药理学-药学英语.ppt

,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,*,Unit 2 Pharmacology,assess the effect of different doses on therapeutic effect,use animal models to screen chemicals with anti-tumor activity,measure plasma half life of a drug in body,evaluate toxicity of a candidate drug in men,determine the minimum inhibitory concentration of an antibiotic,evaluate the inhibitory effect of a candidate drug on an enzyme,History,1.Pharmacology studies the effects of drugs and how they exert their effects.,E.g.penicillin kills susceptible bacteria by specifically inhibiting the transpeptidase(,转肽酶,)that catalyzes the final step in cell wall biosynthesis,the cross-linking of peptidoglycan（,肽聚糖,）.,E.g.acetylsalicylic acid（aspirin）,Phospholipids,phospholipase,arachidonic acid(,花生四烯酸,）,cyclooxygenase(,环氧化酶,),prostaglandin(,前列腺素,),inflammation,Inhibit the activity of COX,Enzyme inhibitor 32.4%,Transport protein inhibitor 16.0%,Receptor agonist 9.1%,Receptor antagonist 10.7%,Drugs acting on ion channels 9.1%,DNA,RNA/ribosome,Typically a,drug target,is a key molecule involved in a particular metabolic or signaling pathway that is specific to a disease condition or pathology,or to the infectivity or survival of a microbial pathogen.,A survey in 2000 indicated that:,Definitions,Pharmacology has been defined as an experimental science that studies changes brought about in vivo and in vitro by chemically acting substances,whether used for therapeutic purpose or not.In the broadest sense,pharmacology is the science of studying the effect of drugs on living organisms.It attempts to describe the biological response produced by drugs and to define the underlying mechanisms by which the responses are generated.,Drugs:,Broadly defined,a drug is a chemical substance that can alter or influence the responsiveness of a biological system.The action of a drug is mediated by a naturally occurring process of the body.A drug either mimics,facilitate,or antagonizes a normally occurring phenomenon.,Classification of drugs:,Drugs used to combat infection,Selective toxicity is the ability of a chemical or drug to kill a microorganism without harming its host,Chemotherapy,in its most general sense,is the treatment of a disease by chemicals especially by killing micro-organisms or cancerous cells.,bacteria,Humans,penicillin,cell wall biosynthesis,without cell wall,sulfa drugs,(,磺胺药物,),folic acid synthesis,the synthetic pathway is not needed,Drugs used to replace inadequacies of naturally occurring substance,insulin,:is a,hormone,that is central to regulating energy and glucose metabolism in the body.When insulin is absent,glucose is not taken up by body cells and accumulate,diabetes mellitus,（,糖尿病,）,will result.,L-dopa,:After passing though the blood brain barrier,（,血脑屏障,）,it is,enzymatically,transformed into dopamine,the insufficiency of which will cause parkinsonism(,帕金森症,),Drugs that change regulation,antihypertensives,antianginals,diuretics,anticoagulants,analgesics,antipyretic,sedatives,birth,contrl,pills(contraceptives),Drugs to alter mood or behavior(psychoactive drug,，,精神药物,),a,chemical substance,that crosses the,blood-brain barrier,and acts primarily upon the,central nervous system,where it alters,brain,function,resulting in changes in,perception,mood,consciousness,cognition,and,behavior,。,Drug at site,of administration,Drug in plasma,Drug/metabolites,in urine,feces,bile,Drug/metabolites,in tissues,Absorption,Distribution,Excretion,Biotransformation,1.Pharmacokinetics(,药物代谢动力学,):,Scope,2.Pharmacodynamics（,药物效应动力学,）:,is the study of the physiological effects of drugs on the body or on microorganisms or parasites within or on the body and the mechanisms of drug action，,including the correlation of their actions with concentrations as well as the relationship between the activity and the chemical structure.,Dose-response curve(,量效曲线,),minimum effective dose,maximum,efficacy,（,最大效能,）,median effective dose,slope,（,斜率,）,Structure-activity relationship:the relationship between the chemical or three-dimensional structure of a molecule and its biological activity.The analysis of SAR enables the determination of the chemical groups responsible for evoking a target biological effect in the organism.This allows to modify the effect or the potency of a drug by changing its chemical structure,Preclinical pharmacology(animal pharmacology or comparative pharmacology),Pharmacological studies of candidate drugs in animal systems to provide evidence of their potential activity,serving as predictors of human responses with the goals of assuring safety and effectiveness in humans,Clinical pharmacology:,is the science of drugs and their clinical use.It is underpinned by the basic science of pharmacology,with added focus on the application of pharmacological principles and methods in the real world.It connects the gap between medical practice and laboratory science.The main objective is to promote the safety of prescription,maximize the drug effects and minimize the side effects,Pharmacotherapeutics（,药物治疗学,）:the use of drugs in the prevention and treatment of disease.,Toxicology:the aspect of pharmacology that,deals with the adverse effects of drugs,Translation,1.While the medicinal/organic chemist may create the candidate compound(sometimes referred to as a new chemical entity,NCE),it is the pharmacologist who is responsible for testing it for pharmacological activity.,2.Through research we now know that penicillin can disrupt the synthesis of cell wall in susceptible bacterial strains by inhibiting a key enzyme,while ASA can inhibit the action of human cell membrane enzyme known as cyclooxygenase.,3.Structure-activity relationships are an integral link in the analysis of drug action,and exploitation of these relationships among established therapeutic agents has often led to the development of better drugs.,4.Whether a drug is useful for therapy is crucially dependent upon its ability to produce its desired effects with only tolerable undesired effects.,5.吸收是药物自用药部位进入血液循环的过程。,6.胰岛素为内源性的激素，它的缺乏可引起糖尿病。,7.药物效应动力学研究药物的生理学作用和作用机制。,8.药物代谢动力学和剂量一起决定了药物在其作用位点的浓度。,