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Understanding Drug Interactions: Cytochrome P450 and Inhibitor Effects

Understanding Drug Interactions: Cytochrome P450 And Inhibitor Effects

Explore the complexities of drug interactions based on Chapter 11, Page 140 of RxPrep, supplemented with additional resources. This focused assessment aids in understanding the critical interactions within pharmacology, essential...

Questions: 29 | Attempts: 10 | Last updated: Aug 4, 2025

Sample Question 1
What are CYP's? Where are CYP's located? What is the most predominant CYP?

CYPs are the major enzymes involved in drug metabolism and bioactivation, accounting for about 75% of the total number of different metabolic reactions. Found primarily in liver and intestines. CYP 450 3A4 accounts for 1/2 of all CYP drug metabolism.

CYPs are structures in the heart responsible for pumping blood throughout the body.

CYPs are neurotransmitters located in the brain that regulate mood and behavior.

CYPs are proteins found in plants that are responsible for photosynthesis.

Sample Question 2
How do inducers and inhibitors affect substrate drug levels?

Inducers - increase in the amount / activity of enzymes involved in liver metabolism (CYP's, P-pg efflux transporters that are in the gut, resulting in DECREASED substrate drug conc. Inhibitors - block / inactivate CYP's, P-gp efflux transporters in the gut resulting in less substrate metabolism and higher (INCREASED) substrate conc. NET EFFECT: Inducers = DECREASED drug levels Inhibitors = INCREASED drug levels

Inducers - decrease the amount/activity of enzymes involved in liver metabolism, resulting in increased substrate drug concentrations. Inhibitors - enhance the activity of enzymes involved in liver metabolism leading to decreased substrate drug concentrations.

Inducers - do not have any effect on liver metabolism enzymes, resulting in no change in substrate drug concentrations. Inhibitors - cause a temporary spike in liver enzyme activity followed by a rapid decrease in substrate drug concentrations.

Inducers - inhibit the activity of enzymes involved in liver metabolism, resulting in increased substrate drug concentrations. Inhibitors - promote enzyme activity in liver metabolism leading to decreased substrate drug concentrations.

Sample Question 3
How does the FDA define Strong Inhibitors?

Drugs that have no impact on plasma AUC values

Drugs that cause > 5-fold increase in plasma AUC values OR> 80% decrease in substrate clearance

Drugs with mild effects on substrate clearance

Drugs that enhance the metabolism of substrates