组胺和抗组胺药
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Gastric ulcer
❷ Erosive Esophagitis ❸ Hypersecretory Conditions
H2 receptor antagonists
Toxicity
Gastrointestinal reaction,
CNቤተ መጻሕፍቲ ባይዱ reaction,
Endocrine system reaction Cytochrome P-450 inhibition
Ranitidine Famotidine Nizatidine
H2 receptor antagonists
Receptor Subtype
Pharmacodynamics
Effects after being activated
Expand blood vessel Permeability↑ stimulate sensory nerve endings Cardiovascular system Cause gastric acid, gastric pepsin and intrinsic factor production. 2 H immunological regulation and Cause a decrease in systolic diastolic blood pressure and a increase in heart rate.
Histamine and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
H2 receptor antagonists
Chemistry & Pharmacokinetics
Cimetidine
Cimetidine, ranitidine
H3
R-αMethylhistamine
Thioperamide
Histamine
Receptor Subtype
Pharmacodynamics
Effects after being activated
bronchoconstriction and contraction ❶ of intestinal S.M.tissue Secretory H1 Expand blood vessel Permeability↑ ❷ stimulate sensory nerve endings Smooth muscle Cause gastric acid, gastric pepsin and intrinsic factor production. H2 ❸ Cardiovascular systolic and Cause a decrease in system diastolic blood pressure and a increase in heart rate.
Histamine
Histamine receptor subtypes
Receptor Subtype Distribution Smooth muscle, endothelium, brain Gastric mucosa, cardiac muscle, mast cells, brain Presynaptic: brain, myenteric plexus, other neurons Postreceptor Mechanism
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 its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
H1 receptor antagonists
Chemistry
First-generation blockers Diphenhydramine, promethazine, astemizole
Histamine and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
Together with endogenous peptides, prostaglandins and Introduction leukotrienes, and cytokines, Histamine is biologically active they are sometimes in many amine that is found called autacoids or local hormones or tissue (such as mast cells basophils ),has complex physiologic and pathologic effects, and is often released locally.
❹ The “triple response”
❹ 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 and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
Histamine Antagonists
Physiologic antagonists Epinephrine Release inhibitors Cromolyn Histamine receptor antagonists H1 receptor antagonists H2 receptor antagonists
Second-generation blockers
Cimetidine, ranitidine
Pharmacokinetics
rapidly absorbed orally widely distributed and the first-generation drugs enter the CNS readily. Most metabolized in the liver Most excreted from the kidney
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
H1 receptor antagonists
Receptor Subtype
Pharmacodynamics Effects after being activated
bronchoconstriction and contraction ❶ Histamine Receptor
of intestinal S.M. Blockade vessel Permeability↑ H1 Expand blood ❷ stimulate sensory nerve endings CNS Inhibition Cause gastric acid, gastric pepsin ❸ and intrinsic factor production. Anticholinoceptor action H2 Cause a anesthesia and Localdecrease in systolic and diastolic blood pressure and a increase in heart rate.
H2
Histamine receptor subtypes
Receptor Partially Selective Partially Selective Subtype Agonists Antagonists H1 H2
2-(m-Flurophenyl)histamine Dimaprit, impromidine, amthamine Diphenhydramine, promethazine, astemizole
H1 receptor antagonists
Clinical Uses
❶ Allergic Reaction ❷ Nausea and Vomiting
❸ Sedation and hypnogenesis
H1 receptor antagonists
Toxicity
Sedation, antimuscarinic action, drug allergy, cardiac arrhythmias (astemizole) and possible teratogenic effects.
Acid bronchoconstriction and contraction secretion and gastric of intestinal S.M. motility H
1
H2 receptor antagonists
Clinical Uses
❶ Peptic Duodenal Ulcer and
H1 H2
↑ IP3,DAG ↑ cAMP
H3
G proteincoupled
Histamine receptor subtypes
Receptor Subtype H1 Effects after being activated bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability↑ stimulate sensory nerve endings Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.
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
❷ Erosive Esophagitis ❸ Hypersecretory Conditions
H2 receptor antagonists
Toxicity
Gastrointestinal reaction,
CNቤተ መጻሕፍቲ ባይዱ reaction,
Endocrine system reaction Cytochrome P-450 inhibition
Ranitidine Famotidine Nizatidine
H2 receptor antagonists
Receptor Subtype
Pharmacodynamics
Effects after being activated
Expand blood vessel Permeability↑ stimulate sensory nerve endings Cardiovascular system Cause gastric acid, gastric pepsin and intrinsic factor production. 2 H immunological regulation and Cause a decrease in systolic diastolic blood pressure and a increase in heart rate.
Histamine and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
H2 receptor antagonists
Chemistry & Pharmacokinetics
Cimetidine
Cimetidine, ranitidine
H3
R-αMethylhistamine
Thioperamide
Histamine
Receptor Subtype
Pharmacodynamics
Effects after being activated
bronchoconstriction and contraction ❶ of intestinal S.M.tissue Secretory H1 Expand blood vessel Permeability↑ ❷ stimulate sensory nerve endings Smooth muscle Cause gastric acid, gastric pepsin and intrinsic factor production. H2 ❸ Cardiovascular systolic and Cause a decrease in system diastolic blood pressure and a increase in heart rate.
Histamine
Histamine receptor subtypes
Receptor Subtype Distribution Smooth muscle, endothelium, brain Gastric mucosa, cardiac muscle, mast cells, brain Presynaptic: brain, myenteric plexus, other neurons Postreceptor Mechanism
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 its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
H1 receptor antagonists
Chemistry
First-generation blockers Diphenhydramine, promethazine, astemizole
Histamine and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
Together with endogenous peptides, prostaglandins and Introduction leukotrienes, and cytokines, Histamine is biologically active they are sometimes in many amine that is found called autacoids or local hormones or tissue (such as mast cells basophils ),has complex physiologic and pathologic effects, and is often released locally.
❹ The “triple response”
❹ 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 and its agonists Histamine antagonists
H1 receptor antagonists
H2 receptor antagonists
Histamine Antagonists
Physiologic antagonists Epinephrine Release inhibitors Cromolyn Histamine receptor antagonists H1 receptor antagonists H2 receptor antagonists
Second-generation blockers
Cimetidine, ranitidine
Pharmacokinetics
rapidly absorbed orally widely distributed and the first-generation drugs enter the CNS readily. Most metabolized in the liver Most excreted from the kidney
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
H1 receptor antagonists
Receptor Subtype
Pharmacodynamics Effects after being activated
bronchoconstriction and contraction ❶ Histamine Receptor
of intestinal S.M. Blockade vessel Permeability↑ H1 Expand blood ❷ stimulate sensory nerve endings CNS Inhibition Cause gastric acid, gastric pepsin ❸ and intrinsic factor production. Anticholinoceptor action H2 Cause a anesthesia and Localdecrease in systolic and diastolic blood pressure and a increase in heart rate.
H2
Histamine receptor subtypes
Receptor Partially Selective Partially Selective Subtype Agonists Antagonists H1 H2
2-(m-Flurophenyl)histamine Dimaprit, impromidine, amthamine Diphenhydramine, promethazine, astemizole
H1 receptor antagonists
Clinical Uses
❶ Allergic Reaction ❷ Nausea and Vomiting
❸ Sedation and hypnogenesis
H1 receptor antagonists
Toxicity
Sedation, antimuscarinic action, drug allergy, cardiac arrhythmias (astemizole) and possible teratogenic effects.
Acid bronchoconstriction and contraction secretion and gastric of intestinal S.M. motility H
1
H2 receptor antagonists
Clinical Uses
❶ Peptic Duodenal Ulcer and
H1 H2
↑ IP3,DAG ↑ cAMP
H3
G proteincoupled
Histamine receptor subtypes
Receptor Subtype H1 Effects after being activated bronchoconstriction and contraction of intestinal S.M. Expand blood vessel Permeability↑ stimulate sensory nerve endings Cause gastric acid, gastric pepsin and intrinsic factor production. Cause a decrease in systolic and diastolic blood pressure and a increase in heart rate.
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