Medical Pharmacology: Drug Metabolism Practice Questions

Medical Pharmacology: Drug Metabolism Practice Questions

Choose the correct answer for each question.

Which one(s) of the following will be appropriately described as (a) prodrug(s)?
1. Tamoxifen
2. Losartin
3. Both
4. Neither
Mitomycin C, an anticancer prodrug, requires activation by among others, a cytochrome P450 reductase to convert the parent compound into a DNA alkylating drug.
1. True
2. False
Mitomycin C exhibits selective killing of hypoxic cancer cells associated with core regions of solid tumors.
1. True
2. False
Mitomycin selectivity for hypoxic malignant cells in solid tumor core regions occurs because:
1. These cells have higher concentrations of cytochrome P450 reductase, which activates mitomycin C.
2. Under hypoxic conditions, re-oxidation of the reduced, active mitomycin C metabolite is inhibited.
3. Both
4. Neither
Phase I enzymes
1. Cytochrome P450 enzymes
2. Flavin containing monooxygenase enzymes
3. Non-cytochrome P450 enzymes
4. A & B
5. B & C
6. A & C
7. A, B & C
Cytochrome P450 enzymes:
1. Hepatic microsomal enzymes
2. Mitochondrial P450 enzymes
3. Both
4. Neither
The cytochrome P450 isoform CYP3A4:
1. Responsible for most cytochrome P450 activity for anesthetic drugs.
2. CYP3A4 is involved in metabolism of more than 50% of currently available drugs.
3. Both
4. Neither
Example/examples of reactions that may utilize cytochrome P450 enzymes:
1. Hydrolysis reactions
2. Conjugation
3. Both
4. Neither
Conjugation reactions and drug metabolism:
1. Involves cytochrome P450 enzymes
2. When glucuronic acid is added to lipid-soluble drugs, the resultant glucuronide conjugates are more water-soluble and more readily excreted.
3. Both
4. Neither
Ester-hydrolysis of drugs, typically at an ester bond, do not require cytochrome P450 enzyme systems.
1. True
2. False

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Source Material:
- Buxton ILO Chapter 2: Pharmcokinetics: The Dynamics of Drug Absorption, Distribution, Metabolism, and Elimiation in Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 14e, (Brunton LL H Knollmann BC, eds) McGraw-Hill Education, 2023.
- Gonzalez FJ Coughtrie M Chapter 5: Drug Metabolism in Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 14e, (Brunton LL H Knollmann BC, eds) McGraw-Hill Education, 2023.
- Holford NHG Chapter 3: Pharmacokinetics & Pharmacodynamics: Rational Dosing & the Time Course of Drug Action: in Basic & Clinical Pharmacology (Katzung BG, Editor; Vanderah TW, Associate editor) 15e McGraw Hill 2021.
- Correia MA Chapter 4 Drug Biotransformation in Basic & Clinical Pharmacology (Katzung BG, Editor; Vanderah TW, Associate editor) 15e McGraw Hill 2021.
- Baca QJ Golan DE Pharmacokinetics Chapter 3: Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. (Golan DE, editor-in chief, Armstrong EJ Armstrong AW, associate editors) 4e Wolters Kluwer 2017.
- Guengerich FP Chapter 4: Drug Metabolism in Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. (Golan DE, editor-in chief, Armstrong EJ Armstrong AW, associate editors) 4e Wolters Kluwer 2017.
- Flood P Shafer SL Chapter 2 Basic Principles of Pharmacology in Stoelting's Pharmacology & Physiology in Anesthetic Practice (Glood P Rathmell JP Urman RD, eds) 6e Wolters Kluwer 2022.
- Burchum JR Rosenthal LD Lehne's Pharmacology for Nursing Care Unit II Chapter 4 Pharmcokinetics 11 e Elsevier 2022.