Abstract

This study was conducted to evaluate some biochemical parameters of levofloxacin in male rats. It was carried out on fifty four of the albino male rats, they were divided into three main groups equally and orally dosed levofloxacin and assigned as, the first group was dosed with the therapeutic dose 7.5mg/kg/bw, the second group was dosed with the double therapeutic dose 15mg/kg/bw, the third group was dosed with distilled water (negative control). The three groups were divided into three subgroups equally according to dosing period of 2 weeks, 4 weeks, 1 week after discontinuation of dosing. The results showed, there were significant P<0.05 increases in creatine kinase myocardial band of group 1 after 4 weeks of treatment and 1 week of levofloxacin withdrawal in comparison with control group, also there were significant P<0.05 increases in troponin-t of group 2 after 1 week of levofloxacin withdrawal in comparison with control group. While aspartate aminotransferase, total plasma protein, and creatinine levels showed significant P<0.05 increases and significant P<0.05 decreases in total plasma bilirubin level, but within normal limits, between experimental groups and control group. Whereas, there were no significant P>0.05 changes in blood urea nitrogen levels between the experimental groups. We concluded that levofloxacin revealed minor toxic effects on organs tissue and most of these effects were reversible.

Highlights

  • The main mechanism of action of levofloxacin and other fluoroquinolones antibacterials are the inhibition of DNA gyrase, which is an enzyme required for DNA replication, transcription, repair and recombination [3]

  • Repeated administration of levofloxacin have been shown to cause arthropathy, Synovitis and articular cartilage lesions in immature dogs and juvenile rats [4] phototoxicity, central nervous system (CNS) stimulatory effects in mice and crystalluria has been observed in some intravenous rat studies [5]

  • 54 healthy adult male rats were obtained from the National Center for Drug Control and Research (NCDCR) / Ministry of Health

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Summary

Introduction

The main fluoroquinlones active substances are cinoxacin, ciprofloxacin, enoxacin, flumequin levofloxacin, lomefloxacin, moxifloxacin, nalidixic acid, norfloxacin, ofloxacin, pefloxacin, pipemidic acid, prulifloxacin, and rufloxacin which are widely prescribed and are important for treating serious, life threatening bacterial infections for their specificity as broad spectrum antibiotics[1,2].The main mechanism of action of levofloxacin and other fluoroquinolones antibacterials are the inhibition of DNA gyrase, which is an enzyme required for DNA replication, transcription, repair and recombination [3].Levofloxacin is well distributed toward target body tissues, so it uses mainly in treatment of urinary tract infection and community-acquired pneumonia, including multidrug resistant strains of several bacteria [4].Repeated administration of levofloxacin have been shown to cause arthropathy, Synovitis and articular cartilage lesions in immature dogs and juvenile rats [4] phototoxicity, central nervous system (CNS) stimulatory effects in mice and crystalluria has been observed in some intravenous rat studies [5].Plasma alanine aminotransferase (ALT), aspartate aminotransferase When body tissue or an organ such as the heart or liver is diseased or damaged, additional AST and ALT are released into the bloodstream. Increase in plasma ALT and AST has been reported in conditions involving necrosis of hepatocytes [7]. These enzymes, AST, alkaline phosphatase (ALP), and ALT, are diagnostic enzymes, and their release above normal physiological levels indicates a disease condition including various bone disorders and jaundice (ALP); viral hepatitis (ALT); and myocardial infarction (AST). The elevation in the activity of these enzymes by levofloxacin may be as a result of their release in response to tissue damage during routine normal destruction of erythrocytes, leukocytes, and other cells like liver cells [8]

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