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.