PSYOi335iMidtermi1iStudyiGuide
WhatiisiaiDrug?i-i
iiiiiiiiiiiiiiAisubstanceithatialtersitheiphysiologyiofitheibodyibutiisinotiaifoodiorinutrient.
psychoactiveidrugsi-i
iiiiiiiiiiiiiicrossitheiblood-brainibarrier
actiuponitheicentralinervousisystemi
affectibrainifunctioni
changeiperception,imood,iconsciousness,icognition,ibehavior
usedirecreationally,ientheogenetically,imedically
NamesiofiDrugsi-i
iiiiiiiiiiiiiiChemicaliName
GenericiName
TradeiName
StreetiName
DrugiNamesi-i
iiiiiiiiiiiiiiAidrug'sichemicalinameirevealsiitsichemicalicompositioniandimolecularistructure
Pharmaceuticalicompaniesialsoimayipatentibrandinames,ioritradeinames,iforitheiriproduct
GenericiDrugsi-i
iiiiiiiiiiiiiicontainisameiactiveiingredientsiasitheioriginalibrandinameidrug
mustibeipharmacologicallyiequivalent.
Excipientsi-i
iiiiiiiiiiiiiiCarrierimedium
Moreiweightiincreasesichargeiwithisameidoses
USAi-isellingi100idosesiofipureiLSDi=iminimumisentencei<i1yri
100idosesionipaperi=iMinisentenceitwoiyears,ithreeimonths
100idosesionisugaricubesi=iMinisentencei>i15iyears
Sarafemi-i
iiiiiiiiiiiiiiMarketedibyiitsimanufacturer,iEliiLilly,iforiPMDDitreatmentiafteriitiacquiredianother
ipatent--Prozac'sipatentiwasidueitoiexpire.i
1i|iP a g e
,Lillyispentimoreithani$30imillionipromotingitheidrug
Pharmacodynamics/Pharmacokineticsi-i
iiiiiiiiiiiiiiWhatiaidrugidoesitoitheibody
pharmacodynamicsiisitheieffectithatidrugsihaveionitheibody
pharmacokineticsiisitheistudyiofitheiwayiiniwhichidrugsimoveithroughitheibodyiduringiabsorp
tion,idistribution,imetabolismiandiexcretion
DescribingiDosesi-i
iiiiiiiiiiiiiiMilligrams:i1/1000iofiaigram
Dosesigiveniiniaccordanceitoibodyiweighti(/kg)
DoseiResponseiRelationshipsi-i
iiiiiiiiiiiiiifindidrugieffectsibyistudyingidifidosesiandimeasureiresponseichanges.
Relationshipibetweenidoseiandiresponseiisicalleditheidose-responseicurvei(DRC).
ImportanticharacteristiciofiDRCi-i
iiiiiiiiiiiiiiSlope
Slopei-i
iiiiiiiiiiiiiiRefersitoitheimostlyilinearicentralipartiofitheicurve;ihowisharplyitheieffectichangesiwi
thieachichangeiinidose.
Ifiaismallichangeiinidoseiproducesiailargeichangeiinieffect,itheislopeiisisteep.
Ifilargeichangesiinidoseiproducesismallichangesiinieffect,itheislopeiisishallow.
DescribingiDosesi-i
iiiiiiiiiiiiiiED50
LD50
ED50i-i
iiiiiiiiiiiiiiTheiMedianieffectiveidose
Theidoseithatiisieffectiveiini50%iofitheisubjectsitested.
LD50i-i
iiiiiiiiiiiiiiMedianilethalidose
Theidoseithatiwasilethaliini50%iofitheisubjectsitested.
TherapeuticiIndexi-i
iiiiiiiiiiiiiiTIi=iLD50i/iED50
2i|iP a g e
,TheigreateritheiTI,itheisaferitheidrug;itheidifferenceibetweenitheidesiredieffectianditheiundesir
ediorilethalieffectiisilarger.
Toibeisafer,itheiTIicanibeicalculatedibyiusingitheiLD1i/iED99
TheiloweritheiTI,itheiloweritheisafety.
THCi-i>1000,iMorphinei-i70,iCocainei-i15,iAlcoholi-i10,iHeroini-i6
Otherifactorsitoiconsideri-iease/ispeedioficonsumption
TherapeuticiWindowi-i
iiiiiiiiiiiiiiTheitherapeuticiwindowiisiairangeiofibloodiconcentrationsiofiaimedicineiaboveiaileve
lithatiisiineffectivei(therapeuticilevel)iandiailevelithatihasitoxicisideieffectsi(toxicilevel).
Complicatedibyiabsorptioni/iexcretionicurves
PotencyiandiEffectivenessi-i
iiiiiiiiiiiiiiTheiextentiofitheidrugsieffect
Potencyi-i
iiiiiiiiiiiiiiDifferencesiinitheiED50
E.g.ifetanyliisimuchimoreipotentithaniheroin
Effectivenessi-i
iiiiiiiiiiiiiiDifferencesiinitheimaximumieffectithatidrugsiwilliproduceiatianyidose
e.g.itakingi50iaspiriniversusimorphine
Morphineiwilliworkibetter
EffectivenessiDefinitioni-i
iiiiiiiiiiiiiiTheimaximumieffectiobtainable,iwithiadditionalidosesiproducinginoieffect.i
Someidrugsimayibeipotent,ibutitheyimightineveribeiableitoiproduceiaipeakiresponseinoimatter
ihowimuchiisigiven
Aidrugithatiisimoreieffectiveicaniproduceiaigreateripeak,iorimaximum,ieffectithaniaidrugithatii
silessieffective.
Primary/mainieffecti-i
iiiiiiiiiiiiiiIntendediresultiinitreatment
Sideieffecti-i
iiiiiiiiiiiiiiUnintended;i
Mayibeiharmful
Addiction?
3i|iP a g e
, DrugiInteractionsi-i
iiiiiiiiiiiiiiDrugiAntagonism
AdditiveiEffect
SuperadditiveiEffect
DrugiAntagonismi-i
iiiiiiiiiiiiiiOneidrugidiminishesitheieffectiofitheiother
AdditiveiEffecti-i
iiiiiiiiiiiiiiShiftsitheiDRCitoitheileft
SuperadditiveiEffect/Potentiation/iAgonismi-i
iiiiiiiiiiiiiiCombiningidrugsiincreasesitheieffect
Physiological
-Alcoholi&isedatives
Behavioral
-Alcoholi&istimulants
Pharmacokinetics:i-i
iiiiiiiiiiiiiiWhatitheibodyidoesitoiaidrug
Absorption,iTransport,iExcretion
Administrationi-i
iiiiiiiiiiiiiihowiaidrugigetsiintoitheibody
Absorbtioni-i
iiiiiiiiiiiiiiHowiaidrugigetsiintoitheiblood
Distributioni-i
iiiiiiiiiiiiiiHowiititravels
Bindingiatisitesiofiactioni-i
iiiiiiiiiiiiiiwhereitheidrugineedsitoigo
Inactivationiandiexcretioni-i
iiiiiiiiiiiiiihowitheidrugileaves
Routesiforiadministration:
parenterali-i
iiiiiiiiiiiiiiunderitheiskini
vehicleiisineededi(e.g.iliquid)
Parenteraliroutesi-i
4i|iP a g e
WhatiisiaiDrug?i-i
iiiiiiiiiiiiiiAisubstanceithatialtersitheiphysiologyiofitheibodyibutiisinotiaifoodiorinutrient.
psychoactiveidrugsi-i
iiiiiiiiiiiiiicrossitheiblood-brainibarrier
actiuponitheicentralinervousisystemi
affectibrainifunctioni
changeiperception,imood,iconsciousness,icognition,ibehavior
usedirecreationally,ientheogenetically,imedically
NamesiofiDrugsi-i
iiiiiiiiiiiiiiChemicaliName
GenericiName
TradeiName
StreetiName
DrugiNamesi-i
iiiiiiiiiiiiiiAidrug'sichemicalinameirevealsiitsichemicalicompositioniandimolecularistructure
Pharmaceuticalicompaniesialsoimayipatentibrandinames,ioritradeinames,iforitheiriproduct
GenericiDrugsi-i
iiiiiiiiiiiiiicontainisameiactiveiingredientsiasitheioriginalibrandinameidrug
mustibeipharmacologicallyiequivalent.
Excipientsi-i
iiiiiiiiiiiiiiCarrierimedium
Moreiweightiincreasesichargeiwithisameidoses
USAi-isellingi100idosesiofipureiLSDi=iminimumisentencei<i1yri
100idosesionipaperi=iMinisentenceitwoiyears,ithreeimonths
100idosesionisugaricubesi=iMinisentencei>i15iyears
Sarafemi-i
iiiiiiiiiiiiiiMarketedibyiitsimanufacturer,iEliiLilly,iforiPMDDitreatmentiafteriitiacquiredianother
ipatent--Prozac'sipatentiwasidueitoiexpire.i
1i|iP a g e
,Lillyispentimoreithani$30imillionipromotingitheidrug
Pharmacodynamics/Pharmacokineticsi-i
iiiiiiiiiiiiiiWhatiaidrugidoesitoitheibody
pharmacodynamicsiisitheieffectithatidrugsihaveionitheibody
pharmacokineticsiisitheistudyiofitheiwayiiniwhichidrugsimoveithroughitheibodyiduringiabsorp
tion,idistribution,imetabolismiandiexcretion
DescribingiDosesi-i
iiiiiiiiiiiiiiMilligrams:i1/1000iofiaigram
Dosesigiveniiniaccordanceitoibodyiweighti(/kg)
DoseiResponseiRelationshipsi-i
iiiiiiiiiiiiiifindidrugieffectsibyistudyingidifidosesiandimeasureiresponseichanges.
Relationshipibetweenidoseiandiresponseiisicalleditheidose-responseicurvei(DRC).
ImportanticharacteristiciofiDRCi-i
iiiiiiiiiiiiiiSlope
Slopei-i
iiiiiiiiiiiiiiRefersitoitheimostlyilinearicentralipartiofitheicurve;ihowisharplyitheieffectichangesiwi
thieachichangeiinidose.
Ifiaismallichangeiinidoseiproducesiailargeichangeiinieffect,itheislopeiisisteep.
Ifilargeichangesiinidoseiproducesismallichangesiinieffect,itheislopeiisishallow.
DescribingiDosesi-i
iiiiiiiiiiiiiiED50
LD50
ED50i-i
iiiiiiiiiiiiiiTheiMedianieffectiveidose
Theidoseithatiisieffectiveiini50%iofitheisubjectsitested.
LD50i-i
iiiiiiiiiiiiiiMedianilethalidose
Theidoseithatiwasilethaliini50%iofitheisubjectsitested.
TherapeuticiIndexi-i
iiiiiiiiiiiiiiTIi=iLD50i/iED50
2i|iP a g e
,TheigreateritheiTI,itheisaferitheidrug;itheidifferenceibetweenitheidesiredieffectianditheiundesir
ediorilethalieffectiisilarger.
Toibeisafer,itheiTIicanibeicalculatedibyiusingitheiLD1i/iED99
TheiloweritheiTI,itheiloweritheisafety.
THCi-i>1000,iMorphinei-i70,iCocainei-i15,iAlcoholi-i10,iHeroini-i6
Otherifactorsitoiconsideri-iease/ispeedioficonsumption
TherapeuticiWindowi-i
iiiiiiiiiiiiiiTheitherapeuticiwindowiisiairangeiofibloodiconcentrationsiofiaimedicineiaboveiaileve
lithatiisiineffectivei(therapeuticilevel)iandiailevelithatihasitoxicisideieffectsi(toxicilevel).
Complicatedibyiabsorptioni/iexcretionicurves
PotencyiandiEffectivenessi-i
iiiiiiiiiiiiiiTheiextentiofitheidrugsieffect
Potencyi-i
iiiiiiiiiiiiiiDifferencesiinitheiED50
E.g.ifetanyliisimuchimoreipotentithaniheroin
Effectivenessi-i
iiiiiiiiiiiiiiDifferencesiinitheimaximumieffectithatidrugsiwilliproduceiatianyidose
e.g.itakingi50iaspiriniversusimorphine
Morphineiwilliworkibetter
EffectivenessiDefinitioni-i
iiiiiiiiiiiiiiTheimaximumieffectiobtainable,iwithiadditionalidosesiproducinginoieffect.i
Someidrugsimayibeipotent,ibutitheyimightineveribeiableitoiproduceiaipeakiresponseinoimatter
ihowimuchiisigiven
Aidrugithatiisimoreieffectiveicaniproduceiaigreateripeak,iorimaximum,ieffectithaniaidrugithatii
silessieffective.
Primary/mainieffecti-i
iiiiiiiiiiiiiiIntendediresultiinitreatment
Sideieffecti-i
iiiiiiiiiiiiiiUnintended;i
Mayibeiharmful
Addiction?
3i|iP a g e
, DrugiInteractionsi-i
iiiiiiiiiiiiiiDrugiAntagonism
AdditiveiEffect
SuperadditiveiEffect
DrugiAntagonismi-i
iiiiiiiiiiiiiiOneidrugidiminishesitheieffectiofitheiother
AdditiveiEffecti-i
iiiiiiiiiiiiiiShiftsitheiDRCitoitheileft
SuperadditiveiEffect/Potentiation/iAgonismi-i
iiiiiiiiiiiiiiCombiningidrugsiincreasesitheieffect
Physiological
-Alcoholi&isedatives
Behavioral
-Alcoholi&istimulants
Pharmacokinetics:i-i
iiiiiiiiiiiiiiWhatitheibodyidoesitoiaidrug
Absorption,iTransport,iExcretion
Administrationi-i
iiiiiiiiiiiiiihowiaidrugigetsiintoitheibody
Absorbtioni-i
iiiiiiiiiiiiiiHowiaidrugigetsiintoitheiblood
Distributioni-i
iiiiiiiiiiiiiiHowiititravels
Bindingiatisitesiofiactioni-i
iiiiiiiiiiiiiiwhereitheidrugineedsitoigo
Inactivationiandiexcretioni-i
iiiiiiiiiiiiiihowitheidrugileaves
Routesiforiadministration:
parenterali-i
iiiiiiiiiiiiiiunderitheiskini
vehicleiisineededi(e.g.iliquid)
Parenteraliroutesi-i
4i|iP a g e