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Fluoroquinolones

  1. Generation-1
    1. Cinnoxacin
    2. Enoxacin
    3. Nalidixic (Oldest)
  2. Generation-II
    1. Ciprofloxacin
    2. Norfloxacin
    3. Pefloxacin
    4. Lomefloxacin
  3. Generation -III
    1. Levofloxacin
    2. Gatifloxacin
    3. Sparfloxacin
    4. Trovafloxacin
  4. Generation -IV
     
    a. Gemifloxacin

MOA

Inhibit DNA gyrase (Topoisomerase-II)

  1. Also inhibit Topoisomerase-IV
  2. Normal function of TI is to introduce negative supercoils, & unwind DNA
  3. Step needed for DNA repair

MOR

  1. Mutation in DNA gyrase

P/K

  1. 100% oral absorption
  2. Food does not interfere
  3. Moxifloxacin (Gen-II), trofloxaxin, sparfloxacin (partly); eliminated by bile

Uses

  1. Nalidixic acid
    1. Diarrhea & UTI
    2. Active against aerobic gram negative bacteria only
    3. Should not be combined with nitrofurantoin
  2. Nitrofurantoin
    1. Bacteristatic
    2. Damages DNA
    3. Food increases absorption
    4. Prolonged use-neuropathy, interstitial pneumonitis
    5. Used in prophylaxis of UTI
    6. Discontinued just before delivery; otherwise safe in pregnancy
    7. Contraindicated in real failure 
  3. Ciprofloxacin
    1. Typhoid fever
    2. Shiegella
    3. Staphylococcal (MRSA also)
    4. Pseudomonas
    5. Anthrax
    6. Prophylaxis of meningococcal meningitis (health care workers)
       
      i. Nosopharyngeal eradication is done with rifampinn+minocycline
  4. Gen-III, IV
     
    a. Respiratory infections (Chest)

S/E

  1. MC-GI upset
  2. Can damage cartilages, ligaments, tendons
     
    a. C/I
    1. Pregnancy
    2. Children
    3. Lactation
  3. Ciprofloxacin (IV)
    1. Hypotension
    2. Seizures
  4. Photosensitivity
    1. Pefloxacin (Max)
    2. Sparfloxacin
    3. Levofloxacin
  5. Trovafloxacin
     
    a. Hepatic failure
  6. Gatifloxacin
     
    a. Dysglycemia
  7. Sparfloxacin
     
    a. QT interval prolongation
Extra edge
  1. Fluroqinolones have enzyme inhibiting properties:
  2. Ciprofloxacin is most potent enzyme inhibitor: given with theophylline can lead to increased risk of tremors.
  3. Ciprofloxacin along with older antihistaminics such as terfenadine or astemazole can cause torsa de depointes.





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