DNA Gyrase and Topoisomerase IV
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Questions and Answers

What is Nalidixic Acid considered as?

  • A 4th generation quinolone
  • A 3rd generation quinolone
  • A 1st generation quinolone (correct)
  • A 2nd generation quinolone
  • What is the main difference between the new fluoroquinolones and ciprofloxacin?

  • They have improved pharmacokinetics
  • They are more active against G+ve organisms (correct)
  • They are less active against G+ve organisms
  • They have a broader spectrum of antimicrobial activity
  • Why were modifications made to Nalidixic Acid?

  • To increase the incidence of Clostridium difficile infection
  • To decrease the spectrum of antimicrobial activity
  • To reduce the cost of production
  • To expand the spectrum, improve pharmacokinetics, and increase stability against common mechanisms of resistance (correct)
  • What is a common issue associated with the use of fluoroquinolones?

    <p>The development of antimicrobial resistance in many organisms</p> Signup and view all the answers

    What is the mechanism of action of fluoroquinolones?

    <p>Blockage of bacterial DNA replication</p> Signup and view all the answers

    Which enzyme is inhibited by fluoroquinolones in Gram-positive bacteria?

    <p>Topoisomerase IV</p> Signup and view all the answers

    What is the target of fluoroquinolones in Gram-negative bacteria?

    <p>Topoisomerase II (DNA gyrase)</p> Signup and view all the answers

    Which of the following is a type of fluoroquinolone?

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

    What distinguishes 2nd generation Fluoroquinolones from other generations?

    <p>Activity against aerobic gram-negative and atypical bacteria</p> Signup and view all the answers

    What is unique about the 3rd and 4th generation Fluoroquinolones?

    <p>They are newer generations with improved efficacy</p> Signup and view all the answers

    What is the primary target of Fluoroquinolones in bacterial cells?

    <p>Topoisomerase IV</p> Signup and view all the answers

    Which of the following is a characteristic of Ciprofloxacin?

    <p>It is effective against Enterobacteriaceae and E. coli</p> Signup and view all the answers

    What sets Eukaryotic cells apart from bacterial cells in terms of DNA management?

    <p>Eukaryotic cells have a different type of topoisomerase</p> Signup and view all the answers

    What is the primary difference between Nalidixic acid and Norfloxacin?

    <p>Nalidixic acid is a 1st generation Fluoroquinolone, while Norfloxacin is a 2nd generation</p> Signup and view all the answers

    Why are Fluoroquinolones ineffective against eukaryotic cells?

    <p>They are inhibited by eukaryotic topoisomerase</p> Signup and view all the answers

    What is unique about the antibacterial spectrum of 2nd generation Fluoroquinolones?

    <p>They are effective against aerobic gram-negative and atypical bacteria</p> Signup and view all the answers

    Which generation of fluoroquinolones has poor activity against Pseudomonas aeruginosa?

    <p>4th generation</p> Signup and view all the answers

    Which fluoroquinolone has excellent activity against Streptococcus pneumoniae respiratory infections?

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

    Which fluoroquinolone is used as an alternative to more toxic drugs such as aminoglycosides?

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

    Which of the following is a characteristic of 2nd generation fluoroquinolones?

    <p>Used in treating tuberculosis</p> Signup and view all the answers

    Which fluoroquinolone has 100% bioavailability and is dosed once daily?

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

    Which generation of fluoroquinolones has improved activity against atypical organisms and gram-positive bacteria?

    <p>3rd generation</p> Signup and view all the answers

    Which fluoroquinolone is used in the treatment of prostatitis due to E-coli?

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

    Which of the following is a characteristic of 4th generation fluoroquinolones?

    <p>Activity against gram-positive organisms</p> Signup and view all the answers

    Study Notes

    Fluoroquinolones

    • Fluoroquinolones are derivatives of nalidixic acid, with broad antimicrobial activity, effective for treating various infectious diseases.
    • Nalidixic acid is considered a 1st generation quinolone.

    Mechanism of Action

    • Fluoroquinolones block bacterial DNA replication by inhibiting DNA gyrase in Gram (-ve) bacteria and topoisomerase IV in Gram (+ve) bacteria.

    Generations of Fluoroquinolones

    • 1st generation: Nalidixic acid
    • 2nd generation: Norfloxacin, Ciprofloxacin
    • 3rd generation: Levofloxacin
    • 4th generation: Moxifloxacin, Gemifloxacin

    Antibacterial Spectrum of 2nd Generation Fluoroquinolones

    • Norfloxacin and Ciprofloxacin have activity against:
      • Aerobic Gram (-ve) bacteria (Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria spp.)
      • Atypical bacteria (Chlamydia, Mycoplasma)
    • Ciprofloxacin is particularly useful in treating:
      • Infections caused by Enterobacteriaceae, Gram (-ve) bacilli, and E-coli
      • Typhoid fever caused by Salmonella typhi
      • Pseudomonal infections associated with cystic fibrosis
      • Traveler's diarrhea and urinary tract infections

    Antibacterial Spectrum of 3rd Generation Fluoroquinolones

    • Levofloxacin has:
      • Expanded activity against Gram (-ve) bacteria
      • Improved activity against atypical organisms and Gram (+ve) bacteria
      • Excellent activity against S. pneumoniae respiratory infections
      • 100% bioavailability and is dosed once daily
      • Used in treating:
        • Skin infections
        • Acute sinusitis
        • Acute exacerbation of chronic bronchitis
        • Nosocomial pneumonia
        • Prostatitis due to E-coli and sexually transmitted diseases (except syphilis)

    Antibacterial Spectrum of 4th Generation Fluoroquinolones

    • Moxifloxacin has:
      • Enhanced activity against Gram (+ve) organisms (e.g., S. pneumoniae)
      • Excellent activity against many anaerobes, although resistance to Bacteroides fragilis has been reported
      • Poor activity against P. aeruginosa

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    Learn about the role of DNA gyrase and topoisomerase IV in DNA replication and cell division. Understand how they prevent the relaxation of supercoiled DNA and facilitate the separation of replicated chromosomal DNA.

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