Bioprecursor Prodrugs Lecture: Activation Types

Play an AI-generated podcast conversation about this lesson

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?

It must be reduced metabolically to the active sulfide Signup and view all the answers

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

Inactivation of the compound Signup and view all the answers

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

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

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

Nabumetone Signup and view all the answers

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

Increased release of gastric acid Signup and view all the answers

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

Lower intracellular pH Signup and view all the answers

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

It contains no acidic functionality Signup and view all the answers

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

It produces the active compound Signup and view all the answers

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

Increased release of gastric acid Signup and view all the answers

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

Reductive activation Signup and view all the answers

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

Mitomycin C Signup and view all the answers

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

Bladder and lung cancer Signup and view all the answers

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

Alkylating active drug species Signup and view all the answers

Bioprecursor Prodrugs Lecture: Activation Types

Podcast Beta

Questions and Answers