Pharmacokinetics Study Guide

1. Define pharmacokinetics. What does pharmacokinetics tell us about the

relationship between a drug and the body?
2. List 5-6 ways that a physiochemical makeup of a drug influences its
pharmacokinetics.
3. Define ADME.
4. Describe/draw the basic mechanisms involved in the passive transport of
drugs through membranes; do the same for the active transport of drugs.
5. In a sentence or two (at most), list the typical absorption patterns of the
following routes of drug administration:
- Intravenous
- Subcutaneous
- Intramuscular
- Oral ingestion
6. What does bioavailability refer to? Which routes of drug administration
result in the fastest increase in bioavailability? The least?
7. What is first pass metabolism? Describe the biological pathways involved
in it. How does first pass metabolism influence bioavailability?
8. Which routes of administration bypass first pass metabolism?
9. Name four factors that influence drug distribution, and an
anatomical/physiological example of each.
10. Which type of capillary will allow for the most rapid release/distribution of
a drug?
11. List the main classes/types of plasma proteins that bind drugs. Is a drug
that is bound to a plasma protein able to reach its targets and have a
therapeutic effect? List the factors plasma protein factors that influence the
percent of a drug in the blood that is bound to plasma proteins.

12. How does clearance interact with plasma protein binding to influence the
concentration of a drug in the plasma?
13. List 5 main anatomical sites where metabolism of drugs can can occur.
14. Define Phase I and Phase II metabolism. How are they different?
15. List the main metabolizing enzymes associated with Phase I metabolism.
Where are they located? What does each do?
16. CYP450 induction or inhibition by one drug can greatly influence the
actions of another drug. Describe what happens to the second drug when the
first induces CYPs, and when the first inhibits them. What is the biggest
cause of inhibition?
17. What are oxygenases, and what does each class listed in the lecture
slides do? Where is each type found, both cellularly and anatomically (i.e.
organs)?
18. What do Phase II metabolism enzymes do (in general)? What changes do
they cause drugs and/or drug metabolites in order to increase their
excretion?
19. Define the following enzymes, and what each adds to their drug targets?
- SULTs
- UGTs
- GSTs
- NATs
- MTs
- Alcohol dehydrogenases, aldehyde dehydrogenases, NQOs

20. What is the most common conjugation reaction in phase II metabolism?

Where are the highest levels of the enzymes causing this found?
21. Briefly describe the role(s) of the kidney in drug elimination. Which types
of drugs are eliminated here? Which are not?

22. What are the two main superfamilies of transporters discussed in class?
How (in general) does each work?
23. ~ slide 46 shows various types of transporters. Know each type, and
which direction(s) they transport drugs, metabolites, or ions!