Thursday, 26 February 2015

Fluoroquinolones

MECHANISM:
              Fluroquinolones inhibit DNA GYRASE and TOPOISOMERASE-4. 
Thus inhibiting replication of DNA .

CLASSIFICATION:

1st generation - Norfloxacin, Lomefloxacin
                        ( active against few gram -ve organism )

2nd generation - Ciprofloxacin , Ofloxacin
                        ( active against all gram +ve organism )

3rd generation - Sparfloxacin, Levofloxacin , Gatifloxacin 
               ( active against all gram -ve organism and few gram +ve)
4th generation - Moxifloxacin , Trovafloxacin
                (active against all gram -ve and gram +ve )

Pharmacokinetics :

  1. All drugs can be given orally and parenterally . 
  2. Metabolized by liver
  3. Moxifloxacin and Trovafloxacin excreted in feces 
  4. Others are excreted via urine
Uses:
  1. Norfloxacin is excreted in urine in large quantities , hence used in UTI
  2. Ciprofloxacin and Ofloxacin used in gonorrhoea , pseudomonas , anthrax , meningococcal meningitis , TB 
  3. Levofloxacin , Gatifloxacin , Sparfloxacin are active against all gram -ve , few gram +ve and atypical microoraganisms . Hence used in respiratory infections
  4. Moxifloxacin amd Trovafloxacin are the broadest spectrum antibiotic.
ADVERSE EFFECTS:
  1. GI distress
  2. Affect cartilages and hence not used in children below 18 yrs 
  3. They cause tendinitis 
  4. Photosenstivity
  5. Seizures
  6. Moxifloxacin and Trovafloxacin causes hepatotoxicity.

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