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PubMed1993

Contribution to the pathobiochemistry of furazolidone-induced oxidative toxicity in chickens.

Furazolidone (F) and its 5-nitrofuran derivatives, occasionally used in veterinary and human medicine, are active against some microorganisms. This drug is considered to be mutagenic in special bacterial test systems. For public health reasons, the presence of F and other 5-nitrofuran residues in edible mammalian and poultry tissues is strictly prohibited. One-month-old experimental chickens (n = 2 x 25) were fed 300 mg.kg-1 furazolidone for 3 days. A separate subgroup (n = 11) was used for monitoring the kinetics of F in the blood plasma. Liver, lung and blood plasma samples taken from the experimental and control chickens after treatment were tested for glutathione-peroxidase (GSH-Px), glutathione reductase (GSH-R), catalase (CAT), superoxide dismutase (SOD) activities, reduced and oxidized glutathione (GSH and GSSG), malondialdehyde (MDA), alpha-tocopherol (vE), selenium (Se) and F concentrations. On post-treatment day 2, SOD activity was significantly lowered in the liver only. GSH-Px did not show any characteristic change in any of the tissues. CAT and GSH-R activities were significantly reduced in both organs until post-treatment day 5. At the same time, a significant decrease of GSH accompanied by an increase in GSSG concentration, was found in both tissues. Oral F treatment produced a transient increase in lipid peroxidation levels measured by the formation of MDA. Alpha-tocopherol content significantly decreased in both organs by post-treatment day 2. Se concentrations showed an insignificant rate of decrease. F concentration in the blood plasma reached its peak already 30 min after treatment. In the liver and lungs, F decreased sharply, reaching the detection limit between days 2-5 after treatment. Furazolidone administered per os was found to alter the in vivo antioxidative enzymatic defense mechanisms. Increased lipid peroxidation and the concomitant oxidative stress may affect the functional integrity of the tissues.

Animals↗
PubMed1996

[Furazolidone resistance of E. coli from chicken intestines after prophylactic treatment with bioptivet GB in animal feed].

This study describes the influence of bioptivet GB on minimum inhibitory concentrations (MIC) for furazolidone of the intestinal E. coli flora of young broiler chickens after prophylactic treatment. From day 6 until day 15 one group of 50 birds received a diet containing 326 ppm furazolidone, another group of 75 birds served as non medicated control. Investigated E. coli had been isolated from cloacal swabs and from caecal contents. MIC of 1581 E. coli strains were determined by agar dilution test. MIC of furazolidone for the investigated strains ranged from 2 micrograms/ml to 64 micrograms/ml. For classification as "resistant" or "susceptible" limits of 16 micrograms/ml and 8 micrograms/ml respectively were used. Strains obtained from undosed birds mainly had MIC values of 4 micrograms/ml or 8 micrograms/ml, i.e. two or three times higher than MIC of E. coli ATCC 25 922, MIC values of 16 micrograms/ml or more were recorded only among isolates obtained from chickens which had received the drug. Administration of bioptivet GB resulted in a statistically significant increase in the average MIC. Statistically higher average MIC were recorded among isolates from cloacal swabs only during application of the drug. For strains from caecal contents, the effect became obvious only at the end of the experiment.

Animal Feed↗
PubMed1981

Rapid distinction between micrococci and staphylococci with furazolidone agars.

Furazolidone agar proved to be a suitable medium for separating strains of the genera Micrococcus and Staphylococcus. 720 isolates (including 24 type strains) of gram- and catalase-positive cocci were tested for growth on tryptone soya and peptone agar with the addition of 50 microgram/ml furazolidone. The results were compared with the classification obtained by the standard-O/F-test and by the test system of Schleifer and Kloos. For routine identification and separation of staphylococci from micrococci a peptone agar with 20 microgram furazolidone/ml is recommended.

Bacteriological Techniques↗
PubMed1984

Metabolism in vivo of furazolidone: evidence for formation of an open-chain carboxylic acid and alpha-ketoglutaric acid from the nitrofuran in rats.

The in vivo metabolism of an antibacterial nitrofuran, furazolidone [N-(5-nitro-2-furfurylidene)-3-amino-2-oxazolidone] was investigated. When the nitrofuran was administered orally to rats, two new-type nitrofuran metabolites, N-(4-carboxy-2-oxobutylideneamino)-2-oxazolidone and alpha-ketoglutaric acid, were isolated from the urine, together with 3-(4-cyano-2-oxobutylideneamino)-2-oxazolidone and N-(5-acetamido-2-furfurylidene)-3-amino-2-oxazolidone. In addition, the present study showed that the corresponding aminofuran was an intermediate in the conversion of furazolidone to these metabolites.

Administration, Oral↗
PubMed1986

Quantitative morphological alterations during the development of furazolidone-induced cardiomyopathy in turkeys.

Cardiac structures were measured to determine the sequence of alterations during the development of spontaneous and furazolidone-induced cardiomyopathy in turkey poults 20 to 31 days after hatching. Samples of tissue from the free walls of the ventricles were removed and processed for electron microscopy. Volumetric density of cardiac structures was determined by the point-counting technique. The results indicate that the sequence of myocardial alterations is similar in both spontaneous and furazolidone-induced cardiomyopathy, but that these changes are more pronounced in the latter condition. Major changes include an early diminution in myofibrillar density, accompanied by a small reduction in mitochondrial density. This is followed by dilatation of the ventricular lumina and a decrease in the volume fraction of Z-bands. The increase in mass of the free walls of the ventricles in affected poults is due primarily to an increase in extracellular components and sarcoplasm devoid of organelles. The results suggest that the development of this myopathy is initiated by damage to the myofibrils of the cardiocytes.

Age Factors↗
PubMed1995

Inter-strand cross-linking of Vibrio cholerae DNA induced by furazolidone: a quantitative assay by four simple methods.

Four simple methods, i.e., (i) UV absorption spectrophotometry, (ii) hydroxyapatite chromatography, (iii) fluorescence analysis of ethidium bromide bound to DNA and (iv) assay of S1 endonuclease action, were used in parallel for the estimation of furazolidone-induced inter-strand cross-links in Vibrio cholerae DNA. The data produced by the four methods were in reasonable agreement with each other and provided similar linear dose-response relations, the correlation (between dose and response) coefficient being in any case numerically greater than 0.98. When the data obtained by four independent methods were plotted in a single graph, the resulting dose-response relation could be described by the equation log NR = 1.41 - 0.54 log D, where NR is the % non-reversible DNA remaining in the cells treated by furazolidone at dose D micrograms/ml x h. The correlation coefficient in this plot was -0.98 and significant to a level better than 0.1%. This study thus brings out that any one of these four methods can be used with reasonable confidence for the diagnosis and assay of inter-strand cross-links in DNA.

Chromatography, Liquid↗
PubMed1989

Furazolidone-induced interstrand cross-links in Vibrio cholerae DNA. Study of conformational change by circular dichroism.

Vibrio cholerae DNA bearing furazolidone-induced interstand cross-links show a change in the characteristic circular dichroism spectra of the DNA itself in dilute buffer. The change in c.d. spectra was characterized by a shift of the positive band around 272 nm to lower wavelength and a loss of ellipticity of the negative band around 242 nm, and is similar to that exhibited by mitomycin linked Vibrio cholerae DNA under identical conditions and is suggestive of a conformational change of DNA bearing such cross-links. Both furazolidone-induced and mitomycin-induced cross-linking of Vibrio cholerae DNA inhibited the salt-induced conformation change, i.e. increase in winding angle of DNA, the percentage inhibition being greater for mitomycin-linked DNA.

Buffers↗
PubMed1982

A study on the urinary and fecal excretion of furazolidone in rats by means of mutagenicity assays.

The urinary and fecal excretion of furazolidone in rats was studied by means of mutagenicity assays: when animals received a single dose by gavage (1 to 10 mg/100 g body wt) the mutagenic activity recovered in urines accounted for less than 0.1% of the administered dose and quickly disappeared. After prolonged (1 week) treatments, however, some mutagenicity was retained in urine concentrates until the fifth to seventh days. Similarly the fecal excretion of mutagenicity accounted for less than 0.1% of the administered dose and disappeared within the third day. The efficient deactivation of furazolidone observed in vivo was shown to be unaffected by the amount of gut bacteria in treated animals; in in vitro experiments it turned out to be actively performed by a rat intestine homogenate fraction, working more efficiently under hypoxic conditions.

Animals↗
PubMed1982

Role of taurine in furazolidone-induced cardiomyopathy.

1. Taurine levels were determined in the heart, and red and white muscle of turkey poults fed furazolidone (FZ) at a dose of 700 ppm from 2 to 5 weeks of age and/or 0.1 M taurine from 1 to 5 weeks of age. 2. In FZ-fed poults, taurine levels in the myocardium decreased significantly (P less than 0.001), but not in brain or muscle indicating a specific effect of FZ on the heart. 3. Exogenous administration of taurine significantly (P less than 0.001) increased taurine content of brain and muscle in all poults. 4. Myocardial taurine levels were significantly elevated (P less than 0.01) in poults fed a normal ration, but not in those fed FZ. 5. Although taurine treatment restored myocardial taurine to normal levels in the FZ-fed poults, the treatment did not decrease the incidence of FZ-induced cardioyopathy. 6. Since taurine is a membrane stabilizer and protects against calcium overload, our data suggests that sarcolemmal damage leading to tissue calcium overload is not the mechanism of the furazolidone-mediated syndrome.

Animals↗
PubMed1990

Myocardial biochemical changes in furazolidone-induced cardiomyopathy of turkeys.

This study tested the hypothesis that membrane transport is the major biochemical system of the myocardium altered in furazolidone-induced cardiomyopathy (round heart disease), before the development of myocardial failure, and that metabolic enzymes and contractile proteins are less affected. Compared with controls, maximal percentage depression of activities of myocardium from furazolidone-treated birds were 40 for creatine kinase, 30 for glycolysis, 30 for glycogen, 20 for myofibrils, 20 for Krebs's cycle enzymes, 15 for fatty acid oxidation and 10 for total soluble protein. Sodium and potassium transport, antioxidant system activity, myosin, myosin isoenzyme patterns and amino acid aminotransferases were unaffected. In marked contrast, the calcium-transport ATPase activity of the sarcoplasmic reticulum had undergone a 60 per cent compensatory increase in activity. The pattern of biochemical changes observed is consistent with a role of ischaemia in the pathogenesis of round heart disease and indicates that calcium transport by the sarcoplasmic reticulum is the major biochemical system affected.

Animals↗
PubMed1988

Reversible interaction of a reactive intermediate derived from furazolidone with glutathione and protein.

Swine liver microsomes convert the nitrofuran furazolidone into N-(4-cyano-2-oxo-3-butenylidene)-3-amino-2-oxazolidone, a reactive open-chain acrylonitrile derivative. This derivative may be trapped with such thiol-group-containing agents as glutathione and mercaptoethanol. However, this reaction is reversible; e.g., adding an excess of mercaptoethanol to an aqueous solution (pH 7.4) of the glutathione conjugate results in conversion of 43% of this compound into the mercaptoethanol conjugate. In addition, when microsomal protein is added to the glutathione conjugate or the mercaptoethanol conjugate, 36 and 44%, respectively, become covalently bound to the protein. The amount of this covalently bound radioactivity decreases again on prolonged incubation at 37 degrees C (42% disappearance within 24 hr), suggesting that the acrylonitrile derivative also reacts reversibly with thiol groups of microsomal protein. Indeed an excess of mercaptoethanol could remove covalently bound radioactivity from microsomal protein resulting in the formation of the mercaptoethanol conjugate. The reversibility of the reaction is dependent on pH, as is demonstrated for the mercaptoethanol conjugate. Below pH 2 this conjugate is stable; optimal exchange to microsomal protein is found between pH 7 and 10. At very high pH (greater than 11) no binding to protein is found, although the conjugate disappears rapidly. The mercaptoethanol conjugate exhibits mutagenic activity in the Salmonella/microsome test indicating that the acrylonitrile derivative of furazolidone also interacts with DNA.

Animals↗
PubMed1997

Determination of the furazolidone metabolite, 3-amino-2-oxazolidinone, in porcine tissues using liquid chromatography-thermospray mass spectrometry and the occurrence of residues in pigs produced in Northern Ireland.

A method is presented for the detection of the furazolidone metabolite, 3-amino-2-oxazolidinone (AOZ), in porcine tissue. Bound and extractable residues are detected following methanol-water homogenisation, repeated solvent washing and derivatisation with 2-nitrobenzaldehyde. Samples are analysed by using thermospray mass spectrometry-liquid chromatography, monitoring the positive ion m/z 253 with filament-assisted ionisation. There is no interference from tissue matrices or excess 2-nitrobenzaldehyde reagent. The limit of determination for liver and muscle is 10 ng/g. Recoveries are greater than 80%. The assay was used to investigate the occurrence of furazolidone residues in pigs from Northern Ireland. One hundred samples were analysed. Seventeen of these contained bound AOZ residues. The stability of tissue samples post mortem was investigated in order to achieve optimum storage conditions for samples. When liver was stored at 4 degrees C, the concentration of bound AOZ decreased by 22% within 48 h. However, there were no significant changes in AOZ concentrations in liver that was stored at -20 degrees C for six months.

Animals↗
PubMed2004

Serum profiles of luteinizing hormone, oestradiol and cholesterol and ovarian functions in layer poultry birds (Gallus domesticus) fed diets containing furazolidone.

This study was carried out to assess the serum profiles of luteinizing hormone (LH), oestradiol, cholesterol and ovarian functions in layer poultry birds (Rhode Island Red: Gallus domesticus) fed a diet containing various concentrations of furazolidone (FZ). A total of 40 birds were randomly assigned to receive FZ 0, 200, 400 or 800 mg/kg feed (ppm) daily during the pre-laying age, i.e. 13-18 weeks (for 5 weeks). Blood samples were collected at weekly intervals. Concentrations of LH and oestradiol in serum were estimated at alternate weeks using radioimmunoassays. Serum cholesterol levels were analysed by an enzymatic calorimetric method. Furazolidone administration was terminated at the 18th week of age. The birds were sacrificed at 22nd week of age and ovarian tissues were processed for morphometric studies. Serum LH, oestradiol and cholesterol levels were affected by age (p < 0.001) and FZ dose (p < 0.001). Serum LH and oestradiol levels were lower (p < 0.05) in birds receiving FZ 800 mg/kg feed daily compared with the controls, whereas serum cholesterol profiles were lower (p < 0.05) in all FZ-administered groups than in the control group. The mean weight of ovaries having no yolky follicles observed in the group receiving FZ 400 or 800 mg/kg feed per day was reduced (p < 0.05) compared with the control group. Dosing FZ at 800 mg/kg feed per day reduced (p < 0.05) the mean volume of ovaries having no yolky follicles compared with the control group. In birds receiving FZ 800 mg/kg feed per day, the mean length of the oviduct was reduced (p < 0.05) as compared with the control group. Morphometric studies revealed that the mean number of oocytes with diameter in the range 401-800 microm decreased (p < 0.05) in birds fed FZ 400 or 800 mg/kg feed per day. Initial egg production was affected by age (p < 0.001) and dose (p < 0.001) of FZ. The mean number of eggs laid by different groups revealed that egg production was reduced (p < 0.05) in birds receiving FZ 800 mg/kg feed per day as compared with the controls. The present data suggest that FZ causes suppression in serum profiles of LH, oestradiol, cholesterol and ovarian functions in Rhode Island Red layer poultry birds. Therefore, great care must be taken with use of FZ in layer poultry birds (Gallius domesticus) with regard to dosage and duration of administration.

Animals↗
PubMed1995

Determination of furazolidone in porcine tissue using thermospray liquid chromatography-mass spectrometry and a study of the pharmacokinetics and stability of its residues.

A method is presented for the detection of the nitrofuran, furazolidone, in porcine tissue. Following methanol-buffer extraction of the tissue, liquid partitioning, and solid-phase clean-up, samples are analysed by using thermospray LC-MS monitoring the positive ion m/z 243 with filament-assisted ionization. The LOD is 1 microgram kg-1. The assay is used to investigate the depletion of furazolidone from tissue and sample stability post mortem. It is necessary to snap-freeze samples by immersion in liquid nitrogen immediately upon collection in order to improve the stability of residues in tissue.

Animals↗
PubMed1996

Analysis of protein-bound metabolites of furazolidone and furaltadone in pig liver by high-performance liquid chromatography and liquid chromatography-mass spectrometry.

Studies undertaken using radiolabelled furazolidone have demonstrated the covalent binding of residues of the drug to cellular protein in vivo. A portion of these bound residues and those formed by furaltadone, a related nitrofuran drug, possess intact side-chains, 3-amino-2-oxazolidinone (AOZ) and 5-morpholino-methyl-3-amino-2-oxazolidinone (AMOZ), respectively. These side-chains have molecular characteristics in common with the parent compounds and may be released from liver tissue under mild acidic conditions. Derivatization with 2-nitrobenzaldehyde (NBA) serves to isolate the released side-chains and the derivatives NPAOZ and NPAMOZ are chromophoric, thereby permitting UV detection. This paper reports the introduction of an extract clean-up step to the existing procedure which eliminates or decreases interference from NBA in the HPLC-UV determination of NPAOZ. The modified procedure was also applied to the determination of AMOZ. The development of an LC-MS method for the quantitative and confirmatory determination of AOZ and AMOZ extracted and derivatized according to the same procedure as that for HPLC-UV is described. The methods were validated for AOZ and AMOZ in fortified (intra- and inter-assay studies) and incurred (inter-assay studies) pig liver samples. The limit of determination for fortified control liver samples was 5 ng AOZ g-1 and 10 ng AMOZ g-1 by HPLC-UV and 10 ng AOZ or AMOZ g-1 by LC-MS. In addition, a study to determine the ratio of released AOZ to the total bound residues present in incurred liver samples from pigs treated with furazolidone is described.

Animals↗
PubMed2002

Furazolidone-based triple 'rescue therapy' vs. quadruple 'rescue therapy' for the eradication of Helicobacter pylori resistant to metronidazole.

BACKGROUND: The optimal treatment of patients with Helicobacter pylori resistant to metronidazole has not been established. AIM: To compare the efficacy of quadruple and furazolidone-based triple therapy in the eradication of H. pylori resistant to metronidazole. METHODS: Duodenal ulcer patients (n = 70) in whom initial eradication therapy failed and who harboured H. pylori strains resistant to metronidazole were randomized to receive one of the following 7-day regimens: colloidal bismuth subcitrate, 240 mg, tetracycline, 750 mg, and furazolidone, 200 mg, each given twice daily (BTF), or omeprazole, 20 mg b.d., colloidal bismuth subcitrate, 240 mg b.d., tetracycline, 500 mg q.d.s., and metronidazole, 500 mg b.d. (OBTM). H.pylori status was assessed by culture, histology and rapid urease test before treatment and 4-6 weeks after therapy. Susceptibility to metronidazole was assessed by the agar dilution method. RESULTS: H. pylori eradication rates with intention-to-treat/per protocol analyses were: BTF, 85.7%/90.9%; OBTM, 74.2%/89.6%. Duodenal ulcers were healed in nine of 10 (90%) patients in the BTF group and in all patients (12/12) (100%) in the OBTM group (P = N.S.). A significantly lower rate of adverse events was observed in the BTF group than in the OBTM group (31.4% vs. 60%, P = 0.03), but there was no difference in terms of discontinuation of treatment (2/35 vs. 6/35, P = N.S.). CONCLUSIONS: The 1-week BTF regimen was as effective as the OBTM regimen, and produced less adverse events. Thus, it may be used in patients in whom resistance of H. pylori to metronidazole is suspected.

Adolescent↗
PubMed2000

Prevalence of Helicobacter pylori resistance to metronidazole, clarithromycin, amoxicillin, tetracycline, and furazolidone in Brazil.

BACKGROUND: Helicobacter pylori infection is associated with a wide range of digestive diseases and is very prevalent in developing countries, although few data exist on the susceptibility of H. pylori to antimicrobials commonly used in eradication schedules in these countries. The aim of this study was to evaluate the resistance of H. pylori to metronidazole, clarithromycin, amoxicillin, tetracycline, and furazolidone in dyspeptic Brazilian patients. Material and Methods. Ninety consecutive H. pylori-positive patients were enrolled. Resistance was evaluated by an agar dilution test. RESULTS: Resistance to metronidazole was detected in 38 patients (42%); to amoxicillin in 26 individuals (29%); to clarithromycin in 6 patients (7%); to tetracycline in 6 patients (7%); and to furazolidone in 4 individuals (4%). Thirteen strains were resistant to two agents, and eight strains were resistant to three antimicrobials. CONCLUSIONS: These results confirm the need for culture and susceptibility testing to define H. pylori resistance patterns in particular geographical areas before the general use of an eradication schedule. They also suggest the possibility of resistance to such antimicrobials as amoxicillin or tetracycline in geographical areas with a high prevalence of H. pylori infection and still not fully evaluated for antimicrobial susceptibility.

Adolescent↗
PubMed1988

The activity of nitrofurazone and furazolidone against Leishmania donovani, L. major and L. enriettii in vitro and in vivo.

Furazolidone and nitrofurazone showed in vitro activity against amastigotes of Leishmania donovani, L. enriettii and L. major in macrophages, at concentrations which were also toxic to the macrophages. A low grade of activity was observed against L. donovani infections in BALB/c mice by furazolidone but not with nitrofurazone. Nitrofurazone, in two concentrations, was not active when applied to the lesions of cutaneous leishmaniasis due to L. enriettii (guinea-pig infection) or L. major strain P (BALB/c mouse infection). After systemic administration to BALB/c mice infected with L. major strain JISH 252 clone 1, low-grade activity was observed at the highest level tested.

Animals↗