药理学PPT课件（南开大学）第十五章影响自体活性物质的药物.ppt

组胺和抗组胺药 Histamine and Antihistamine Agents,南开大学 医学院 张京玲 王侃 代红胜,Histamine and Antihistamine Agents,目的 了解组胺与变态反应的关系。掌握抗组胺药H1、H2受体拮抗剂的作用与应用。,Histamine and Antihistamine Agents,内容 组胺：来源，内源性组胺与过敏反应的关系，作用，为诊断用药。H1、H2受体的划分。,Histamine and Antihistamine Agents,内容 抗组胺药：H1受体阻断剂：对H1受体的阻断作用。中枢作用及其它。临床用途，主要不良反应。苯海拉明、异丙嗪（非那根）、氯苯那敏（扑尔敏）、布克利嗪（安其敏）。H2受体阻断剂：对H2受体的阻断作用。西米替丁（甲氰咪呱）的抑酸作用，对消化性溃疡病的评价，不良反应。,H1 receptor antagonists,H2 receptor antagonists,Histamine,Introduction Histamine is biologically active amine that is found in many tissue (such as mast cells or basophils ),has complex physiologic and pathologic effects, and is often released locally.,Together with endogenous peptides, prostaglandins and leukotrienes, and cytokines, they are sometimes called autacoids or local hormones,Histamine receptor subtypes,Histamine receptor subtypes,Histamine receptor subtypes,Histamine,Pharmacodynamics, Secretory tissue, Smooth muscle, Cardiovascular system, The “triple response”, The “triple response”,Intradermal injection of histamine causes a characteristic wheal-and-flare response, which involves an erythema, an edematous wheal and a red irregular flare surrounding the wheal.,Histamine,Histamine,Clinical use of histamine,To be used in testing gastric acid secretion and diagnosis of leprosy. Decrease of gastric acid can be seen in malignant anemia and true achlorhydia,H1 receptor antagonists,H2 receptor antagonists,Physiologic antagonists Epinephrine Release inhibitors Cromolyn Histamine receptor antagonists H1 receptor antagonists H2 receptor antagonists,Histamine Antagonists,H1 receptor antagonists,H2 receptor antagonists,H1 receptor antagonists,Chemistry,First-generation blockers Diphenhydramine, promethazine, astemizole Second-generation blockers Cimetidine, ranitidine,rapidly absorbed orally widely distributed and the first-generation drugs enter the CNS readily. Most metabolized in the liver Most excreted from the kidney,Pharmacokinetics,H1 receptor antagonists,Pharmacodynamics, Histamine Receptor Blockade, CNS Inhibition, Anticholinoceptor action and Local anesthesia,H1 receptor antagonists, Allergic Reaction, Nausea and Vomiting, Sedation and hypnogenesis,Clinical Uses,Toxicity,Sedation, antimuscarinic action, drug allergy, cardiac arrhythmias (astemizole) and possible teratogenic effects.,H1 receptor antagonists,H1 receptor antagonists,H2 receptor antagonists,H2 receptor antagonists,Chemistry & Pharmacokinetics,Cimetidine,Ranitidine,Famotidine,Nizatidine,H2 receptor antagonists,Pharmacodynamics,Acid secretion and gastric motility,Cardiovascular system,immunological regulation,H2 receptor antagonists, Peptic Duodenal Ulcer and Gastric ulcer, Erosive Esophagitis, Hypersecretory Conditions,Clinical U