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QUINOLONES

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QUINOLONES - PowerPoint PPT Presentation


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QUINOLONES. Classification. Quinolones (1 st generation) Highly protein bound Mostly used in UTIs Fluoroquinolones (2 nd , 3 rd and 4 th generation) Modified 1 st generation quinolones Not highly protein bound Wide distribution to urine and other tissues; limited CSF penetration.

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PowerPoint Slideshow about 'QUINOLONES' - lilah-alvarez


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classification
Classification
  • Quinolones (1st generation)
    • Highly protein bound
    • Mostly used in UTIs
  • Fluoroquinolones (2nd, 3rd and 4th generation)
    • Modified 1st generation quinolones
    • Not highly protein bound
    • Wide distribution to urine and other tissues; limited CSF penetration.
mechanism of action
Mechanism of Action
  • Dual MOA:
    • Inhibition of bacterial DNA Gyrase (Topoisomerase II)
      • Formation of quinolone-DNA-Gyrase complex
      • Induced cleavage of DNA
    • Inhibition of bacterial Topoisomerase IV
      • Mechanism poorly understood

Mechanism of DNA Gyrase

quinolones
[Conc] > serum:

Prostate tissue

Stool

Bile

Lung

Neutrophils

Macrophages

Kidneys

[Conc] < serum:

Prostatic tissue fluid

Bone

CSF

Quinolones
quinolones1
Quinolones
  • Drug interactions:
    • ↓ absorption: Al3+, Mg2+, and Ca2+ antacids
    • CYP450 inhibition potential drug interactions for ciprofloxacin
      • (Ex) can increase warfarin exposure (real changes in INR are rare, but monitor)
  • Adverse effects:
    • GI: Nausea, vomiting
    • CNS: HA, dizziness, confusion, insomnia, delerium, hallucinations, seizure (rare)
    • Cardiovascular: Torsades de pointes (rare)
    • Musculoskeletal: Rupture of tendon (rare)
    • Neurologic: Polyneuropathy (rare)