Select The Single Best Answer: A. Bioavailability

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EXAM I PRACTICE QUESTIONS

SELECT THE SINGLE BEST ANSWER

1.

Which of the following terms is used to designate the ratio of the amount of drug to reach the
systemic circulation to the actual dose of the drug that is administered?
A.
B.
C.
D.
E.

2.

Which of the following would tend to reduce the time required for an orally-administered
drug to reach the systemic circulation?
A.
B.
C.
D.
E.

3.

high degree of ionization in the gastric fluid


high molecular weight
low degree of ionization in the gastric fluid
low lipid solubility (Kp)
retention in the stomach by the presence of food

The discipline of pharmacology known as pharmacokinetics is concerned primarily with an


analysis of which drug property?
A.
B.
C.
D.
E.

4.

bioavailability
first pass fraction
intrinsic clearance
steady state
volume of distribution

absorption and distribution


chemical stability
clinical patterns of use
mechanism of action
time course of action

Which of the following plasma proteins is quantitatively the most important for binding
drugs that are weak acids?
A.
B.
C.
D.
E.

albumin
alpha1-acid glycoprotein
fatty acid binding globulin
high density lipoprotein
plasma cholinesterase

5.

Which of the following statements is a correct description of the distribution of a drug


between two compartments separated by a biological membrane?
A.
B.
C.
D.
E.

6.

When a drug is administered intravenously, the plasma concentration will increase until the
rates of administration and elimination are equal. Which term is used to refer to this general
pharmacokinetic observation?
A.
B.
C.
D.
E.

7.

first pass effect


intrinsic clearance
loading dose kinetics
plateau principle
pharmacokinetic trapping

Phase 1 hepatic biotransformations generally result in relatively minor modifications to the


parent compound to produce a metabolite which:
A.
B.
C.
D.
E.

8.

for a given pKa, the rate at which the drug will cross the membrane is inversely
related to its lipid solubility, Kp
if the drug is a weak acid, its distribution will be independent of local pH
if the drug is a weak base, its distribution will be independent of its pKa
the drug will accumulate in the compartment where its degree of ionization is greatest
weak acids and bases will be cross the membrane more readily than the uncharged
species

contains a functional group that confers resistance to further hepatic metabolism


contains a functional group that provides a site for conjugation reactons
is able to bypass the hepatic phase 2 biotransformations
is conjugated to glucuronic acid or glutathione
is less water soluble than the parent compound

Under which of the following conditions is it most important to consider the impact of the
first-pass effect?
A.
B.
C.
D.
E.

when a drug is administered by a transdermal, intradermal, or subcutaneous route


when a drug is administered parenterally by intravenous or intramuscular injection
when a drug is subject to high affinity binding to plasma proteins
when a drug with a high hepatic extraction ration is administered orally
when a drug with a low hepatic extraction ratio is administered sublingually

A-1

9.

Orally administered estrogens undergo conjugation in the liver, followed by biliary secretion
into the intestine, where the sulfate and glucuronide moieties are removed by bacterial
enzymes and the steroid may then be reabsorbed. What is the general term for this process?
A.
B.
C.
D.
E.

10.

Following coronary artery bypass surgery, a hospitalized patient receives a continuous


infusion of cefuroxime, a cephalosporine antibiotic, for prophylaxis of wound infection. The
drug is infused at a rate of 2.4 grams every 24 hours (100 mg/hour). If the steady-state
concentration established with this procedure is 20 mg/L, what is the total body clearance of
the drug?
A.
B.
C.
D.
E.

11.

enterohepatic recycling
first pass effect
intrinsic clearance
phase 3 biotransformation
steroid trapping

5 mL/min
0.2 L/hr
1 L/hr
5 L/hr
20 L/hr

Css = dosing rate / Cl

Cl

= dosing rate / Css


= (100 mg/hr) / 20 mg/L
= 5 mg/hr * L/mg
= 5 L/hr

The following data applies to the renal excretion of Drug X:


U*V
20 g/mL * 1 mL/min = 40 mL/min
=
P
0.5 g/mL

plasma concentration = 0.5 g/mL


urine concentration = 20 g/mL
urine volume
= 1 mL/min
Based on this information, Drug X is likely:
A.
B.
C.
D.
E.

filtered & completely reabsorbed Cl = 0


filtered & not reabsorbed
Cl = ~120 ml/min
filtered & maximally secreted
Cl = ~650 ml/min

filtered at the glomerulus and completely reabsorbed


filtered at the glomerulus and partially reabsorbed
filtered at the glomerulus with no reabsorption
filtered at the glomerulus and partially secreted at the proximal tubule
filtered at the glomerulus and maximally secreted at the proximal tubule

A-2

For questions 12-14, refer to the following information from the product labeling of atorvastatin, a
widely-prescribed drug administered orally for the treatment of hypercholesterolemia.
CLINICAL PHARMACOLOGY
Distribution: Mean volume of distribution of atorvastatin is approximately 381 liters. Atorvastatin is 98%
bound to plasma proteins. A blood/plasma ratio of approximately 0.25 indicates poor drug penetration into
red blood cells. Based on observations in rats, atorvastatin is likely to be secreted in human milk.
Metabolism: Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various
beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated
metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for
HMG-CoA reductase is attributed to active metabolites. In vitro studies suggest the importance of atorvastatin
metabolism by cytochrome P450 3A4, consistent with increased plasma concentrations of atorvastatin in
humans following coadministration with erythromycin, a known inhibitor of this isozyme. In animals, the
ortho-hydroxy metabolite undergoes further glucuronidation.
Excretion: Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extrahepatic metabolism; however, the drug does not appear to undergo enterohepatic recirculation. Mean plasma
elimination half-life of atorvastatin in humans is approximately 14 hours, but the half-life of inhibitory
activity for HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites. Less than 2%
of a dose of atorvastatin is recovered in urine following oral administration.

12.

These data indicate that atorvastatin is:


A.
B.
C.
D.
E.

extensively reabsorbed from the gastrointestinal tract following its excretion


largely restricted to the extracellular fluid
largely restricted to the vascular space
retained within the gastrointestinal tract, with little systemic bioavailability
sequestered at some extravascular site
based on V = 381 L
d

vs. total body water = 35-50


13.

If atorvastatin is administered once daily for 3 months, a steady-state plasma concentration of


the drug would be achieved within approximately:
A.
B.
C.
D.
E.

14.

6 to 8 hours
2 to 3 days
20 to 35 days
40 to 60 days
2 to 3 months

4 to 6 * T1/2 = 4 to 6 * 14 hours
= 56 to 84 hours
= 2.3 to 3.5 days

The systemic clearance of atorvastatin appears to be primarily dependent on:


A.
B.
C.
D.
E.

glomerular filtration and extensive renal tubular secretion of unchanged drug


glomerular filtration with little or no tubular reabsorption of unchanged drug
hepatic oxidative metabolism
hepatic reduction reactions
the enterohepatic cycle

A-3

15.

Pharmacokinetic changes that are common with aging include:


A.
B.
C.
D.
E.

16.

Which of the following is part of the Spare Receptor Concept?


A.
B.
C.
D.
E.

17.

impaired drug absorption


increased binding to plasma proteins
increased first-pass hepatic metabolism of drugs with flow-dependent clearance
reduced capacity of hepatic conjugation reactions
reduced renal clearance

a drug can produce a maximal effect when a relatively small proportion of its
receptors is occupied
a drug will produce a maximal effect only when all of the occupied receptors are
activated
receptors for a drug that are occupied but not activated are known as spare receptors
the response to a drug is directly proportional to the number of receptors that are
occupied
when the receptors for a drug are saturated, additional, i.e. spare, binding sites are
exposed

If each curve below shows the effects of a single drug (A, B, C, D, and E), which of the
following statements is TRUE in comparing the efficacies and potencies?

A.
B.
C.
D.
E.

A, B, and C have similar potency


B and C are partial agonists
B and C have similar efficacy
C has less efficacy than E
D has less efficacy than E

A-4

18.

Changes that are common with aging that influence the response of a receptor to a given drug
concentration include which of the following?
A.
B.
C.
D.
E.

19.

The study of how inherited genetic differences in humans influence the individuals response
to a drug is known as:
A.
B.
C.
D.
E.

20.

cyclic AMP
drug metabolizing enzymes
kidney active transport processes
plasma proteins and immunoglobulins
the blood brain barrier

In classifying genetic variants of drug metabolizing enzymes, those with two normal alleles,
usually representing the majority of the population, are known as:
A.
B.
C.
D.
E.

22.

gene-targeted therapy
genomic pharmacology
pharmacogenomics
polymorphic pharmacology
proteomic pharmacology

Common pharmacogenomic variations arise from mutations affecting the function of:
A.
B.
C.
D.
E.

21.

increased beta adrenoreceptor sensitivity to drugs


increased frequency of potassium and electrolyte imbalance
reduced frequency of occult blood loss with aspirin
reduced frequency of orthostatic hypotension
reduced sensitivity of drug receptor responses in the CNS

Poor Metabolizers
Intermediate Metabolizers
Extensive Metabolizers
Standard Metabolizers
Typical Metabolizers

Pharmacologic effects of histamine released from mast cells include all of the following
EXCEPT:
A.
B.
C.
D.
E.

bronchoconstriction
peripheral vasodilation
cardiac stimulation
localized itching
relief from edema
A-5

23.

Cimetidine is a histamine receptor antagonist used for which of the following applications?
A.
B.
C.
D.
E.

24.

Leukotrienes and prostaglandin E2 are similar in that they both:


A.
B.
C.
D.
E.

25.

the chosen dose should also have analgesic efficacy


the chosen dose should also have anti-inflammatory activity
the chosen dose should not increase endothelial prostacyclin (PGI2)
the chosen dose should not reduce endothelial prostacyclin
the chosen dose should not reduce thromboxane A2

Which of the following is a correct description of the sequence of disturbances


accompanying progressive aspirin toxicity?
A.
B.
C.
D.
E.

27.

are potent bronchoconstrictors


enhance the rate of urine formation
increase fluid exudation from the vascular compartment
inhibit platelet aggregation
probably play a role in labor and delivery at term

In determining the appropriate dose of aspirin for inhibition of platelet activation, what other
factor must be considered?
A.
B.
C.
D.
E.

26.

to block histamine-induced gastric acid secretion


to induce sleep
to prevent motion sickness
to prevent nausea induced by general anesthesia
to relieve cold and allergy symptoms

metabolic acidosis respiratory acidosis hypoglycemia


metabolic alkalosis respiratory alkalosis gastric bleeding
respiratory acidosis respiratory alkalosis uric acid retention
respiratory alkalosis metabolic acidosis renal dysfunction
respiratory alkalosis respiratory acidosis hyperalgesia

Developed as anti-inflammatory drugs with a lower propensity for causing gastrointestinal


irritation, ulceration and bleeding, selective COX-2 inhibitors are more likely than
nonselective COX inhibitors to cause:
A.
B.
C.
D.
E.

bronchospasm
elevated blood pressure
hepatotoxicity
cardiotoxic events
renal damage
A-6

28.

Which of the following NSAIDs should be avoided in individuals with pre-existing CNS
pathologies or psychiatric illness?
A.
B.
C.
D.
E.

29.

The major life-threatening toxicity of acute acetaminophen overdose is:


A.
B.
C.
D.
E.

30.

febrile responses
inflammation
liver function
platelet function
the gastric mucosa

Which of the following is an immunosuppressant drug that acts by inhibiting calcineurin and
thus reducing the production of cytokines and impairing the response of T cells to antigens?
A.
B.
C.
D.
E.

32.

bleeding
gastric ulcers
irreversible liver damage
kidney failure
metabolic acidosis

Acetaminophen and ibuprofen are similar in their effects on:


A.
B.
C.
D.
E.

31.

diflunisal
ibuprofen
indomethacin
naproxen
piroxicam

azathioprine
cyclosporine
dexamethasone
infliximab
misoprostol

Which immunosuppressant drug inhibits mTOR (the mammalian target of rapamycine), a


key enzyme in cell cycle progression?
A.
B.
C.
D.
E.

azathioprine
cyclosporine
mycophenolate mofetil
sirolimus
tacrolimus

A-7

33.

Significant drug interactions of certain immunosuppressive agents, including cyclosporine,


tacrolimus, and sirolimus are based on:
A.
B.
C.
D.
E.

34.

Which of the following drugs used to treat rheumatoid arthritis acts by binding to TNF-,
thus blocking the activation of its receptors?
A.
B.
C.
D.
E.

35.

block the activation of cytokines 2F and 3C


have antipyretic effects
slow the progression of bone and cartilage destruction
stop the progression of bone and cartilage destruction

What is the mechanism of action of azathioprine?


A.
B.
C.
D.
E.

37.

azathioprine
etanercept
methotrexate
prednisone
sulfasalazine

Patients with rheumatoid arthritis are commonly advised to take aspirin or other salicylates.
In addition to their anti-inflammatory and analgesic effects, these agents:
A.
B.
C.
D.

36.

their ability to inhibit aldehyde dehydrogenase


their affinity for HMG CoA reductase
their binding to chylomicrons
their effects on proximal tubule reabsorption
their metabolism by the cytochrome P450 isoform CYP3A4

it blocks mTOR, which inhibits T cell activation and proliferation


it breaks sulfhydryl bonds selectively in T lymphocytes
it inhibits calcineurin and reduces the production of cytokines
it is metabolized to 6-thiopurines, which competitively inhibit purine synthesis
it is metabolized to sulfapyridine, which inhibits the lipoxygenase pathway

In an effort to increase the uricosuric effects of probenecid, it is recommended that this


medication be used in conjunction with:
A.
B.
C.
D.
E.

a urine acidifying agent


a urine alkalinizing agent
low doses of acetaminophen
low doses of allopurinol
low doses of colchicine

A-8

38.

What is the recommended clinical use of allopurinol?


A.
B.
C.
D.
E.

39.

What is the mechanism of action of febuxostat?


A.
B.
C.
D.
E.

40.

it blocks reabsorption of uric acid in the proximal tubule


it catalyzes the conversion of uric acid to allantoin
it inhibits the active reabsorption of filtered uric acid
it inhibits the uric acid secretory transporter
it selectively inhibits xanthine oxidase

A relatively common but dangerous adverse effect of treatment with standard doses of
penicillin is:
A.
B.
C.
D.
E.

41.

to decrease hyperuricemia caused by uric acid overproduction


to provide rapid relief of the pain and inflammation associated with an acute gout
attack
to relieve nausea, vomiting and other GI side effects produced by the oral
administration of probenecid
to significantly decrease urinary pH, thus increasing the rate of uric acid excretion
to treat uric acid underproduction in patients with familial Mediterranean pseudogout

allergic reaction
gastrointestinal emergency
headache
hypokalemia
seizures

An important difference between the cephalosporins and the penicillins is that the
cephalosporins:
A.
B.
C.
D.
E.

act selectively on bacteria causing urinary tract infections


also inhibit bacterial protein synthesis
are more resistant to hydrolysis by -lactamase enzymes
do not contain a -lactam ring
inhibit bacterial DNA replication and transcription

A-9

42.

A 76 year-old man is sent to the hospital for a suspected stroke. After a correct diagnosis and
appropriate emergency treatment, he is kept in the hospital for further therapy. Three weeks
later, however, the patient shows symptoms of pneumonia. Clinical tests indicate the
infection is caused by Pseudomonas aeruginosa. Under these circumstances, which of the
following should be used for treatment of this patient?
A.
B.
C.
D.
E.

43.

Which of the following agents may induce histamine release and flushing around the neck,
known as red man syndrome?
A.
B.
C.
D.
E.

44.

amoxicillin
botulinum toxin
caspofungin
tacrolimus
vancomycin

Which adverse effect is characteristic of the combination of quinupristin/dalfopristin?


A.
B.
C.
D.
E.

45.

cefepime in combination with clindamycin


clavulanate
methenamine
oxacillin in combination with penicillin G
sulfamethoxazole

glucose intolerance
hyperpigmentation
interaction with alcohol to produce a disulfiram-like reaction
pain and frequent thrombophlebitis at the injection site
restlessness, insomnia, and anxiety

To reduce the development of drug-resistant bacteria and maintain the effectiveness of


antibiotics, which of the following should be used only to treat severe infections caused by
vancomycin-resistant enterococci, methicillin-resistant Staphylococcus aureus, penicillinresistant Streptococcus pneumoniae and/or Streptococcus pyogenes, or be limited to those
indications for which other antimicrobials are ineffective or not tolerable.
A.
B.
C.
D.
E.

clindamycin
erythromycin
gentamicin
linezolid
vancomycin

A-10

46.

Which of the following statements correctly describes the mechanism of action of


chloramphenicol?
A.
B.
C.
D.
E.

47.

Which of the following best describes the clinical application of trimethoprim?


A.
B.
C.
D.
E.

48.

combination therapy with ampicillin to inhibit bacterial lactamase and prevent


resistance
combination therapy with sulfamethoxazole for enhanced inhibition of
tetrahydrofolate synthesis
drug of choice for the treatment of isoniazid-resistant tuberculosis
drug of choice for the treatment of methicillin-resistant Staphylococcus aureus
monotherapy for treatment of complicated skin and skin structure infections with
various resistant organisms, particularly in patients who cannot tolerated other drugs

Which of the following has antibacterial effects as a result of inhibition of DNA replication
and transcription?
A.
B.
C.
D.
E.

49.

inhibits of cytosine deaminase, resulting in inhibition of DNA synthesis


it binds to mitotic spindle fibers, preventing cell division and inducing apoptosis
it binds to the 50S ribosomal subunit A site of bacteria and inhibits protein synthesis
it inhibits hepatic B-lactamase enzymes
it promotes the expression of apoptotic mediators, producing cytolytic changes in
resistant bacteria

chloramphenicol
ciprofloxacin
metronidazole
nitrofurantoin
streptomycin

Which of the following best describes the clinical application for isoniazid?
A.
B.
C.
D.
E.

first-line drug for chemoprophylaxis in those at risk of developing active tuberculosis


after being infected
prophylaxis to prevent development of active leprosy after exposure to an armadillo
second-line drug for the treatment of atypical mycobacterial infections
second-line drug for the treatment of tuberculosis that is resistant to treatment
treatment of active leprosy

A-11

50.

A 26-year-old male was admitted to the hospital with a month-long history of fever and
cough. Sputum culture yielded M. tuberculosis susceptible to all first-line antimycobacterial
drugs. The doctor recommends that the patient be started on:
A.
B.
C.
D.
E.

51.

ethambutol
ethambutol, isoniazid, rifampin, and pyrazinamide
isoniazid
isoniazid plus dapsone
isoniazid plus rifampin

In treating puncture wounds in children, fluoroquinolones are generally avoided because they
have been shown to produce:
A.
B.
C.
D.
E.

cartilage degeneration
glucose intolerance
growth retardation
hypercholesterolemia
severe headache

From the following list, A through E, choose the appropriate mechanism of action of the drugs or
drug classes named in questions 19 to 24. EACH OF THE CHOICES (A THROUGH E) MAY
BE USED AS MANY TIMES AS NECESSARY OR POSSIBLY MAY NOT BE USED AT
ALL.
A.
B.
C.
D.
E.

Disruption of cell membranes


Inhibition of bacterial cell wall synthesis
Inhibition of folic acid biosynthesis
Inhibition of mycolic acid biosynthesis
Inhibition of protein synthesis

52.

amoxicillin

53.

aztreonam

54.

linezolid

55.

macrolides

56.

sulfamethoxazole

57.

vancomycin

A-12

58.

What is the mechanism of action of quinine?


A.
B.
C.
D.
E.

59.

Which of the following agents is used to treat luminal ascariasis, pinworm and hookworm
infections?
A.
B.
C.
D.

60.

acetylcholinesterase inhibitor
alkylating agent
beta adrenergic agonist
beta adrenergic antagonist
blocking heme detoxification

mefloquine
primaquine
pyrimethamine
pyrantel pamoate

Which of the following agents is used to treat infection caused by the amoeba Entamoeba
histolytica?
A.
B.
C.
D.
E.

mebendazole
metronidazole
piperazine
praziquantel
pyrantel pamoate

A-13

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