Chem Basis PPIs 4

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Author:
kyleannkelsey
ID:
251690
Filename:
Chem Basis PPIs 4
Updated:
2013-12-08 15:11:41
Tags:
Chem Basis PPIs
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Chem,Basis,PPIs,4
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Chem Basis PPIs 4
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  1. Why can pantoprazole form a water soluble salt?
    It’s imidazole NH group is uniquely acidic enough

  2. What functional significance does the Methoxy group at R1 have?
    Donates e- to pyridine N through pi bonds

  3. What functional significance does the Methoxy group at R2 have?
    Exerts inductive penalty, pulls electrons through sigma bonds, ↓ pKa 1 and ↓ activity

  4. What effect does the 5-difluromethoxy group have on the Benzimidazole N3?
    ↓ ability of N3 to become protonated

  5. Why is the activation of this drug slow?
    Due to low reactivity of the benzimidazole N3

  6. The slow activation of pantoprazole allows for what?
    The drug to reach the deeper CYS residue

  7. Why is the duration of action longer for Pantoprazole than other PPIs?
    The deeper CYS residue is bound, parietal cells are not subject to glutathione rescue

  8. What CYP enzymes metabolize Pantoprazole?
    CYP2C19 and CYP3A4

  9. How does CYP2C19 alter this drug?
    O-dealkylation of the C5 methoxy

  10. How does CYP3A4 alter this drug?
    Osidation

  11. What significant DDIs does this drug have?
    None

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