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Gastrointestinal drugs

Gastrointestinal drugs. Department of pharmacology Liming zhou 2010,spring. classification. Drugs for treatment of peptic ulcers Drugs for adjusting the function of digestion Drugs promoting gastrointestinal motility Antiemetic drugs laxatives.

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Gastrointestinal drugs

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  1. Gastrointestinal drugs Department of pharmacology Liming zhou 2010,spring

  2. classification • Drugs for treatment of peptic ulcers • Drugs for adjusting the function of digestion • Drugs promoting gastrointestinal motility • Antiemetic drugs • laxatives

  3. Drugs for peptic ulcers Classification of peptic ulcer: • Duodenal (DU) Gastric (GU) • Role of pepsin in peptic ulcer disease: • Secreted gastric acid plus effects of pepsin promote tissue injury

  4. Peptic ulcer disease: an imbalance between aggressive factors (gastric acid pepsin bacteria) and protective factors (gastric mucus, bicarbonate, prostaglandins) • Regulation of gastric acid secretion-- many factors (chemical, neural, hormonal)

  5. Stimulation: • Gastrin-most potent stimulant • Activation of postganglionic vagal fibers

  6. Drugs for peptic ulcers-----antacidsAction • Neutralize secreted acid • Reduce gastric acidity Pepsin inactive Reduce destroy factors

  7. Drugs for peptic ulcers-----antacids • A magnesium hydroxide(氢氧化镁) • B magnesium trislilicate（三硅酸镁） • C aluminum hydrocide（氢氧化铝） • D Calcium carbonate（碳酸钙） • F Sodium bicarbonate（碳酸氢钠）

  8. 1 NaHCO3+HCl NaCl+H2O+CO2 • 2 Al（OH）3 aluminium hydroxide • Al（OH）3+3HCl AlCl3 +3H2O • 3 Mg（OH）2 magnesium hydroxide • Mg（OH）2+2HCl MgCl2 +2H2 O • 4 Mg2Si3O8 magnesium trisilicate • Mg2Si3O8+4HCl 2MgCl2+3SiO2+2H2O • 5 CaCO3 calcium carbonate • CaCO3+2HCl CaCl2+H2O+CO2

  9. Gastric antisecretory drugs • antagonisit of H2 receptor ↓ • decrease the H+ secretion • Basal gastric acid food-stimulated gastric acid

  10. H2 Receptor Antagonists • A cimetidine (西米替丁) + • B ranitidine （雷米替丁）++ • C famotidine（法莫替丁）+++ • Effective inhibitor of stimulated and non-stimulated gastric acid secretion • Healing rates: similar between antacids and H2 receptor antagonists

  11. Effective inhibitor of stimulated and non-stimulated gastric acid secretion • Healing rates: similar between antacids and H2 receptor antagonists

  12. Mucosal protective agents • Prostaglandins • reduction in basal and stimulated gastric acid secretion; • enhanced mucosa resistance to injury (PGE1/PGE2).

  13. Mucosal protective agents • Bismuth compounds • Mechanism of Action • cytoprotective effects • compounds bind to the ulcer base, stimulating mucus and prostaglandin production • antibacterial effect • inhibition of proteolytic, lipolytic, and urease activities • Coating and protecting the ulcer crater

  14. Clinical use of Bismuth compounds • In monotherapy: • ------- eradicate H. pylori in about 20% of patients • combination with antibiotics • -------eradicate H. pylori in up to 95% of patients.

  15. Sucralfate • binds to ulcer bed (granulation tissue, not to gastric or duodenal mucosa) • decreases proton diffusion to the ulcer base • may increase endogenous tissue prostaglandins and may bind epidermal growth factors and other growth factors-- improving mucosal defense

  16. antimicrobials • activity against H.pylori • clarithromycin, amoxicillin, tetracycline

  17. Drugs for adjusting the function of digestion • drugs of aid digestive • A pepsin • B pancreatin • C lactasin

  18. antiemetic drugs and drugs promoting gastrointestinal motility • antiemetic drugs: • H-1 receptor blocker : diphenhydramine • Chloropromazine • M-receptor blocker : scopolamine

  19. drugs promoting gastrointestinal motility • Metoclopramide (甲氧氯普胺)： • domperidone （多潘立酮）blocking D2-receptor • Cisapride(西沙比利）

  20. Metoclopramide (甲氧氯普胺) • Blocking the DA2 receptor in CTZ • Blocking the DA2 receptor in Gastrointestinal

  21. domperidone （多潘立酮） • blocking DA2-receptor in Gastrointestinal

  22. Cisapride(西沙比利） • Increase release of the Ach

  23. antidiarrheal drugs • opium preparation • Laxative Drugs magnesium sulfate sodium sulfate

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