医学ppt课件药物的基本作用

Pharmacodynamics 3 Site of action Mechanisms Effects Clinical uses Target Drug Changes in Living system Effect 药理作用 (Action) 作用机制 (Action mechanism) 兴奋 Exicitation 抑制 Inhibition 掌握： （ 1） ADR （ 2） Con.-Effect Curve （ 3） Receptor （ 4） Drug Classification 第一节 药物的基本作用 Effects of Drugs Target Drug Changes in Living sysytem Effect 药理作用 (Action) (Action mechanism) Selectivity 选择性 Specificity 特异性 一、药物作用与药理效应（药效） Action and Effect of Drug Therapeutic Effect Adverse Reaction 二、治疗效果 Therapeutic Effects 1.Etiological Treatment 2.Symptomatic Treatment 急则治其标 缓则治其本 标本应兼治 二、不良反应 Adverse Reactions 1. 副反应与毒性反应 （ Side reaction and Toxicity） Adverse drug reaction (ADR)： An expression that describes harm associated with the use of given medications at a normal dose. The meaning of this expression differs from the meaning of “side effect“, as this last expression might also imply that the effects can be beneficial. 副作用包括不良反应？现行的不良反应概念似乎与书本不同。毒性反 应医生要负责，不良反应就不必负完全责任。 不良反应 较常见的有恶心、呕吐、上腹部不适或疼痛等胃肠道反应。较少 见或罕见的有（ 1）胃肠道出血或溃疡，表现为血性或柏油样便， 胃部剧痛或呕吐血性或咖啡样物，多见于大剂量服药患者。（ 2） 支气管痉挛性过敏反应，表现为呼吸困难或哮喘。（ 3）皮肤过敏 反应，表现为皮疹、荨麻疹、皮肤瘙痒等。（ 4）血尿、眩晕和肝 脏损害 。 禁忌 孕妇、哺乳期妇女禁用。 哮喘、鼻息肉综合征、对阿司匹林和其他解热镇痛药。 Toxic reactionToxicity： Over dose or too long time l Acute/Chronic toxicity l Teratogenesis l Carcinogenesis l Mutagenesis 三致 2. After effect and Withdrawal Reaction 后遗效应和停药反应 0 20 40 60 80 100 120 0 2 4 6 8 10 3. Allergy and Idiosyncrasy Idiosyncratic drug reaction denotes a non immunological hypersensitivity to a substance, without connection to pharmacological toxicity. Most commonly, this is caused by an enzymopathy, congenital or acquired. 第二节 药物剂量 -效应关系 Dose-effect Relationship Em % Conc. of Drug 100% 50% 0 (EC50或 ED50) 100 patients LD50: Dose with 50% animal death 越大越安全？ Therapeutic Index: TI, safety 第三节 药物与受体 Drug and Receptors D + R DR E KD = DR DR RT = R + DR DR D RT KD + D = E DR D Emax RT KD+D = = Affinity = pD2 = -log KD Intrinsic Activity = Which one has the greater ? What ablout their affinity? Which one has the greater ? What ablout their affinity? 1. Agonist: Full Agonist Partial Agonist 2. Antagonist: Competitive Antagonist Irreversible Antagonist 四、作用于受体的药物分类 Receptor Drug Calssification 阿司匹林和血小板的酶化学键结合，要物消失，作用还在。 阿霉素也如此嵌入癌细胞 DNA。大小： 100-1000，太小，选择 性查，太大，灵活性差。形态：决定选择性的重要因素。激 动剂制和受体结合么，其实很多位点，对 PK有影响。 Which ones are Full Agonists? Agonist Con. Of drug Efficacy （ % ） Competitive Antagonist Irriversible Antagonist 五、受体类型 Receptor Types （一） G蛋白藕连受体 G protein-coupled receptors (1) Receptor (2) G protein (3) Adenylate cyclase(AC) or Phospholipase C(PLC) or Ca,Na Channels （二 ) 配体门控离子通道受体 Ligand-Gated Ion Channel Receptor A group of transmembrane ion channels that are opened or closed in response to the binding of a chemical messenger (i.e., a ligand),such as a neurotransmitter （三）酪氨酸蛋白激酶受体 Tyrosine Kinase Recptor High affinity cell surface receptors for many polypeptide growth factors, cytokines and hormones 六、细胞内信号转导 Signaling Mechanisms cAMP cGMP Phosphatidylinositol Ca2+ 七、受体调节 Receptor Regulation 1. Desensiti