第五章 消化系统药 暨南大学药学院_图文.pptVIP

Chapter 5 Digestive System Agents Outline Section 1　Anti-ulcer Agents(抗溃疡药) Section 2　Antiemetics(止吐药) Section 3 Prokinetics(促动力药) Section 4　Adjuvant for Hepatic and Biliary Disease(肝胆疾病辅助治疗药物) Section 1 Anti-ulcer Agents (抗溃疡药) Request and Purpose To master the structure, chemical name, physico-chemical property, metabolism in vivo, and clinical application of Cimetidine (西咪替丁) and Omeprazole(奥美拉唑). To be familiar with Ranitidine Hydrochloride (盐酸雷尼替丁). Get information about synthesis of Cimetidine and Omeprazole. Peptic ulcer (PU,消化性溃疡) Concept: Factors: Helicobacter Pylori (HP 幽门螺杆菌) A Gram-negative spiral bacterium. Infection by HP can damage the feedback mechanism of gastric acid secretion(胃酸分泌). HP found in virtually all patients with DU, and approximately 75% of patients with GU. Risk factors with recurrence of PU Cigarette smoking Chronic use of ulcerogenic drugs Male gender/age Alcohol consumption Emotional stress Family history Physiology of Gastric Acid Secretion Gastric acid is produced by parietal cells (胃壁细胞) in the stomach. Parietal cells contain an extensive secretory network from which the gastric acid is secreted into the lumen(腔) of the stomach. These cells are part of epithelial fundic glands(胃底腺) in the gastric mucosa. The pH of gastric acid is 2 to 3 in the human stomach lumen, the acidity being maintained by the proton pump H+/K+ ATPase. Hormonal regulation of acid secretionby Gastric Parietal Cells(胃壁细胞) Classification Common antiulcer drugs Development of Cimetidine Cimetidine (西咪替丁) N-Cyano-N’-methyl-N’’-[2-[[(5-methyl-1H-imidazol-4-yl)-methyl ]thio]ethyl] guanidine(胍) It is a colorless crystalline solid. Cimetidine (TagametTM ) became the first billion-dollar drug in the 1980s. This medication is also available without a prescription. Physio-chemical property Solubility: Stability: Heating release H2S gas, make lead acetate testing paper show black. Pharmacological action Drug interactions