3第三章药效学

1、Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Chapter 3 药物对机体的作用药物对机体的作用 药效学药效学 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Object 掌握掌握有关概念有关概念 药药物的治疗疗效果 不良反 应应 效能和效价 TI 亲亲和力 内在活 性 pD2 激动药动药 部分激动动剂剂 竞竞 争性拮抗药药 熟悉熟悉 药药物的基本作用 量效关系及曲线线 非竞竞争性拮抗药药 受体调节调节 了解了解 量 质质反应应 量效曲线线斜率与个 体差异 受体的类类型 第二信使 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Pharmacodynamics include 1 Basic action 2 Therapeutic effect 3 Adverse rea

2、ction 4 Dose effect relationship 5 Mechanism of action Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 1 Basic action of drug Drug action 药药物作用 drugcell primary action 始初作用 molecular reactive mechanism pharmacological effect 药药理效应应 respond of body to drug action result Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Basic actionBasic action excitation inhibition the body functional alterations Guangdong University of TechnologyGuangdong Uni

3、versity of Technology 轻工化工学院 specificity 特异性 eg atropine M R selectivity 选择选择 性 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 the specificity of drug is stronger its selectivity is also higher Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Drug action has double edged Therapeutic effect adverse reaction Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Therapeutic effect Etiological 对对因 treatment e g antibiotics

4、 Symptomatic 对对症 treatment e g analgesics Supplementary 补补充 therapy e g ferrous sulfate Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Etiologic treatment or symptomatic treatment which do you prefer 急则治其标 缓则治其本 标本兼治 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Adverse reaction 不良反应应 unrelated to the therapeutic aim 治疗疗目的 results in discomfort 不适 or harmful 伤伤害 expectable not all could be avoided 可预见预见 Drug induced disease 药药源性疾病 a few

5、serious irreversible ADRa few serious irreversible ADR e g gentamicin deafness 耳聋聋 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 1 Side reaction 副反应应 At the therapeutic dose unrelated to the therapeutic aim Most slight and expectable 预预知 can be allayed 减轻轻 For example atropine mouth dry heart throb 心悸 ephedrine CNS Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 2

6、 Toxic reaction 毒性反应应 dose is overlarge or over accumulation 蓄 积过积过 多 of drug in the body serious reactions may be expectable should be avoided Acute toxicity chronic toxicity Circulation Respiratory Nervous liver kidney bone marrow Endocrine Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Latent toxicity 潜在性毒性 Carcinogenesis 致癌作用 Teratogenesis 致畸作用 Mutagenesis 致突变变作用 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Thalidomide沙利度胺 太胺呱啶酮 太谷山

7、亚胺 太咪呱啶酮 phocomelia 海豹肢症 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 3 residual effect 后遗遗效应应 after the withdraw 停药药 B C D pD2 A B C D A B C D Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Classification of drugs acting on R Agonist Antagonist Full Partial affinityaffinity high 1 high

8、0 1 激动药动药 拮抗药药 Competitive noncompetitive high 0 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Competitive antagonistCompetitive antagonist 竞竞争性拮抗药药 可逆性地与激动药动药 竞竞争同一受体 使激动药动药 的量效曲线线平行右移 Emax不变变 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 拮抗参数 pA2 definition 当拮抗剂剂与激动药动药 合用时时 激动药剂动药剂 量加倍才能达到原效应应 此时时所需的竞竞争 性拮抗剂负对剂负对 数浓浓度为为pA2 Significance of pA2 1 pA2 is larger antagonism is stronger 2 Estimate characters of agonist Guangdong University

9、of TechnologyGuangdong University of Technology 轻工化工学院 Noncompetitive Noncompetitive antagonistantagonist 非竞竞争性拮抗药药 不是与激动药动药 竞竞争同一受体或与受体形成 不可逆性结结合 使激动药动药 的量效曲线线右移 Emax降低 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 others Spare receptor 储备储备 受体 Two status theory 二态态学说说 of receptor Ra active 活动态动态 Ri inactive 静息态态 Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Types of receptor G Protein Coupled Receptor G蛋白耦联联受体 Adr R 5 HT R DA R M R Gu

10、angdong University of TechnologyGuangdong University of Technology 轻工化工学院 Ligand gated ion channel receptor 配体门门控离子通道受体 N R GABA R Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Tyrosine protein kinase receptor 酪氨酸激酶受体 Insulin growth hormone Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Cytosolic receptor 细细胞内受体 Corticosteroids thyroid hormone vitamin D Guangdong University of TechnologyGuangdong University of Technology 轻工化工学院 Intracell

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