Metronidazole citrate ester as the new prodrug of metronidazole

Elżbieta Dąbrowska-Maś,Wojciech Raś

doi:10.5267/j.ccl.2017.6.002

Abstract

Metronidazole citrate ester as the new prodrug of metronidazole

Highlights

Metronidazole is a synthetic agent 1-(2-Hydroxyethyl)-2-methyl-5-nitroimidazole used against different protozoans and bacteria
This hypothesis is probably a result of many experiments, which have provided evidences that DNA is Metronidazole is classified by International Agency for Research on Cancer (IARC) into 2B class, i.e. possible human carcinogen, as it has shown mutagenic activity in vitro including positive Ames test, studies in vivo have failed to demonstrate a potential for genotoxicity[3,4]
This active substance has been used for the treatment of bacterial infections for above 45 years, but still metronidazole is successfully used for the treatment of vaginosis, trichomoniasis, amoebiasis, and giardiasis, and still it is the criterion standard for therapy of anaerobic bacterial infections[5], during last decades many new derivatives of metronidazole were investigated with antibacterial, antifungal and H. pylori urease inhibitory activity

Summary

Introduction

Metronidazole is a synthetic agent 1-(2-Hydroxyethyl)-2-methyl-5-nitroimidazole (see Fig. 1) used against different protozoans and bacteria. The mechanism of the cytotoxic action of metronidazole on anaerobic microorganisms is not well understood, but it is anticipated that derivatives arising from the reduction of the nitro group, especially the nitro anion radical R-ṄO2 ̄, are the most likely candidates for DNA damage in bacteria[1] This hypothesis is probably a result of many experiments, which have provided evidences that DNA is Metronidazole is classified by International Agency for Research on Cancer (IARC) into 2B class, i.e. possible human carcinogen, as it has shown mutagenic activity in vitro including positive Ames test, studies in vivo have failed to demonstrate a potential for genotoxicity[3,4]. Metronidazole for injection available for treatment is a buffered solution at the concentration of 5 mg/mL and the recommendation for treatment is 500 mg of metronidazole in 100 mL to be infused over 20 to 60 minutes

Objectives

Results

Conclusion