12 General Principles of Pharmacology

Difficulty level: Medium • Drug Z was able to antagonize the effects of both drug X
28. The figure below depicts the in vitro log dose−response and drug Y.
curves of different drugs acting on the same receptor. Which of the following terms best defines drug X?
A. Competitive antagonist
100 R S T
B. Partial agonist
Maximum effect (%)

80 C. Inverse agonist
P Q
60 D. Irreversible antagonist
E. Full agonist
40

20
Difficulty level: Medium
0
log dose 30. A clinical trial was conducted by orally administering a
new analgesic drug to a group of patients suffering from
Which of the drugs has the highest affinity for the receptor?
arthritic pain. One hour after administration, the patients
A. Drug P were questioned about pain relief, and a sample of blood was
B. Drug Q collected from each patient to measure plasma drug levels.
C. Drug R Pain relief generally correlated well with plasma levels, but
D. Drug S three patients whose plasma levels were equal to zero re-
E. Drug T ported good pain relief. Which of the following is the most
likely explanation of the analgesic effect of the drug in those
Difficulty level: Easy three patients?
29. Some new drugs acting on the same receptor were studied A. High bioavailability of the drug
in laboratory animals. It was found that B. Small volume of distribution of the drug
• Drug X was able to decrease the constitutive level of activ- C. Very low clearance of the drug
ity of the receptor. D. Poor patient compliance
• Drug Y was able to increase the constitutive level of activ- E. Placebo effect
ity of the receptor.

Questions: I-3 Adverse Effects of Drugs

Difficulty level: Easy

Drug Median Effective
1. A 23-year-old woman complained to her physician that the Dose (mg)
diphenhydramine she used to prevent motion sickness when
P 3
traveling by boat was effective in preventing vomiting but
Q 10
caused drowsiness and dry mouth. Which of the following
R 24
terms best explains the underlying cause of these drug-related
S 35
adverse effects?
T 50
A. Genetic predisposition
B. Nonspecific cytotoxicity Which of the drugs most likely has the highest risk of over-
C. Drug−receptor interaction dose toxicity?
D. Immunologic response
A. Drug P
E. Preexisting pathology
B. Drug Q
C. Drug R
Difficulty level: Medium
D. Drug S
2. Five new anticonvulsant drugs (P, Q, R, S, and T) were tested in E. Drug T
laboratory animals. It was found that all of the drugs had ap-
proximately the same lethal dose that produces death in 50%
of subjects (LD50). The median effective dose of each drug is
reported below:
 Questions: I-3 Adverse Effects of Drugs 13

Difficulty level: Easy

Plasma Concentration (mg/L)
3. A 51-year-old man reported to his physician that in the morn- Drug Minimum Minimum
ing he noticed his urine was cloudy and red. The man had effective toxic
been taking an oral anticoagulant for 3 weeks to treat a deep P 5 20
venous thrombosis. If the patient’s symptoms were caused by Q 1 10
the anticoagulant, which of the following adverse drug reac- R 30 60
tions was most likely involved? S 0.6 3
A. Overdose toxicity T 20 80
B. Autoimmune reaction
C. Idiosyncratic reaction Which of the drugs has the highest probability of therapeutic
D. Pseudoallergic reaction success?
E. Immediate allergic reaction A. Drug P
B. Drug Q
Difficulty level: Hard C. Drug R
4. A 23-year-old woman scheduled for surgical dilation and cu- D. Drug S
rettage was anesthetized with thiopental. Shortly after recov- E. Drug T
ery from the anesthesia, the woman had generalized seizures
followed by a deep coma. Further information given by her Difficulty level: Medium
husband indicated that the patient’s mother had suffered from 7. A 32-year-old African American man who worked as a Peace
acute intermittent porphyria. If the coma was caused by thio- Corps volunteer in Ghana presented with weakness, fatigue,
pental, which of the following drug reactions was most likely yellowing of his skin and sclera, and slight fever. He recently
involved? was given chloroquine as a prophylaxis for malaria. Labora-
A. Type II allergic reaction tory findings confirmed the diagnosis of hemolytic anemia
B. Delayed allergic reaction likely due to chloroquine treatment. This patient’s disease
C. Idiosyncratic reaction was most likely mediated by genetic polymorphism of which
D. Pseudoallergic reaction of the following enzymes?
E. Overdose toxicity A. N-acetyltransferase
B. Glucose-6-phosphate dehydrogenase
Difficulty level: Medium C. Reduced form of nicotinamide adenine dinucleotide
5. A 28-year-old woman who had had a mitral valve replace- (NADH)−methemoglobin reductase
ment for rheumatic heart disease 2 years ago had her sus- D. Pseudocholinesterase
pected pregnancy confirmed by a positive pregnancy test. Her E. Glucuronosyltransferase
current medications include the anticoagulant warfarin (U.S.
Food and Drug Administration [FDA] category for teratogenic Difficulty level: Medium
risk D) and amoxicillin (FDA category B). Which of the follow- 8. A 61-year-old woman complained to her physician of a burn-
ing would be the best course of action to be implemented by ing sensation when she urinated. Past history of the patient
her family physician? was significant for serious hypersensitivity to sulfa drugs. Uri-
A. Stop all medications throughout pregnancy nalysis revealed abundant gram-negative bacteria, and a sen-
B. Suspend warfarin for the first trimester of pregnancy sitivity test showed that they were sensitive to amikacin,
C. Replace warfarin with heparin and continue amoxicillin piperacillin, trimethoprim-sulfametoxazole, ciprofloxacin, and
D. Continue warfarin and replace amoxicillin with penicil- ceftriaxone. A diagnosis of urinary tract infection was made,
lin G and an antibiotic therapy was prescribed. Which of the fol-
E. Reduce the dose of warfarin and continue amoxicillin lowing antibiotics should be avoided in this patient?
A. Trimethoprim-sulfamethoxazole
Difficulty level: Medium B. Piperacillin
6. Five new antihypertensive drugs were tested in healthy vol- C. Amikacin
unteers. All of the drugs were found to be equally effective D. Ciprofloxacin
in controlling hypertension. The minimum effective plasma E. Ceftriaxone
concentrations and the minimum toxic plasma concentra-
tions were determined for each drug. The results are reported
below: