- Hydrolysis of procaine would be most accurately characterized as an example of
Your answer:
active metabolite formation.
bioinactivation.
detoxification.
bioactivation.
prodrug activation.
- N-Demethylation of imipramine would be most accurately characterized as an example of
Your answer:
bioactivation.
detoxification.
bioinactivation.
prodrug activation.
active metabolite formation.
- Which of the following would typically NOT involve or would NOT be characterized as a phase-1 reaction?
Your answer:
Enterohepatic recycling.
Ester hydrolysis.
detoxification.
bioinactivation.
Ketone reduction.
- Suppose that we are dealing with a drug that undergoes extensive "enterohepatic recycling". Now suppose an oral antibiotic is given which completely destroys the gut flora. What change in the pattern of excretion of the drug would you expect to see?
Your answer:
Change to an increase in the phase-2 metabolite in the feces.
Change to an increase in the parent drug in the urine.
Change to an increase in partent drug in the feces.
Change to an increase in drug metabolite in the urine.
Change to an increase in phase-1 metabolite in the feces.
- The heme iron in P-450 is involved in complexing six ligands. Which one of the following is NOT one of those ligands?
Your answer:
Molecular (diatomic) oxygen.
Pyrrole nitrogen (heme)
The substrate.
The P-450 protein (through a cysteine sulfhydryl)
OOPS! ALL OF THE ABOVE are ligands on the heme!!!
- Suppose the substrate para-deuteroaniline was metabolized by P-450 resulting in aromatic hydroxylation. Which of the following metabolites is UNLIKELY to form?
Your answer:
4-hydroxy-3-deuteroaniline.
3-hydroxy-4-deuteroaniline.
2-hydroxy-4-deuteroaniline.
- Which ONE of the following statements concerning O-dealkylation of codeine is incorrect (false)?
Your answer:
This represents the formation of an active metabolite.
The mechanism for this reaction involves the formation of a carbinolamine.
The initial step for this reaction is hydroxylation on a carbon atom.
This results in the formation of a metabolite that is more polar than the parent drug.
This reaction is catalyzed by P-450.
- N-Dealkylation of an N-isopropyl group would result in the formation of
Your answer:
isopropanol and an amine.
an aldehyde and an amine.
an acid and an amine.
acetone and an amine.
an acid and an alcohol.
- Would a nitroaromatic drug like chloramphenicol undergo P-450 mediated aromatic hydroxylation by an arene oxide mechanism?
Your answer:
Yes it would; directly on the nitro group.
Yes, it would, but not on the nitro group.
No, because the aromatic ring is deactivated.
No it would not, because the ring is no longer aromatic if there is a nitro group attached.
No, because the aromatic ring is activated.
- Consider the following series of sequential statements. Which statement is the FIRST one in the series that is FALSE?
Your answer:
Carbamazepine is metabolized by P-450.
Carbamazepine is metabolized by P-450 to form an epoxide.
Carbamazepine is metabolized by P-450 to form an epoxide which is then metabolized by epoxide hydratase.
Carbamazepine is metabolized by P-450 to form an epoxide which is then metabolized by epoxide hydratase to form a cis-dihydrodiol.
Carbamazepine is metabolized by P-450 to form an epoxide which is then metabolized by epoxide hydratase to form a cis-dihydrodiol which is an active metabolite.