Bioprecursor Prodrugs Lecture: Activation Types
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Questions and Answers

What is the main characteristic of bioprecursor prodrugs?

  • Contain a carrier or promoiety
  • Irreversible metabolic oxidation
  • Metabolically or chemically transformed to the active drug molecule (correct)
  • Oxidative activation

    • Which type of activation is most common for bioprecursor prodrugs?

  • Oxidative activation (correct)
  • Reductive activation
  • Chemical activation
  • Phosphorylation

    • What is a widely exploited activation type in the development of antiviral agents?

  • Oxidative activation
  • Reductive activation
  • Phosphorylation (correct)
  • Chemical activation

    • Why is the nonsteroidal anti-inflammatory drug (NSAID) Sulindac inactive as the sulfoxide?

    <p>It must be reduced metabolically to the active sulfide</p> Signup and view all the answers

    What problem is associated with the bioprecursor prodrugs approach due to the participation of alternate metabolic paths?

    <p>Inactivation of the compound</p> Signup and view all the answers

    Why must the metabolite generated after chemical hydrolysis be nontoxic and easily removed?

    <p>To prevent toxicity and allow easy removal after performing its function</p> Signup and view all the answers

    What is an example of a prodrug that requires oxidative activation?

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

    What is the main reason for the stomach irritation associated with NSAIDs?

    <p>Increased release of gastric acid</p> Signup and view all the answers

    Why does the carboxylic acid functionality in NSAIDs become ionized in the cells of the gastric mucosa?

    <p>Lower intracellular pH</p> Signup and view all the answers

    How does nabumetone differ from other NSAIDs in terms of stomach irritation?

    <p>It contains no acidic functionality</p> Signup and view all the answers

    What is the result of metabolism in the liver on nabumetone?

    <p>It produces the active compound</p> Signup and view all the answers

    Inhibition of the target enzyme, cyclooxygenase, by NSAIDs results in:

    <p>Increased release of gastric acid</p> Signup and view all the answers

    What is a less common method of prodrug activation compared to oxidative activation?

    <p>Reductive activation</p> Signup and view all the answers

    What is an example of a drug requiring reductive activation as a prodrug?

    <p>Mitomycin C</p> Signup and view all the answers

    'Mitomycin C' is used in the treatment of which types of cancer?

    <p>Bladder and lung cancer</p> Signup and view all the answers

    What is an important consequence of the reduction of quinone in 'Mitomycin C'?

    <p>Alkylating active drug species</p> Signup and view all the answers

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