Fall Exam I Active Learning Questions

Question 1

The most common mechanism for drug passage across biologic membranes is:
A.  Active transport
B.  Pinocytotic uptake
C.  Phagocytic uptake
D.  Facilitated carrier-mediated diffusion
E.  Lipid diffusion through membrane itself
F.   Aqueous diffusion through membrane pores

Answer 1

E.  Lipid diffusion through membrane itself

Question 2

Alcohol is a SMALL HYDROPHILIC molecule that is most likely to pass across biologic membranes via:
A.  Active transport
B.  Pinocytotic uptake
C.  Phagocytic uptake
D.  Facilitated carrier-mediated diffusion
E.  Lipid diffusion through membrane itself
F.   Aqueous diffusion through membrane pores

Answer 2

F.   Aqueous diffusion through membrane pores

Question 3

First pass effect is most commonly described as:
A.  Destruction of orally administered drug by the low pH of the gastric contents
B.  Destruction of orally administered drug by digestive enzymes
C.  Hepatic metabolism of a drug prior to entry in to the systemic circulation
D.  Gastric metabolism of a drug prior to entry in to the systemic circulation
E.  Inability of a large, ionized drug to cross biologic membranes

Answer 3

C.  Hepatic metabolism of a drug prior to entry in to the systemic circulation

Question 4

The oral bioavailability of a drug will be reduced by:
A.  Destruction of orally administered drug by the low pH of the gastric contents
B.  Destruction of orally administered drug by digestive enzymes
C.  Hepatic metabolism of a drug prior to entry in to the systemic circulation
D.  Gastric metabolism of a drug prior to entry in to the systemic circulation
E.  Inability of a large, ionized drug to cross biologic membranes

Answer 4

ALL!

ABCDE

Question 5

Which of the following types of drugs will have the greatest oral bioavailability?
A.  Drugs with high first pass metabolism
B.  Highly hydrophilic drugs
C.  Largely lipophilic drugs, yet soluble in aqueous solutions
D.  Chemically unstable drugs
E.  Drugs that are P-glycoprotein substrates

Answer 5

C.  Largely lipophilic drugs, yet soluble in aqueous solutions

Question 6

An 18-year-old female patient is brought to the emergency department due to a 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.  Intranasally 
D.  Inhalational 
E.  Transdermal 
F.   Oral
G.  Intravenous

Answer 6

A.  Intramuscular
C.  Intranasally
G.  Intravenous**

Question 7

Which route of drug administration has the most rapid onset of action? 
A.  Oral 
B.  Sublingual 
C.  Intravenous 
D.  Transdermal 
E.  Intramuscular 
F.   Subcutaneous 
G.  Inhalational

Answer 7

C.  Intravenous (most dangerous)

G.  Inhalational*

Question 8

Which of the following statements concerning routes of drug administration is FALSE?
A.  The bioavailability from the intramuscular route of administration approaches 100%.
B.  An increase in gastric motility generally results in an increase in the rate of oral absorption.
C.  The onset of action from the intramuscular route of administration is faster than that from the oral route.
D.  The transdermal route of administration is designed to maximize local effects and avoid systemic effects of the drug.
E.  A permanently charged drug administered by IM injection can enter the peripheral circulation through gaps between endothelial cells.
F.   A permanently charged drug administered by IM injection can enter the peripheral circulation through gaps between endothelial cells and enter the CNS.

Answer 8

D.  The transdermal route of administration is designed to maximize local effects and avoid systemic effects of the drug.
F.   A permanently charged drug administered by IM injection can enter the peripheral circulation through gaps between endothelial cells and enter the CNS.

Question 9

All of the following categories of drugs would cross the blood brain barrier poorly (if at all) and have neglible effects in the central nervous system EXCEPT: 
A.  Highly protein bound drugs 
B.  Highly lipid soluble drugs 
C.  Very large molecules 
D.  Permanently charged drugs 
E.  All of the above will cross poorly

Answer 9

B.  Highly lipid soluble drugs

Question 10

Which of the following is TRUE about the blood-brain barrier?
A.  Endothelial cells of the blood-brain barrier have slit junctions (fenestrations)
B.  Ionized or polar drugs can cross the blood-brain barrier easily
C.  Drugs can cross the blood-brain barrier through specific transporters
D.  Lipid soluble drugs readily cross the blood-brain barrier
E.  The capillary structure of the blood-brain barrier is similar to that of the liver and spleen

Answer 10

C.  Drugs can cross the blood-brain barrier through specific transporters
D.  Lipid soluble drugs readily cross the blood-brain barrier

Question 11

Which of the following statements about drugs that are weak acids is CORRECT?
A.  An acid will most readily cross membranes when it is contained in acidic body fluids.
B.  An acid will have a pKa greater than 7.0.
C.  An acid becomes charged when it takes up a hydrogen ion.
D.  An acid will be trapped into more acidic body fluids.

Answer 11

A.  An acid will most readily cross membranes when it is contained in acidic body fluids.

Question 12

Aspirin is a weak organic acid with a pKa of 5.4.  What is the ratio of the charged to uncharged form at a plasma pH of 7.4?
A.  1:100 
B.  1:10 
C.  1:1 
D.  10:1 
E.  100:1

Answer 12

E.  100:1

Question 13

Aspirin is a weak organic acid with a pKa of 5.4.  What is the ratio of the charged to uncharged form at an intestinal pH of 5.4? 
A.  1:100 
B.  1:10 
C.  1:1 
D.  10:1 
E.  100:1

Answer 13

C.  1:1

Question 14

Hydrochlorothiazide is a weakly acidic drug with a pKa of 6.5. If administered orally, at which of the following sites of absorption will the drug be able to most readily pass through the membrane (based solely of % ionized
considerations)? 
A.  Mouth (pH  ∼ 7.0) 
B.  Stomach (pH ∼ 2.5) 
C.  Duodenum (pH ∼ 6.1) 
D.  Jejunum (pH ∼ 8.0) 
E.  Ileum (pH ∼ 7.0)

Answer 14

B.  Stomach (pH ∼ 2.5)

Question 15

Lidocaine is a local anesthetic that is a weak base with a pKa of 7.9. Relative to normal tissue pH of 7.4, the percentage of lidocaine that is in the protonated form in inflamed tissue at pH 6.4 would be:
A.  Increased
B.  Decreased
C.  Unchanged because both pH’s are below the pKa

Answer 15

A.  Increased

Question 16

Which of the following statements concerning the consequences of increasing the binding of a drug to plasma proteins is TRUE?
A.  Decreases the plasma concentration of therapeutically
active drug.
B.  Decreases elimination of drug by metabolism in the liver and/or excretion in the kidney.
C.  Increases the dose that must be administered to achieve therapeutic effectiveness.
D.  Increases the possibility of adverse interactions withother drugs that bind plasma proteins.
E.  All of the above are true.

Answer 16

E.  All of the above are true

Question 17

“Bolus” or “slug” effects are most likely to be seen when drugs are administered by which of the following routes? 
A.  Intramuscular 
B.  Subcutaneous 
C.  Intravenous 
D.  Oral 
E.  Inhalational

Answer 17

C.  Intravenous

Question 18

A new drug is undergoing pharmacokinetic evaluation during phase 1 testing and it is determined that it has a volume of distribution of 3-5 liters in a 150 lb (70 kg)
patient. Based on this finding alone, this value for Vd is most consistent with:
A.  The drug being highly lipid soluble
B.  The drug being highly bound to plasma proteins
C.  The drug being highly sequestered in fatty tissues
D.  The drug being distributed in total body water (TBW)
E.  The drug being distributed in extracellular fluids (ECF)

Answer 18

A.  The drug being highly lipid soluble

B.  The drug being highly bound to plasma proteins***

Question 19

Drug metabolism usually results in a product that is:
A.  Less likely to distribute intracellularly
B.  More lipid soluble than the parent drug
C.  More likely to be reabsorbed by kidney tubules
D.  More water soluble than the parent drug
E.  More likely to produce adverse effects

Answer 19

A.  Less likely to distribute intracellularly

D.  More water soluble than the parent drug

Question 20

For drugs that are metabolized by the CYP450
(cytochrome P450) enzyme system they:
A.  Require molecular oxygen
B.  Are generally highly lipid soluble
C.  Usually become more highly oxidized
D.  Are metabolized in the smooth endoplasmic reticulum
E.  All of the above

Answer 20

E.  All of the above

Question 21

A 65-year-old female dental patient (60 kg) underwent an
outpatient procedure under local anesthesia. You advised
her that OTC NSAIDs (ibuprofen) should be sufficient for post-procedure pain management – but you would alsogive her a prescription for 2-3 days of Tylenol #3® (acetaminophen-codeine) if pain control was inadequate. She informed you that codeine never really “worked” to control her pain. If true, which of the following CYP450 genetic polymorphisms is the most likely reason she does not respond to codeine analgesia?
A.  Fast CYP1A2 metabolizer
B.  Fast CYP2E1 metabolizer
C.  Fast CYP2D6 metabolizer
D.  Poor CYP2D6 metabolizer
E.  Poor CYP2C9 metabolizer

Answer 21

D.  Poor CYP2D6 metabolizer

Question 22

A phase II drug metabolism reaction:
A.  Must always be preceded by a phase I reaction
B.  Includes non-microsomal oxidation reactions (e.g., MAO)
C.  Is dependent on molecular oxygen (O2) and NADPH as cofactors
D.  Is less likely to reach saturation (Vmax) levels than phase I reactions
E.  Will be less likely to decline in activity with aging than
phase I reactions

Answer 22

E.  Will be less likely to decline in activity with aging than
phase I reactions

Question 23

Local  anesthetics  such  as  lidocaine  or  bupivacaine  are
metabolized in the liver by: 
A.  Amidases 
B.  Esterases 
C.  Alcohol dehydrogenase 
D.  Monoamine oxidase 
E.  Cytochrome 3A4 
F.   Glucuronyl transferase 
G.  None of the above 
H.  Either A or B

Answer 23

A.  Amidases

Question 24

Which of the following phase II metabolic reactions make phase I metabolites more readily excretable in urine? 
A.  Oxidation 
B.  Sulfation 
C.  Hydrolysis 
D.  Glucuronidation 
E.  Alcohol dehydrogenation

Answer 24

B.  Sulfation

D.  Glucuronidation

Question 25

All of the following drugs or foods are inhibitors of
various cytochrome P450 enzymes EXCEPT:
A.  Antifungal agents (e.g., ketoconazole)
B.  Cimetidine
C.  Grapefruit juice
D.  Macrolide antibiotics (e.g., erythromycin)
E.  Phenobarbital

Answer 25

E.  Phenobarbital

Question 26

Alkalinization of urine by giving bicarbonate is used to
treat patients presenting with pentobarbital (weak acid)
overdose. Which of the following best describes the
rationale for alkalinization of urine in this setting?
A. to decrease ionization of pentobarbital
B. to increase glomerular filtration of pentobarbital
C. to decrease proximal tubular secretion
D. to reduce tubular reabsorption of pentobarbital
E. to increase proximal tubular secretion

Answer 26

D. to reduce tubular reabsorption of pentobarbital

Question 27

The addition of glucuronic acid to a drug molecule:
A.  Increases its water solubility
B.  Usually leads to inactivation of the drug
C.  Is an example of a phase I reaction
D.  Occurs at the same rate in adults and newborn
E.  Involves cytochrome P-450

Answer 27

A.  Increases its water solubility

B.  Usually leads to inactivation of the drug

Question 28

Regarding the termination of drug action:
A.  Drugs must be excreted from the body to terminate their action.
B.  Metabolism of drugs will always increase their degree
of ionization.
C.  Metabolism of drugs always abolishes their pharmacologic activity.
D.  Hepatic metabolism and renal excretion are the two
most important mechanisms involved.

Answer 28

D.  Hepatic metabolism and renal excretion are the two

most important mechanisms involved.

Question 29

The best-documented and quantitatively the most
clinically important mechanism by which drug-drug interactions occur is via:
A.  Antibiotic alteration of intestinal flora
B.  Physiochemical inactivation of the drug in the stomach
C.  Displacement of the drug from plasma protein binding
sites
D.  Inhibition or induction of the metabolism of the drug
E.  Interference with renal tubular secretion of the drug F.   Alterations in gastric motility

Answer 29

D.  Inhibition or induction of the metabolism of the drug

Question 30

If the plasma concentration of a drug declines with “first-
order kinetics”, this means that:
A.  There is only one metabolic path for drug elimination
B.  The drug is not distributed outside the vascular system
C.  The half-life is the same regardless of the plasma
concentration
D.  The drug is largely metabolized in the liver after oral administration and has low bioavailability
E.  The rate of elimination is constantly changing as the plasma concentration (Cp) declines

Answer 30

C.  The half-life is the same regardless of the plasma
concentration

E.  The rate of elimination is constantly changing as the plasma concentration (Cp) declines

Question 31

The half-life of a drug:
A.  Is dependent on clearance
B.  Is dependent on the volume of distribution
C.  Is an independent pharmacokinetic parameter
D.  Must be known to calculate the loading dose
E.  Increases when the volume of distribution increases
F.   Increases when the clearance increases

Answer 31

A.  Is dependent on clearance
B.  Is dependent on the volume of distribution

E.  Increases when the volume of distribution increases

Question 32

Erythromycin is an antibacterial agent with a half-life of 6 hours.  The prescribed dosage regimen is 500 mg every 6 hours.  How long will it take to reach steady
state using this dosage regimen? 
A.  12 hrs 
B.  18 hrs 
C.  24 hrs 
D.  30 hrs 
E.  60 hrs 
F.   6 days 

Extra- What is the fold-fluctuation in Cp (plasma levels) between doses?

Answer 32

C.  24 hrs
D.  30 hrs

tau = 1 half-life –> 2^1 = 2-fold fluctuation

Question 33

If the dosage regimen for erythromycin (previous) is
changed to 1000 mg every 12 hours one will observe that:
A.  Steady-state will be achieved more rapidly
B.  A higher steady state plasma level will be attained
C.  Fluctuations in plasma levels (the difference between
Cp
D.  A and B only E. 
All of the above

extra- What will the fold-fluctuations be with the new regimen?

Answer 33

C.  Fluctuations in plasma levels (the difference between Cpmax and Cpmin) will be increased

tau = 2 half-lives –> 2^2 = 4-fold fluctuation

Question 34

Which of the following drug dosage regimens would result in the LEAST amount of fluctuation in the plasma
drug level during the dosing interval?
A. Drug E (t1/2= 1.5 hrs) dosed every 8 hrs
B. Drug A (t1/2= 6 hrs) dosed every 6 hrs
C. Drug B (t1/2= 4 hrs) dosed every 18 hrs
D. Drug C (t1/2= 24 hrs) dosed every 3 hrs
E. Drug D (t1/2= 12 hrs) dosed every 6 hrs

Answer 34

E. Drug D (t1/2= 12 hrs) dosed every 6 hrs

Question 35

A patient inadvertently received an excessive dose of meperidine (Demerol ®) during a conscious sedation procedure and was brought to the emergency room in a
deep coma with severe respiratory depression 2 hours after the dose. An immediate blood analysis shows a meperidine level of 1 mg/L. Assuming that the pharmacokinetics of meperidine in this patient are V L and the half-life is 2 hrs, how much meperidine did the patient receive 2 hours earlier?

-What if the patient showed up in the ED 1 hour after the dose - how much did they receive 1 hour earlier?

Answer 35

400mg

282mg