Chem Basis PPIs 2

The flashcards below were created by user kyleannkelsey on FreezingBlue Flashcards.

  1. Image Upload
    What functional significance does the methoxy group at position 4 (R1) have?
    Donates electrons through resonance to pyridine nitrogen (Omeprazole)
  2. Image Upload
    What functional significance do the methyl groups at positions 3 and 5 have?
    ↑nucleophilic character of unionized pyridine N by ↓ inductive pull of the methoxy group on the pyridine N (Omeprazole)
  3. Image Upload
    What is the functional significance of the methoxy group at position 5 of Benzimidazole ring?
    Enhances N3 protonation, pulls e- from C2 through sigma bonds (Omeprazole)
  4. Image Upload
    What is the relative OOA for Omeprazole? Fast
    Fast
  5. Image Upload
    Can this molecule reach the deeper CYS residue?
    No (Omeprazole)
  6. Image Upload
    Does this drug have a long or short DOA?
    Long (Omeprazole)
  7. Image Upload
    Is this molecule susceptible to Glutathione rescue?
    Yes (Omeprazole)
  8. Image Upload
    Is this drug susceptible to CYP2C19 metabolism?
    Yes (Omeprazole)
  9. Image Upload
    What changes to this molecule would CYP2C19 make?
    Hydroxylation of C5 (Omeprazole)
  10. Image Upload
    Is this drug susceptible to CYP3A4 metabolism?
    Yes (Omeprazole)
  11. Image Upload
    What changes to this molecule would CYP3A4 make?
    Sulfoxidation to a sulfone (Omeprazole)
  12. Image Upload
    Which CYP enzyme catalyzes the reduction of this drug to a Thioether?
    None, occurs by a non-enzymatic reaction (Omeprazole)
  13. Image Upload
    What effect does this drug have on CYP2C19?
    Can inhibit it when dosed chronically (in turn inhibiting own metabolism) (Omeprazole)
  14. Image Upload
    What is the only clinically significant DDI for this drug?
    Causes 25-50% ↓ in diazepam clearance (Omeprazole)
  15. Image Upload
    In what race would you need to decrease the dose of this drug and why?
    Asians as b/c typically slow CYP2C19 metabolizers (Omeprazole)
Author:
kyleannkelsey
ID:
251686
Card Set:
Chem Basis PPIs 2
Updated:
2013-12-08 20:06:40
Tags:
Chem Basis PPIs
Folders:

Description:
Chem Basis PPIs 2
Show Answers: