Chem Basis - AGNs 2

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Chem Basis - AGNs 2
2014-02-11 14:24:51
Chem Basis AGNs
Chem Basis - AGNs 2
Chem Basis - AGNs 2
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  1. What is this drug?

  2. Would you use this drug to treat Mycobacterium avium?
    • You could, it has activity, but it is not a first line therapy
    • (Amikacin)

  3. What are the side effects of this drug?
    • Ototoxicity
    • (Amikacin)
  4. How is Ototoxicity manifested?
    • Hearing loss
    • Tinnitus
    • Often Irreversible
  5. How is Vestibular toxicity manifested?
    • Dizziness
    • Vertigo
    • Ataxia

  6. What is the significance of this group?
    • Prevents Acetylation at the 3-NH2 position by Aminoacetyltransferase
    • Provides resistance to inactivation by P. aeruginosa and M. tuberculosis that other AGs are susceptible to
    • Inhits phosphorylation of the 3”-OH (see image)
    • Inhibits adenylation of the 2’-OH (see image)
    • (Amikacin)

  7. What is this group called?
    • L-alpha-hydroxy-alpha-aminobutyric-acid (HABA)
    • (Amikacin)

  8.  What is the significance of this group?
    • Susceptible to acetylation by aminoacetyltransferase 
    • (Amikacin)

  9. When would you use this drug?
    • Reserved for strains resistant to other AGs
    • (Amikacin)

  10. Is this drug first line?
    • No
    • (Amikacin)

  11. Is this a Diguanidine (1, 3-Diaminohexose) or a 2-Deoxystreptamine (1,3-Diaminocyclohexane)?
    • 2-Deoxystreptamine (1,3-Diaminocyclohexane)

  12. What is this drug?

  13. What is unique about the structure of this drug?
    • It is a mix of three components
    • (Kanamycin)

  14. Why is this drug no longer used?
    • Resistance has developed
    • (Kanamycin)

  15. Can this drug be given orally?
    • Yes
    • (Kanamycin)

  16. Is this drug effective against Mycobacteria, such as M. tuberculosis?
    • Yes
    • (Kanamycin)

  17. What is the significance of these 2 structures?
    • Susceptible to adenylation by Nucleotidyltransferase
    • (Kanamycin)

  18. What is the significance of these 3 structures?
    • Susceptible to Acetylation by Aminoacetyltransferase
    • (Kanamycin)

  19.  What is the significance of these 3 structures?
    • Susceptible to Phosphorylation by Phosphotranseferases
    • (Kanamycin)

  20. Which AGS would you choose if an organism were resistant to Kanamycin?
    • Gentamicin or Tobramycin
    • Because both lack an R3”-OH
    • Gentamicin also lacks a 4”-OH
    • So, they are resistant to Phosphotraneferases, the most troubling inactivation of Kanamycin

  21.  Which subspecies: A, B or C is susceptible to phosphotranseferases, aminoacetyltransferases and Nucleotidyl transferases?
    • B
    • (Kanamycin)

  22. Which drug is a semisynthetic Kanamycin A derivative?
    • Amikacin