組胺和抗組胺藥

1、組胺和抗組胺藥Histamine and Antihistamine Agents,南開大學 醫(yī)學院張京玲 王侃 代紅勝,Histamine and Antihistamine Agents,目的 了解組胺與變態(tài)反應的關系。掌握抗組胺藥H1、H2受體拮抗劑的作用與應用。,Histamine and Antihistamine Agents,內容 組胺：來源，內源性組胺與過敏反應的關系，作用，為診斷用藥。H1、H2受體的劃

2、分。,Histamine and Antihistamine Agents,內容 抗組胺藥：H1受體阻斷劑：對H1受體的阻斷作用。中樞作用及其它。臨床用途，主要不良反應。苯海拉明、異丙嗪（非那根）、氯苯那敏（撲爾敏）、布克利嗪（安其敏）。H2受體阻斷劑：對H2受體的阻斷作用。西米替?。浊柽溥桑┑囊炙嶙饔茫瑢ο詽儾〉脑u價，不良反應。,,,,,,,H1 receptor antagonists,,H2 receptor an

3、tagonists,Histamine,IntroductionHistamine 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.,Toget

4、her 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,Hist

5、amine,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

6、 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

7、 gastric acid can be seen in malignant anemia and true achlorhydia,,,,,,,H1 receptor antagonists,,H2 receptor antagonists,Physiologic antagonists EpinephrineRelease inhibitors CromolynHistamine rece

8、ptor antagonists H1 receptor antagonists H2 receptor antagonists,Histamine Antagonists,,,,,,,H1 receptor antagonists,,H2 receptor antagonists,H1 receptor antagonists,Chemistry,First-generation blocker

9、sDiphenhydramine, promethazine Second-generation blockers Astemizole, acrivastine,rapidly absorbed orallywidely distributed and the first-generation drugs enter the CNS readily.Most metabolized in the liver Most ex

10、creted from the kidney,Pharmacokinetics,H1 receptor antagonists,Pharmacodynamics,? Histamine Receptor Blockade,? CNS Inhibition,? Anticholinoceptor action and Local anesthesia,H1 receptor antagonists,? Allergic Reaction,

11、? Nausea and Vomiting,? Sedation and hypnogenesis,Clinical Uses,Toxicity,Sedation, antimuscarinic action, drug allergy, cardiac arrhythmias (astemizole) and possible teratogenic effects.,H1 receptor antagonists,,,

12、,,,,H1 receptor antagonists,,H2 receptor antagonists,H2 receptor antagonists,Chemistry & Pharmacokinetics,Cimetidine,Ranitidine,Famotidine,Nizatidine,H2 receptor antagonists,Pharmacodynamics,Acid secretion and gastri

13、c motility,Cardiovascular system,immunological regulation,H2 receptor antagonists,? Peptic Duodenal Ulcer and Gastric ulcer,? Erosive Esophagitis,? Hypersecretory Conditions,Clinical Uses,H2 receptor antagonists,Toxicity