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An 18-year-old female patient is brought to the emergency department due to drug overdose.
Which of the following routes of administration is the most desirable for administering the
antidote for the drug overdose?
A. Intramuscular.
B. Subcutaneous.
C. Transdermal.
D. Oral.
E. Intravenous. - Answer E. Intravenous.
The intravenous route of administration is the most desirable because it results in achievement
of therapeutic plasma levels of the antidote rapidly.
KR2250 is an investigational cholesterol-lowering agent. KR2250 has a high molecular weight
and is extensively bound to albumin. KR2250 will have a(n) _______________ apparent volume
of distribution (Vd).
A. High
B. Low
C. Extremely high
D. Normal - Answer B. Low
Because of its high molecular weight and high protein binding, KR2250 will be effectively
trapped within the plasma (vascular) compartment and will have a low apparent volume of
distribution.
A 40-year-old male patient (70 kg) was recently diagnosed with infection involving methicillin-
resistant S. aureus. He received 2000 mg of vancomycin as an IV loading dose. The peak plasma
concentration of vancomycin was 28.5 mg/L. The apparent volume of distribution is:
,D. 14 L/kg
E. 70 L/kg - Answer A. 1 L/kg
Vd = dose/C = 2000 mg/28.5 mg/L = 70.1 L. Because the patient is 70 kg, the apparent volume
of distribution in L/kg will be approximately 1 L/kg (70.1 L/70 kg).
A 55-year-old woman is brought to the emergency department because of seizures. She has a
history of renal disease and currently undergoes dialysis. She receives an intravenous infusion of
antiseizure Drug X. Which of the following is likely to be observed with use of Drug X in this
patient in terms of the half life and dosing as compared to a normal patient?
A. Half life increase, dosage increase
B. Half life decrease, dosage decrease
C. Half life increase, dosage same
D. Half life increase, dosage decrease
E. Half life same, dosage same - Answer D. Half life increase, dosage decrease
Because the patient has a renal disorder, she may not be able to excrete the drug effectively.
Therefore, the half-life of Drug X will be prolonged. As the half-life is prolonged, the dosage
must be reduced so the patient will not have serious toxic effects of Drug X.
A 64-year-old female patient (60 kg) is treated with experimental Drug A for type 2 diabetes.
Drug A is available as tablets with an oral bioavailability of 90%. If the Vd is 2 L/kg and the
desired steady-state plasma concentration is 3.0 mg/L, which of the following is the most
appropriate oral loading dose of Drug A?
A. 6 mg
B. 6.66 mg
C. 108 mg
D. 360 mg
E. 400 mg - Answer E. 400 mg
For oral dosing, loading dose = [(Vd) × (desired steady-state plasma concentration)/F]. The Vd in
this case is corrected to the patient's weight is 120 L. The F value is 0.9 (because bioavailability
is 90%, that is, 90/100 = 0.9). Thus, loading dose = (120 L × 3.0 mg/L)/0.9 = 400 mg.
,patient has an estimated Vd of 400 L, calculate the additional dose of digoxin needed for this
patient to achieve the desired plasma concentration.
A. 128 mcg
B. 160 mcg
C. 320 mcg
D. 480 mcg
E. 640 mcg - Answer C. 320 mcg
The additional dosage of digoxin needed to achieve the desired plasma concentration can be
calculated using the equation Vd (C2 - C1). C1 is the current plasma concentration (0.4 ng/mL)
and C2 is the desired plasma concentration (1.2 ng/mL). Therefore, the additional dosage of
digoxin is [400 L × (1.2 - 0.4) ng/mL)] = 320 mcg.
Which of the following best describes how a drug that acts as an agonist at the A subtype of
GABA receptors affects signal transduction in a neuron?
A. Activation of this receptor subtype alters transcription of DNA in the nucleus of the neuron.
B. Activation of this receptor subtype opens ion channels that allow sodium to enter cells and
increases the chance of generating an action potential.
C. Activation of this receptor subtype opens ion channels that allow chloride to enter cells and
decreases the chance of generating an action potential.
D. Activation of this receptor subtype results in G protein activation and increased intracellular
second messenger levels. - Answer C. Activation of this receptor subtype opens ion channels
that allow chloride to enter cells and decreases the chance of generating an action potential.
The GABA-A receptor is a ligand-gated ion channel selective for chloride. Agonists for the GABA-
A receptor increase opening of channels, resulting in chloride entry into the neuron,
hyperpolarization, and decreased action potential events.
If 1 mg of lorazepam produces the same anxiolytic response as 10 mg of diazepam, which is
correct?
A. Lorazepam is more potent than is diazepam.
B. Lorazepam is more efficacious than is diazepam.
, A drug that causes the same effect at a lower dose is more potent. B and C are incorrect
because without information about the maximal effect of these drugs, no conclusions can be
made about efficacy or intrinsic activity. D is incorrect because the maximal response obtained
is often more important than the amount of drug needed to achieve it.
If 10 mg of oxycodone produces a greater analgesic response than does aspirin at any dose,
which is correct?
A. Oxycodone is more efficacious than is aspirin.
B. Oxycodone is less potent than is aspirin.
C. Aspirin is a full agonist, and oxycodone is a partial agonist.
D. Oxycodone and aspirin act on the same drug target. - Answer A. Oxycodone is more
efficacious than is aspirin
Drugs with greater response at maximally effective concentrations are more efficacious than
drugs with a lower maximal response. Choice B is incorrect since no information is given about
the half maximal concentrations of either drug. Choices C and D are incorrect since it is not
known if both drugs bind to the same receptor population.
In the presence of propranolol, a higher concentration of epinephrine is required to elicit full
antiasthmatic activity. Propranolol has no effect on asthma symptoms. Which is correct
regarding these medications?
A. Epinephrine is less efficacious than is propranolol.
B. Epinephrine is a full agonist, and propranolol is a partial agonist.
C. Epinephrine is an agonist, and propranolol is a competitive antagonist.
D. Epinephrine is an agonist, and propranolol is a noncompetitive antagonist. - Answer C.
Epinephrine is an agonist, and propranolol is a competitive antagonist.
Since propranolol decreases the effect of epinephrine but the inhibition can be overcome by
giving a higher dose of epinephrine, propranolol must be a competitive antagonist. If D were
correct, even very high concentrations of epinephrine would not be able to elicit a maximal
effect in the presence of propranolol. Since propranolol has no effect by itself, A and B are
incorrect.
In the presence of picrotoxin, diazepam is less efficacious at causing sedation, regardless of the