GERD_胃食管反流英文版试题.ppt

References Bak, Young-Tae. Management Strategies for Gastroesophageal Reflux Disease. Journal of Gastroenterology and Hepatology (2004), 19, S49-S53. Horn, J. Understanding the Pharmacodynamic and Pharmacokinetic Differences between proton pump inhibitors- focus on pKa and metabolism. APT (2006), 2, 340-350. Pettit, M. Treatment of Gastroesophageal Reflux Disease. Pharm World Sci (2005) 27, 432-435. Vakil, N., New Pharmacological Agents for the Treatment of Gastroesophageal Reflux Disease. APT (2006), 19, 1041-1049. Vesper, J.B. et all, Gastroesophageal Reflux Diesease, Is there More to the Story?, ChemMedChem (2008), 3, 552-559. Goodman and Gilman pg 967-980. Patrick pg 643-671. Sucralfate (Carafate) Proton Pump Inhibitors Proton pump inhibitors (PPIs) Inhibits the gastric acid pump, H+/K+ ATPase Are prodrugs PPIs Diffuse into the parietal cells of the stomach and accumulates Activated by proton-catalyzed formation of sulfenic acid This prevents the drug from diffusing out Activated form then irreversibly binds at the sulfhydryl groups of the cysteins of the H+/K+ ATPase Link Cysteine PPIs Rabeprazol (Acipex) PPIs Lansoprazole (Prevacid) PPIs Esomeprazole (Nexium) PPIs Omeprazole (Prilosec) Omeprazole/sodium bicarbonate (Zegerid) PPIs Pantoprazole (Protonix) Treatments Histamine H2-recptor antagonists (H2RAs) The hormone, histamine stimulates the release of acid by interacting with the histamine receptor, or H2 receptor. Inhibit acid secretion by competitively and reversibly blocking parietal cell H2-receptors Less potent then PPI’s Agonist vs. Antagonist An agonist is a drug that produces the same response at a receptor as the natural messenger An antagonist is a drug which binds to a receptor without activating it, prevent an agonist or natural messenger from binding Histamine H2RAs Cimetidine (Tagamet) H2RAs Nizatidine (Axid) Other H2RAs Ranitidine HCl (Zantac) Famotidine (Pepcid) Treatments Prokinetics Increase LES function Release stomach co