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,单击此处编辑母版标题样式,*,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,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,H,1,、,H,2,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。,H,1,、,H,2,受体的划分。,Histamine and Antihistamine Agents,内容,抗组胺药,：,H,1,受体阻断剂：对,H,1,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）。,H,2,受体阻断剂：对,H,2,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,H,1,receptor antagonists,H,2,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,H,1,Smooth muscle, endothelium, brain, IP3,DAG,H,2,Gastric mucosa, cardiac muscle, mast cells, brain, cAMP,H,3,Presynaptic: brain, myenteric plexus, other neurons,G protein-coupled,Histamine receptor subtypes,Receptor Subtype,Effects after being activated,H,1,bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability,stimulate sensory nerve endings,H,2,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,H,1,2-(m-Flurophenyl)-histamine,Diphenhydramine, promethazine, astemizole,H,2,Dimaprit, impromidine, amthamine,Cimetidine, ranitidine,H,3,R-Methylhistamine,Thioperamide,Histamine,Pharmacodynamics,Secretory tissue,Smooth muscle,Cardiovascular system,The “triple response”,Receptor Subtype,Effects after being activated,H,1,bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability,stimulate sensory nerve endings,H,2,Cause gastric acid, gastric pepsin and intrinsic factor production.,Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.,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,Histamine and Antihistamine Agents,Histamine and its agonists,Histamine antagonists,H,1,receptor antagonists,H,2,receptor antagonists,Physiologic antagonists,Epinephrine,Release inhibitors,Cromolyn,Histamine receptor antagonists,H,1,receptor antagonists,H,2,receptor antagonists,Histamine Antagonists,Histamine and Antihistamine Agents,Histamine and its agonists,Histamine antagonists,H,1,receptor antagonists,H,2,receptor antagonists,H,1,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,H,1,receptor antagonists,Pharmacodynamics,Histamine Receptor Blockade,CNS Inhibition,Anticholinoceptor action and Local anesthesia,Receptor Subtype,Effects after being activated,H,1,bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability,stimulate sensory nerve endings,H,2,Cause gastric acid, gastric pepsin and intrinsic factor production.,Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.,H,1,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.,H,1,receptor antagonists,Histamine and Antihistamine Agents,Histamine and its agonists,Histamine antagonists,H,1,receptor antagonists,H,2,receptor antagonists,H,2,receptor antagonists,Chemistry & Pharmacokinetics,Cimetidine,Ranitidine,Famotidine,Nizatidine,H,2,receptor antagonists,Pharmacodynamics,Acid secretion and gastric motility,Cardiovascular system,immunological regulation,Receptor Subtype,Effects after being activated,H,1,bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability,stimulate sensory nerve endings,H,2,Cause gastric acid, gastric pepsin and intrinsic factor production.,Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.,H,2,receptor antagonists,Peptic Duodenal Ulcer and Gastric ulcer,Erosive Esophagitis,Hypersecretory Conditions,Clinical Uses,H,2,receptor antagonists,Toxicity,Gastrointestinal reaction,CNS reaction,Endocrine system reaction,Cytochrome P-450 inhibition,THANK YOU,！,
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