Pharmacology: Drug Metabolism

Questions and Answers

What is the primary role of metabolic enzymes when drugs enter the body?

To degrade or modify the foreign structure for excretion (correct)

To prolong the half-life of the drug

To enhance the side effects of the drug

To increase the potency of the drug

Which statement accurately describes drug metabolites?

They can only result in beneficial effects.

They are always less toxic than the original drug.

They may lose activity, retain some activity, or be more active than the parent drug. (correct)

They always retain the activity of the original drug.

What consequence can arise from drug metabolism?

Metabolism decreases the chance of drug interactions.

All drugs are always inactive after metabolism.

It guarantees that drugs will be effective for a longer duration.

Some metabolites may cause side effects or toxicity. (correct)

What is a prodrug strategy?

A strategy to activate drugs in the body via metabolism. Signup and view all the answers

What must be done before a new drug can be approved?

The metabolites must be identified, and their biological activities tested. Signup and view all the answers

Why is understanding drug metabolism important for medicinal chemists?

To prevent the formation of unacceptable metabolites and design better drugs. Signup and view all the answers

What is required about the structure and stereochemistry of each metabolite?

They must be determined and tested for biological activity. Signup and view all the answers

Study Notes

Drug Metabolism Overview

Drugs entering the body are attacked by metabolic enzymes aiming to degrade or modify them for easier excretion.
Metabolic reactions lead to the formation of metabolites, which can differ significantly in activity compared to the original drug.

Metabolites and Their Effects

Common outcome: metabolites often lose the pharmacological activity of the parent drug.
Possible scenarios:
- Some metabolites retain partial activity.
- In rare cases, metabolites exhibit greater activity than the original drug.
- Certain metabolites may produce different effects, potentially leading to side effects or toxicity.

Implications for Drug Development

Understanding drug metabolism is crucial for medicinal chemists to avoid creating drugs that lead to harmful metabolites.
The prodrug strategy utilizes metabolism to activate drugs once in the body, enhancing therapeutic effectiveness.

Regulatory Requirements

Drug approval mandates comprehensive identification of all drug metabolites.
Each metabolite's structure and stereochemistry must be determined.
Assessment of the biological activity of metabolites is essential prior to approval.

Description

Explore the fascinating process of drug metabolism in this quiz. Learn how metabolic enzymes modify drugs to form metabolites and their implications on drug activity. Test your knowledge on the various reactions and outcomes that occur once drugs enter the body.