Concepts in Pharmaceutical Science Name:

Midterm PSC G100

Fall, 2005, Dr. Loring’s section ID:

Please answer the questions on this form. You may use the back if necessary, but please
keep your answers as brief as possible. Multiple choice questions are 2 points.

1) A drug that binds to a cell receptor and directly causes a physiological response is
called:

A. An Agonist
B. An Antagonist
C. A Receptor blocker
D. An Activator

4) A Hill plot with a slope significantly less than one indicates:

A. Negative cooperativity
B. Positive cooperativity
C. The presence of more than one binding site
D. Either A or C

15) (3 pt) Define Therapeutic index in your own words. If a drug has an ED50 of 3 times less
than its LD50, does this drug have a large therapeutic index? Briefly explain your answer, but
include the difference between ED50 and LD50.

16) (8 points). How does the volume of distribution affect the potency of a drug in a clinical
setting? In your answer be sure to define the volume of distribution, and indicate how
distribution of a drug into body compartments can alter the potency of that drug from the
potency predicted by measurements of the drug binding to its molecular target.

1
25) (4 points) Explain how smoking, diet, and/or alcohol consumption can change the
metabolism of drugs. Be sure to include a description of the process of enzyme induction and
contrast that with the processes of enzyme activation or enzyme inhibition.

2
26) (9 points) Refer to the figure on the next page (You can tear it out if necessary, since
there are no questions on it). The figure shows metabolic pathways for a hypothetical drug.
(1 point each) Match the labeled arrows on the figure with the possible metabolic reaction
steps (fill in the number corresponding to the name of that reaction step given on the list
below), indicate whether the step is a phase I or phase II reaction, and, if phase I, whether
cytochrome P450 is involved (Yes or No). Fill in your answers below in the space provided:
Each arrow is worth 1 point, ½ for each reaction step, and ¼ each for the phase I/II and
cytochrome P450 sections.

Possible Reaction Steps:

1. Glucuronidation 10. Sulfoxide formation
2. Epoxidation 11. O-Dealkylation
3. N-hydroxylation 12. Aliphatic oxidation
4. O-methylation 13. Aromatic hydroxylation
5. Hydrolysis 14. Oxidative deamination
6. Mercapturide formation 15. Reduction
7. Sulfation 16. Epoxide hydration
8. Desulfuration 17. Acetylation
9. Oxidative dehalogenation 18. Purine oxidation

Arrow Reaction Step Phase I or II?Cytochrome P450 (Y/N)?

A.
B.
C.
D.
E.
F.
G.
H.
I.

3
 Hypothetical drug metabolic pathways

CH3 CH3
O
C O C O
O S OH
N NH NH NH2
O N N

N N N
D

A C
E OCH3 OCH3 OCH3
CH3
B CH3
CH3
C O
OH C O C O
N NH
N NH
N NH

N
N N
O

F
OCH3
OH
CH3 OCH3 H
C O CH3
OCH3 G CH3
NH C O
N C O
N NH
N NH
N
HO N
HO N
OH
S
CH2
CH3
OCH3 I CH NH
C O
OCH3 C OC O OCH3
N NH
COOH OH CH3

O
O N
OH

OCH3