Drugs for Gastrointestinal Tract Disorders 消化系统药物 Classification(分类) Drugs that inhibit gastric acid secretion ·Antacids Cytoprotective drugs Drugs for H.pylori infection ·Digestants Laxatives,catharitics Antidiarrheal agents ·Antiemetic agents 1
1 Drugs for Gastrointestinal Tract Disorders 消化系统药物 Classification (分类) • Drugs that inhibit gastric acid secretion • Antacids • Cytoprotective drugs • Drugs for H. pylori infection • Digestants • Laxatives, catharitics • Antiemetic agents • Antidiarrheal agents
Drugs that inhibit gastric acid 胃酸分祕抑制药 Blood Gastric lumen Epithelial cell上皮细胞 Sucralfate Cytoprotective effect Mucus- Mucus Bicarbonate一 Bicarbonate Misoprostol Parietal cell壁细胞 PG CAMP④ Protein kinases Histamine- H2 质子泵 H Cimetidine, Lansoprazole and famotidine, omeprazole ATPase Aluminum and and ranitidine K hydroxides and calcium Acetylcholine- -M3 carbonate ⑧ Gastrin G 2
2 Drugs that inhibit gastric acid 胃酸分泌抑制药 质子泵 壁细胞 上皮细胞
奥美拉唑Omeprazole Proton Pump Inhibitor(PPL,质子泵抑制剂 A proton pump inhibitor used in the treatment of peptic ulcer disease(PUD),gastroesophageal reflux disease (GORD/GERD),laryngopharyngeal reflux(LPR)and Zollinger-Ellison syndrome. Weak base that enters parietal cells easily A prodrug that is activated in low pH(applies to all PPIs). CYP2C19 metabolized;T=1 h,effect lasts 24-48 h. Other Proton Pump Inhibitor(其它质子泵抑制剂) 兰索拉唑Lansoprazole 泮托拉唑Pantoprazole 雷贝拉唑Rabeprazole 埃索美拉唑Esomeprazole 3
3 奥美拉唑 Omeprazole A proton pump inhibitor used in the treatment of peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux (LPR) and Zollinger–Ellison syndrome. Weak base that enters parietal cells easily A prodrug that is activated in low pH (applies to all PPIs). CYP2C19 metabolized; T ½ = 1 h, effect lasts 24-48 h. Proton Pump Inhibitor (PPI, 质子泵抑制剂) 兰索拉唑 Lansoprazole Other Proton Pump Inhibitor (其它质子泵抑制剂) 泮托拉唑 Pantoprazole 雷贝拉唑 Rabeprazole 埃索美拉唑 Esomeprazole
H2 receptor blocker(H2受体阻断剂) CH2-CH2-NH2 HO CH2-CH2-NH2 N N ○ Histamine Serotonin CH2一N CHa CH2SCH2CH2N =CNHCH3 N N HN一C=N CHa Cimetidine Ondansetron Cimetidine(西咪替丁) A histamine H2-receptor antagonist that inhibits the production of acid in the stomach.It is largely used in the treatment of heartburn and peptic ulcers.Approved in 1976,it is marketed under the trade name Tagamet. Cimetidine is a known inhibitor of many isozymes of the cytochrome P450 enzyme system,specifically CYP1A2, CYP2C9,CYP2C19,CYP2D6,CYP2E1,and CYP3A4. This inhibition forms the basis of the numerous drug interactions that occur between cimetidine and other drugs.For example,cimetidine may decrease metabolism of some drugs. 4
4 H2 receptor blocker (H2 受体阻断剂) A histamine H2-receptor antagonist that inhibits the production of acid in the stomach. It is largely used in the treatment of heartburn and peptic ulcers. Approved in 1976, it is marketed under the trade name Tagamet. Cimetidine is a known inhibitor of many isozymes of the cytochrome P450 enzyme system, specifically CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4. This inhibition forms the basis of the numerous drug interactions that occur between cimetidine and other drugs. For example, cimetidine may decrease metabolism of some drugs. Cimetidine (西咪替丁)
哌仑西平Pirenzepine Pirenzepine is used in the treatment of peptic ulcers,as it reduces gastric acid secretion and reduces muscle spasm.It is in a class of drugs known as muscarinic receptor antagonists(M receptor blockers). Acetylcholine is the neurotransmitter of the parasympathetic nervous system which initiates the rest-and-digest state (as opposed to fight-or-flight),the result being an increase in gastric motility and digestion. It has no effects on the brain and spinal cord as it cannot diffuse through the blood-brain barrier. Antacids 抗酸药 5
5 哌仑西平 Pirenzepine Pirenzepine is used in the treatment of peptic ulcers, as it reduces gastric acid secretion and reduces muscle spasm. It is in a class of drugs known as muscarinic receptor antagonists (M receptor blockers). Acetylcholine is the neurotransmitter of the parasympathetic nervous system which initiates the rest-and-digest state (as opposed to fight-or-flight), the result being an increase in gastric motility and digestion. It has no effects on the brain and spinal cord as it cannot diffuse through the blood-brain barrier. Antacids 抗酸药