Treatment of peptic ulcer

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Treatment of peptic ulcer

  1. 1. ANTACIDS Systemic ANC Sodium bicarbonate- 1-12 mEq HCl sodium citrate- 1- 10 mEq HCl
  2. 2. Non-Systemic ANC Magnesium Hydroxide 1- 30 mEq HCl Magnesium trisilicate 1- 10 mEq HCl Aluminium Hydroxide gel 1- 2.5 mEq HCl Magaldrate 1- 28 mEq HCl Calcium carbonate 1- 20 mEq HCl
  3. 3. Treatment of Peptic Ulcer
  4. 4. ACh PGE 2 Histamine Gastrin Adenyl cyclase ATP cAMP Protein Kinase (Activated) Ca ++ Ca ++ Proton pump K K + H + Gastric acid Parietal cell Lumen of stomach H 2 M PGE receptor Gastrin receptor Proglumide _ + + Antacid Omeprazole _ _ _ _ + + + + + + Misoprostol Ranitidine Pirenzepine _
  5. 5. <ul><li>Reversible competitive inhibitors of H 2 receptor </li></ul><ul><li>Highly selective, No action on H 1 or H 3 receptors </li></ul><ul><li>Very effective in inhibiting nocturnal acid secretion ( as it depends largely on Histamine ) </li></ul><ul><li>Modest impact on meal stimulated acid secretion (As it depends on gastrin, acetyl choline and histamine) </li></ul>Histamine H 2 Receptor Antagonist
  6. 6. Bioavailability 80 50 40 >90 Relative Potency 1 5 -10 32 5 -10 Half life (hrs) 1.5 - 2.3 1.6 - 2.4 2.5 - 4 1.1 -1.6 Duration of 6 8 12 8 action (hrs) Inhibition of 1 0.1 0 0 CYP 450 Dose mg(bd) 400 150 20 150 Cimetidine Ranitidine Famotidine Nizatidine
  7. 7. H 2 Blockers- Uses 1. Duodenal ulcer 2. Gastric ulcer 3. Stress ulcers and gastritis 4. Zollinger-Ellison syndrome 5. Gastroesophageal reflux disease (GERD)
  8. 8. H 2 Blockers–Side effects & Interactions <ul><li>Extremely safe drugs </li></ul><ul><li>Cimetidine causes gynecomastia, galactorrhea </li></ul><ul><li>( as it is antiandrogenic & increases orolactin level ) </li></ul><ul><li>Cimetidine inhibits CYP450 & increases conc. of Warfarin, Theophylline, Phenytoin, Ethanol. </li></ul>
  9. 9. Proton Pump Inhibitors (PPIs) <ul><li>Most effective drugs in antiulcer therapy </li></ul><ul><li>Irreversible inhibitor of H + K + ATPase </li></ul><ul><li>Prodrugs requiring activation in acid environment </li></ul><ul><li>Weakly basic drugs & so accumulate in canaliculi of parietal cell </li></ul><ul><li>Activated in canaliculi & binds covalently to extracellular domain of H + K + ATPase </li></ul><ul><li>Acid secretion resumes only after synthesis of new molecules </li></ul>
  10. 10. Drugs Omeprazole 20 mg o.d. Esomeprazole 20 - 40 mg o.d. Lansoprazole 30 mg o.d. Pantoprazole 40 mg o.d. Rabeprazole 20 mg o.d.
  11. 11. Proton Pump Inhibitors – Kinetics <ul><li>Given as enteric coated granules in capsule or enteric coated tablets </li></ul><ul><li>Pantoprazole also given intravenously </li></ul><ul><li>Half life – 1.5 hrs </li></ul><ul><li>Since it requires acid for activation - given 1 hr before meals </li></ul><ul><li>Other acid suppressing agents not coadministered </li></ul>
  12. 12. Uses 1. Gastric ulcer 2. Zollinger-Ellison syndrome 3. Gastroesophageal reflux disease (GERD) Note : drug of choice for NSAID induced gastric/duodenal ulcer
  13. 13. P.P.I. – Side effects & Interactions <ul><li>Extremely safe drugs </li></ul><ul><li>Causes hypergastrinemia which leads to carcinod tumor in rats </li></ul><ul><li>But no evidence of such tumors in man </li></ul><ul><li>Inhibit CYP 450 & hence metabolism of warfarin, phenytoin, etc </li></ul><ul><li>Pantoprazole & Rabeprazole have no significant interactions </li></ul>
  14. 14. Prostaglandin Analogues <ul><li>Misoprostil, Enprostil, Rioprostil. </li></ul><ul><li>Inhibit acid secretion </li></ul><ul><li>↑ mucus and HCO 3 - secretion </li></ul><ul><li>Short duration of action </li></ul>
  15. 15. Misoprostol <ul><li>PGE 1 analogue </li></ul><ul><li>Modest acid inhibition </li></ul><ul><li>Stimulate mucus & bicarbonate secretion </li></ul><ul><li>Enhance mucusal blood flow </li></ul><ul><li>Approved for prevention of NSAID induced ulcer </li></ul><ul><li>Diarrhoea & cramping abd. pain – 20 % </li></ul><ul><li>Not so popular as P.P.I are more effective & better tolerated </li></ul>
  16. 16. Uses 1. NSAID associated GI disease 2. Patients not responding to H 2 blocker 3. Ulcer Patients who continue to smoke Side effects Diarrhoea Abdominal cramps Abortion
  17. 17. Anticholinergics Pirenzipine - M 1 selective Propantheline Oxyphenonium Atropine ↓ volume of gastric juice
  18. 18. Mucosal Protective Agents/Ulcer protectives <ul><li>Sucralfate </li></ul><ul><li>Colloidal Bismuth compounds </li></ul>
  19. 19. Sucralfate <ul><li>Salt of sucrose complexed to sulfated aluminium hydroxide </li></ul><ul><li>In acidic pH polymerises to viscous gel that adheres to ulcer crater </li></ul><ul><li>Taken on empty stomach 1 hr. before meals </li></ul><ul><li>Concurrent antacids, H 2 antagonist avoided </li></ul><ul><li>( as it needs acid for activation ) </li></ul>
  20. 20. Colloidal Bismuth Compounds <ul><li>Coats ulcer, stimulates mucus & bicarbonate secretion </li></ul><ul><li>Direct antimicrobial activity against H.pylori </li></ul><ul><li>May cause blackening of stools & tongue </li></ul><ul><li>Not used for long periods – bismuth toxicity </li></ul><ul><li>Available compounds : </li></ul><ul><li>Bismuth subsalicylate – in USA </li></ul><ul><li>Bismuth sobcitrate – in Europe </li></ul><ul><li>Bismuth dinitrate </li></ul>
  21. 21. Ulcer Healing Drugs <ul><li>Carbenoxolone sodium </li></ul><ul><li>Steroid </li></ul><ul><li>Derivative of glycyrrhetinic acid </li></ul><ul><li>Augmentation of mucus production </li></ul><ul><li>Prolongation of lifespan of gastric epithelial cells </li></ul><ul><li>Prevention of bile reflux </li></ul><ul><li>Slowing of PG degradation in gastric mucosa </li></ul><ul><li>Side effect </li></ul><ul><li>Mineralocorticoid action </li></ul>
  22. 22. Eradication of H.pylori (Anti-H.Pylori Drugs) Triple Therapy Omeprazole / Lansoprazole - 20 / 30 mg bd Clarithromycin - 500 mg bd Amoxycillin / Metronidazole - 1gm / 500 mg bd <ul><li>Given for 14 days followed by P.P.I for 4 – 6 weeks </li></ul><ul><li>Short regimens for 7 – 10 days not very effective </li></ul>
  23. 23. Some other Triple Therapy Regimens are <ul><li>Bismuth subsalicylate – 2 tab qid </li></ul><ul><li>Metronidazole - 250 mg qid </li></ul><ul><li>Tetracycline - 500 mg qid </li></ul><ul><li>Ranitidine Bismuth citrate - 400 mg bd </li></ul><ul><li>Tetracycline - 500 mg bd </li></ul><ul><li>Clarithromycin / Metronidazole - 500 mg bd </li></ul>
  24. 24. Quadruple Therapy <ul><li>Given when Triple Therapy fails </li></ul><ul><li>Omeprazole / Lansoprazole - 20 / 30 mg bd </li></ul><ul><li>Bismuth subsalycilate - 2 tabs qid </li></ul><ul><li>Metronidazole - 250 mg qid </li></ul><ul><li>Tetracycline - 500 mg qid </li></ul>
  25. 25. Thank You

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