Fall Exam I Active Learning Questions Flashcards
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
E. Lipid diffusion through membrane itself
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
F. Aqueous diffusion through membrane pores
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
C. Hepatic metabolism of a drug prior to entry in to the systemic circulation
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
ALL!
ABCDE
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
C. Largely lipophilic drugs, yet soluble in aqueous solutions
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
A. Intramuscular
C. Intranasally
G. Intravenous**
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
C. Intravenous (most dangerous)
G. Inhalational*
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.
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.
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
B. Highly lipid soluble drugs
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
C. Drugs can cross the blood-brain barrier through specific transporters
D. Lipid soluble drugs readily cross the blood-brain barrier
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.
A. An acid will most readily cross membranes when it is contained in acidic body fluids.
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
E. 100:1
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
C. 1:1
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)
B. Stomach (pH ∼ 2.5)
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
A. Increased
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.
E. All of the above are true
“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
C. Intravenous
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)
A. The drug being highly lipid soluble
B. The drug being highly bound to plasma proteins***
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
A. Less likely to distribute intracellularly
D. More water soluble than the parent drug
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
E. All of the above
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
D. Poor CYP2D6 metabolizer
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
E. Will be less likely to decline in activity with aging than
phase I reactions
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
A. Amidases
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
B. Sulfation
D. Glucuronidation
