Macrolides in Antibiotics
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Questions and Answers

What is one of the mechanisms of aminoglycoside resistance that involves modification of the drug?

  • Mutation of the bacterial ribosome
  • Increased accumulation within the bacterium
  • Presence of efflux pumps
  • Bacterial enzymes such as acetyltransferases (correct)
  • What is the purpose of Neomycin* when given orally?

  • To treat bacterial infections in the gut
  • To prevent bacterial infections in the skin
  • For bowel decontamination (correct)
  • To treat bacterial infections in the blood
  • Which of the following mechanisms of aminoglycoside resistance does not involve modification of the bacterium?

  • Decreased accumulation within the bacterium
  • Mutation of the bacterial ribosome
  • Bacterial enzymes such as acetyltransferases
  • Presence of efflux pumps (correct)
  • What is the general term for the enzymes that modify aminoglycosides and prevent them from binding to ribosomes?

    <p>Acetyltransferases</p> Signup and view all the answers

    What is the result of decreased accumulation within the bacterium?

    <p>Aminoglycoside resistance due to the presence of efflux pumps</p> Signup and view all the answers

    What is the mechanism of aminoglycoside resistance that involves a change in the bacterial ribosome?

    <p>Mutation of the bacterial ribosome</p> Signup and view all the answers

    What is the name of the aminoglycoside shown in Figure 6-2?

    <p>Amikacin</p> Signup and view all the answers

    Which of the following is NOT a mechanism of aminoglycoside resistance?

    <p>Inhibition of bacterial protein synthesis</p> Signup and view all the answers

    What is the main mechanism of action of macrolides?

    <p>Blocking the exit of the newly synthesized peptide from the 50S ribosome</p> Signup and view all the answers

    How do macrolides function in a manner similar to aminoglycosides?

    <p>By targeting the bacterial ribosome and preventing protein production</p> Signup and view all the answers

    What is the location of the macrolide binding site on the bacterial ribosome?

    <p>The 50S subunit</p> Signup and view all the answers

    What is the result of methylation of the ribosome binding site in some bacteria?

    <p>Impaired accumulation of macrolides within the bacterium</p> Signup and view all the answers

    What is the effect of the mef gene on macrolide accumulation in some gram-positive bacteria?

    <p>It decreases macrolide accumulation</p> Signup and view all the answers

    What is a common mechanism of resistance to macrolides in some bacteria?

    <p>Inhibition of drug entry and accumulation</p> Signup and view all the answers

    What is the result of resistance to one member of the macrolide group?

    <p>Resistance to all members of the macrolide group</p> Signup and view all the answers

    What is the structural feature of macrolides that gives them their name?

    <p>A large cyclic core called a macrocyclic lactone ring</p> Signup and view all the answers

    What is the mechanism of action of efflux pumps in bacterial resistance to aminoglycosides?

    <p>Prevention of accumulation of the aminoglycoside in the cytosol of the bacterium</p> Signup and view all the answers

    Which of the following is a mechanism of bacterial resistance to aminoglycosides that involves changes to the ribosome?

    <p>Mutations within the ribosome</p> Signup and view all the answers

    What is the target of aminoglycoside binding in bacterial cells?

    <p>Ribosome</p> Signup and view all the answers

    Which of the following is NOT a mechanism of bacterial resistance to aminoglycosides?

    <p>Inhibition of protein synthesis</p> Signup and view all the answers

    What is the result of modification of the aminoglycoside in bacterial resistance?

    <p>Reduced binding of the aminoglycoside to the ribosome</p> Signup and view all the answers

    Which mechanism of bacterial resistance to aminoglycosides involves the pumping of the antibiotic out of the cell?

    <p>Efflux pumps</p> Signup and view all the answers

    What is the site of action of aminoglycosides in bacterial cells?

    <p>30S subunit</p> Signup and view all the answers

    Which of the following is a mechanism of bacterial resistance to aminoglycosides that does not involve changes to the antibiotic?

    <p>Mutations within the ribosome</p> Signup and view all the answers

    Study Notes

    Macrolides

    • Macrolides consist of a large cyclic core called a macrocyclic lactone ring, decorated with sugar residues.
    • Macrolides bind tightly to the 50S subunit of the bacterial ribosome, blocking the exit of the newly synthesized peptide.
    • They function similarly to aminoglycosides, targeting ribosomes and preventing protein production.

    Mechanisms of Resistance

    • Resistance to macrolides occurs by three mechanisms:
      • Inhibition of drug entry and accumulation due to difficulty penetrating the outer membrane of aerobic gram-negative bacilli and active efflux pumps in some resistant bacteria.
      • Enzyme-mediated ribosome binding site alteration, such as methylation, which prevents macrolide interaction.
      • Mutation of the ribosome binding site, which rarely occurs.

    Aminoglycosides

    • Aminoglycosides are active against various bacteria, including gram-positive and gram-negative bacteria, as well as mycobacteria.
    • Resistance to aminoglycosides occurs via three mechanisms:
      • Efflux pumps prevent accumulation of the aminoglycoside in the cytosol of the bacterium.
      • Modification of the aminoglycoside prevents binding to the ribosome.
      • Mutations within the ribosome prevent aminoglycoside binding.

    Antimicrobial Activity of Aminoglycosides

    • Aminoglycosides are effective against:
      • Gram-positive bacteria, including Staphylococci, Streptococci, Enterococci, and Listeria monocytogenes.
      • Gram-negative bacteria, including Haemophilus influenzae, Enterobacteriaceae, and Pseudomonas aeruginosa.
      • Mycobacteria, including Mycobacterium tuberculosis and Mycobacterium avium complex.

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    Description

    Learn about the structure and function of macrolides, a type of antibiotic that targets bacterial ribosomes and prevents protein production. Understand how they work and how resistance occurs.

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