藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物

1、組胺和抗組胺藥Histamine and Antihistamine Agents張京玲 王侃 代紅勝藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine Agents目的了解組胺與變態(tài)反應(yīng)的關(guān)系。掌握抗組胺藥H1、H2受體拮抗劑的作用與應(yīng)用。藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine Agents內(nèi)容組胺：來源，內(nèi)源性組胺與過敏反應(yīng)的關(guān)系，作用，為診斷用藥。H1、H2受體的劃分。藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine Agents內(nèi)容抗組胺藥：H1受體阻斷

2、劑：對(duì)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(yīng)。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(duì)H2受體的阻斷作用。西米替丁（甲氰咪呱）的抑酸作用，對(duì)消化性潰瘍病的評(píng)價(jià)，不良反應(yīng)。藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine AgentsHistamine and its agonistsHistamine antagonistsH1 receptor antagonistsH2 receptor antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物HistamineIntroducti

3、onHistamine 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 autacoi

4、ds or local hormones藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine receptor subtypesReceptor SubtypeDistributionPostreceptor MechanismH1Smooth muscle, endothelium, brain IP3,DAGH2Gastric mucosa, cardiac muscle, mast cells, brain cAMPH3Presynaptic: brain, myenteric plexus, other neuronsG protein-coupled藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的

5、藥物Histamine receptor subtypesReceptor SubtypeEffects after being activatedH1 bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability stimulate sensory nerve endingsH2 Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and

6、diastolic blood pressure and a increase in heart rate.藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine receptor subtypesReceptor SubtypePartially Selective AgonistsPartially Selective AntagonistsH12-(m-Flurophenyl)-histamineDiphenhydramine, promethazine, astemizoleH2Dimaprit, impromidine, amthamineCimetidine, ranitidine

7、H3R-MethylhistamineThioperamide藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物HistaminePharmacodynamics Secretory tissue Smooth muscle Cardiovascular system The “triple response”Receptor SubtypeEffects after being activatedH1 bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability stimulate senso

8、ry nerve endingsH2 Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物 The “triple response” Intradermal injection of histamine causes a characteristic wheal-and-flare response,

9、which involves an erythema, an edematous wheal and a red irregular flare surrounding the wheal.藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物HistamineHistamineClinical 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 achlorh

10、ydia藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine AgentsHistamine and its agonistsHistamine antagonistsH1 receptor antagonistsH2 receptor antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Physiologic antagonists EpinephrineRelease inhibitors CromolynHistamine receptor antagonists H1 receptor antagonists H2 receptor anta

11、gonistsHistamine Antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine AgentsHistamine and its agonistsHistamine antagonistsH1 receptor antagonistsH2 receptor antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H1 receptor antagonistsChemistryFirst-generation blockersDiphenhydramine, promethazine, astemizoleSecond-gene

12、ration blockers Cimetidine, ranitidine藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物rapidly absorbed orallywidely distributed and the first-generation drugs enter the CNS readily.Most metabolized in the liver Most excreted from the kidneyPharmacokinetics藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H1 receptor antagonistsPharmacodynamics Histamine Recept

13、or Blockade CNS Inhibition Anticholinoceptor action and Local anesthesiaReceptor SubtypeEffects after being activatedH1 bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability stimulate sensory nerve endingsH2 Cause gastric acid, gastric pepsin and intrinsic factor pr

14、oduction. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H1 receptor antagonists Allergic Reaction Nausea and Vomiting Sedation and hypnogenesisClinical Uses藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Toxicity Sedation, antimuscarinic action, drug al

15、lergy, cardiac arrhythmias (astemizole) and possible teratogenic effects.H1 receptor antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物Histamine and Antihistamine AgentsHistamine and its agonistsHistamine antagonistsH1 receptor antagonistsH2 receptor antagonists藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H2 receptor antagonistsChemistry & Pharma

16、cokineticsCimetidineRanitidineFamotidineNizatidine藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H2 receptor antagonistsPharmacodynamicsAcid secretion and gastric motilityCardiovascular systemimmunological regulationReceptor SubtypeEffects after being activatedH1 bronchoconstriction and contraction of intestinal S.M. Expand blo

17、od vessel Permeability stimulate sensory nerve endingsH2 Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物藥理學(xué)南開大學(xué)影響自體活性物質(zhì)的藥物H2 receptor antagonists Peptic Duodenal Ulcer and Gastric