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