Select The Single Best Answer: A. Bioavailability
Select The Single Best Answer: A. Bioavailability
Select The Single Best Answer: A. Bioavailability
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.
4.
bioavailability
first pass fraction
intrinsic clearance
steady state
volume of distribution
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.
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.
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
Under which of the following conditions is it most important to consider the impact of the
first-pass effect?
A.
B.
C.
D.
E.
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.
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
Cl
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.
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
A-3
15.
16.
17.
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-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.
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.
25.
27.
In determining the appropriate dose of aspirin for inhibition of platelet activation, what other
factor must be considered?
A.
B.
C.
D.
E.
26.
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.
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
31.
diflunisal
ibuprofen
indomethacin
naproxen
piroxicam
azathioprine
cyclosporine
dexamethasone
infliximab
misoprostol
azathioprine
cyclosporine
mycophenolate mofetil
sirolimus
tacrolimus
A-7
33.
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.
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.
A-8
38.
39.
40.
A relatively common but dangerous adverse effect of treatment with standard doses of
penicillin is:
A.
B.
C.
D.
E.
41.
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.
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
45.
glucose intolerance
hyperpigmentation
interaction with alcohol to produce a disulfiram-like reaction
pain and frequent thrombophlebitis at the injection site
restlessness, insomnia, and anxiety
clindamycin
erythromycin
gentamicin
linezolid
vancomycin
A-10
46.
47.
48.
Which of the following has antibacterial effects as a result of inhibition of DNA replication
and transcription?
A.
B.
C.
D.
E.
49.
chloramphenicol
ciprofloxacin
metronidazole
nitrofurantoin
streptomycin
Which of the following best describes the clinical application for isoniazid?
A.
B.
C.
D.
E.
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.
52.
amoxicillin
53.
aztreonam
54.
linezolid
55.
macrolides
56.
sulfamethoxazole
57.
vancomycin
A-12
58.
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