1、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
2、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 AgentsHistamine and its agonistsHistamine antagonistsH1 receptor antagonistsH2 receptor antagonistsHistamineIntroductionHistamine is biologically active amine that is found in many tissue (su
3、ch 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 hormonesHistamine receptor subtypesReceptor Subtype Distributi
4、onPostreceptor MechanismH1 Smooth muscle, endothelium, brain IP3,DAGH2Gastric mucosa, cardiac muscle, mast cells, brain cAMPH3Presynaptic: brain, myenteric plexus, other neuronsG protein-coupledHistamine receptor subtypesReceptor Subtype Effects after being activatedH1bronchoconstriction and contrac
5、tion of intestinal S.M. Expand blood vessel Permeability stimulate sensory nerve endingsH2Cause 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 subtypesReceptor SubtypePartially Sel
6、ective AgonistsPartially Selective AntagonistsH1 2-(m-Flurophenyl)-histamine Diphenhydramine, promethazine, astemizoleH2 Dimaprit, impromidine, amthamine Cimetidine, ranitidineH3 R-Methylhistamine ThioperamideHistaminePharmacodynamics Secretory tissue Smooth muscle Cardiovascular system The “triple
7、response”Receptor Subtype Effects after being activatedH1bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability stimulate sensory nerve endingsH2Cause gastric acid, gastric pepsin and intrinsic factor production.Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.
