PHARMACODYNAMICS

1. A 68-year-old m an recently diagnosed with atrial fibrillation started therapy with atenolol, a β-
receptor blocker. Which of the following changes most likely occurred in cardiac myocytes
during the first 2 weeks of therapy?
A. Spare β receptors became activated.
B. The G-protein number decreased.
C. The β-receptor number increased.
D. Most β receptors became phosphorylated.
E. The ability to respond to intracellular cyclic adenosine monophosphate (cAMP) declined.

2. A new drug was tested in an in vitro system. It was found that only one enantiomer of the
racemic pair bound substantially to a specific receptor, whereas the other enantiomer showed
negligible binding. Which of the following term s best defines this property?
A. Intrinsic activity
B. Affinity
C. Stereoselectivity
D. Potency
E. Variability
F. Maxim al efficacy

3. A 14-year-old girl suffering from seasonal rhinitis started a therapy with loratadine, a drug that
binds to H1 histamine receptors. Which of the following term s describes a characteristic of
loratadine binding to the H1 receptor?
A. Intrinsic activity
B. Potency
C. Maximal efficacy
D. Affinity
E. Receptor activation

4. Two new drugs were tested in laboratory animals. Which of the following drug parameters
was most likely recorded to estimate the relative potency of both drugs?
A. The therapeutic index of both drugs
B. The maximal responses produced by each drug
C. The graded log dose−response curve of both drugs
D. The volume of distribution of both drugs
E. The clearance of both drugs

5. A 65-year-old man suffering from osteoarthritis has been taking naproxen, 500 mg daily for 1
month. The drug was effective, but the patient suffered from nausea and heartburn. The
physician decided to try another nonsteroidal anti-inflammatory drug (NSAID) and prescribed
celecoxib, a drug ~5 times more potent than naproxen, with negligible gastrointestinal side
effects. Which of the following would be the most appropriate daily dose of celecoxib (in mg) to
prescribe to the patient?
A. 50
B. 1000
C. 10
D. 25
E. 100
F. 75

6. A 2-year-old boy was admitted to the emergency department after a generalized tonic-colonic
seizure. His mother reported that the boy apparently ingested several tablets of propranolol, a β-
blocker, which he had found in his father’s dresser drawer. Vital signs on admission were blood
pressure 85/50 mm Hg, heart rate 40 beats per minute (bpm), respiratory rate 20/m in. The boy
received an intramuscular injection of glucagon, a hormone that activates glucagon receptors in
the heart, causing a significant increase in heart contractility. Which of the following terms best
defines the antagonism between glucagon and β-blockers?
A. Chemical
B. Functional
C. Competitive
D. Pharmacokinetic
E. Pharmacological

7. The effect of a new autonomic drug was tested on a healthy volunteer during a clinical trial.
The subject was treated with saline or with the drug, and cardiac rate was recorded at rest or
after exercise. The results are reported below.
Which of the following term s best defines the tested drug?
A. Noncompetitive antagonist
B. Competitive antagonist
C. Partial agonist
D. Physiologic antagonist
E. Full agonist
F. Chemical antagonist

8. A 65-year-old woman suffering from atrial fibrillation had been taking a drug to treat this
condition for 6 months. The drug had no intrinsic activity and bound reversibly to β1 receptors.
Which of the following term s best defines this drug?
A. Partial agonist
B. Functional antagonist
C. Inverse agonist
D. Noncompetitive antagonist
E. Competitive antagonist
F. Full agonist

9. A new β-blocker was tested in healthy volunteers. The cumulative frequency distribution of
subjects showing a decrease of 10 bpm in the heart rate was plotted against the log dose.
Which of the following drug parameters can be determined from this cumulative frequency
distribution?
A. Receptor affinity
B. Median effective dose
C. Therapeutic index
D. Therapeutic window
E. Maxim al efficacy
10. In the figure below, curve X depicts the in vitro log dose−response curve for a full α1 agonist
on contraction of vascular smooth muscle. Which of the curves best depicts the log
dose−response curve of that agonist when a fixed dose of a competitive α1 antagonist is given
concomitantly?

A. Curve P
B. Curve Q
C. Curve R
D. Curve S
E. Curve T