Pharmacodynamics-3: Drug-Receptor Interaction
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Questions and Answers

What is the drug concentration which achieves 50% of the maximum effect called?

  • Potency
  • Affinity
  • EC50 (correct)
  • Emax
  • Which drug has the highest affinity according to the given text?

  • Codeine
  • Adrenaline
  • Morphine
  • Fentanyl (correct)
  • What type of drug binds to the receptor but does not cause a cellular response?

  • Inverse agonist
  • Full agonist
  • Antagonist (correct)
  • Partial agonist
  • What happens to the efficacy of a full agonist when combined with a noncompetitive antagonist?

    <p>It decreases</p> Signup and view all the answers

    According to the given text, what is the factor affecting affinity?

    <p>Receptor density</p> Signup and view all the answers

    What is the mathematical relationship that defines the dissociation constant (Kd)?

    <p>Kd = Koff / Kon</p> Signup and view all the answers

    What determines the concentration of a drug around the receptor needed to form a certain number of drug-receptor complexes?

    <p>Drug affinity</p> Signup and view all the answers

    What follows the law of mass action in drug-receptor interaction?

    <p>Effect</p> Signup and view all the answers

    What is the capacity to activate a receptor called in drug-receptor interaction?

    <p>Drug efficacy</p> Signup and view all the answers

    What determines the fraction of receptors at each state during equilibrium in drug-receptor interaction?

    <p>Dissociation constant</p> Signup and view all the answers

    What determines the fraction of receptors at each state during equilibrium in drug-receptor interaction?

    <p>Dissociation constant</p> Signup and view all the answers

    What is the mathematical relationship that defines the dissociation constant (Kd)?

    <p>Kd = [R] [D] / [DR]</p> Signup and view all the answers

    Which factor affects the drug affinity in drug-receptor interaction?

    <p>Kon rate of association</p> Signup and view all the answers

    What happens to the efficacy of a full agonist when combined with a competitive antagonist?

    <p>Decreases</p> Signup and view all the answers

    What type of drug binds to the receptor but does not cause a cellular response?

    <p>Antagonist</p> Signup and view all the answers

    What is the effect of a competitive antagonist on the dose-response curve of a full agonist?

    <p>Parallel right shift</p> Signup and view all the answers

    Which drug is an example of a partial agonist acting as an antagonist in the presence of an agonist?

    <p>Aripiprazole</p> Signup and view all the answers

    What determines the maximal efficacy of a partial agonist?

    <p>Maximal efficacy of the full agonist</p> Signup and view all the answers

    What is the main difference between a competitive and a noncompetitive antagonist?

    <p>Competitive antagonist competes for the agonist-binding site</p> Signup and view all the answers

    What is the effect of a noncompetitive antagonist on the efficacy of a full agonist?

    <p>Vertical shift downwards</p> Signup and view all the answers

    Study Notes

    Drug-Receptor Interaction

    • The drug concentration that achieves 50% of the maximum effect is called EC50.

    Types of Drugs

    • A drug that binds to the receptor but does not cause a cellular response is called an antagonist.
    • A partial agonist is a drug that binds to the receptor and causes a cellular response, but with lower efficacy than a full agonist.
    • An example of a partial agonist acting as an antagonist in the presence of an agonist is the drug buspirone.

    Affinity and Dissociation Constant

    • The factor affecting affinity is the strength of binding between the drug and the receptor.
    • The mathematical relationship that defines the dissociation constant (Kd) is Kd = [R] [D] / [RD], where [R] is the concentration of receptors, [D] is the concentration of drug, and [RD] is the concentration of drug-receptor complexes.

    Receptor Binding

    • The concentration of a drug around the receptor needed to form a certain number of drug-receptor complexes is determined by the law of mass action.
    • The law of mass action states that the rate of a reaction is proportional to the concentrations of the reactants.

    Receptor Activation

    • The capacity to activate a receptor is called efficacy.
    • The fraction of receptors at each state during equilibrium is determined by the affinity and efficacy of the drug.

    Antagonists

    • A competitive antagonist increases the EC50 of a full agonist, shifting the dose-response curve to the right.
    • A noncompetitive antagonist decreases the efficacy of a full agonist, without changing the EC50.
    • The main difference between a competitive and a noncompetitive antagonist is that competitive antagonists bind to the same receptor as the agonist, while noncompetitive antagonists bind to an allosteric site.

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    Description

    Test your understanding of drug-receptor interaction in pharmacodynamics with this quiz. Explore concepts such as drug-receptor complex formation, the law of mass action, drug affinity, and drug efficacy.

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