Lecture 5
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Questions and Answers

Which organ is the main site involved in drug metabolism?

  • Heart
  • Kidney
  • Liver (correct)
  • Brain

    • How many phases does drug metabolism go through?

  • Three
  • One
  • Four
  • Two (correct)

    • What is the group of enzymes within the cells of the liver that function to metabolize drugs?

  • Drug Metabolic Ensemble (DME)
  • Metabolic Enzyme Group (MEG)
  • Drug Microsomal Metabolizing System (DMMS) (correct)
  • Hepatic Enzyme Coalition (HEC)

    • Which factor does not alter the drug metabolizing pathway?

    <p>Gender</p> Signup and view all the answers

    Which of the following is not a major site of drug elimination?

    <p>Spleen</p> Signup and view all the answers

    What is the concept used to demonstrate the differences between zero order and first order kinetics?

    <p>Half-life concept</p> Signup and view all the answers

    Which enzyme system utilizes cytochrome P450 enzymes to transform drugs into metabolites through oxidation and reduction reactions?

    <p>Drug Metabolism: Phase I</p> Signup and view all the answers

    What type of metabolism primarily involves oxidation and reduction, yielding slightly polar metabolites that can still be active?

    <p>Phase I (R-OH)</p> Signup and view all the answers

    Where are Cytochrome P-450 Enzymes (3A4) found?

    <p>Both liver and gut lumen</p> Signup and view all the answers

    What is the impact of aging on drug metabolism rate?

    <p>Decreases drug metabolism rate</p> Signup and view all the answers

    What is the time required for the plasma drug concentration to decrease to half of its initial level called?

    <p>Half-life</p> Signup and view all the answers

    Which factor influences the half-life of a drug?

    <p>Volume of distribution</p> Signup and view all the answers

    In a practice scenario, what is used to determine the time it takes to reach a specific plasma concentration of a drug?

    <p>Half-life</p> Signup and view all the answers

    Which type of elimination results in constant elimination rates?

    <p>Zero order elimination</p> Signup and view all the answers

    What is the main process involved in Drug Metabolism: Phase II?

    <p>Methylation and glucuronidation</p> Signup and view all the answers

    What is the effect of neonates/infants on drug metabolism capacity?

    <p>Reduced drug metabolism capacity</p> Signup and view all the answers

    What type of metabolites does Drug Metabolism: Phase II (conjugation) produce?

    <p>Polar, inactive metabolites</p> Signup and view all the answers

    Which enzyme system is responsible for transforming drugs into metabolites through oxidation and reduction reactions?

    <p>Cytochrome P-450 Enzymes (3A4)</p> Signup and view all the answers

    What is the main process involved in Drug Metabolism: Phase II?

    <p>Conjugation</p> Signup and view all the answers

    What factor does not alter the drug metabolizing pathway?

    <p>Elimination kinetics</p> Signup and view all the answers

    Where are Cytochrome P-450 Enzymes (3A4) found?

    <p>Liver</p> Signup and view all the answers

    Which type of metabolism primarily involves oxidation and reduction, yielding slightly polar metabolites that can still be active?

    <p>Phase I metabolism</p> Signup and view all the answers

    What type of metabolites does Drug Metabolism: Phase II (conjugation) produce?

    <p>Water-soluble metabolites</p> Signup and view all the answers

    What is the impact of aging on drug metabolism rate?

    <p>Decreases drug metabolism rate</p> Signup and view all the answers

    Which of the following is not a major site of drug elimination?

    <p>Spleen</p> Signup and view all the answers

    What is the effect of neonates/infants on drug metabolism capacity?

    <p>Reduces drug metabolism capacity</p> Signup and view all the answers

    What is used to determine the time it takes to reach a specific plasma concentration of a drug?

    <p>Half-life</p> Signup and view all the answers

    What is the concept used to demonstrate the differences between zero order and first order kinetics?

    <p>Graphical demonstration concept</p> Signup and view all the answers

    Which type of elimination results in constant elimination rates?

    <p>Zero order elimination</p> Signup and view all the answers

    What is the primary function of Cytochrome P450 enzymes in the Drug Metabolizing Microsome System (DMMS)?

    <p>Transformation of drugs into metabolites through oxidation and reduction reactions</p> Signup and view all the answers

    Which factor contributes to the reduced drug metabolism capacity in neonates/infants?

    <p>High concentration of cytochrome P450 enzymes</p> Signup and view all the answers

    What type of metabolites does Drug Metabolism: Phase I (R-OH) primarily yield?

    <p>Slightly polar metabolites that can still be active</p> Signup and view all the answers

    What is the impact of aging on drug metabolism rate?

    <p>Decrease in drug metabolism rate due to reduced liver blood flow and increased body fat</p> Signup and view all the answers

    Which process is involved in Drug Metabolism: Phase II?

    <p>Methylation and glucuronidation</p> Signup and view all the answers

    Which factor influences the half-life of a drug?

    <p>Volume of distribution</p> Signup and view all the answers

    Where are Cytochrome P-450 Enzymes (3A4) found?

    <p>Systemic circulation</p> Signup and view all the answers

    What type of elimination results in constant elimination rates?

    <p>$Zero-order$ elimination</p> Signup and view all the answers

    What is the main process involved in Renal elimination?

    <p>Distal tubular reabsorption</p> Signup and view all the answers

    What is the concept used to demonstrate the differences between zero order and first order kinetics?

    <p>Michaelis-Menten equation</p> Signup and view all the answers

    In a practice scenario, what is used to determine the time it takes to reach a specific plasma concentration of a drug?

    <p>Area under the plasma concentration-time curve (AUC)</p> Signup and view all the answers

    Study Notes

    • The Drug Metabolizing Microsome System (DMMS) utilizes cytochrome P450 enzymes, which transform drugs into metabolites through oxidation and reduction reactions.

    • Drug metabolism can lead to enzyme induction or inhibition, affecting drug duration of action.

    • Drug Metabolism: Phase I (R-OH) primarily involves oxidation and reduction, yielding slightly polar metabolites that can still be active.

    • Drug Metabolism: Phase II (conjugation) involves methylation, glucuronidation, acetylation, and sulfation, producing highly polar, inactive metabolites for renal excretion.

    • Cytochrome P-450 Enzymes (3A4) are found in the liver, gut lumen, enterocytes, and systemic circulation.

    • Neonates/Infants have a reduced drug metabolism capacity, resulting in slower elimination and prolonged drug duration of action. Conversely, aging causes a decrease in drug metabolism rate due to reduced liver blood flow and increased body fat.

    • Renal elimination involves glomerular filtration, proximal tubular secretion, and distal tubular reabsorption.

    • Elimination kinetics include zero order and first order elimination, where zero-order elimination results in constant elimination rates and first-order elimination follows an exponential decay.

    • Half-life is the time required for the plasma drug concentration to decrease to half of its initial level and is essential for determining drug administration frequency.

    • Half-life is influenced by factors like liver and kidney function, volume of distribution, and clearance, making these essential in calculating drug half-life.

    • In a practice scenario, given a drug's half-life (5 hours) and initial plasma drug concentration (24 mg/L), the time it takes to reach a plasma concentration of 3 mg/L can be calculated. The answer is C. 15 hours.

    • The Drug Metabolizing Microsome System (DMMS) utilizes cytochrome P450 enzymes, which transform drugs into metabolites through oxidation and reduction reactions.

    • Drug metabolism can lead to enzyme induction or inhibition, affecting drug duration of action.

    • Drug Metabolism: Phase I (R-OH) primarily involves oxidation and reduction, yielding slightly polar metabolites that can still be active.

    • Drug Metabolism: Phase II (conjugation) involves methylation, glucuronidation, acetylation, and sulfation, producing highly polar, inactive metabolites for renal excretion.

    • Cytochrome P-450 Enzymes (3A4) are found in the liver, gut lumen, enterocytes, and systemic circulation.

    • Neonates/Infants have a reduced drug metabolism capacity, resulting in slower elimination and prolonged drug duration of action. Conversely, aging causes a decrease in drug metabolism rate due to reduced liver blood flow and increased body fat.

    • Renal elimination involves glomerular filtration, proximal tubular secretion, and distal tubular reabsorption.

    • Elimination kinetics include zero order and first order elimination, where zero-order elimination results in constant elimination rates and first-order elimination follows an exponential decay.

    • Half-life is the time required for the plasma drug concentration to decrease to half of its initial level and is essential for determining drug administration frequency.

    • Half-life is influenced by factors like liver and kidney function, volume of distribution, and clearance, making these essential in calculating drug half-life.

    • In a practice scenario, given a drug's half-life (5 hours) and initial plasma drug concentration (24 mg/L), the time it takes to reach a plasma concentration of 3 mg/L can be calculated. The answer is C. 15 hours.

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