged hypochlorhydria and secondary hypergastrinemia • (3) Others: gynecomastia (男性乳房发育),hypersensitivity • 4. Drug interactions • Inhibiting hepatic P450, raising plasma concentrations of warfarin, phenytoin, diazepam, etc.

  29. A. Drugs used for peptic ulcers • Other PPIs • Lansoprazole兰索拉唑 • Pantoprazole泮他拉唑 • Rebeprazole雷贝拉唑

  30. A. Drugs used for peptic ulcers • Mucosal protective drugs • Misoprostol 米索前列醇 • Enprostil 恩前列素 • Sucralfate 硫糖铝 • Colloidal bismuth subcitrate胶体次枸橼酸铋(枸橼酸铋钾） • Teprenone 替普瑞酮 • Marzulene 麦滋林 • Smectite 蒙脱石（思密达）

  31. misoprostol Sucralfate Bismuth, etc.

  32. A. Drugs used for peptic ulcers Misoprostol 米索前列醇

  33. A. Drugs used for peptic ulcers • Misoprostol米索前列醇 • 1. Pharmacological effects • Inhibiting gastric acid secretion • Promoting mucus and HCO3- secretion, and mucosal repair • 2. Clinical uses • Ulcers, especially for NSAIDs-induced ulcers • 3. Adverse effects • Side effects (13%): nausea, abdominal pain, diarrhea, headache, etc. • Contraindicated in pregnancy women

  34. A. Drugs used for peptic ulcers • Antimicrobial drugs • (for Helicobacter pylori) • 1. Anti-ulcer drugs • H+-K+-ATPase inhibitors; bismuch ; sucralfate • Weaker, combined with antimicrobial drugs • 2. Antimicrobial drugs • metronidazole (甲硝唑); amoxicillin (阿莫西林); • tetracycline (四环素); gentamicin (庆大霉素); • clarithromycin (克拉霉素)

  35. Helicobacter pylori in the gastric mucosa

  36. misoprostol Sucralfate Bismuth, etc.

  37. B. Modulators of gastrointestinal functions

  38. B. Modulators of gastrointestinal functions

  39. B. Modulators ofgastrointestinal functions • Antiemetic and prokinetic drugs • antiemetic drugs（止吐药） • prokinetic drugs（增强胃肠动力药） • Drugs for treatment of diarrhea • antimotility drugs（抑制肠蠕动药） • astringents（收敛药） • absorbants（吸附药） • Laxatives • contact (stimulant) laxatives（接触/刺激性泻药） • osmotic laxatives（渗透性泻药） • faecal softners (emollients)（软便药）

  40. B. Modulators ofgastrointestinal functions • Antiemetic and prokinetic drugs • Antiemetic drugs • H1 receptor antagonists: diphenhydramine 苯海拉明; • dimenhydrinate 茶苯海明; meclozine 美克洛嗪 • Muscarinic receptor antagonists: scopolamine东莨菪碱 • D2 receptor antagonists: chlorpromazine氯丙嗪 • 5-HT3 receptor antagonists：ondansetron昂丹司琼; • granisetron格拉司琼; alosetron阿洛司琼

  41. 孤束核

  42. B. Modulators ofgastrointestinal functions Ondansetron 昂丹司琼

  43. B. Modulators ofgastrointestinal functions • 1. Pharmacological effects • Blocking 5-HT3 receptor (central and peripheral) • 2. Clinical uses • Emesis induced by chemotherapy and radiotherapy in the patients with cancers • 3. Adverse effects • side effects:headache, constipation or diarrhea, etc.

  44. 孤束核

  45. B. Modulators ofgastrointestinal functions • Prokinetic drugs • Metoclopramide 甲氧氯普胺(胃复安，灭吐灵) • D2 receptor block:antiemetic effects (CTZ), promoting GI motility (GI) • Adverse effects: CNS reactions, extrpyramidal effects, etc. • Domperidone 多潘立酮(吗丁啉) • D2 receptor block: promoting GI motility (GI) • Adverse effects: headache, prolactin , gastric acid  • Cisapride 西沙必利 • ACh release: promoting intestinal and colon motility

  46. Action sites of prokinetic drugs GI tract smooth muscle cells

  47. B. Modulators ofgastrointestinal functions • Drugs for treatment of diarrhea • Antimotility drugs:agonists for  receptors in GI tract • opium preparations 阿片制剂 • diphenoxylate 地芬诺酯（CNS effects at larger doses) • loperamide 洛哌丁胺 • Astringents （收敛药）: • tannalbin 鞣酸蛋白 • bismuth subsalicylate; bismuth subcarbonate (铋制剂) • Absorbants （吸附药） ： • medicinal charcoal 药用炭（活性炭） • agysical 矽炭银

  48. B. Modulators ofgastrointestinal functions • Laxatives • Contact (stimulant) laxatives（接触性/刺激性泻药） • phenolphthalein 酚酞 • bisacodyl 必沙可啶 • anthraquinones 蒽醌类（大黄等中药成分） • Osmotic laxatives （渗透性泻药，容积性泻药） • magnesium sulfate 硫酸镁 sodium sulfate 硫酸钠 • lactulose 乳果糖sorbitol 山梨醇 • glycerol 甘油celluloses 纤维素类 • Faecal softners (emollients) （润滑性泻药） • liquid paraffin 液状石蜡

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