Metronidazone



Metronidazole:
A prototype nitroimidazole. Tissue amoebicide
Broad spectrum cidal activity
Mechanism of action:
                 Diffusion into cell of amoeba
 
 Nitro group reduced into highly reactive nitro radical by redox     potential of anaerobes                                                              
 
           Causes cytotoxicity by damaging DNA
Nitro radical acts as electron sink which competes with the biological electron acceptor of anaerobic organism for the electrons generated by pyruvate oxidation
         Disruption of energy metabolism of anaerobes
  Uses and dosage regimens:
1. Amoebiasis:
Ø  mild intestinal disease: 400mg TDS for 5-7 days
Ø Invasive dysentery and liver abscess: 800mg TDS for 7-10 days
2. Giardiasis:
Ø 400mg TDS for 7 days
3. Trichomonas vaginitis:
Ø 400mg TDS for 7 days
4. Anaerobic bacterial infection:
Ø For serious cases, iv 15mg/kg infused over 1 hour followed by 7.5mg/kg every 6 hours till oral therapy can be substituted with 400-800mg TDS
5. Pseudomembranous enterocolitis:
Ø 400mg TDS for 10 days
6. Ulcerative gingivitis, trench mouth:
Ø 200-400mg TDS (15-30mg/kg/day) for 5 days
7. Helicobacter pylori gastritis/peptic ulcer:
Ø Metronidazole 400mg TDS along with amoxicillin/clarithromycin and a proton pump inhibitor in triple drug 2 week regimen
8.Guinea worm infestation:
Ø 200-400mg TDS for 7 days
  Summary:
Metronidazole:
      Acts by disrupting energy metabolism of anaerobes
      An important drug in the triple drug regimen against H. pylori associated gastritis as well as in amoebiasis, giardiasis, anaerobic bacterial infections etc.
  References:
  Essentials of Medical Pharmacology, K D Tripathi, 6th Edition
  Basic and Clinical Pharmacology, Bertram G. Katzung, 11th Edition
  Davidson’s Practice and Principles of Medicine,21st Edition
  Clinical Pharmacy and Therapeutics, Walker and Rogers,4th Edition

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