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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