2022-09-24T16:13:59+03:00[Europe/Moscow] en true <p>Dose</p>, <p>Concentration</p>, <p>Efficacy </p>, <p>true</p>, <p>EC50</p>, <p>Potency </p>, <p>Affinity</p>, <p>Kd</p>, <p>B max</p>, <p>Kd</p>, <p>high affinity</p>, <p>drug affinity, degree of spareness</p>, <p>Degree of spareness</p>, <p>coupling</p>, <p>Complex</p>, <p>Spare receptors</p>, <p>Intermediate activation</p>, <p>can't be activated</p>, <p>true</p>, <p>10</p>, <p>less efficient</p>, <p>by binding a partial agonist</p>, <p>Inverse Agonist</p>, <p>Agonist</p>, <p>Competitive antagonist</p>, <p>Noncompetitive antagonist</p>, <p>false</p>, <p>drug affinity; degree of spareness</p>, <p>coupling</p>, <p>Kd=EC50</p>, <p>Partial agonists</p>, <p>true</p>, <p>prevents endogenous ligand/agonist binding to Ri</p>, <p>block transition; orthosteric site</p>, <p>block transition; allosteric site</p>, <p>c</p>, <p>Ki</p>, <p>false</p>, <p>voltage-gated, transporters, enzymes</p> flashcards
Quantifying Pharmacodynamics

Quantifying Pharmacodynamics

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  • Dose

    amount of a drug administered to an organism

  • Concentration

    amount of drug in a given compartment

  • Efficacy

    the maximal effect produced by the drug

  • true

    Not all drugs reach 100% effect in the system, but they still reach their Emax. T/f?

  • EC50

    the concentration of a drug that produces 50% of its maximal effect

  • Potency

    the concentration/dose required to produce an effect of a given intensity

  • Affinity

    measure of the strength and probability that a drug will bind an available receptor at a given time

  • Kd

    the equilibrium dissociation constant when half of the drug is bound and the other half is unbound.

  • B max

    the maximal amount of receptors bound by drug at plateau

  • Kd

    Which is usually greater? EC50 or Kd

  • high affinity

    What does low kd signify ?

  • drug affinity, degree of spareness

    Why aren't EC50 and Kd always the same?

  • Degree of spareness

    the total # of receptors present vs total # of receptors needed to elicit Emax

  • coupling

    What ties drug binding to the end effect?

  • Complex

    Is coupling usually simple or complex?

  • Spare receptors

    when an Emax is reached but there are still receptors left unbinded

  • Intermediate activation

    maximal effect elicited by activation of relatively few receptors because the response initiated by an individual drug-receptor binding event persists longer than the binding event itself.

  • can't be activated

    The receptor is available for drug binding, however, intermediate activation is taken place; this means downstream signaling ________

  • true

    Spare receptors dramatically influence Kd. T/F?

  • 10

    If your EC50 is 10 and you have 10 receptors, what is your Kd?

  • less efficient

    Partial agonists are ______ couplers

  • by binding a partial agonist

    How can we inhibit the response of a full agonist clinically?

  • Inverse Agonist

    -receptors can be in active form (Ra) or inactive form (Ri)

    -shift equilibrium to Ri

  • Agonist

    -receptors can be in active form (Ra) or inactive form (Ri)

    -shift equilibrium to Ra

  • Competitive antagonist

    -block transition to Ra by competing for orthosteric site

    -can be overcome with increasing [agonist], thereby shifting potency (EC50)

  • Noncompetitive antagonist

    -block transition to Ra by binding to an allosteric site

    -cannot be overcame by increased [agonist], thereby shifting efficacy (Emax)

  • false

    All drugs are either agonists or antagonists. T/F

  • drug affinity; degree of spareness

    Why aren't EC50 and Kd always the same?

  • coupling

    ______ is what ties drug binding to the end effect

  • Kd=EC50

    If you have 10 receptors, Kd is 10.

    If no spare receptors exist,

  • Partial agonists

    -receptors that produce a lower effect at full receptor occupancy

  • true

    Partial agonists can competitively inhibit the responses of a full agonist. True or false?

  • prevents endogenous ligand/agonist binding to Ri

    What is antagonists role in Ra and Ri equilibrium?

  • block transition; orthosteric site

    Competitive antagonists ________ to Ra by competing for the ________

  • block transition; allosteric site

    Noncompetitive antagonists _______ to Ra by binding to an __________

  • c

    Which type of antagonists can be overcame with increasing agonist? Which cannot?

    a. competitive; uncompetitive

    b. noncompetitive; competitive

    c. competitive; noncompetitive

  • Ki

    -this measuring factor utilizes the ratio of a known concentration of antagonist and compares it to an agonist without antagonist present vs with antagonist present.

    -defines the strength of competitive antagonist

  • false

    All drugs are either agonist or antagonist. True or false?

  • voltage-gated, transporters, enzymes

    Which type of receptors don't respond to typical ligand binding interactions?