(AD, E) M

Question 1

what are the 2 steps to CYP metabolism?

Answer 1

1. activation of o2
2. oxidation of drug
   drug + o2 + NADPH + 2H+ –> drug - OH + NADP+ H20

Question 2

what are the 2 binding sites on the CYP enzyme?

Answer 2

substrate (drug) and one for O2 (or CO)

Question 3

what are the Michaelis mention enzyme kinetic principles?

Answer 3

• assume a single substrate binding site

- rapid equilibrium and formation of ES complex

Question 4

what are the determinants of CYP metabolism

Answer 4

• location of AS
• degree of steric hinderance
• ease of e- or hydrogen abstraction from the C (or N or S) atom

Question 5

aside from drugs, what is glucuronidation important for?

Answer 5

metabolism of endogenous molecules such as bilirubin, bile acids (lack of UGTs in children leads to congenital jaundice and in adults is gilberts syndrome)