《药理学》课程教学大纲 Pharmacology（英文）

PHARMACOLOGYCOURSEINTRODUCTIONPharmacology is the study of drug actions on biological systems. It embraces knowledge of the sourceschemical properties, biological effects and therapeutic uses of drugsHistorically,the roots of pharmacology go back to the ancient civilizations which used plants and plantextracts both in healing and as poisons, The accumulated total of this empirical knowledge, acquired bymankind through the ages, provided a foundation for the evolution of scientific pharmacology as it existstoday. The well known discovery of the beneficial effects of foxglove extracts for treating some kinds ofheart disease, the use of the bark of the willow and cinchona trees in treating fever and the effectiveness ofextracts of the poppy in the treatment of dysenteries are outstanding examples of such knowledge which haveresulted in important advances in pharmacology, developments which continue today.The rise of organicchemistry in the last half of the nineteenth century,together with the development of physiology and, later,biochemistry,allowed empiricism to be discarded in favour of arational approach which today underpins thediscipline of pharmacology.Pharmacology is truly multidisciplinary in scope. Research in this field is closely interwoven with thesubject matter and experimental techniques of analytical chemistry, biochemistry, cellular and molecularbiology,genetics, immunology,medicinal chemistry,microbiology,pathology,and physiology.Consequentlythere are a number ofdistinct sub-disciplines of pharmacology that one maydevelop a career.Somecomponents of pharmacologyinclude:1. Study of how drugs work at the cellular and molecular level.2. The use of drugs as tools to dissect aspects of cell function3.Development of new synthetic drugs to improve on existing drugs or to treat new human conditions whichwill respond to drug treatment.4.Formulation of clinical guidelines for the safe and effective use of drugs.COURSECONTENTI.Introduction toPharmacology+Objectives:1.Definethedefinitionof pharmacology2. The nature of drugs3.Pharmacodynamic principles

PHARMACOLOGY ■COURSE INTRODUCTION Pharmacology is the study of drug actions on biological systems. It embraces knowledge of the sources, chemical properties, biological effects and therapeutic uses of drugs. Historically, the roots of pharmacology go back to the ancient civilizations which used plants and plant extracts both in healing and as poisons. The accumulated total of this empirical knowledge, acquired by mankind through the ages, provided a foundation for the evolution of scientific pharmacology as it exists today. The well known discovery of the beneficial effects of foxglove extracts for treating some kinds of heart disease, the use of the bark of the willow and cinchona trees in treating fever and the effectiveness of extracts of the poppy in the treatment of dysenteries are outstanding examples of such knowledge which have resulted in important advances in pharmacology, developments which continue today. The rise of organic chemistry in the last half of the nineteenth century, together with the development of physiology and, later, biochemistry, allowed empiricism to be discarded in favour of a rational approach which today underpins the discipline of pharmacology. Pharmacology is truly multidisciplinary in scope. Research in this field is closely interwoven with the subject matter and experimental techniques of analytical chemistry, biochemistry, cellular and molecular biology, genetics, immunology, medicinal chemistry, microbiology, pathology, and physiology. Consequently, there are a number of distinct sub-disciplines of pharmacology that one may develop a career . Some components of pharmacology include: 1. Study of how drugs work at the cellular and molecular level. 2. The use of drugs as tools to dissect aspects of cell function. 3. Development of new synthetic drugs to improve on existing drugs or to treat new human conditions which will respond to drug treatment. 4. Formulation of clinical guidelines for the safe and effective use of drugs. ■COURSE CONTENT I. Introduction to Pharmacology ◆Objectives: 1. Define the definition of pharmacology 2. The nature of drugs 3. Pharmacodynamic principles

4. Pharmacodynamic principles5.Characteristic ofabsorption,distribution,and elimination ofdrugs6. Define the definition of receptor7. Macromolecule nature of drug recaptor8. Relation between drug concentration and response9. Signaling mechanisms and drug action10. Variation in drug responsivenessIl.Clinical Selectivity: Beneficial versus toxic effects of Ddrugs12. Rational dosing and the time course of drug ActionLectures:Lecture I: Introduction to Pharmacology1. Mutual introduction of personae in the teaching process2. Know the Department3. Pharmacology: what and why?4. History of Pharmacology development5. Drug-Body Interaction6.Thefuture of Pharmacology7. How to learn PharmacologyLecture 2: Absorption of Drugs1. Routes of drug administration1) Oral2) Sublingual3) Rectal4) Intravascular(IV)5) Intramuscular(IM)6) Subcutaneous(SC)2. Absorption of drugs1) Modes of drug transport: Passive diffusion, Active diffusion2) Factors influencing absorptionpHBlood flow to the absorption Site

4. Pharmacodynamic principles 5. Characteristic of absorption, distribution, and elimination of drugs 6. Define the definition of receptor 7. Macromolecule nature of drug recaptor 8. Relation between drug concentration and response 9. Signaling mechanisms and drug action 10. Variation in drug responsiveness 11. Clinical Selectivity: Beneficial versus toxic effects of Ddrugs 12. Rational dosing and the time course of drug Action ◆Lectures: Lecture 1: Introduction to Pharmacology 1. Mutual introduction of personae in the teaching process 2. Know the Department 3. Pharmacology: what and why? 4. History of Pharmacology development 5. Drug-Body Interaction 6. The future of Pharmacology 7. How to learn Pharmacology Lecture 2: Absorption of Drugs 1. Routes of drug administration 1) Oral 2) Sublingual 3) Rectal 4) Intravascular(IV) 5) Intramuscular(IM) 6) Subcutaneous(SC) 2. Absorption of drugs 1) Modes of drug transport: Passive diffusion, Active diffusion 2) Factors influencing absorption pH Blood flow to the absorption Site

Total surface area available for absorptionContact time at the absorption surface4) First pass hepatic eliminationLecture3:Distribution,and Elimination of Drugs1. Drug distribution1)Factorsinfluencingdistribution2) Volume of distribution2. Drug metabolism1) Major organ of metabolism: liver2) Reactions of drug metabolism3) Results of drug metabolism4) Kinetics of metabolism5) Factors affecting drug metabolism3. Drug excretion1) Major organ of excretion:2)Factorsinfluencingrenalexcretion3) Plasma and Total body clearance4) Clearance half-lifeLecture4RationalDosingandtheTimeCourseofDrugAction1. Steady-state concentration1) Factors affecting Css2) Rate of drug decline when the infusion is stopped3) Loading dose2. Kinetics of fix-dose, fix-time-interval regimen1) Single intravenous injection2) Multiple intravenous injection3) Multiple orally administered drugsBasic Animal Operation Instruments (3 hours required)Lecture 5:Drug Receptors1. Definition

Total surface area available for absorption Contact time at the absorption surface 4) First pass hepatic elimination Lecture 3: Distribution, and Elimination of Drugs 1. Drug distribution 1) Factors influencing distribution 2) Volume of distribution 2. Drug metabolism 1) Major organ of metabolism: liver 2) Reactions of drug metabolism 3) Results of drug metabolism 4) Kinetics of metabolism 5) Factors affecting drug metabolism 3. Drug excretion 1) Major organ of excretion: 2) Factors influencing renal excretion 3) Plasma and Total body clearance 4) Clearance half-life Lecture 4:Rational Dosing and the Time Course of Drug Action 1. Steady-state concentration 1) Factors affecting Css 2) Rate of drug decline when the infusion is stopped 3) Loading dose 2. Kinetics of fix-dose, fix-time-interval regimen 1) Single intravenous injection 2) Multiple intravenous injection 3) Multiple orally administered drugs Basic Animal Operation Instruments (3 hours required) Lecture 5:Drug Receptors 1. Definition

2. Macromolecule nature of drug recaptor1) Sensitivity2)Specificity3) High Affinity4) Saturable5) Reversible3.Relation between drug concentration and response1)Concentration-EffectCurvesandReceptorBindingofAgonists2)Receptor-EffectorCouplingandSpareReceptors4. Interaction of drug and receptor1) Agonists2)Antagonists3) Competitive and Irreversible Antagonists4) Partial Agonists5) Other Mechanisms of Drug Antagonism6) Classification of drugs binding to RLecture 6: Signaling Mechanisms and Drug Action1. Intracellular receptors for lipid-soluble agents2. Ligand-regulated transmembrane enzymes including recaptor tyrosine kinases3. Cytokine recaptors4. Ligand-gated channels5.Receptor regulateonLecture Z: dose and clinical response1.Relation between drug dose and clinical response1) Dose & Response in Patients2) Graded Dose-Response Relation3) Shape of Dose-Response Curves4) Quantal Dose-Effect Curves2. Variation in Drug Responsiveness1)Alteration in Concentration of Drug That Reaches the Receptor2) Variation in Concentration of an Endogenous Receptor ligand

2. Macromolecule nature of drug recaptor 1) Sensitivity 2) Specificity 3) High Affinity 4) Saturable 5) Reversible 3. Relation between drug concentration and response 1) Concentration-Effect Curves and Receptor Binding of Agonists 2) Receptor-Effector Coupling and Spare Receptors 4. Interaction of drug and receptor 1) Agonists 2) Antagonists 3) Competitive and Irreversible Antagonists 4) Partial Agonists 5) Other Mechanisms of Drug Antagonism 6) Classification of drugs binding to R Lecture 6: Signaling Mechanisms and Drug Action 1. Intracellular receptors for lipid-soluble agents 2. Ligand-regulated transmembrane enzymes including recaptor tyrosine kinases 3. Cytokine recaptors 4. Ligand-gated channels 5. Receptor regulateon Lecture 7: dose and clinical response 1. Relation between drug dose and clinical response 1) Dose & Response in Patients 2) Graded Dose-Response Relation 3) Shape of Dose-Response Curves 4) Quantal Dose-Effect Curves 2. Variation in Drug Responsiveness 1) Alteration in Concentration of Drug That Reaches the Receptor 2) Variation in Concentration of an Endogenous Receptor ligand

3) Alteration in Number or Function of Receptors4)ChangesinComponentsofResponseDistaltoReceptor3. Graded dose-response curve1) Definition2) Efficacy3) Potency4)Slopeof thedose-response curve4. Therapeutic index (TI)1) Definition2) ComprehensionLecture &:AmphipathicProperties of DrugAction1. Terapeutic action1) Etiological Treatment2) Symptomatic Treatment2. Adverse reactions of drug1)Sidereaction2) Toxic reaction, Toxicity3) After effect4) Allergy3. Beneficial Versus Toxic Effects of Drugs1)Beneficial and Toxic Effects Mediated by the Same Receptor-Effector Mechanism2)BeneficialandToxicEffectsMediatedbyIdenticalReceptorsbutinDifferentTissuesorbyDifferentEffector Pathways3) Beneficial and Toxic Effects Mediated by Different Types of Receptors+Practicals:1. Handling the Laboratory Animals (3 hours required)2. The influence on drug action with different doses (3 hours required)3. The influence on drug action with different route of administrationIII. Drugs Affecting the Central Nervous System+Objectives:1. Describe the etiology of parkinson's disease

3) Alteration in Number or Function of Receptors 4) Changes in Components of Response Distal to Receptor 3. Graded dose-response curve 1) Definition 2) Efficacy 3) Potency 4) Slope of the dose-response curve 4. Therapeutic index (TI) 1) Definition 2) Comprehension Lecture 8: Amphipathic Properties of Drug Action 1. Terapeutic action 1) Etiological Treatment 2) Symptomatic Treatment 2. Adverse reactions of drug 1) Side reaction 2) Toxic reaction, Toxicity 3) After effect 4) Allergy 3. Beneficial Versus Toxic Effects of Drugs 1) Beneficial and Toxic Effects Mediated by the Same Receptor-Effector Mechanism 2) Beneficial and Toxic Effects Mediated by Identical Receptors but in Different Tissues or by Different Effector Pathways 3) Beneficial and Toxic Effects Mediated by Different Types of Receptors ◆Practicals: 1. Handling the Laboratory Animals (3 hours required) 2. The influence on drug action with different doses (3 hours required) 3. The influence on drug action with different route of administration III. Drugs Affecting the Central Nervous System ◆Objectives: 1. Describe the etiology of parkinson’s disease

2. Describe therapy method of Parkinsonism3. To grasp mechanism, therapeutic uses, adverse effects of Levodopa (L-dopa) and Carbidopa4. Know specific agents of treatment Parkinsonism5. Know definition of sedatives and hypnotics6.Knowtwo phases of sleep7. To grasp mechanism, therapeutic uses, adverse effects of diazepam8. Benzodiazepines Antagonist -------Flumazenil9. Describe mechanism, therapeutic uses, adverse effects of barbiturates10. Know other sedative-hypnotics11. Know the classification of affective disorders (Mania,depression)12. Know the mechanism of depression13. To grasp mechanism, therapeutic uses, adverse effects of tricyclic antidepressants14. Selective 5-HT Reuptake Inhibitors15. Describe Selective MAO-A inhibitor16. Know treatment of bipolar affective disorders (BPAD)17.Know basic concepts of psychotic disorders18. Know the dopamine theory for schizophrenia19. Know dopaminergic systems, dopamine receptors20.Know the classifications of neuroleptic drugs21. To grasp mechanism, therapeutic uses, adverse effects of phenothiazines22.Describe other phenothiazines23. Describe the antimanic drugs24. Describe the classification of the pain25. Describe classification of the opioid analgesics26. Describe mechanism of action of the opioid analgesics27. To grasp tolerance and physical dependence28. To grasp Organ system effects of morphine and its surrogates29. To grasp Clinical use of opioid analgesics30. To grasp toxicity and adverse reaction of opioid analgesics31. To grasp diagnosis and treatment of opioid overdosage32. Describe specific agents, meperidine

2. Describe therapy method of Parkinsonism 3. To grasp mechanism, therapeutic uses, adverse effects of Levodopa (L-dopa) and Carbidopa 4. Know specific agents of treatment Parkinsonism 5. Know definition of sedatives and hypnotics 6. Know two phases of sleep 7. To grasp mechanism, therapeutic uses, adverse effects of diazepam 8. Benzodiazepines Antagonist -Flumazenil 9. Describe mechanism, therapeutic uses, adverse effects of barbiturates 10. Know other sedative-hypnotics 11. Know the classification of affective disorders (Mania,depression) 12. Know the mechanism of depression 13. To grasp mechanism, therapeutic uses, adverse effects of tricyclic antidepressants 14. Selective 5-HT Reuptake Inhibitors 15. Describe Selective MAO-A inhibitor 16. Know treatment of bipolar affective disorders (BPAD) 17. Know basic concepts of psychotic disorders 18. Know the dopamine theory for schizophrenia 19. Know dopaminergic systems, dopamine receptors 20. Know the classifications of neuroleptic drugs 21. To grasp mechanism, therapeutic uses, adverse effects of phenothiazines 22. Describe other phenothiazines 23. Describe the antimanic drugs 24. Describe the classification of the pain 25. Describe classification of the opioid analgesics 26. Describe mechanism of action of the opioid analgesics 27. To grasp tolerance and physical dependence 28. To grasp Organ system effects of morphine and its surrogates 29. To grasp Clinical use of opioid analgesics 30. To grasp toxicity and adverse reaction of opioid analgesics 31. To grasp diagnosis and treatment of opioid overdosage 32. Describe specific agents, meperidine

33. Describe the opiod antagonist34.Describe classificationof epilepsy35.Describe mechanism of action of antiepileptic drugs36. To grasp therapeutic indications for anticonvulsant agents37. To grasp therapeutic uses, adverse effects of phenytoin, carbamazepine, phenobarbita38. Know other antiepileptic drugsLectures:Lecture 17: Treatment of Parkinson's Disease1.NeurotransmissionintheCNS1) Glutamate and aspartate2)-aminobutyric acid（GABA)3) Serotonin4) Acetylcholine5)Dopamine6) Norepinephrine7) Endorphins and enkephalins8)Other neurotransmitters:Dynorphins、Substance P, Nitric oxide(NO)2. Synaptic Potentials1) Excitatory Pathways2) Inhibitory Pathways3) Combined Effects of the EPSP and IPSP3. Overview of Parkinson's Disease4. Etiology: the loss of striatal dopamine produces an imbalance5. Levodopa (L-dopa) and Carbidopa1) Mechanism of Action2) Fate of Administered L-dopa3) Therapeutic Uses4) Adverse Effects5) Drug Interactions6) Contraindications6. Specific Agents

33. Describe the opiod antagonist 34. Describe classification of epilepsy 35. Describe mechanism of action of antiepileptic drugs 36. To grasp therapeutic indications for anticonvulsant agents 37. To grasp therapeutic uses, adverse effects of phenytoin, carbamazepine, phenobarbital 38. Know other antiepileptic drugs ◆Lectures: Lecture 17: Treatment of Parkinson’s Disease 1. Neurotransmission in the CNS 1) Glutamate and aspartate ￾2) γ-aminobutyric acid （GABA） 3) Serotonin ￾4) Acetylcholine ￾5) Dopamine ￾6) Norepinephrine ￾7) Endorphins and enkephalins ￾8) Other neurotransmitters: Dynorphins 、Substance P, Nitric oxide (NO) 2. Synaptic Potentials 1) Excitatory Pathways 2) Inhibitory Pathways 3) Combined Effects of the EPSP and IPSP 3. Overview of Parkinson’s Disease 4. Etiology: the loss of striatal dopamine produces an imbalance 5. Levodopa (L-dopa) and Carbidopa 1) Mechanism of Action 2) Fate of Administered L-dopa 3) Therapeutic Uses 4) Adverse Effects 5) Drug Interactions 6) Contraindications 6. Specific Agents

1)DopamineAgonists:Bromocriptine2) Monoamine oxidase inhibitors: rasagiline3)Catechol-O-Methyl Transferase Inhibitors :tolcapone and entacapone4) Anticholinergic Drugs1.Definition of Sedatives and Hypnotics2.Two phases of sleep3.Benzodiazepines-------Diazepam1)Classification2)Pharmacokinetics 3)Mechanism of benzodiazepines4) Therapeutic Uses5) Adverse Effects6)Tolerance and Dependence7) Drug Interactions8) Characteristics of different drugs4. Benzodiazepines Antagonist ---Flumazenil5.Barbiturates1)Classification2) Pharmacokinetics3) Mechanism of benzodiazepines4) Therapeutic Uses5)Adverse Effects6. Other Sedative-HypnoticsLecture 19: Antidepressants drugs1.Theclassification of affectivedisorders(Mania,depression)2.themechanismofdepression1)Monoamine theoryof depression2) The other theory of depression3. Tricyclic AntidepressantsD)Pharmacologiceffectsandmechanismofaction2)Clinical uses3) Side effects Tetracyclic

1) Dopamine Agonists : Bromocriptine 2) Monoamine oxidase inhibitors: rasagiline 3) Catechol-O-Methyl Transferase Inhibitors :tolcapone and entacapone 4) Anticholinergic Drugs 1. Definition of Sedatives and Hypnotics 2. Two phases of sleep 3. Benzodiazepines-Diazepam 1) Classification 2) Pharmacokinetics 3) Mechanism of benzodiazepines 4) Therapeutic Uses 5) Adverse Effects 6) Tolerance and Dependence 7) Drug Interactions 8) Characteristics of different drugs 4. Benzodiazepines Antagonist -Flumazenil 5. Barbiturates 1) Classification 2) Pharmacokinetics 3) Mechanism of benzodiazepines 4) Therapeutic Uses 5) Adverse Effects 6. Other Sedative-Hypnotics Lecture 19: Antidepressants drugs 1. The classification of affective disorders(Mania,depression) 2. the mechanism of depression 1) Monoamine theory of depression 2) The other theory of depression 3. Tricyclic Antidepressants 1) Pharmacologic effects and mechanism of action 2) Clinical uses 3) Side effects Tetracyclic

4.Selective5-HTReuptakeInhibitors5. Selective MAO-A inhibitor6.Treatmentofbipolaraffectivedisorders(BPAD)1) Mechanism of action2) Indictions3) Adverse effectsLecture 20:Neuroleptic drugs1.Basic concepts of psychoticdisorders2. The Dopamine theory for Schizophrenia3. The introduction for Dopaminergic Systems4.The introduction for Dopamine Receptors5. The classifications of Neuroleptic drugs6. Mode of drugs action1) Depamine receptor-blocking activity in brain2)Serotonin receptor-blocking activity in brain7.Phenothiazines1) Chemistry2)Pharmacological Effects3) Clinical Uses4) Side Effects8. Other phenothiazines9. The Antimanic Drugs(Lithium carbonate1)Pharmacokinetics2) Pharmacological Effects and Mechanism of Action3)ClinicalUses4) Side Effects and IntoxicationLecture 2l: Opioid Analgesics and Antagonists1. The classification of the pain2. Classification of the opioid analgesics3. Mechanism of action of the opioid analgesics4. Tolerance and Physical Dependence

4. Selective 5-HT Reuptake Inhibitors 5. Selective MAO-A inhibitor 6. Treatment of bipolar affective disorders (BPAD) 1) Mechanism of action 2) Indictions 3) Adverse effects Lecture 20: Neuroleptic drugs 1. Basic concepts of psychotic disorders 2. The Dopamine theory for Schizophrenia 3. The introduction for Dopaminergic Systems 4. The introduction for Dopamine Receptors 5. The classifications of Neuroleptic drugs 6. Mode of drugs action 1) Depamine receptor-blocking activity in brain 2)Serotonin receptor-blocking activity in brain 7. Phenothiazines 1) Chemistry 2) Pharmacological Effects 3) Clinical Uses 4) Side Effects 8. Other phenothiazines 9. The Antimanic Drugs(Lithium carbonate 1) Pharmacokinetics 2) Pharmacological Effects and Mechanism of Action 3) Clinical Uses 4) Side Effects and Intoxication Lecture 21: Opioid Analgesics and Antagonists 1. The classification of the pain 2. Classification of the opioid analgesics 3. Mechanism of action of the opioid analgesics 4. Tolerance and Physical Dependence

5. Organ system effects of morphine and its surrogates1) Central nervous system effects2)Peripheral effects6. Clinical use of opioid analgesics7. Toxicity and adverse reaction of opioid analgesics8. Diagnosis and treatment of opioid overdosage9.Contraindication and cautions in therapy1)Useofpureagonistswithweakpartial agonists2) Use in patients with head injuries3) Use during pregnancy4) Use in patients with impaired pulmonary function5) Use in patients with impaired hepatic or renal function6) Use in patients with endocrine disease10. Specific agents, Meperidine11. The opiod antagonistLecture 22:Drugs Used to Treat Epilepsy1. Overview of epilepsy2. Classification of epilepsy1) PartialSimple partialComplex partial2) GeneralizedTonic-clonic (grand mal)Absence (petit mal)MyoclonicFebrile seizuresStatus epilepticus3. Mechanism of action of antiepileptic drugs4.Antiepileptic drugs1) Therapeutic indications for anticonvulsant agents2)Phenytoin

5. Organ system effects of morphine and its surrogates 1) Central nervous system effects 2) Peripheral effects 6. Clinical use of opioid analgesics 7. Toxicity and adverse reaction of opioid analgesics 8. Diagnosis and treatment of opioid overdosage 9. Contraindication and cautions in therapy 1) Use of pure agonists with weak partial agonists 2) Use in patients with head injuries 3) Use during pregnancy 4) Use in patients with impaired pulmonary function 5) Use in patients with impaired hepatic or renal function 6) Use in patients with endocrine disease 10. Specific agents, Meperidine 11. The opiod antagonist Lecture 22:Drugs Used to Treat Epilepsy 1. Overview of epilepsy 2. Classification of epilepsy 1) Partial Simple partial Complex partial 2) Generalized Tonic-clonic (grand mal) Absence (petit mal) Myoclonic Febrile seizures Status epilepticus 3. Mechanism of action of antiepileptic drugs 4. Antiepileptic drugs 1) Therapeutic indications for anticonvulsant agents 2) Phenytoin