Quinolones and Fluoroquinolones
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Questions and Answers

Which of the following bacteria are resistant to ciprofloxacin?

  • E. coli, Klebsiella, and Salmonella
  • Bacteroides fragilis, Clostridium difficile, and most anaerobes (correct)
  • Staphylococcus aureus, Pseudomonas aeruginosa, and Mycobacterium tuberculosis
  • Vibrio cholerae and Campylobacter jejuni
  • Which of the following routes of administration is NOT mentioned for ciprofloxacin?

  • Topical
  • Intramuscular (correct)
  • Oral
  • Intravenous
  • Which of the following adverse effects of ciprofloxacin is NOT mentioned in the text?

  • Headache, dizziness, insomnia, and confusion
  • Muscle weakness and fatigue (correct)
  • Nausea, vomiting, and abdominal discomfort
  • Skin rashes, urticaria, and eosinophilia
  • Which newer fluoroquinolone has greater activity against streptococci and some activity against anaerobes?

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

    Which of the following is NOT mentioned as a bacterium susceptible to ciprofloxacin?

    <p>Acinetobacter baumannii</p> Signup and view all the answers

    Which of the following drug interactions with ciprofloxacin is NOT mentioned in the text?

    <p>Increased plasma concentration of theophylline</p> Signup and view all the answers

    What is the mechanism of action of nalidixic acid?

    <p>Inhibition of DNA gyrase enzyme in gram-negative bacteria</p> Signup and view all the answers

    Which bacteria is nalidixic acid NOT effective against?

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

    What is the main adverse effect associated with fluoroquinolones?

    <p>Central nervous system (CNS) effects</p> Signup and view all the answers

    What is the mechanism of action of fluoroquinolones?

    <p>Inhibition of DNA gyrase enzyme in gram-negative bacteria</p> Signup and view all the answers

    Which of the following is a second-generation fluoroquinolone?

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

    What is the antibacterial spectrum of ciprofloxacin?

    <p>Highly effective against aerobic gram-negative organisms</p> Signup and view all the answers

    Study Notes

    Quinolones and Fluoroquinolones

    • The first quinolone, nalidixic acid, is a urinary antiseptic effective against gram-negative bacteria including E. coli, Proteus, Klebsiella, Enterobacter, Salmonella, and Shigella, but not Pseudomonas.
    • Nalidixic acid inhibits DNA gyrase enzyme and interferes with the replication of bacterial DNA.
    • It is useful in the treatment of uncomplicated UTI due to gram-negative bacteria and diarrhea due to Shigella or Salmonella.

    Mechanism of Action

    • Fluoroquinolones (FQs) inhibit bacterial DNA synthesis (bactericidal) by inhibiting DNA gyrase in gram-negative bacteria and topoisomerase IV in gram-positive bacteria.

    Antibacterial Spectrum

    • Ciprofloxacin is the prototype drug and is highly effective against aerobic gram-negative organisms:
    • E. coli
    • Coli
    • Enterobacter
    • Proteus
    • Klebsiella
    • Salmonella
    • Shigella
    • H. ducreyi
    • H. influenzae
    • N. gonorrhoeae
    • N. meningitidis
    • V. cholerae
    • Campylobacter jejuni
    • Ciprofloxacin also has activity against S. aureus, Pseudomonas aeruginosa, and M. tuberculosis.

    Pharmacokinetics

    • Ciprofloxacin is administered by oral, i.v., or topical routes.
    • It is well absorbed from the gut, but food delays its absorption.
    • It is widely distributed in the body and reaches high concentration in kidney, lung, prostatic tissue, bile, macrophages, etc.
    • It is excreted mainly in urine.

    Adverse Effects

    • Common adverse effects are related to the Gl tract (nausea, vomiting, abdominal discomfort), CNS (headache, dizziness, insomnia, confusion, hallucinations, convulsions), and skin (rashes, urticaria, itching, eosinophilia, photosensitivity).
    • Tenosynovitis and tendon rupture can occur, especially in athletes.
    • Moxifloxacin can cause prolongation of QT interval.

    Contraindications and Precautions

    • FQs are contraindicated in pregnancy.
    • FQs should be avoided in young children due to the risk of cartilage damage.

    Drug Interactions

    • Ciprofloxacin increases the plasma concentration of theophylline, warfarin, etc., by inhibiting their metabolism.
    • Nonsteroidal anti-inflammatory drugs (NSAIDs) may potentiate CNS side effects of FQs (confusion, irritability, and rarely convulsions).
    • Absorption of FQs is reduced by antacids, ferrous salts, and sucralfate.

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    Description

    Test your knowledge about the first quinolone, nalidixic acid, its mechanism of action, and its effectiveness against various gram-negative bacteria including E.coli, Proteus, and Klebsiella.

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