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parenteral administration, fluoroquinolones are widely distributed Models to explain the activity of quinolones at the target site
only exist for DNA gyrase: During the supercoiling process,
in most extracellular and intracellular fluids and are concentrated
both DNA strands are cleaved by DNA gyrase at 4 base pair
in the prostate, lungs, and bile. staggered sites, forming a "quinolone binding pocket".
Most fluoroquinolones are metabolized in the liver and excreted
Two quinolone molecules self-assemble inside the pocket in
in urine, reaching high levels in urine. Moxifloxacin is eliminated dimer structure and attach to the gyrase-DNA complex
primarily in bile. electrostatically, which stabilizes the intermediate stage of
Fluoroquinolones have traditionally been considered to be this reaction step.
contraindicated in children because they may cause cartilage
lesions if growth plates are open. However, some experts, who Permanent gaps in the DNA strands induce synthesis of
challenge this view because evidence is weak, have recommended repair enzymes (exonucleases), initiating uncoordinated
prescribing fluoroquinolones as a 2nd-line antibiotic and repair processes, which results in irreversible damage to the
restricting use to a few specific situations, including P. DNA and, finally, cell death.
aeruginosa infections in patients with cystic fibrosis, prophylaxis
and treatment of bacterial infections in immunocompromised
patients, life-threatening multiresistant bacterial infections in
neonates and infants, and Salmonella or Shigella GI tract
infections.