Chem Basis CPNs 2

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  1. Why do CPNs not treat Enterococcus species well?
    PBPs in Enterococcus do not allow CPNs to bind (but do allow PCNs)
  2. What drugs would you use to treat Enterococcus species?
    Ampicillin and Vancomycin
  3. (True/False) CPNS are classified based on general features of antimicrobial activity to four generations.
  4. (True/False) First CPNs generation have good G+ activity.
  5. (True/False) Second CPNs generation have decreased activity against G-
  6. (True/False) Third CPNs generation have increased activity against G- including Pseudomonas
  7. (True/False) Fourth CPNs generation has activity against enterococcus.
  8. Which of the following sould be used to treat an enterococcus infection, Cephalexin, Cefepime, Ceftazidime or Cefotetan?
  9. Which of the following sould be used to treat a Citrobacter infection, Cephalexin, Cefepime, Ceftazidime or Cefotetan?
  10. Which of the following sould be used to treat a B. fragilis infection, Cephalexin, Cefepime, Ceftazidime or Cefotetan?
  11. Which of the following sould be used to treat a Proteus infection, Cephalexin, Cefepime, Ceftazidime or Cefotetan?
  12. What is the pharmacophore for CPNs?
    • 7-aminocephalosporonic acid
  13. Describe the composition fo the 7-aminocephalosporonic acid pharmacophore for CPNs?
    B-lactam ring attached to a dihydrothiazine (3-cephem ring)
  14. A substituent is tolerated at what part of the 3-cephem ring on a CPN?
    • C3
  15. What is a Carbecephem?
    • A CPN with a C instead of an S at the 3-cephem ring
  16. What is a Cephamycin?
    • A CPN with a 7-methoxy group
  17. The goal of structural modifications of CPNs is to add what characteristics to the drug?
    Increase spectrum, B-lactamase resistance and bioavailability
  18. Which generation of cephalosporins will have the best G+ activity?
    1st generation
  19. Why are 2nd, 3rd and 4th generation CPNs not used for G+ species, even if they show susceptibility?
    Simpler antibiotics available and CPN costs are higher
  20. What is the more unique feature of the CPN spectrum?
    Treat Klebsiella species
  21. Would the dose be higher or lower for CPNs and why?
    Lower, because they are more potent
  22. Is the Na in CPNs a concern for patients with heart failure?
    Not as much as with Penicillins, but should still be monitored
  23. Why is pseudomonas resistant to CPNs, even when they have Methoxyimine groups at R’ that sterically block B-lactamases?
    Pseudomonas blocks penetration of the drug, resistance is not call due to B-lactamase secretion
  24. What is the R-1 group on Cefepime and benefits does it impart?
    • 2-aminothiazolyl-acetoamido, enhances B-lactamase resistance, creates a zwitterion ( due to C3 quaternary N) that can rapidly penetrate G- porin channels
  25. Why does an R1 actoxymethyl group impart acid degredation?
    • O is open for hydrolysis by H+,which is followed by lactonization and creation of an inactive lactone compound

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Chem Basis CPNs 2
2014-01-26 20:10:46
Chem Basis CPNs

Chem Basis CPNs 2
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