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Nonotesforslide
PharmacodynamicsPPT
1.1.PHARMACODYNAMICS
2.2.InGreekPharmacon=DrugDynamics=Action/PowerItcoversalltheaspectsrelatingtoWhat
adrugdoestothebodyMechanismofaction
3.3.Action:HowandWheretheeffectisproducediscalledasAction.Effect:Thetypeofresponse
producingbydrug.
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4.4.SiteofDrugActionWhere:1.Extracellular2.Cellular3.Intracellular
5.5.TypesofDrugActionEFFECT(Typeofresponses):1.Stimulation2.Inhibition/Depression
3.Replacement4.Irritation5.Cytotoxic
6.6.MechanismofActionofDrugsDrugacteitherbyreceptororbynonreceptororbytargeting
specificgeneticchanges.Majorityofdrugsactsby(HOW)ReceptormediatedNonreceptormediated
7.7.ReceptorMediatedactionDrugproducetheireffectthroughinteractingwithsomechemical
compartmentoflivingorganismc/sReceptor.ReceptorsaremacromoleculesMostareproteins
Presenteitheronthecellsurface,cytoplasmorinthenucleus
8.8.ReceptorFunctions:Twoessentialfunctions1.Recognizationofspecificligandmolecule(Ligand
bindingdomain)2.Transductionofsignalintoresponse(Effectordomain)Ligandbindingdomain
Transductionofsignalintoresponse
9.9.Drug(D)+ReceptorDrugreceptorcomplexResponseDrugreceptorinteraction:1.Selectivity:
Degreeofcomplimentarycorelationbetweendrugandreceptor.Ex:AdrenalineSelectivityfor,
Receptor2.Affinity:Abilityofdrugtogetboundtothereceptor.3.Intrinsicactivity(IA)or
Efficacy:Abilityofdrugtoproduceapharmacologicalresponseaftermakingthedrugreceptor
complex.
10.10.Drugclassification(onthebasisofaffinity&efficacy)
11.11.ResponseNoresponse
12.12.Partialagonist:Thesedrughavefullaffinitytoreceptorbutwithlowintrinsicactivity(IA=0to
1).Theseareonlypartlyaseffectiveasagonist(Affinityislesserwhencomparisontoagonist)Ex:
Pindolol,Pentazocine
13.13.Inverseagonist:Thesehavefullaffinitytowardsthereceptorbutintrinsicactivityiszeroto1
i.e.,produceseffectisjustoppositetothatofagonist.Ex:Carbolineisinverseagonistfor
Benzodiazepinesreceptors.
14.14.ReceptorfamiliesFourtypesofreceptorsfamilies1.Ligandgatedionchannels(inotropic
receptors)2.Gprotiencoupledreceptor(Metabotropicreceptors)3.Enzymaticreceptors
(tyrosinekinase)4.Receptorregulatinggeneexpression(transcriptionfactors/Steroid)
15.15.CharacteristicsofreceptorfamiliesLigandgatedGproteincoupledEnzymaticNuclearLocation
MembraneMembraneMembraneIntracellularEffectorIonchannelIonChannelorenzymeEnzyme
GenecouplingDirectGproteinDirectViaDNAExampleNicotinicMuscarinicInsulinSteroid,
hormone
16.16.SignaltransductionmechanismIongatedreceptors:Localizedoncellmembraneandcoupled
directlytoanionchannel.ReceptorAgonistHyperpolarizationordepolarizationReceptorBlocker
PermeationofionisblockedCellulareffectNocellulareffectIonNa+2
17.17.Ex:Nicotiniccholinergicreceptor
18.18.GproteincoupledreceptorsMembranebound,whicharecoupledtoeffectorsystemthroughGTP
bindingproteinscalledasGproteinsBoundtoinnerfaceofplasmamembrane(2ndmessenger)
19.19.VarietiesofGproteinGproteinReceptorforSignalingpathway/EffectorGsadrenegic,
H,5HT,GlucagonACcAMPGi1,2,32adrenergic,Ach,ACcAMP,OpenK+GqAch
PhospholipaseC,IP3cytoplasmicCa+2GoNeurotransmittersinbrainNotyetclear
20.20.Gproteineffectorsystems1.Adenylasecyclase:cAMPsystem2.PhospholipaseC:Inositol
phosphatesystem3.Ionchannels
21.21.cAMPsystem
22.22.PhospholipaseCsystem
23.23.IonchannelregulationGproteincoupledreceptorscancontrolthefunctioningofionchannelby
don'tinvolvinganysecondmessengerEx:Incardiacmuscle
24.24.Thesereceptoraredirectlylinkedtyrosinekinase.Receptorbindingdomainpresentinextra
cellularsite.ProduceconformationalchangesinintracellularEx:InsulinreceptorsEnzymatic
receptors
25.25.EnzymaticreceptorsExtracellularreceptorbindingdomainIntracellularchanges
26.26.Receptorregulatinggeneexpression(transcriptionfactors)Unfoldsthereceptorandexpose
normallymaskedDNAbindingsiteIncreaseRNApolymeraseactivity
27.27.ReceptorregulationtheoryReceptorsareindynamicstate.Theaffinityoftheresponsetodrugs
isnotfixed.Italtersaccordingtosituation.Receptordownregulation:Prolongeduseofagonist
ReceptornumberandsensitivityDrugeffectEx:Chronicuseofsalbutamoldownregulates2
adrenergicreceptors.
28.28.Receptorupregulation:ProlongeduseofantagonistReceptornumberandsensitivityDrugeffect
Ex:propranololisstoppedafterprolonguse,producewithdrawalsymptoms.RiseBP,induceof
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angina.
29.29.Agonist:Boththehighaffinityaswellasintrinsicactivity(IA=1)Thesedrugtriggerthemaximal
biologicalresponseormimiceffectoftheendogenoussubstance.Ex:Methacholineisa
cholinomimeticdrugwhichmimicstheeffectofAchoncholinergicreceptors.
30.30.TypesofagonismSummation:Twodrugselicitingsameresponse,butwithdifferentmechanism
andtheircombinedeffectisequaltotheirsummation.(1+1=2)AspirinCodienePGOpiodsreceptor
Analgesic+Analgesic+++
31.31.TypesofagonismAdditive:combinedeffectoftwodrugsactingbysamemechanismAspirinPG
PGAnalgesic+Analgesic+++
32.32.Synergism(Supraadditive):(1+1=3)Thecombinedeffectoftwodrugeffectishigherthaneither
individualeffect.Ex:1.Sulfamethaxazole+Trimethoprim2.Levodopa+Carbidopa.
33.33.TypesofantagonismAntagonism:Effectoftwodrugsislessthansumoftheeffectsofthe
individualdrugs.1.ChemicalantagonismEx:heparin(ve)protamine+ve,Chelatingagents1.
Physiological/Functionalantagonism2.Pharmacokineticantagonism3.Pharmacologicalantagonism
I.Competitive(Reversible)II.Noncompetitive(Irreversible)
34.34.PharmacokineticantagonismOnedrugaffectstheabsorption,metabolismorexcretionofother
drugandreducetheireffect.Ex:Warfarininpresenceofphenobarbitone,warfarinmetabolismis
increased,iteffectisreduced.
35.35.PharmacologicalantagonismPharmacodynamicantagonismbetweentwodrugsactingatsame
receptors.Twoimportantmechanismaccordingtowhichtheseantagonists
1.Reversible(Competitive)2.Irreversible(Non)
36.36.Reversibleantagonism(Competitiveantagonism)Theseinhibitioniscommonlyobservedwith
antagoniststhatbindreversiblytothesamereceptorsiteasthatofanagonist.Thesetypeinhibition
canbeovercomeincreasingtheconcentrationofagonistEx:Atropineisacompetitiveantagonistof
Ach.
37.37.IrreversibleAntagonismItoccurswhentheantagonistdissociatesveryslowornotatallfromthe
receptorsresultthatnochangewhentheagonistapplied.Antagonisteffectcannotbeovercomeeven
afterincreasingtheconcentrationofagonist
38.38.NonreceptormediatedactionAlldrugsactionarenotmediatedbyreceptors.Someofdrugsmay
actthroughchemicalactionorphysicalactionorothermodes.ChemicalactionPhysicalaction
(Astringents,sucralfate)Falseincorporation(PABA)Beingprotoplasmicaction(antiseptics)
Formationofantibody(Vaccines)Targetingspecificgeneticchanges.
39.39.DoseItistherequiredamountofdruginweight,volumes,molesorIUtoprovideadesired
effect.InclinicalitiscalledasTherapeuticdoseInexperimentalpurposeitiscalledaseffective
dose.Thetherapeuticdosevariesfrompersontoperson
40.40.Singledose:1.Piperazine(45g)issufficienttoeradicateroundworm.2.SingleIMdoseof250mg
ofceftriaxonetotreatgonorrhoea.Dailydose:Itisthequantityofadrugtobeadministeredin24hr,all
atonceorequallydivideddose.1.10mgofcetrizine(allatonce)issufficienttoreliveallergic
reactions.2.Erythromycinis1gperdaytobegivenin4equallydivideddose(i.e.,250mgevery6hr)
41.41.Totaldose:Itisthemaximumquantityofthedrugthatisneededthecompletecourseofthe
therapy.Ex:procainepenicillin earlysyphilisis6millionunit givenas0.6millionunitsperday
for10days.Loadingdose:Itisthelargedoseofdrugtobegiveninitiallytoprovidetheeffective
plasmaconcentrationrapidly.ThedrugshavinghighVdofdistribution.ChloroquineinMalaria600
mgStat300mgafter8hours300mgafter2days.
42.42.Maintenancedose:Loadingdosenormallyfollowedbymaintenancedose.Neededtomaintain
thesteadystateplasmaconcentrationattainedaftergivingtheloadingdose.
43.43.Therapeuticindex:MarginofsafetyDependuponfactorofdoseproducingdesirableeffect
doseelicitingtoxiceffect.TI shouldbemorethanone5050EDLDindexcTherapeuti
44.44.ToxicTherapeuticwindow:Optimaltherapeuticrangeofplasmaconcentrationsatwhichmosto
thepatientsexperiencethedesiredeffect.Therapeuticrange TherapeuticwindowSuboptimal
optimal
45.45.Cyclosporine100400ng/mlCarbamazapine410g/mlDigoxin0.82ng/mlLithium0.8
1.4mEq/LPhenotoin1020g/mlQunindine26g/ml
46.46.Tolerance:Increasedamountofdrugrequiredtoproduceinitialpharmacologicalresponse.
Usuallyseenwithalcohol,morphine,barbiturates,CNSactivedrugsReversetolerance:Same
amountdrugproducesincpharmacologicalresponse.Cocaine,amphetamine ratsinc.motor
activity
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47.47.TypesoftolerancesInnatetolerance:Geneticallylackofsensitivitytoadrug.Ex:Rabbits
toleratetoatropinelargedosesChinese CastoroilNegros Mydriaticactionof
sympathomimeticsEskimos highfattydiets
48.48.Acquiredtolerances:OccursduetorepeateduseofdrugPharmacokinetictolerances
PharmacodynamictoleranceAcutetolerancePharmacokinetictolerances:Repetitiveadministration
causesdecreasetheirabsorptionorinc.itsownmetabolismEx:Alcohol dec.absorption
Barbiturates Inc.ownmetabolism
49.49.PharmacodynamictoleranceDownregulationofreceptorsImpairmentinsignaltransduction
Ex:Morphine,caffeine,nicotine.Acutetolerance:TachyphylaxisAcutedevelopmentoftolerance
afterarapidandrepeatedadministrationofadruginshorterintervalsExEphedrine,tyramine
50.50.Ex:Mondaydisease.NitroglycerineMonday,Tuesdayworkersgetheadache,aftertheyget
tolerances.Afterholiday(Sunday)theygetagainheadache.Crosstolerances:Crosstolerance
amongdrugsbelongingtosamecategory.MORPHIN HEROIN NARCOTIC
51.51.FACTORSMODIFYINGTHEEFFECTSOFDRUGS
52.52. Individualsdifferbothinthedegreeandthecharacteroftheresponsethatadrugmayelicit
Variationinresponsetothesamedoseofadrugbetweendifferentpatientsandeveninthesame
patientondifferentoccasions.
53.53. Oneormoreofthefollowingcategoriesofdifferencesamongindividualsareresponsibleforthe
variationsindrugresponse: Individualsdifferinpharmacokinetichandlingofdrugs Variationin
numberorstateofreceptors,couplingproteinsorothercomponentsofresponse Variationin
neurogenic/hormonaltoneorconcentrationsofspecificconstituents
54.54. Thesefactorsmodifydrugactioneither:a)Quantitatively Theplasmaconcentrationand/or
thedrugactionisincreasedordecreasedb)Qualitatively Thetypeofresponseisaltered,eg:drug
allergyandidiosyncrasy
55.55. Thevariousfactorsare:1.Bodyweight/size: Itinfluencestheconcentrationofdrugattained
atthesiteofaction Theaverageadultdosereferstoindividualsofmediumbuilt
56.56.Forexceptionallyobeseorleanindividualsandforchildrendosemaybecalculatedonbody
weightbasis BSA=BW(Kg)0.425xHeight(cm)0.725x0.007184doseadultAveragex70(kg)BW
doseIndividualdoseadultAveragex1.7(m2)BSAdoseIndividual
57.57.2.Age:InfantsandChildren: Thedoseofdrugforchildrenoftencalculatedfromtheadultdose
formula)sYoung'.........(doseadultx12AgeAgedoseChildformula)sg'...(Dillindose......adultx20Age
doseChild
58.58. However,infantsandchildrenarehaveimportantphysiologicaldifferences Higherproportion
ofwater Lowerplasmaproteinlevels Moreavailabledrug Immatureliver/kidneys Liver
oftenmetabolizesmoreslowly Kidneysmayexcretemoreslowly
59.59.Elders: Inelderly,renalfunctionprogressivelydeclines(intactnephronloss)anddrugdoses
havetobereduced Chronicdiseasestates Decreasedplasmaproteinbinding Slower
metabolism Slowerexcretion Dietarydeficiencies Useofmultiplemedications Lackof
compliance
60.60.3.Sex: Femaleshavesmallerbodysize,andsorequiredosesofdrugsonthelowersideofthe
doserange Theyshouldnotbegivenuterinestimulantsduringmenstruation,quinineduring
pregnancyandsedativesduringlactation
61.61.4.Pregnancy: Profoundphysiologicalchangeswhichmayaffectdrugresponses: GImotility
reduceddelayedabsorptionoforallyadministereddrugs PlasmaandECFvolumeexpands
Albuminlevelfalls Renalbloodflowincreasesmarkedly Hepaticmicrosomalenzymeinduction
62.62.5.Food: Delaysgastricemptying,delaysabsorption(ampicillin) Calciuminmilkinterferes
withabsorptionoftetracyclinesandironbychelation Proteinmalnutrition LossofBW
Reducedhepaticmetabolizingcapacity Hypoproteinemia
63.63.6.Speciesandrace: Rabbitsresistanttoatropine Rat&miceareresistanttodigitalis In
humans:blacksrequirehigherMongolsrequirelowerconcentrationsofatropineandephedrineto
dilatetheirpupil
64.64.7.Routeofdrugadministration: I.Vroutedosesmallerthanoralroute Magnesiumsulfate:
Orallypurgative Parenterallysedative Locallyreducesinflammation
65.65.8.Biorhythm:(Chronopharmacolgy) Hypnoticstakenatnight Corticosteroidtakenata
singlemorningdose9.Psychologicalstate: Efficacyofdrugscanbeeffectedbypatientsbeliefs,
attitudesandexpectations Particularlyapplicabletocentrallyactingdrugs Insomepatientsinert
drugs(placebo)mayproducebeneficialeffectsequivalenttothedrug,andmayinducesleepin
insomnia
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66.66.10.Presenceofdiseases/pathologicalstates: Drugmayaggravateunderlyingpathology
Hepaticdiseasemayslowdrugmetabolism Renaldiseasemayslowdrugelimination Acid/base
abnormalitiesmaychangedrugabsorptionorelimination Severeshockwithvasoconstrictiondelays
absorptionofdrugsfroms.c.ori.m Drugmetabolismin: Hyperthyroidismenhanced
Hypothyroidismdiminished
67.67.11.Cumulation: Anydrugwillcumulateinthebodyifrateofadministrationismorethanthe
rateofelimination Eg:digitalis,heavymetalsetc.
68.68.12.Geneticfactors: Lackofspecificenzymes Lowermetabolicrate Acetylation Plasma
cholinesterase(Atypicalpseudocholinesterase) G6PD Glucuronideconjugation
69.69.13.Tolerance: Itmeansrequirementofahigherdoseofthedrugtoproduceaneffect,whichis
ordinarilyproducedbynormaltherapeuticdoseofthedrug Drugtolerancemaybe: Natural
Acquired Crosstolerance Tachyphylaxis(ephedrine,tyramine,nicotine) Drugresistance
70.70.14.Otherdrugs: Byinteractionsinmanyways
71.71.Drugclassification(onthebasisofaffinity&efficacy)Agonist:Boththehighaffinityaswellas
intrinsicactivity(IA=1)Thesedrugtriggerthemaximalbiologicalresponseormimiceffectofthe
endogenoussubstance.Ex:MethacholineisacholinomimeticdrugwhichmimicstheeffectofAchon
cholinergicreceptors.
72.72.Antagonist:Whichhaveonlytheaffinitynointrinsicactivity(IA=0).IA=0sono
pharmacologicalactivity.Ratherthesedrugbindtothereceptorandproducereceptorblockade.
AtropineblockstheeffectsofAchonthecholinergicmuscarinicreceptors.
73.73.cAMPsystemSomedrugs,hormonesorneurotransmittersproducetheireffectbyincreasingor
decreasingtheactivityofadenylatecyclaseandthusraisingorlowercAMPwithinthecell.
74.74.StimulationSomeofdrugactbyincreasingtheactivityofspecializedcells.Ex:Catecholamines
stimulatetheheartandHeartrate,Forceofcontraction
75.75.InhibitionSomedrugactbydecreasingtheactivityofspecializedcells.Ex:Alcohol,
Barbiturates,GeneralanestheticthesedrugdepresstheCNSsystem.AtropineinhibitsAchaction.
76.76.ReplacementWhenthereisadeficiencyofendogenoussubstances,theycanreplacedbydrugs.
Ex:InsulininDiabetesmellitusThroxineincretinismandmyxedema
77.77.IrritationCertaindrugsontopicalapplicationcauseirritationoftheskinandadjacenttissues.
Thesedrugsareusingforcounterirritant.Ex:Eucalyptusoil,methylsalicylates(Usedinsprains,joint
pain,myalgia.
78.78.CytotoxicTreatmentofinfectiousdisease/cancerwithdrugsthatareselectivelytoxicfor
infectingorganism/cancercellsEx:AnticancerdrugsAllAntibiotics
79.79.ECamE*GqPLCPIP2DAGSAgonistHydrolysisActivationIP3PKCATPADPProduct
Ca+2CamWatersolublereleaseResponsePhospholipaseCsystemHydrolysisPLC=PhospholipaseC
PIP2=Phosphotiydlinositol4,5diphosphateIP3=InositoltriphosphateDAG=DiacylglycerolE=
EzymePKC=PhosphokinaseC
80.80.Extracellularsiteofaction1.Antacidsneutralizinggastricacidity.2.Chelatingagentsforming
complexeswithheavymetals.3.MgSo4actingaspurgativebyretainingthefluidinsidethelumenof
intestine.
81.81.CellularSiteofAction1.AchonNicotinicreceptorsofmotorendplate,leadingtocontractionof
skeletalmuscle.2.Effectofsympathomimeticsonheartmuscleandbloodvessels.
82.82.IntracellularsiteofactionFolicacidsynthesisinhibitors.Folicacidwhichisintracellular
componentessentialforsynthesisofproteins.Trimethoprimandsulfadruginterferewithsynthesis.
83.83.orFCofheartmuscleLipolysisGlycogenGlycogenbreakdownsynthesistoglucoseGprotein+
EffectorACcAMPATPProteinkinaseActiveCa+2releasePhosphorylationGs/Gi
84.84.PhysicalactionAbsorption:Kaolinabsorbsbacterilaltoxinandthusactsasantidiarrhoealagent.
Protectives:Variousdustingpowders.
85.85.Antagonist:Whichhaveonlytheaffinitynointrinsicactivity(IA=0).IA=0sono
pharmacologicalactivity.Ratherthesedrugbindtothereceptorandproducereceptorblockade.
AtropineblockstheeffectsofAchonthecholinergicmuscarinicreceptors.
86.86.PhysicalActionOsmosis:MgSo4actsasapurgativebyexertingosmaticeffectwithinlumenof
theintestine.Astringents:TheyprecipitatethesurfaceproteinsandprotectthemucosaEx:tannic
acidingumpatientsDemulcent:Thesedrugscoattheinflamedmucusmembraneandprovide
soothingeffect.Ex:Menthol
87.87.FalseincorporationBacteriasynthesisfolicacidfromPABA(ParaAminoBenzoicAcid),for
growthsanddevelopment.SulfadrugsresemblePABA,thereforefalselyenterintothesynthesis
processofPABA,causenonfunctionalproductionandnoutilityforbacterialgrowth.
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88.88.ProtoplasmicpoisonGermicidesandantisepticslikephenolandformaldehydeactasnon
specificallyasprotoplasmicpoisoncausingthedeathofbacteria
89.89.ThroughformationofantibodiesVaccinesproducetheireffectbyinducingtheformationof
antibodiesandthusstimulatethedefensemechanismofthebodyEx:Vaccinesagainstsmallpoxand
cholera
90.90.Targetingspecificgeneticchanges.Anticancerdrugsthatspecificallytargetgeneticchanges.
Inhibitorsofspecifictyrosinekinasethatthatblocktheactivityofoncogenickinases.
91.91.PhysiologicalantagonismTwoantagonists,actingatdifferentsites,counterbalanceeachotherby
producingopp.effectonsamephysiologicalsystem.HistamineVasodilatationNorepinephrine
Vasoconstriction
92.92.Chemicalaction1.IonExchanges:Anticoagulanteffectofheparin(vecharge)antagonizedby
protamine(+vecharged)protein.2.Neutralization:Excessivegastricacidisneutralizedbyantacids.3.
Chelation:Thesearetraptheheavymetals.Ex:EDTA,BAL.
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cAMPsystem
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PhospholipaseCsystem
IonchannelregulationGproteincoupledreceptorscancontrolthefunctioningofionchannelbydon't
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involvinganysec...
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Thesereceptoraredirectlylinkedtyrosinekinase.Receptorbindingdomainpresentinextracellularsite.
Produce...
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EnzymaticreceptorsExtracellularreceptorbindingdomainIntracellularchanges
Receptorregulatinggeneexpression(transcriptionfactors)Unfoldsthereceptorandexposenormally
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ReceptorregulationtheoryReceptorsareindynamicstate.Theaffinityoftheresponsetodrugsisnot
fixed.Italte...
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PharmacodynamicsPPT
Receptorupregulation:ProlongeduseofantagonistReceptornumberandsensitivityDrugeffectEx:
propranololisst...
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PharmacodynamicsPPT
Agonist:Boththehighaffinityaswellasintrinsicactivity(IA=1)Thesedrugtriggerthemaximalbiological
responseor...
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PharmacodynamicsPPT
TypesofagonismSummation:Twodrugselicitingsameresponse,butwithdifferentmechanismandtheir
combinedeffect...
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PharmacodynamicsPPT
TypesofagonismAdditive:combinedeffectoftwodrugsactingbysamemechanismAspirinPGPG
Analgesic+Analgesic+++
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Analgesic+Analgesic+++
PharmacodynamicsPPT
Synergism(Supraadditive):(1+1=3)Thecombinedeffectoftwodrugeffectishigherthaneither
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PharmacodynamicsPPT
individualeffect.Ex:...
TypesofantagonismAntagonism:Effectoftwodrugsislessthansumoftheeffectsoftheindividualdrugs.
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PharmacodynamicsPPT
1.Chemicala...
PharmacokineticantagonismOnedrugaffectstheabsorption,metabolismorexcretionofotherdrugand
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PharmacodynamicsPPT
reducetheireffec...
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PharmacodynamicsPPT
PharmacologicalantagonismPharmacodynamicantagonismbetweentwodrugsactingatsamereceptors.
Twoimportantmechan...
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PharmacodynamicsPPT
Reversibleantagonism(Competitiveantagonism)Theseinhibitioniscommonlyobservedwithantagonists
thatbindreversib...
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PharmacodynamicsPPT
IrreversibleAntagonismItoccurswhentheantagonistdissociatesveryslowornotatallfromthereceptors
resultthat...
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PharmacodynamicsPPT
NonreceptormediatedactionAlldrugsactionarenotmediatedbyreceptors.Someofdrugsmayact
throughchemicalacti...
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PharmacodynamicsPPT
DoseItistherequiredamountofdruginweight,volumes,molesorIUtoprovideadesiredeffect.In
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PharmacodynamicsPPT
clinicalitis...
Singledose:1.Piperazine(45g)issufficienttoeradicateroundworm.2.SingleIMdoseof250mgof
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PharmacodynamicsPPT
ceftriaxonetotreat...
Totaldose:Itisthemaximumquantityofthedrugthatisneededthecompletecourseofthetherapy.Ex:
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PharmacodynamicsPPT
procainepeni...
Maintenancedose:Loadingdosenormallyfollowedbymaintenancedose.Neededtomaintainthesteady
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PharmacodynamicsPPT
stateplasmaconcen...
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PharmacodynamicsPPT
Therapeuticindex:MarginofsafetyDependuponfactorofdoseproducingdesirableeffect dose
elicitingtoxiceffec...
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PharmacodynamicsPPT
ToxicTherapeuticwindow:Optimaltherapeuticrangeofplasmaconcentrationsatwhichmostothepatients
experiencethed...
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PharmacodynamicsPPT
Cyclosporine100400ng/mlCarbamazapine410g/mlDigoxin0.82ng/mlLithium0.81.4
mEq/LPhenotoin102...
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PharmacodynamicsPPT
Tolerance:Increasedamountofdrugrequiredtoproduceinitialpharmacologicalresponse.Usuallyseen
withalcohol,m...
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PharmacodynamicsPPT
TypesoftolerancesInnatetolerance:Geneticallylackofsensitivitytoadrug.Ex:Rabbitstolerateto
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PharmacodynamicsPPT
atropinelarg...
Acquiredtolerances:OccursduetorepeateduseofdrugPharmacokinetictolerances
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PharmacodynamicsPPT
PharmacodynamictoleranceAcu...
PharmacodynamictoleranceDownregulationofreceptorsImpairmentinsignaltransductionEx:
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PharmacodynamicsPPT
Morphine,caffeine,n...
Ex:Mondaydisease.NitroglycerineMonday,Tuesdayworkersgetheadache,aftertheygettolerances.
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PharmacodynamicsPPT
Afterholiday...
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PharmacodynamicsPPT
FACTORSMODIFYINGTHEEFFECTSOFDRUGS
Individualsdifferbothinthedegreeandthecharacteroftheresponsethatadrugmayelicit Variationin
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PharmacodynamicsPPT
responset...
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PharmacodynamicsPPT
Oneormoreofthefollowingcategoriesofdifferencesamongindividualsareresponsibleforthe
variationsindrugresp...
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PharmacodynamicsPPT
Thesefactorsmodifydrugactioneither:a)Quantitatively Theplasmaconcentrationand/orthedrug
actionisincrea...
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PharmacodynamicsPPT
Thevariousfactorsare:1.Bodyweight/size: Itinfluencestheconcentrationofdrugattainedatthesite
ofaction ...
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PharmacodynamicsPPT
Forexceptionallyobeseorleanindividualsandforchildrendosemaybecalculatedonbodyweightbasis
BSA=BW(Kg)0.4...
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PharmacodynamicsPPT
2.Age:InfantsandChildren: Thedoseofdrugforchildrenoftencalculatedfromtheadultdose
formula)sYoung'...........
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formula)sYoung'...........
PharmacodynamicsPPT
However,infantsandchildrenarehaveimportantphysiologicaldifferences Higherproportionofwater
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PharmacodynamicsPPT
Lowerplasmap...
Elders: Inelderly,renalfunctionprogressivelydeclines(intactnephronloss)anddrugdoseshavetobe
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PharmacodynamicsPPT
reduced Chro...
3.Sex: Femaleshavesmallerbodysize,andsorequiredosesofdrugsonthelowersideofthedoserange
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PharmacodynamicsPPT
Theyshould...
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PharmacodynamicsPPT
delayedabsorption...
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PharmacodynamicsPPT
absorptionoftetrac...
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PharmacodynamicsPPT
blacksrequireh...
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PharmacodynamicsPPT
purgative Paren...
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PharmacodynamicsPPT
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PharmacodynamicsPPT
morningdose9.Psycholo...
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PharmacodynamicsPPT
mayslowdrugme...
11.Cumulation: Anydrugwillcumulateinthebodyifrateofadministrationismorethantherateof
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PharmacodynamicsPPT
elimination Eg:...
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PharmacodynamicsPPT
cholinesterase(Atypicalpse...
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PharmacodynamicsPPT
13.Tolerance: Itmeansrequirementofahigherdoseofthedrugtoproduceaneffect,whichisordinarily
producedbyn...
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PharmacodynamicsPPT
14.Otherdrugs: Byinteractionsinmanyways
Drugclassification(onthebasisofaffinity&efficacy)Agonist:Boththehighaffinityaswellasintrinsic
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PharmacodynamicsPPT
activity(I...
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PharmacodynamicsPPT
Antagonist:Whichhaveonlytheaffinitynointrinsicactivity(IA=0).IA=0sonopharmacological
activity.Ratherth...
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PharmacodynamicsPPT
cAMPsystemSomedrugs,hormonesorneurotransmittersproducetheireffectbyincreasingordecreasing
theactivityofade...
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PharmacodynamicsPPT
StimulationSomeofdrugactbyincreasingtheactivityofspecializedcells.Ex:Catecholaminesstimulate
theheartand...
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PharmacodynamicsPPT
InhibitionSomedrugactbydecreasingtheactivityofspecializedcells.Ex:Alcohol,Barbiturates,General
anesthetic...
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PharmacodynamicsPPT
ReplacementWhenthereisadeficiencyofendogenoussubstances,theycanreplacedbydrugs.Ex:Insulin
inDiabetesmel...
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inDiabetesmel...
PharmacodynamicsPPT
IrritationCertaindrugsontopicalapplicationcauseirritationoftheskinandadjacenttissues.Thesedrugs
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PharmacodynamicsPPT
areusi...
CytotoxicTreatmentofinfectiousdisease/cancerwithdrugsthatareselectivelytoxicforinfecting
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PharmacodynamicsPPT
organism/cancercel...
ECamE*GqPLCPIP2DAGSAgonistHydrolysisActivationIP3PKCATPADPProductCa+2Cam
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PharmacodynamicsPPT
WatersolublereleaseResponsePho...
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PharmacodynamicsPPT
Extracellularsiteofaction1.Antacidsneutralizinggastricacidity.2.Chelatingagentsformingcomplexes
withheavymet...
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PharmacodynamicsPPT
CellularSiteofAction1.AchonNicotinicreceptorsofmotorendplate,leadingtocontractionofskeletal
muscle.2.Effe...
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PharmacodynamicsPPT
IntracellularsiteofactionFolicacidsynthesisinhibitors.Folicacidwhichisintracellularcomponent
essentialfors...
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PharmacodynamicsPPT
orFCofheartmuscleLipolysisGlycogenGlycogenbreakdownsynthesistoglucoseGprotein+Effector
ACcAMPATPProtei...
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PharmacodynamicsPPT
PhysicalactionAbsorption:Kaolinabsorbsbacterilaltoxinandthusactsasantidiarrhoealagent.
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PharmacodynamicsPPT
Protectives:Vario...
Antagonist:Whichhaveonlytheaffinitynointrinsicactivity(IA=0).IA=0sonopharmacological
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PharmacodynamicsPPT
activity.Ratherth...
PhysicalActionOsmosis:MgSo4actsasapurgativebyexertingosmaticeffectwithinlumenofthe
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PharmacodynamicsPPT
intestine.Astringe...
FalseincorporationBacteriasynthesisfolicacidfromPABA(ParaAminoBenzoicAcid),forgrowthsand
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PharmacodynamicsPPT
development.Su...
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PharmacodynamicsPPT
ProtoplasmicpoisonGermicidesandantisepticslikephenolandformaldehydeactasnonspecificallyas
protoplasmicpois...
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PharmacodynamicsPPT
ThroughformationofantibodiesVaccinesproducetheireffectbyinducingtheformationofantibodiesand
thusstimulate...
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PharmacodynamicsPPT
Targetingspecificgeneticchanges.Anticancerdrugsthatspecificallytargetgeneticchanges.Inhibitors
ofspecific...
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PharmacodynamicsPPT
PhysiologicalantagonismTwoantagonists,actingatdifferentsites,counterbalanceeachotherby
producingopp.effect...
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PharmacodynamicsPPT
Chemicalaction1.IonExchanges:Anticoagulanteffectofheparin(vecharge)antagonizedbyprotamine
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PharmacodynamicsPPT
(+vecharged)protei...
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PharmacodynamicsPPT
PharmacodynamicsPPT
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PharmacodynamicsPPT
UpcomingSlideShare
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PharmacodynamicsPPT
Loadingin5
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