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ID:46946420
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页数:19页
时间:2019-12-01
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1、BasicpharmacokineticsProfessorFKamaliWolfsonUnitofClinicalPharmacologyBasicpharmacokineticsPharmacokineticsconceptOnecompartmentmodelSemi-logarithmdrugconcentrationvtimeplotMeasurementofdrugpharmacokineticparametersBasicpharmacokineticsPharmacokineticsisadisciplinethatusesmathematicalmode
2、lstodescribeandpredictdrugamountsandconcentrationsinvariousbodyfluidsthatchangesinthesequantitiesovertime.Absorption,distribution,biotransformationandelimination.Plasmadrugconcentration:-netresultsoftheaboveprocessestakingplacesimultaneously.Whatispharmacokinetics?Whatisthevalueofpharmaco
3、kinetics?Establishandmaintaintherapeutic,yetnon-toxicamountsofdruginbodyandatthepharmacologicsiteofaction.Morespecifically:Rationalchoiceofdrugdoses,frequencyofadministration,androuteofadministration.CharacteristicsofthepatientandhisdiseaseCanalterthepharmacokineticpropertiesofadrugAdju
4、stmentofdosage,dosingfrequencycancompensateforkineticchangesProblemsofineffectivenessand/ortoxicitymaybeavoided.Theunderstandingofpharmacokineticsshouldenhancethelikelihoodofsafeandeffectivedrugtherapy.FactorsaffectingdrugpharmacokineticsPatientcharacteristics:AgeSexTotalbodyweightSmoking
5、habitsAlcoholconsumptionOtherco-ingesteddrugsFactorsaffectingdrugpharmacokineticsDiseasestates:Liverdisease(cirrhosis,hepatitis)RenaldiseaseCongestiveheartfailureInfectionFeverShockSevereburnsAnaemiaOnecompartmentmodelDyedoesnotdisappearatasteadyrateRateofeliminationofdyeisproportionaltot
6、heconcentrationAnyprocessinwhichtherateofchangeofavariableisproportionaltothemagnitudeofthatvariableissaidtobeanexponentialprocessSemi-logarithmplotAKelof0.1/himplies10%ofdrugeliminatedperhour.-Kel=slope=1nC1-1nC2/tRewrite1nC1–1nC2as:1n(C1/C2)Whentimeintervalt=t½;C1/C2=2As1n2=0.693Kel=0.6
7、93t½Semi-logarithmplotSemi-logarithmplotCalculationofdrughalf-life(t½)Calculationofeliminationconstant(Kel)TwomethodsGradientmethod2.EquationKel=0.7(time)-1t½abSlope=a/bEliminationclearance(CL)ClearanceusedasameasureofeliminationAppliestobothexcretionandmetabolismMo
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