Pharmacokinetic interactions: Enzyme induction, Enzyme inhibition. Adverse effects: Side reaction, Toxic reaction; Allergic reaction, Secondary reacti

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1 上海中医药大学授课教案课程名称 : 药理学 ( 全英语 ) 授课教师 : 沈云辉授课时间 :2011 年度 1 学期 2 周 Content 1. 2 药动学 (Pharmacokinetics Pharmacokinetics) Purposes and demands Have a good grasp of the concepts of Pharmacokinetics. Understand well the factors that determine the drug fate in the human body. Teaching content Pharmacokinetics deals with the ways of drug disposition including its absorption, distribution, metabolism, and excretion. The way of drug transportation; 1 passive transport; active transport; the factors that affect the transportation : Cell membrane ; Lipid solubility, Size,concentration and pka value of the drug; ph of the environment where the drugs dissolve. 2the concept of active transport: (the special transportation), against concentration, energy consume, specific carrier. 1. Drug absorption: route of drug administration, factors that affect the absorption. 2.Drug distribution: factors that affect the Drug distribution;(physiochemical properties of the drugs, ph of the tissue fluids Ratio of the drug bound to plasma albumin or globulin or tissue;.membrane barrier, Blood-brain barrier; Placental barrier. 3.Drug metabolism: Sites of metabolism- liver, Orally administration:first-pass metabolism Phase 1 metabolic reactions. Phase 1 and Phase 2 metabolic reactions, Enzyme induction;enzyme inhibition 4.Drug excretion: Renal;Gastrointestinal 5.Mathematical aspects of pharmacokinetics: Half-life(t1/2); Steady-state; Bioavailabilit Time planed: 2.5h and other organs Kinetic order; 第页教具时间分配使用教材和参考书 Time planed:2.5h textbook Principles of Pharmacology reference The Pharmacological Basis of Therapeutics 1.3 Drug interactions and adverse effects Purposes and demands Master the types of drug interactions and adverse effects. Teaching content Pharmacodynamic interaction : Antagonism, Potentiation, Additive effect.

2 Pharmacokinetic interactions: Enzyme induction, Enzyme inhibition. Adverse effects: Side reaction, Toxic reaction; Allergic reaction, Secondary reaction, Residual effects, Drug dependent, Carcinogenic reaction, Teratogenesis, Mutagenesis Time planed: 0.5h Thinking cap 1.What factors affect drug absorption and distribution? 2. Describe the main sites and mechanisms of drug metabolism and excretion. Glossary disposition 处置 absorption 吸收 distribution 分布 metabolism 代谢 excretion 排泄 Topical 局部给药 Enteral 消化道给药 Oral 口服 Sublingual 舌下给药 Rectal 直肠给药 Parenteral 非消化道给药 intravenous (iv) 静脉注射给药 subcutaneous (sc ) 皮下注射给药 intramuscular (im) 肌内注射给药 transdermal 经皮给药 patch 贴膜 passive transport 被动转运 simple diffusion 简单扩散 active transport 主动转运 Half-life (t1/2) 半衰期 plasma albumin 血浆蛋白 Apparent volume of distribution (Vd) 表观分布容积 Blood-brain barrier 血脑屏障 Placental barrier 胎盘屏障 First-pass metabolism 首过代谢 First-pass effect 首过效应 Phase 1 metabolic reactions 第一相反应 Oxidation 氧化 Reductions 还原 Hydrolysis 水解 Phase 2 metabolic reactions 第二相反应

3 Conjugation 结合反应 Enzyme induction 酶的诱导作用 : Enzyme inhibition 酶的抑制作用 : Enzyme inducer: 能增强药酶活性的药 Enzyme inhibitor: 能减弱药酶活性的药 Renal excretion 经肾排泄 Glomerular filtration 肾小球滤过 Tubular secretion 肾小管分泌 Tubular reabsorption 肾小管重吸收 Gastrointestinal excretion 胃肠道排泄 Bile excretion 胆汁排泄 Enterohepatic circulation 肝肠循环 Zero-order kinetic 零级动力学恒量消除 First-order kinetic 一级动力学恒比消除 Two-compartment model 二室模型 Central compartment 中央室 Peripheral compartment 周边室 Steady-state 稳态血浓度 Bioavailability 生物利用度 Drug interaction 药物的相互作用 Antagonism 拮抗 Potentiation 增强作用 Additive effect 相加作用 Enzyme induction 酶的诱导作用 : Enzyme inhibition 酶的抑制作用 Adverse effects 不良反应 Side reaction 副作用 Toxic reaction 毒性作用 Allergic reaction 变态反应 Secondary reaction 继发反应 Residual effects 后遗反应 Drug dependent 药物依赖性 Carcinogenic reaction 致癌作用 Teratogenesis 致畸作用 Mutagenesis 致突变作用 Preview: Somatic and autonomic nervous system 2.1 Autonomic nervous system and drugs acting on the sympathetic system

4 1. The classification of autonomic nervous system. 2. The transmitters of autonomic nervous system and their actions 3. Effects mediated by M N 1 N 2 α,β 1,β 2 and D receptors 4.Effects of ganglion-stimulatiing or -blocking drugs, Presynaptic agents, Sympathomimetics,,Noradrenoline, Metaraminol, Phenylephrine, Adrenaline Isoprenaline, Dobutamine(, Adrenoceptor antagonists : Phentolamine, Prazosin, β -adrenoceptor blockers, β-adrenoceptor antagonists, propranolol, metoprolol,, labetalol 撰写人 : 沈云辉教研室 : 药理撰写日期 : 可加页

Half- 4. Drug excretion: Renal;Gastrointestinal and other organs 5. Mathematical aspects of pharmacokinetics: Kinetic order; life(t1/2); Steady-state;

Half- 4. Drug excretion: Renal;Gastrointestinal and other organs 5. Mathematical aspects of pharmacokinetics: Kinetic order; life(t1/2); Steady-state; 上海中医药大学授课教案课程名称 : 药理学 ( 双语 ) 授课教师 : 陈长勋授课时间 :2006 2006~2007 2007 学年第二学期第 24 周内容 1. 2 药动学 (Pharmacokinetics Pharmacokinetics) 目的要求掌握药动学的一些基本概念熟悉影响