NU578 - UNIT 1AH QUESTIONS WITH
CORRECT ANSWERS
SchedulesIs-
sans✔✔DrugssinsthissscheduleshavesnosacceptedsmedicalsusesinsthesUnitedsStatessandsh
avesashighsabusespotential.s
Examplessaresheroin,smarijuana,sLSD,speyote,setc.
SchedulesIIs-
sans✔✔Drugssinsthissscheduleshavesashighsabusespotentialswithsseverespsychicsorsphysic
alsdependencesliability.sIncludedsarescertainsnarcoticsanalgesics,sstimulants,sandsdepress
antsdrugs.s
Examplessaresopium,smorphine,scodeine,shydromorphone,smethadone,smeperidine,soxyc
odone,sanileridine,scocaine,samphetamine,smethamphetamine,sphenmetrazine,smethylph
enidate,samobarbital,spentobarbital,ssecobarbital,smethaqualone,sandsphencyclidine.
SchedulesIIIs-
sans✔✔DrugssinsthissscheduleshavesansabusespotentialslesssthansthosesinsSchedulessIsan
dsIIsandsincludescompoundsscontainingslimitedsquantitiessofscertainsnarcoticsanalgesicsdru
gs,sandsothersdrugsssuchsassbarbiturates,sglutethimide,smethyprylon,sandschlorphentemin
e.s
Anyssuppositorysdosagesformscontainingsamobarbital,ssecobarbital,sorspentobarbitalsissins
thissschedule.
SchedulesIVs-
sans✔✔DrugssinsthissscheduleshavesansabusespotentialslesssthansthoseslistedsinsSchedule
sIIIsandsincludessuchsdrugssassbarbital,sphenobarbital,schloralshydrate,sethchlorvynol,smep
robabmate,schlordizepoxide,sdiazepam,soxazepam,schloroazepate,sflurazepam,setc.
SchedulesVs-
sans✔✔DrugssinsthissscheduleshavesansabusespotentialslesssthansthoseslistedsinsSchedule
sIVsandsconsistsprimarilysofspreparationsscontainingslimitedsquantitiessofscertainsnarcoticsa
nalgesicsdrugssusedsforsantitussivesandsantidiarrhealspurposes.
Absorptions-
sans✔✔Processsofsdrugsmovementsfromsitsssitesofsadministrationsintosthesblood
Mostscommonsmechanismsforsdrugsabsorptions-sans✔✔passivesdiffusion
,First-passseffects
(presystemicsmetabolism)s-sans✔✔Rapidshepaticsinactivationsofscertainsoralsdrugs
drugsissmetabolizeds(chemicallysaltered)sassitspassessthroughseithers1)sgutswall,sands2)sliv
er.
Distributions-
sans✔✔drugsmovementsfromsthesbloodstosthesinterstitialsspacesofstissuessandsfromstheresi
ntoscells
Barriersstosdistributions-sans✔✔-sBloodsbrainsbarrier
-sPlacenta
PhysiologicsFactorssAffectingsDistributions-sans✔✔-sPerfusion
-sBindingsofsdrugstosplasmasprotein
-sSpecializedsDistributionsBarriers
Albumins-sans✔✔Bindssacidicsdrugs
Proteins(albumin)sbindings-
sans✔✔Preventssboundsdrugsmoleculessfromsleavingsthesbloodstream
Prolongssthesdistributionsphases(Increasesshalf-life)
alpha-1sacidsglycoproteins-sans✔✔Bindssbasicsdrugs
Reservoirseffects-sans✔✔
Blood-BrainsBarriers(BBB)s-
sans✔✔nosintercellularsporessbetweensbrainscapillarysendothelialsmembranessduestosthes
presencesofstightsjunctionssbetweenscells
Tosgainsaccessstosthesbrainsfromsthescapillaries,sdrugssmusts-
sans✔✔1)sdiffusesacrossscellss(lipid-soluble,
nonionizedsform)s
or
2)sorsbesactivelystransportedsbysascarrier
PlacentalsBarriers-sans✔✔Transfersofsdrugssissrelativelysslowswithsthe
equilibrationstimesbetweensmaternalsbloodsandsfetalstissuessestimatedsatsabouts15sminute
ssforssomesdrugssandsalmostsanshoursforsothersdrugs.
, (Virtuallyseverysdrugsusedsforstherapeuticspurposesscansandsdoesscrosssthesplacenta.)
Drugsscrosssthesplacentasbys-sans✔✔diffusions(lipid-soluble,snonionizedsdrugs
penetratesmostsrapidly.)
PharmacokineticsFactors
AffectingsDistributions-sans✔✔-sCompetitionsforsproteinsbindingssites
-sAlterationsofsextracellularspH
Metabolisms-sans✔✔Chemicalsalterationsofsdrugsstructure
Metabolisms-sans✔✔Usuallysproducessaspolar,swater-
solublessubstanceswhichsissmoreseasilysexcretedsfromsthesbody.
Lipid-solublesdrugss-sans✔✔notseasilyseliminatedsbysthesbody'ssexcretorysmechanisms
Sitessofsdrugsmetabolisms-sans✔✔-slivers(smoothsERsandshepatocytes)
-sgutswallsandsmucosalssurface
-splasma
PhasesIs(nonsynthetic)smetabolicsreactionss-
sans✔✔oxidationsbysthescytochromesP450ssystemswhichsissasfamilysofsdrug-
metabolizingsenzymessinsthesliver.
CytochromesP450ssystem
(Hepaticsmicrosomalsenzymessystem)s-
sans✔✔Thesmajorsfunctionsofsthissenzymessystemsisstosaddsansoxygensatomstosthesdrugss
ubstrate.
drugs+sO2s-------->sdrug-OH
EnzymessinsthesP450ssystemsthatsmetabilizesdrugss-sans✔✔CYP1,sCYP2,sCYP3
Consequencessofsdrugsmetabolisms-sans✔✔Acceleratedsrenalsdrugsexcretion
Drugsinactivation
Increasedstherapeuticsaction
Activationsofsprodrugs
Increasedsorsdecreasedstoxicity
Prodrugs-
sans✔✔Ansinactivesdrugsdosagesformsthatsissconvertedstosansactivesmetabolitesbysvarious
sbiochemicalsreactionssoncesitsissinsidesthesbody.
ex:sfosphenytoins-->sCodeine