SectionI Basic PrinciplesIntroduction2Total hours required --1Total Classes required -MonDays of Study =-Period of Study =Week1&2-FirstsemesterLecture 1 Class Ii Howtodefinepharmacologyii.TheNatureof Drugsa, The Physical Nature of Drugsb.Drug Sizec.DrugReactivity andDrug-ReceptorBondsd. Drug Shapee.RationalDrugDesignii.Drug-Body Interactioniv.PharmacodynamicPrinciplesa.Types ofDrug-ReceptorInteractionsb.Agonists That Inhibit Their Binding Molecules andPartial Agonistsc.DurationofDrugActiond.Receptors and Inert Binding SitesV.PharmacokineticPrinciplesa.PermeationiAqueous diffusionii Lipid diffusionii. Special carriersiv.EndocytosisandExocytosisb.Fick'sLawof Diffusionc.Ionization of Weak Acids and Weak Bases: theHenderson-HasselbalchEquationDrugReceptors&Pharmacodynamics6Total hours required =3Total Classes required =Tue, WedDays of Study =Period of Study=Week3&4-First semestera. Lecture 1 Class IIi.What is the receptor?ii,Macromoleculenatureofdrugrecaptor
Section I Basic Principles Introduction Total hours required = 2 Total Classes required = 1 Days of Study = Mon Period of Study = Week 1&2 –First semester Lecture 1 Class I i. How to define pharmacology ii. The Nature of Drugs a. The Physical Nature of Drugs b. Drug Size c. Drug Reactivity and Drug-Receptor Bonds d. Drug Shape e. Rational Drug Design iii. Drug-Body Interaction iv. Pharmacodynamic Principles a. Types of Drug-Receptor Interactions b. Agonists That Inhibit Their Binding Molecules and Partial Agonists c. Duration of Drug Action d. Receptors and Inert Binding Sites v. Pharmacokinetic Principles a. Permeation i. Aqueous diffusion ii. Lipid diffusion iii. Special carriers iv. Endocytosis and Exocytosis b. Fick’s Law of Diffusion c. Ionization of Weak Acids and Weak Bases; the Henderson-Hasselbalch Equation Drug Receptors & Pharmacodynamics Total hours required = 6 Total Classes required = 3 Days of Study = Tue, Wed Period of Study = Week 3&4 –First semester a. Lecture 1 Class II i. What is the receptor? ii. Macromolecule nature of drug recaptor
iiRelationbetweendrugconcentration&responsea.Concentration-EffectCurves&ReceptorBindingofAgonistsb,Receptor-EffectorCoupling&SpareReceptorsc.Competitive&IrreversibleAntagonistsd.Partial Agonistse.OtherMechanismsofDrugAntagonismb. Lecture 2 Class I1Ii.Signaling mechanisms&drugactiona.Intracellularreceptors forlipid-soluble agentsb. Ligand-regulated transmembrane enzymes includingrecaptortyrosinekinasesc.Cytokine recaptorsd.Ligand-gated channelse.Receptorregulateonc.Lecture3ClassIViRelationbetweendrugdose&clinical responsea.Dose&ResponseinPatientsb.Graded Dose-ResponseRelationc.Shapeof Dose-Response Curvesd.QuantalDose-EffectCurvesii.VariationinDrugResponsivenessa.Alteration in Concentration of Drug That Reaches theReceptorb.VariationinConcentration of anEndogenousReceptorligandc.Alteration inNumberorFunctionofReceptorsd.ChangesinComponents ofResponseDistal toReceptoriliClinical Selectivity:Beneficial Versus Toxic EffectsofDrugsa.Beneficial and Toxic EffectsMediated bytheSameReceptor-EffectorMechanismb.BeneficialandToxicEffectsMediated byIdenticalReceptors but in DifferentTissuesorbyDifferentEffectorPathwaysc.Beneficial and Toxic Effects Mediated by DifferentTypes of ReceptorsPharmacokinetics &Pharmacodynamics:
iii. Relation between drug concentration & response a. Concentration-Effect Curves & Receptor Binding of Agonists b. Receptor-Effector Coupling & Spare Receptors c. Competitive & Irreversible Antagonists d. Partial Agonists e. Other Mechanisms of Drug Antagonism b. Lecture 2 Class III i. Signaling mechanisms & drug action a. Intracellular receptors for lipid-soluble agents b. Ligand-regulated transmembrane enzymes including recaptor tyrosine kinases c. Cytokine recaptors d. Ligand-gated channels e. Receptor regulateon c. Lecture 3 Class IV i. Relation between drug dose & clinical response a. Dose & Response in Patients b. Graded Dose-Response Relation c. Shape of Dose-Response Curves d. Quantal Dose-Effect Curves ii. Variation in Drug Responsiveness a. Alteration in Concentration of Drug That Reaches the Receptor b. Variation in Concentration of an Endogenous Receptor ligand c. Alteration in Number or Function of Receptors d. Changes in Components of Response Distal to Receptor iii. Clinical Selectivity: Beneficial Versus Toxic Effects of Drugs a. Beneficial and Toxic Effects Mediated by the Same Receptor-Effector Mechanism b. Beneficial and Toxic Effects Mediated by Identical Receptors but in Different Tissues or by Different Effector Pathways c. Beneficial and Toxic Effects Mediated by Different Types of Receptors Pharmacokinetics & Pharmacodynamics:
Rational Dosing&the Time Course of DrugActionTotal hours required =63Total Classes required =ThuDays of Study=Period of Study=Week1&2-Firstsemestera. Lecture 1 Class Vi PHARMACOKINETICSa.VolumeofDistributionb.Clearancei Capacity-Limited Eliminationi.Flow-DependentEliminationc.Half-Lifed.DrugAccumulationb.Lecture2ClassVIiPHARMACOKINETICSe.Bioavailabilityi.Extentof Absorptionii.First-Pass EliminationiliRateofAbsorptionf.ExtractionRatio&theFirst-PassEffectg.Alternative Route of Administration&the First-PassEffectiiTHETIMECOURSEOFDRUGEFFECTa.ImmediateEffectsb.Delayed Effectsc.CumulativeEffectsiii THETARGET CONCENTRATION APPROACHTOAGDESIN1NGRATIONALDOSAGEREGIMENa.Maintenance Doseb.LoadingDosec. Lecture 3 Class VIIi..THERAPEUTICDRUGMONITORING:RELATINGPHARMACOKINETICS&OPHARMACODYNAMICSa. PharmacokineticVariablesiAbsorption
Rational Dosing & the Time Course of Drug Action Total hours required = 6 Total Classes required = 3 Days of Study = Thu Period of Study = Week 1&2 –First semester a. Lecture 1 Class V i. PHARMACOKINETICS a. Volume of Distribution b. Clearance i. Capacity-Limited Elimination ii. Flow-Dependent Elimination c. Half-Life d. Drug Accumulation b. Lecture 2 Class VI i. PHARMACOKINETICS e. Bioavailability i. Extent of Absorption ii. First-Pass Elimination iii. Rate of Absorption f. Extraction Ratio & the First-Pass Effect g. Alternative Route of Administration & the First-Pass Effect ii. THE TIME COURSE OF DRUG EFFECT a. Immediate Effects b. Delayed Effects c. Cumulative Effects iii. THE TARGET CONCENTRATION APPROACH TO D E S I G N I N G A RATIONAL DOSAGE REGIMEN a. Maintenance Dose b. Loading Dose c. Lecture 3 Class VII i. THERAPEUTIC DRUG MONITORING: RELATING PHARMACOKINETICS & OPHARMACODYNAMICS a. Pharmacokinetic Variables i. Absorption
ii. Clearanceili.VolumeofDistributioniv.Half-Lifeb.Pharmacodynamic Variablesi Maximumeffecti. Sensitivityi.INTERPRETATIONOFDRUGCONCENTRATIONMEASUREMENTSa. ClearanceiAlbuminConcentrationii.aj-AcidGlycoproteinConcentrationili. Capacity-Limited ProteinBindingb.Timing of SamplesforConcentration Measurementc.Initial Predictionsof Volumeof Distribution&Clearancei Volume ofDistributioniiClearanced.RevisingIndividual Estimates of VolumeofDistribution&ClearanceDrug Biotransformation4Total hours required =2Total Classes required =Days of Study=Fri, MonPeriod of Study=Week1&2-First semestera. Lecture 1 Class VIIIi WHYISDRUGBIOTRANSFORMATIONNECESSARY?i THE ROLE OF BIOTRANSFORMATIONIN DRUGDISPOSITIONiiWHEREDODRUGBIOTRANSFORMATIONSOCCUR?iv.MICROSOMALMIXEDFUNCTIONOXIDASE&ISYSTEMPHASEREACTIONSa.EnzymeInductionb.EnzymeInhibitionv.PHASEIIREACTIONSb. Lecture 2 Class IX
ii. Clearance iii. Volume of Distribution iv. Half-Life b. Pharmacodynamic Variables i. Maximum effect ii. Sensitivity ii. INTERPRETATION OF DRUG CONCENTRATION MEASUREMENTS a. Clearance i. Albumin Concentration ii. α1-Acid Glycoprotein Concentration iii. Capacity-Limited Protein Binding b. Timing of Samples for Concentration Measurement c. Initial Predictions of Volume of Distribution & Clearance i. Volume of Distribution ii. Clearance d. Revising Individual Estimates of Volume of Distribution & Clearance Drug Biotransformation Total hours required = 4 Total Classes required = 2 Days of Study = Fri, Mon Period of Study = Week 1&2 –First semester a. Lecture 1 Class VIII i. WHY IS DRUG BIOTRANSFORMATION NECESSARY? ii. THE ROLE OF BIOTRANSFORMATION IN DRUG DISPOSITION iii. WHERE DO DRUG BIOTRANSFORMATIONS OCCUR? iv. MICROSOMAL MIXED FUNCTION OXIDASE S Y S T E M & P H A S E I REACTIONS a. Enzyme Induction b. Enzyme Inhibition v. PHASE II REACTIONS b. Lecture 2 Class IX
iMETABOLISMOFDRUGSTOTOXICPRODUCTSiiCLINICALRELEVANCEOFDRUGMETABOLISMa.Individual Differencesb.GeneticFactorsc.Diet&EnvironmentalFactorsd.Age&Sexe.Drug-DrugInteractions DuringMetabolismf.InteractionsBetweenDrugs&EndogenousCompoundsSection IlAutonomic DrugsIntroductionToAutonomicPharmacology2Total hours required =1Total Classes required -MonDaysof StudyPeriod of Study=Week 1&2-First semesterLecture 1 Class XiIntroductiontonervous systemii.Anatomyof theautonomicnervous systema.Autonomicnervoussystemb.Somatic SystemiliThe anatomic classification of theautonomic Systema.Parasympatheticb.Sympatheticiv.Theclassificationofautonomicsystembasedontheprimarytransmittera.Cholinergic fibersb.Noradrenergicfibers(alsoc.non-adrenergic and non-cholinergic nervev.The constitutionof synapsea.Presynapticmembraneb.Synapticcleftc.Postsynapticmembranevi.Neurotrasmitterchemistryoftheautonomicsystema.Cholinergictransmissionb.Adrenergic transmission:vii.Autonomicreceptorsa.Theclassificationofautonomicreceptors(cholinoceptorsadrenoceptors)b.Locationsofautonomicreceptors:vili.Functional organizationofautonomicactivity
i. METABOLISM OF DRUGS TO TOXIC PRODUCTS ii. CLINICAL RELEVANCE OFDRUG METABOLISM a. Individual Differences b. Genetic Factors c. Diet & Environmental Factors d. Age & Sex e. Drug-Drug Interactions During Metabolism f. Interactions Between Drugs & Endogenous Compounds Section II Autonomic Drugs Introduction To Autonomic Pharmacology Total hours required = 2 Total Classes required = 1 Days of Study = Mon Period of Study = Week 1&2 –First semester Lecture 1 Class X i. Introduction to nervous system ii. Anatomy of the autonomic nervous system a. Autonomic nervous system b. Somatic System iii. The anatomic classification of the autonomic System a. Parasympathetic b. Sympathetic iv. The classification of autonomic system based on the primary transmitter a.Cholinergic fibers b.Noradrenergic fibers(also c.non-adrenergic and non-cholinergic nerve v. The constitution of synapse a.Presynaptic membrane b.Synaptic cleft c.Postsynaptic membrane vi. Neurotrasmitter chemistry of the autonomic system a.Cholinergic transmission b.Adrenergic transmission: vii. Autonomic receptors a.The classification of autonomic receptors(cholinoceptors, adrenoceptors) b.Locations of autonomic receptors: viii. Functional organization of autonomic activity