usIbecause: Answer: marginIofIerrorIbetweenItherapeutic IandItoxicIisInarrow Q:IMetabolism Answer: -MostlyIinItheIliver -
Biotransformation IorIchangeIitItoIinactiveIformIorImakeIitImoreIwaterIsolubleItoIfacilitateIexc
retion •Itransformed IsubstanceIisIcalledItheImetabolite. Q:ITheIrateIofImetabolism IisIaffectedIby: Answer: -age,IliverI&IdrugItolerance •IBodyImayIproduceImoreIenzymesI&ItheIliverIbecomesIfasterIatIbreakingIthatIparticularIdrug
Idown Q:IhalfIlife Answer: thisIisItheItimeIitItakesItheIpeakIlevelItoIfallIbyI½ Q:ISteadyIstateIofIaIdrug: Answer: -WhenItheIrateIofIdrugIadministration I&Ielimination IareIequal -canIbeIachievedIinI4I-I5IhalfIlives Q:IPhaseIIIreactions: Answer: Transforms Idrug,ICYP450IOxidases.IMakeIitIavailableIforItheIbodyItoIuse Q:IPhaseIIIIreactions: Answer: Conjugation IreactionsIorIattachIdrugIwithIsomething. IEndIproductsItendItoIbeIlessIactiveIthanI
theirIsubstrates Q:IExcretion: Answer: -KidneysIareItheImainIexcretoryIgland.I -OtherImodesIincludeIfeces,Ibile,Irespiration, Imilk,Iperspiration IandItears Q:IGlomerular IFiltration: Answer: RemovesIdrugsIorImetabolites InotIboundItoIproteinsIpresentIinItheIbloodIplasma. -Metabolite IexcretedIinItheIurine Q:Iinducers Answer: speedsIupImetabolism Q:Iinhibitors Answer: slowIdownImetabolism Q:ICytochrome IP450Imetabolizing Ienzymes Answer: -Cytochrome IP450:IAltersIjustIhowItheIbodyImetabolizes ImanyIdrugs -
Nomenclature: IExampleICYP2D6:ICYPI(cytochrome IP450Ienzyme)2I(Family)IDI(Subfamily) I
6I(Individual Ienzyme) -Pharmacogenetic Itesting •Idetermines ICYP450Idifferences •IPredictsIHighIvs.ILowISubstratesIofI2D6,I2C19,I3A4 -Prodrug:ILiverImetabolism IactivatesItheIdrug.I•IExample:ICodeine •IConvertedItoImorphineIviaICYP2D6 Q:ICYPI1A2 Answer: -CYPI1A2ISubstrates: •ICaffeine,ITheophylline, IsomeITCA'sI(Amitriptyline, Iclomipramine, Iimipramine), IHaloperidol
,IOlanzapine I&Iothers. -CYP1A2IInhibitors: •ICiprofloxacin, IVerapamil, IFluvoxamine -CYP1A2IInducers: •IOmeprazole, ICharbroiled Ifoods,IPhenobarbital, ITobaccoIsmokingI •ITobaccoIsmokingIwillIinduceItheImetabolism IofIOlanzapine I(Zyprexa)I&IHaloperidol I(Haldo
l) Q:ICYPI2D6 Answer: GreatlyIaffectedIbyIpolymorphism -CYPI2D6ISubstrates: •IVenlafaxine, IDuloxetine, IFluoxetine, IParoxetine, IFluvoxamine, IseveralIantipsychotics, IBetaIB
lockers,IStimulants, IOpioids -CYP2D6IInhibitors: •IFluoxetine, IParoxetine, IBupropion I&I(SertralineImoderateIinhibitor) -CYP2D6IInducers: •INoIstrongIinducers Q:ICYPI3A4 Answer: