CP450 enzymes and drug metabolism 1

• What is the title of the document?

  INTRO TO DRUG METABOLISM
• What role do enzymes play in drug metabolism?

  Enzymes are involved in conjugation and excretion processes.
• What are the important enzymes mentioned in drug metabolism?

  UDP-glucuronic acid transferases and glutathione S-transferases.
• What is the significance of ester metabolism pathways?

  They are involved in various metabolic processes for drug elimination.
• How do enzymes typically metabolize drugs?

  They convert drugs into metabolites, which often have no biological activity.
• What is the role of secondary enzymes in drug metabolism?

  They assist in the metabolism of drugs by facilitating further reactions.
• What does the term 'metabolic rate' refer to in drug metabolism?

  It refers to the speed at which drugs are metabolized in the body.
• What is the role of cytochrome P450 enzymes in drug metabolism?

  They are involved in the oxidation of various substrates, including drugs.
• What is the most common type of oxidation reaction in drug metabolism?

  Hydroxylation.
• Which enzyme is responsible for the metabolism of R-warfarin?

  CYP2C9.
• Which enzyme metabolizes S-warfarin?

  CYP2C19.
• How do enzymes handle chiral molecules?

  Different stereocenters are metabolized differently, leading to different products.
• What is the mechanism by which cytochrome enzymes work?

  They require O₂, NADPH, and a reductant to catalyze reactions.
• What is the result of positive catalysis in cytochrome enzymes?

  It generates highly reactive chemical species and expels unnecessary ones.
• What is the oxidation state of iron in the catalytic cycle of cytochrome enzymes?

  (FeO)²⁺.
• What happens to type 2 substrates in the catalytic cycle?

  They do not coordinate to Fe³⁺.
• What are uncoupled reactions in cytochrome enzymes?

  They consume O₂ and NADPH without oxidizing the substrate.
• What defines enzyme superfamilies like CYPs?

  • Group of enzymes catalyzing similar reactions
  • Share ≥ 40% sequence homology or identity
  • Important for drug metabolism
• What is the significance of CYP3A4 in drug metabolism?

  • Most abundant CYP enzyme in humans
  • Varies in expression between individuals
  • Influences pharmacokinetics and drug interactions
• How does drug metabolism differ between children and adults?

  • Different expression levels of CYP enzymes
  • Affects the rate of drug metabolism
  • Can lead to variations in drug efficacy and safety
• How can drugs with different structures be metabolized by the same enzyme?

  • Enzymes can have broad substrate specificity
  • Allows for the metabolism of structurally diverse compounds
  • Important for understanding drug interactions