药物ppt课件38.组胺与抗组胺药.pptVIP

H2受体阻断药(竞争性) 西咪替丁 雷尼替丁 法莫替丁 相对强度 1 5~10 32 生物利用度 80 50 40 维持时间(h) 6 8 12 抑制P450强度 1 0.1 0 对以基础胃酸分泌为主的夜间胃酸分泌效果好，晚餐后或入睡前给药 十二指肠、胃溃疡、食道炎及其引起的消化道出血疗效较好，不良反应少 4-6周，75%治愈，易复发，延长用药可减少 不良反应 长期大量应用西咪替丁，男性青年可引起勃起障碍、性欲消失及乳房发育 西咪替丁可抑制细胞色素P450肝药酶活性，抑制华法林、苯妥因钠、茶碱、苯巴比妥等代谢 Drug Interactions Cimetidine interferes with several important hepatic cytochrome P450 drug metabolism pathways, the half-lives of some drugs include warfarin, phenytoin, lidocaine, quinidine, propranolol，may be prolonged. It is best to avoid cimetidine in patients using these drugs Questions: What are the pharmacologic actions, clinical uses and adverse effects of H1 receptor antagonists and H2 receptor antagonists? Chapter 30 Drugs Affecting Autacoids影响自体活性物质的药物 School of Pharmaceutical Sciences Autacoids have been described as local hormones. They are grouped together in large part because they participate, at least in some settings, in physiological or pathophysiological response to injury. Autacoids includs : prostaglandins histamine 5-hydroxytryptamine leukotrienes vasoactive peptides, etc 磷脂代谢产物类药物及拮抗药 5-羟色胺药物及拮抗药 组胺及抗组胺药 多肽类 一氧化氮及其供体与抑制剂 腺苷与药理性预适性 影响自体活性物质的药物 Histamine and Antihistamine Drugs 组胺和抗组胺药 I. Histamine(组胺） Histamine is an autacoid and released mainly from mast cells or basophils Marked species variation is observed, but in humans histamine is an important mediator of immediate allergic and inflammatory reactions; has an important role in gastric acid secretion; and functions as a neurotransmitter and neuromodulator Most tissue histamine is bound in granules in mast cells or basophils The bound form of histamine is biologically inactive, but many stimuli can trigger the release of mast cell histamine, allowing the free amine to exert its actions on surrounding tissues Mast cells are especially rich at sites of potential tissue injury—nose, mouth, and feet; internal body surfaces; and blood vessels Non-mast cell histamine is found in several tiss