Pharmakokinetics Flashcards
Which of the following mechanisms of drug transport across cell membranes is energy-dependent?
A) Passive diffusion
B) Facilitated diffusion
C) Active transport
D) Osmosis
Answer: C
Explanation: Active transport requires energy to move substances against their concentration gradient, unlike passive and facilitated diffusion.
What factor primarily influences the efficiency of passive drug diffusion across cell membranes?
A) Water solubility
B) Lipid solubility
C) Molecular weight
D) Ionization
Answer: B
Explanation: Passive diffusion depends mainly on the lipid solubility of the drug, allowing it to pass through the lipid bilayer of cell membranes.
First-pass metabolism primarily occurs in which organ?
A) Kidney
B) Stomach
C) Liver
D) Lungs
Answer: C
Explanation: First-pass metabolism predominantly occurs in the liver, where the drug is metabolized before reaching systemic circulation.
Which of the following does NOT affect drug absorption?
A) Gastric pH
B) Gastric emptying time
C) Plasma protein binding
D) Intestinal motility
Answer: C
Explanation: Plasma protein binding affects drug distribution, not absorption.
Which characteristic of a drug leads to a high volume of distribution (Vd)?
A) High plasma protein binding
B) High molecular weight
C) High lipid solubility
D) Low tissue binding
Answer: C
Explanation: High lipid solubility leads to extensive tissue distribution, resulting in a high volume of distribution.
What is the approximate volume of distribution for warfarin in a 70 kg adult?
A) 7 liters
B) 16 liters
C) 35 liters
D) 140 liters
Answer: A
Explanation: Warfarin has a small volume of distribution, around 7 liters, indicating it primarily remains in the plasma.
Ion trapping of drugs occurs when:
A) A drug is weakly acidic and the environment is basic
B) A drug is weakly basic and the environment is acidic
C) A drug is strongly acidic and the environment is neutral
D) Both A and B
Answer: D
Explanation: Ion trapping occurs when a drug is in an environment where it becomes ionized and cannot easily cross cell membranes.
Which phase of drug metabolism involves conjugation reactions?
A) Phase I
B) Phase II
C) Both Phase I and II
D) Neither Phase I nor II
Answer: B
Explanation: Phase II metabolism involves conjugation reactions, where a polar molecule is added to the drug.
Cytochrome P450 enzymes are primarily involved in:
A) Phase I oxidative reactions
B) Phase II conjugative reactions
C) Both Phase I and II reactions
D) Excretion of drugs
Answer: A
Explanation: Cytochrome P450 enzymes catalyze Phase I oxidative reactions, introducing a functional group to the drug.
Which cytochrome P450 enzyme is predominantly found in the intestinal epithelium?
A) CYP1A2
B) CYP2D6
C) CYP3A4
D) CYP2C9
Answer: C
Explanation: CYP3A4 is abundant in the intestinal epithelium and plays a significant role in first-pass metabolism.
Which of the following processes is NOT involved in renal drug excretion?
A) Glomerular filtration
B) Tubular secretion
C) Tubular reabsorption
D) Biliary excretion
Answer: D
Explanation: Biliary excretion involves the liver, not the kidneys, which primarily handle glomerular filtration, tubular secretion, and reabsorption.
Which organ is primarily responsible for the excretion of volatile anesthetics?
A) Liver
B) Kidney
C) Lungs
D) Skin
Answer: C
Explanation: Volatile anesthetics are mainly excreted through the lungs.
Grapefruit juice is known to inhibit which cytochrome P450 enzyme, leading to increased blood levels of certain drugs?
A) CYP1A2
B) CYP2D6
C) CYP3A4
D) CYP2C9
Answer: C
Explanation: Grapefruit juice inhibits CYP3A4, affecting the metabolism of drugs that are substrates of this enzyme.
Which of the following is a consequence of enzyme induction?
A) Decreased drug metabolism
B) Increased drug plasma levels
C) Reduced therapeutic effect of the drug
D) Increased risk of drug toxicity
Answer: C
Explanation: Enzyme induction increases the metabolism of drugs, potentially lowering their plasma levels and reducing their therapeutic effect.
What is the primary determinant of the half-life (t1/2) of a drug?
A) Volume of distribution (Vd)
B) Clearance (Cl)
C) Both Vd and Cl
D) Plasma protein binding
Answer: C
Explanation: The half-life of a drug is determined by both its volume of distribution and clearance.
A drug with a high clearance rate will:
A) Have a long half-life
B) Accumulate in the body
C) Be rapidly removed from the bloodstream
D) Have high bioavailability
Answer: C
Explanation: A high clearance rate means the drug is quickly eliminated from the bloodstream.
Which phase of metabolism is most likely affected by genetic polymorphisms?
A) Phase I
B) Phase II
C) Both Phase I and II
D) Neither Phase I nor II
Answer: A
Explanation: Genetic polymorphisms often affect Phase I enzymes like cytochrome P450s, leading to variability in drug metabolism.
In a patient with renal impairment, what adjustment is typically necessary for renally excreted drugs?
A) Increase the dose
B) Decrease the dose
C) No adjustment needed
D) Switch to a different drug
Answer: B
Explanation: In renal impairment, the dose of renally excreted drugs often needs to be decreased to prevent toxicity.
Which of the following factors does NOT affect the bioavailability of a drug?
A) First-pass metabolism
B) Drug formulation
C) Plasma protein binding
D) Gastrointestinal pH
Answer: C
Explanation: Plasma protein binding affects distribution rather than bioavailability.
The therapeutic index of a drug is:
A) The ratio of its toxic dose to its effective dose
B) The ratio of its absorption rate to its elimination rate
C) The time required to reach peak plasma concentration
D) The proportion of the drug that reaches systemic circulation
Answer: A
Explanation: The therapeutic index is a measure of the drug’s safety margin, calculated as the ratio of the toxic dose to the effective dose.
Which of the following drugs is known to have a large volume of distribution?
A) Warfarin
B) Gentamicin
C) Theophylline
D) Digoxin
Answer: D
Explanation: Digoxin has a large volume of distribution, indicating extensive tissue binding.
Which process is primarily responsible for the renal excretion of highly protein-bound drugs?
A) Glomerular filtration
B) Tubular secretion
C) Tubular reabsorption
D) Biliary excretion
Answer: B
Explanation: Highly protein-bound drugs are not efficiently filtered by the glomerulus and rely more on tubular secretion for renal excretion.
Which of the following can decrease the oral bioavailability of a drug?
A) Increased gastric pH
B) Decreased gastric emptying time
C) Increased hepatic first-pass metabolism
D) Decreased intestinal motility
Answer: C
Explanation: Increased hepatic first-pass metabolism reduces the amount of drug reaching systemic circulation, thereby decreasing oral bioavailability.
In which situation would a drug’s half-life be prolonged?
A) Increased clearance
B) Decreased volume of distribution
C) Decreased clearance
D) Increased hepatic metabolism
Answer: C
Explanation: Decreased clearance results in a prolonged half-life, as the drug is removed from the body more slowly.
What does the term ‘bioequivalence’ refer to?
A) Similar therapeutic effects of two drugs
B) Similar bioavailability of two drug formulations
C) Identical chemical structure of two drugs
D) Same route of administration for two drugs
Answer: B
Explanation: Bioequivalence means that two drug formulations have similar bioavailability and produce the same effect at the site of physiological activity.
Which factor can lead to drug accumulation in the body?
A) High clearance
B) Long dosing interval
C) Slow absorption rate
D) Long half-life
Answer: D
Explanation: A long half-life can lead to drug accumulation, especially if the dosing interval is shorter than the half-life.
Which of the following statements about facilitated diffusion is TRUE?
A) It requires energy expenditure.
B) It is a form of active transport.
C) It requires a carrier protein.
D) It moves substances against their concentration gradient.
Answer: C
Explanation: Facilitated diffusion requires a carrier protein to move substances across cell membranes but does not require energy.
What is the primary site of action for cytochrome P450 enzymes?
A) Kidney
B) Intestine
C) Liver
D) Lungs
Answer: C
Explanation: Cytochrome P450 enzymes are primarily located in the liver, where they metabolize drugs.
What is the effect of competitive inhibition on enzyme activity?
A) Decreases the enzyme’s maximum velocity (Vmax)
B) Increases the enzyme’s affinity for the substrate
C) Increases the enzyme’s maximum velocity (Vmax)
D) Decreases the enzyme’s affinity for the substrate
Answer: A
Explanation: Competitive inhibitors decrease the enzyme’s maximum velocity (Vmax) by competing with the substrate for the active site.
Which of the following drugs is a known substrate for CYP2D6?
A) Warfarin
B) Theophylline
C) Risperidone
D) Omeprazole
Answer: C
Explanation: Risperidone is metabolized by CYP2D6.
A drug with high first-pass metabolism will have:
A) High oral bioavailability
B) Low oral bioavailability
C) High plasma protein binding
D) Low plasma protein binding
Answer: B
Explanation: Drugs with high first-pass metabolism have low oral bioavailability because a significant portion is metabolized before reaching systemic circulation.
The bioavailability of a drug administered intravenously is:
A) 50%
B) 75%
C) 90%
D) 100%
Answer: D
Explanation: Intravenous administration ensures 100% bioavailability, as the drug is directly introduced into systemic circulation.
Which factor does NOT significantly affect drug distribution?
A) Blood flow to tissues
B) Drug solubility
C) Drug metabolism
D) Plasma protein binding
Answer: C
Explanation: Drug metabolism primarily affects drug clearance, not distribution.
In patients with liver disease, doses of drugs primarily metabolized by the liver should be:
A) Increased
B) Decreased
C) Unchanged
D) Given intravenously
Answer: B
Explanation: In liver disease, the metabolism of drugs is impaired, so doses should be decreased to avoid toxicity.
Which of the following is a characteristic of zero-order kinetics?
A) Rate of elimination is constant
B) Rate of elimination is proportional to drug concentration
C) Half-life remains constant
D) Clearance is constant
Answer: A
Explanation: In zero-order kinetics, the rate of elimination is constant regardless of drug concentration.
A drug with a small volume of distribution is likely to be:
A) Lipid-soluble
B) Highly protein-bound
C) Extensively distributed in tissues
D) Rapidly metabolized
Answer: B
Explanation: A small volume of distribution indicates that the drug remains primarily in the plasma, often due to high protein binding.
Which process is most affected by a drug’s pKa value?
A) Absorption
B) Distribution
C) Metabolism
D) Excretion
Answer: A
Explanation: A drug’s pKa affects its ionization, which in turn influences its absorption across biological membranes.
The main purpose of Phase II metabolism is to:
A) Introduce a functional group
B) Increase lipid solubility
C) Make the drug more water-soluble
D) Increase bioavailability
Answer: C
Explanation: Phase II metabolism involves conjugation reactions that make the drug more water-soluble and amenable to renal excretion.
Which enzyme is most likely to be involved in the oxidative metabolism of drugs?
A) Amylase
B) Lipase
C) Cytochrome P450
D) Protease
Answer: C
Explanation: Cytochrome P450 enzymes are key players in the oxidative metabolism of drugs.