DA Protein Synthesis Inhibitors

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HUSOP2014
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134272
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DA Protein Synthesis Inhibitors
Updated:
2012-02-13 16:52:14
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HUSOP DA EXAM2 protein synthesis inhibitors
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Protein Synthesis Inhibitors
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  1. Tetracyclines bind to the ____ site of the ___ ribosomal subunit.
    A, 30s
  2. Tetracyclines prevent ________ ____ from binding, inhibiting elongation of the protein being synthesized.
    aminoacyl tRNA
  3. True or false. Tetracyclines are taken up efficiently by mammalian cells.
    False
  4. What are the 3 primary mechanisms for resistance for tetracyclines.
    1. decreased entry or acquistion of efflux transporter

    2. Presence of ribosomes protection proteins which blocks tetracycline access to the ribosome.

    3. Enzymatic inactivation of tetracylines
  5. Are tetracylines broad spectrum or narrow spectrum antibiotics.
    Broad spectrum
  6. Tetracyclines have more activity against gram ____ bacteria and also some against gram _____ bacteria.
    • Postitive,
    • Negative
  7. Tetracylines can be used for Acne treatment and inhibit _________.
    propionibacteria
  8. A major adverse effect with women who took tetracylines while pregnant, and the adverse effect seen in their children is?
    Teeth discoloration
  9. Tetracycline absorption is impaired by the concurrent ingestion of ________, antacids, _______, dietary Fe and ___ supplements
    • dairy products,
    • Pepto-Bismol,
    • Zn
  10. Chloramphenicol binds to the bacterial ____s large ribosomal subunit
    50
  11. The primary route of elimination for most tetracylines is the kidney. But Doxycyline is _________ and Minocycline is mostly _______
    • Both Hepatic and renal,
    • hepatic
  12. Chloramphenicol Blocks protein synthesis by which MOA.
    inhibits the transfer of the peptide form the P site to the A site. (TRANSPEPTIDATION reaction)
  13. T/F. Chloramphenicol can also bind to and inhibit mitochondrial large ribosomal subunit. Mostly in the cells of bone marrow.
    True
  14. What is the primary mechanism of resistance for Chlormaphenicol?
    Acetylation of the drug
  15. The antibacterial spectrum for Cholamphenical most gram negative bacteria and most gram positive _________.
    anaerobic cocci
  16. Which drugs can be used to treat Rickettsia (rocky mountain spotted fever)
    • Chlormphenicol,
    • Tetracylines
  17. When Chloramphenicol is given in high doses to infants and can cause_________.
    Gray Baby syndrome
  18. Chloramphenicol inhibits CYP______ causing prolonged half lives of other drugs.
    CYP 450
  19. _________ and _________ bind to nearby sites of the ribosome, and thus bind _________ with chloramphenicol.
    • Macrolides,
    • clindamycin,
    • Competitively
  20. The differences on the macrolide stucture are responsible for 3 things.
    • stability
    • antibacterial spectrum
    • tissue penetration
  21. T/F macrolides bind reversibly to bacterial 50s large ribosomal subunits.
    True
  22. Macrolides inhibit ______ and block ______ synthesis.
    Translocation, protein
  23. Most Macrolides are bacteriostatic but can they be bactericidal and if so when?
    YES, at high concentrations
  24. Name the 4 main mechanisms of reistance for Macrolides.
    1. Drug efflux form the cell

    2. Addition of methly group to the ribosome (by a methylase) causing a reduction in the affintiy of the ribosome to the macrolide.

    3. Hydrolysis of macrolide by an esterase

    4. Chromosomal mutations that alter a 50s ribsomal protein
  25. Erythromycin and Clarithromycin (macrolide) are most effective against Gram ______ bacteria and some activity against Gram ______ bacteria..
    Postitive, Negative
  26. T/F Azithromycin has more activty against Gram positive bacteria than other macrolides.
    FALSE
  27. Erythromycin and Clarithromycin interfere with CYP _____
    CYP450
  28. T/F Macrolides, chloramphenicol and chlindamycin bind to nearby sites of the ribosome , thus interact competitively.
    TRUE
  29. Teliithromycin is a ketolide and is a semi-synthetic derivative of _________.
    erythromcyin
  30. Telithromycin has ______ resistance because it is less susceptible to __________ mediated and efflux- mediated mechanicams of reistance.
    • Less,
    • methylase
  31. Clindamycin has a similar MOA with _______ because it; inhibits the transfer of the peptide form the ____ site to the ____ site (TRANSPEPTIDATION reaction)
    • chloramphenicol
    • P
    • A
  32. Clindamycin binds to the ____ ribosomal subunit
    50s
  33. Clindamycin is effective against Gram ____ bacteria and some against Gram _____ bacteria. and is used to treat acne _______.
    • Postitive
    • Negative
    • vulgaris
  34. T/ F Macrolides, chloramphenicol, and clindamycin bind to nearby sites on the ribosome, and thus interact competitively with one another.
    True
  35. Streptogramins are adminstered in a 30:70 combination. What is the 30 and what is the 70?
    30= Streptogramin B (Quinupristin)

    70= Streptogramin A (Dalfopristin)
  36. Is Streptogramins bacterostatic or bacterocidal?
    Bacterocidal
  37. What are the MOAs for Streptogramins?
    1. Bind to 50s ribosomal subunit.

    2. Steptogramin B Binds to the same site as macolides inhibiting Translocation.

    3. Streptogramin A binds to a nearby site. causing Streptogramin B to be enchance binding and also interferes with the polypepide chain formation
  38. Streptogramins becomes resistant by which 4 ways.
    1. Ribosomal methlyase

    2. Lactonase (hydrolis)

    3. Acetyltransferase

    4.Efflux transporter
  39. Streptogramins are effective against many Gram _____ cocci.
    Postitive
  40. T/F Streptogramin is effective against most gram negative bacteria.
    FALSE
  41. Streptogramin are inhibitors of what CYP?
    CYP 450
  42. Linezolid binds to the 50s ribosomal subunit, and also prevents formation of the complete _____ ribosome, causing the blockage of _______ initiation.
    70s, translation
  43. T/F Linezolid can be bacterodstatic or bactericidal depending on concentration.
    True
  44. Linezolid is effective against gram -_______ and ineffective against most gram _____ bacteria
    • postive
    • negative
  45. Which 2 drugs are used in reserved for treating multi-drug resistant bacteria (e.g. Enterrococcus faecium, Staphylococcus aureus, and Streptococcus pyogenes).
    • Linezolid
    • streptogramins

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