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。 Histamine and Antihistamine Agents Histamine and its agonists Histamine antagonists 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 Receptor Subtype Distribution Postreceptor Mechanism H1 Smooth muscle, endothelium, brain ↑ IP3,DAG H2 Gastric mucosa, cardiac muscle, mast cells, brain ↑ cAMP H3 Presynaptic: brain, myenteric plexus, other neurons G protein-coupled Histamine receptor subtypes Receptor Subtype Effects after being activated H1 bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability↑ stimulate sensory nerve endings H2 Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate. Histamine receptor subtypes Receptor Subtype Partially Selective Agonists Partially Selective Antagonists H1 2-(m-Flurophenyl)-histamine Diphenhydramine, promethazine, astemizole H2 Dimaprit, impromidine, amthamine Cimetidine, ranitidine H3 R-α-Methylhistamine Thioperamide Histamine Pharmacodynamics ? Secretory tissue ? Smooth muscle ? Cardiovascular system ? The “triple response” Receptor Subtype Effects after being activated H1 bronchoconstriction and contraction of