上海交通大学：《药理学 Pharmacology》课程教学资源（讲义课件）Chapter 26：Drugs for Digestive Disorders

Chapter 26: Drugs for Digestive Disorders Prof.R.D.Ye 2012-11-19

Chapter 26: Drugs for Digestive Disorders Prof. R.D. Ye 2012-11-19

Classification（分类) I.Drugs for peptic ulcers 胃溃疡 Il.Antiemetics and Prokinetic drugs 止吐药，促进胃肠蠕动药 IlI.Laxatives 泻药 IV.Antidiarrheal drugs 止泻药 V.Choleretic drugs 促胆汁分泌药

Classification (分类 ) II. Antiemetics and Prokinetic drugs I. Drugs for peptic ulcers III. Laxatives IV. Antidiarrheal drugs V. Choleretic drugs 止吐药，促进胃肠蠕动药 胃溃疡 泻药 止泻药 促胆汁分泌药

Drugs for peptic ulcers I.Antacids and inhibitors of gastric acid secretion 抗酸药 ll.Mucosal protective drugs 胃粘膜保护药 Ill.Drugs against H.pylori infection 抗幽门螺旋杆菌药

I. Antacids and inhibitors of gastric acid secretion II. Mucosal protective drugs III. Drugs against H. pylori infection Drugs for peptic ulcers 抗酸药 胃粘膜保护药 抗幽门螺旋杆菌药

Antacids 抗酸药

Antacids 抗酸药

Aluminium hydroxide 氢氧化铝 (also magnesium hydroxide) 氢氧化鎂 This compound is used as an antacid.The hydroxide reacts with excess acid in the stomach,reducing its acidity.This decreases acidity of the contents of the stomach and may in turn help to relieve the symptoms of ulcers,heartburn or dyspepsia.It can also cause constipation and is therefore often used with magnesium hydroxide or magnesium carbonate,which have counterbalancing laxative effects.It is also used to control phosphate(phosphorus)levels in the blood of people suffering from kidney failure

Aluminium hydroxide 氢氧化铝 This compound is used as an antacid. The hydroxide reacts with excess acid in the stomach, reducing its acidity. This decreases acidity of the contents of the stomach and may in turn help to relieve the symptoms of ulcers, heartburn or dyspepsia. It can also cause constipation and is therefore often used with magnesium hydroxide or magnesium carbonate, which have counterbalancing laxative effects. It is also used to control phosphate (phosphorus) levels in the blood of people suffering from kidney failure. (also magnesium hydroxide) 氢氧化鎂

Calcium carbonate 碳酸钙 Sodium bicarbonate 碳酸钠 Their pharmacological effect is produced by reacting with HCI to form carbon dioxide and CaCl,(and NaCl in the case of sodium bicarbonate).In doing so,the two drugs reduce HCI in the stomach. Side effects are those caused by excessive CO2(belching, gastric distention).Unreacted alkali can be absorbed and can produce alkalosis

Calcium carbonate 碳酸钙 Their pharmacological effect is produced by reacting with HCl to form carbon dioxide and CaCl2 (and NaCl in the case of sodium bicarbonate). In doing so, the two drugs reduce HCl in the stomach. Side effects are those caused by excessive CO2 (belching, gastric distention). Unreacted alkali can be absorbed and can produce alkalosis. Sodium bicarbonate 碳酸钠

Drugs that inhibit gastric acid 胃酸分泌抑制药 H2-receptor antagonists, Proton pump inhibitors(PPI), Antimuscarinic drugs, Antagonist of gastrin receptor

Drugs that inhibit gastric acid 胃酸分泌抑制药 • H2-receptor antagonists, • Proton pump inhibitors (PPI), • Antimuscarinic drugs, • Antagonist of gastrin receptor

Blood Gastric lumen Epithelial cell上皮细胞 Sucralfate Cytoprotective effect Mucus Mucus ⊕ Bicarbonate Bicarbonate PG Misoprostol Parietal cell壁细胞 PG cAMP ⊕ ⊕ Protein kinases Histamine ⊕ 质子泵 H+/ Cimetidine, Lansoprazole and famotidine, omeprazole ATPase Aluminum and and ranitidine magnesium K+ hydroxides and calcium ⊕ Acetylcholine →M3 Ca2+ carbonate Gastrin- G

质子泵 壁细胞 上皮细胞

Cimetidine CH3 CH2SCH2CH2N=CNHCH3 (also ranitidine,famotidine,nizatidine) HN一C三N H2-R antagonist 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

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 (also ranitidine, famotidine, nizatidine) H2-R antagonist

Omeprazole Proton Pump Inhibitor(PPI) 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. A weak base that enters parietal cells easily,has short serum half-life,long duration of action,and highly effective. A prodrug that is activated in low pH (applies to all PPIs)

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. A weak base that enters parietal cells easily, has short serum half-life, long duration of action, and highly effective. A prodrug that is activated in low pH (applies to all PPIs). Proton Pump Inhibitor (PPI) 质子泵抑制剂