2 - Rush University (Questions &
Answers)
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1. Pharmacodynamics::what the drug does to the body y
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2. What is an LDR curve?:A log dose response curve, or a curve that describes the
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relationship bewteen the drug effect (Y axis) and the log of the dose (X axis).
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3. What is the difference between quantal and graded LDR curves?: Graded: the
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effectofthedrugfallsonascale(i.e.howmanymmHGdidtheBPdeclinewhen plotted
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against an increasing log dose?)
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Quantal:the "response" is predefined (i.e.a SBP < 130 mmHg) and data is plotted to show
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who was affected and who wasn't.an either/or situation.
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4. Potency: The dose of a drug necessary to produce 50% of a drug's maximal effect gy gy gy gy gy gy gy gy gy gy gy gy gy gy
(ED50).Sort of tells you "howmuch bang you get for your buck"in terms of solely dosage
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amount.
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5. If themaximalresponsetoa newmedicationis a 50mmHgdeclineinSBP, what
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is the ED50 on a graded LDR curve?: The dosage that will produce a 25mmHg
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declined in SBP.
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6. If the desired response for a new medication is a decrease in SBP to < 130
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mmHg, what is the ED50 on a quantal LDR curve?: The dosage associated with
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reaching the target BP (< 130) in 50% of the population.
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,7. Efficacy:The maximum response that a drug is capable of producing. y
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8. Compare each drug's potency and efficacy: gy gy gy gy gy
9. What does the steepness of an LDR curve indicate?: What degree of effect a
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dose change willhave (slight change on a steep curve will elicit large effects, big change
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on a flat curve will elicit small effects).
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10. ED50:The dose of a medication thatproducesa specific therapeutic effect in 50% y
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of the population.
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11. TD50:The dose of a medication that produces a specific toxic effect in 50% of the y
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population.
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12. Therapeuticindex:TD50/ED50,orthespacebetweenthetherapeuticandtoxic LDR y
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curves of a drug.
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13. True or false:adrug with a wide therapeuticindex is generally saferthan a drug
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with a narrow therapeutic index.: True
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14. Calculate the therapeutic index of a drug if the ED50 = 0.4 and the TD50 = 40.: y
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40/0.4 = 100
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15. True or false: you can visually compare the therapeutic indexes, and safety, of y
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two drugs with different slopes.: False - if the two drugs have curves that are not
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parallel to each other they are not easily compared.
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16. Stereoisomer:Adrugthathasbothanactiveandinactiveisomer,formulated so y
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that the active isomer is at a dose that achieves the therapeutic response.
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17. Enantiomers:Mirrorimagestereoisomers(havethesamechemicalstructure with y
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a different orientation) that have different pharmacological effects.
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, 18. Racemicmixture:Anequalmixtureoftwoenantiomers.Ex:Albuterol,consist- ing of j
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the active isomer (R-albuterol) and an inactive isomer (S-albuterol).Effects from the
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inactive isomer are usually clinically insignificant.
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19. Ka:Thevolumeneededtogetonemoleofunbounddrugwhen50%ofthetarget
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receptors are occupied.
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20. Kd:The concentration of drug in the plasma when 50% of the target receptors are
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occupied
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21. Partialagonist:Adrugthatbindstoareceptorandstimulatesaneffectthathas both j
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lower potency (curve is shifted right of the full agonist) and efficacy (curve is shorter in
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height).
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22. Whywouldwegiveapartialagonist?:Topreventundesirablesideeffectsof the full
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agonist, or because the full agonist isn't necessary.Ex:greater pain relief and
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psychotropic effects from methadone, but less respiratory depression from
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buprenorphine.
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23. Competitiveantagonism:Reversible;effectsdependontherelativeconcen- j
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tration of the agonist and antagonists (which also occupy receptor sites)
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24. What will the LDR curve of an agonist combined with a fixed dose of a gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j
competitive antagonist look like?: Parallel to the agonist curve, but shifted to the
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right.Effects of the antagonist can be overcome with an increased dose of the agonist.
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25. Noncompetitiveantagonism:Irreversible;effectsareindependentoftherela- tive j
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concentration of the agonist and antagonist (which don't occupy the agonists' receptor
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sites).
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26. What will the LDR curve of an agonist combined with a fixed dose of a gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j gy j
noncompetitiveantagonistlooklike?:Shifteddownwardandtotheright.Effects of
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the antagonist cannot be overcome with an increased dose of the agonist.
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27. What is the clinical relevance of giving an irreversible, non-competitive gy j gy j gy j gy j gy j gy j gy j gy j gy j
antagonist?:Mustwaitfortheeffectsoftheantagonisttowearoff,sincegivingmore
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agonist will have no effect (ex:pt stops taking aspirin 10-14 days prior to surgery).
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28. What type of antagonist drug do we most oftenadminister?:Reversible, j
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competitive antagonists (much easier to control).
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29. True or false:no matterhow high the molar concentration of a reversible, j
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competitive antagonist,you can always overcome it by giving a higher dose of
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