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Questions and Answers
What is the main characteristic of bioprecursor prodrugs?
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?
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?
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?
Why is the nonsteroidal anti-inflammatory drug (NSAID) Sulindac inactive as the sulfoxide?
What problem is associated with the bioprecursor prodrugs approach due to the participation of alternate metabolic paths?
What problem is associated with the bioprecursor prodrugs approach due to the participation of alternate metabolic paths?
Why must the metabolite generated after chemical hydrolysis be nontoxic and easily removed?
Why must the metabolite generated after chemical hydrolysis be nontoxic and easily removed?
What is an example of a prodrug that requires oxidative activation?
What is an example of a prodrug that requires oxidative activation?
What is the main reason for the stomach irritation associated with NSAIDs?
What is the main reason for the stomach irritation associated with NSAIDs?
Why does the carboxylic acid functionality in NSAIDs become ionized in the cells of the gastric mucosa?
Why does the carboxylic acid functionality in NSAIDs become ionized in the cells of the gastric mucosa?
How does nabumetone differ from other NSAIDs in terms of stomach irritation?
How does nabumetone differ from other NSAIDs in terms of stomach irritation?
What is the result of metabolism in the liver on nabumetone?
What is the result of metabolism in the liver on nabumetone?
Inhibition of the target enzyme, cyclooxygenase, by NSAIDs results in:
Inhibition of the target enzyme, cyclooxygenase, by NSAIDs results in:
What is a less common method of prodrug activation compared to oxidative activation?
What is a less common method of prodrug activation compared to oxidative activation?
What is an example of a drug requiring reductive activation as a prodrug?
What is an example of a drug requiring reductive activation as a prodrug?
'Mitomycin C' is used in the treatment of which types of cancer?
'Mitomycin C' is used in the treatment of which types of cancer?
What is an important consequence of the reduction of quinone in 'Mitomycin C'?
What is an important consequence of the reduction of quinone in 'Mitomycin C'?
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