Fluoroquinolones

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Anonymous
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45775
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Fluoroquinolones
Updated:
2010-10-28 20:00:11
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Fluoroquinolones
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Fluoroquinolones
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  1. Nalidixic Acid
    • Original quinolone
    • Narrow spectrum of activity
    • Historic interest only
  2. Drugs of Importance
    • Ciprofloxacin
    • Levofloxacin
    • Moxifloxacin
    • Gemifloxacin (Oral only)
  3. Mechanism of Action
    • Bactericidal agent
    • Targets enzymes important for DNA replication (DNA Gryase and Topoisomerase IV)
  4. Mechanisms of Resistance
    • Efflux Pumps
    • Cell membrane permeability (ex. Pseudomonas)
    • DNA mutations resulting in decreases affinity for DNA Gyrase and Topoisomerase IV
  5. Pharmacokinetics
    • Bioavailability: 80-90%
    • Distribution: Wide volume of distribution into most body sites.
  6. Spectrum of Activity
    • PEcK (with some exceptions)
    • Enterobacter
    • Variable S. Aureus
    • S. pneumoniae (with one exception)
    • S. pyogenes
    • Leginella
    • Atypical bacteria
  7. Ciprofloxacin
    • Metabolism: Partially metabolized in liver
    • Elimination: Parent and metabolites through urine
    • Doesn't cover S. aureus and S. pneumoniae
  8. Levofloxacin
    • Metabolism: No significant metabolism
    • Elimination: Through urine
  9. Moxifloxacin
    • Metabolism: Significant hepatic metabolism (more than ciprofloxacin) Can't be used in UTIs
    • Elimination: Parent (minor) and metabolites (major) through feces and urine.

    • Effective against B. fragilis
    • Not effective against Pseudomonas
  10. Gemifloxacin
    • Oral only
    • Metabolism: Very limited hepatic metabolism
    • Elimination: Parent (major) and metabolities (minor) through urine

    Not effective against Pseudomonas
  11. Therapeutic Uses
    • Respiratory Tract Infections: CAP, HAP/VAP/HCAP
    • GU Infections: Cystitis/pyelonephritis (not moxi.)
    • STDs
    • Bacterial Gastroenteritis
    • Osteomyelitis
    • SSTI (newer agents)
  12. Adverse Reactions
    • N/V/D and Abdominal discomfort
    • H/A, Dizziness, Insomnia, Alteration in mood (More so in the elderly)
    • Seizures (Rare)
    • Cardiac Toxicity - Boxed Warning
    • Tendon toxicity
    • Cartilage Malformation
    • Glycemic Abnormalities
    • Photosensitivity
    • Rash
    • Hepatic toxicity
  13. Drug Interactions
    • Antacids - reduce absorption
    • Sucralfate
    • Theophylline and Caffeine (inc conc. by cipro.)
    • Warfarin
    • Drugs known to prolong QT interval

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