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Calculations of Bioavailability and Bioequivalence

1.

Ifthebioavailabilityfactor(F)fora100mgtabletofadrugis0.70comparedwiththe
bioavailabilityfactorof1.0foraninjectionofthesamedrug,howmanymillilitersof
theinjectioncontaining40mg/mLwouldbeconsideredbioequivalenttothetablet?

2.If5mLofanelixircontaining2mg/mLofadrugisbioequivalenttoa15mgtablet
havingabioavailabilityfactorof0.60,whatisthebioavailabilityfactor(F)oftheelixir?

3.If500mgofadrugareadministeredorallyand300mgareabsorbedintothe
circulation,calculatethebioavailabilityfactor(F).

4.Adrugis40%bioavailablebytheoralrouteand58%bioavailablebythetransdermal
route.Ifapatientistakinga2.5mgoraldosetwiceadayandisswitchedtothe
counterpart2%ointment,howmanygramsoftheointmentshouldbeadministeredto
providetheequivalentdoseofthedrug?

5.

Adrugusedtotreatasthmais55%bioavailableas5mgtablets.Ifapatientis
switchedtotheinhalantformofthedrug,whichis87%bioavailable,howmanymetered
500gspraysshouldthepatientadministerevery12hourstoreceiveanequivalentdrug
dose?

Calculations of Bound Drug, Elimination Half-Life, and Volume of Distribution

6.4Ifa6mgdoseofadrugisadministeredintravenouslyandproducesabloodcon
centrationof0.4g/mL,calculateitsapparentvolumeofdistribution.

7.Ifatequilibrium,twothirdsoftheamountofadrugsubstanceinthebloodisboundto
protein,whatwouldbethealpha()valueofthedrug?

8.Thealpha()valueforadruginthebloodis0.90,equatingto0.55ng/mL.Whatisthe
concentrationoftotaldrugintheblood?

9.Apatientreceivedanintravenousdoseof10mgofadrug.Abloodsamplewasdrawn,
anditcontained40g/100mL.Calculatetheapparentvolumeofdistributionforthe
drug.

10.Thevolumeofdistributionforadrugwasfoundtobe10literswithabloodlevel
concentrationof2g/mL.Calculatethetotalamountofdrugpresentinthepatient.

11.Calculatetheeliminationrateconstantforadrughavinganeliminationhalflifeof
1.7hours.

12.Plotthefollowingdataonsemilogarithmicgraphpaperanddetermine(a)the
eliminationhalflifeofthedrugand(b)theeliminationrateconstant.
PlasmaDrugConcentration/Time
(g/100mL)8.50.56.81.05.41.54.02.03.22.52.53.0

13.Whatpercentageofanoriginallyadministeredintravenousdoseofadrugremainsin
thebodyfollowingthreehalflives?

14.Ifthehalflifeofadrugis4hours,approximatelywhatpercentageofthedrug
administeredwouldremaininthebody15hoursafteradministration?

15.If100mgofadrugareadministeredintravenously,andtheresultantdrugplasma
concentrationisdeterminedtobe2.5g/mL,calculatetheapparentvolumeofdistribution.
(hours)

16.Ifadoseof1gofadrugisadministeredintravenouslytoapatientandthedrug
plasmaconcentrationisdeterminedtobe65g/mL,calculatetheapparentvolumeof
distribution.

17.Thevolumeofdistributionforchlordiazepoxidehasbeendeterminedtobe34liters.
Calculatetheexpecteddrugplasmaconcentrationofthedrug,inmicrogramsper
deciliter,immediatelyafteranintravenousdoseof5mg.

18.Innormalsubjects,bloodmakesupabout7%ofthebodyweight.
.

(a)Calculatetheapproximatebloodvolume,inliters,foramanweighing70kg.

(b)IfthedrugZANTACreachedpeakbloodlevelsofabout500ng/mL2to3hours
afteranoraldose,calculatethetotalamountofthedrug,inmilligrams,inthebloodof
thepatientdescribedin(a)whenpeakbloodlevelsareachieved.

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