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PubMed1997

Determination of nitrofurantoin, furazolidone and furaltadone in milk by high-performance liquid chromatography with electrochemical detection.

A HPLC method with coulometric detection has been established to carry out the separation of the three nitrofuran derivatives, nitrofurantoin, furazolidone and furaltadone. A Nova-Pak C18 column (150 x 3.9 mm) and a Coulochem II detector from ESA have been used. After obtaining the hydrodynamic curves of the three compounds in the porous graphite electrode a potential of -600 mV was selected as the working potential. The influence of other variables such as mobile phase composition and flow-rate were studied. The mobile phase considered as an optimum was acetonitrile-0.1 M aqueous solution of sodium perchlorate (28:72), with 0.5% glacial acetic acid. The oxygen of the mobile phase was removed with a vacuum system on-line and a nitrogen stream was used to remove the oxygen of the samples. The calibration graphs and the detection limits were established. The method proposed was used, with good results, for the determination of the three compounds in milk.

Animals↗
PubMed2002

Resolution of ternary mixtures of nitrofurantoin, furaltadone and furazolidone by partial least-square analysis to the spectrophotometric signals after photo-decomposition.

An UV spectroscopic method is proposed to analyze mixtures of the nitrofuran derivatives, nitrofurantoin, furaltadone and furazolidone, used in veterinary. The change of absorption spectra due to photo-decomposition is used. A 20% dimethylformamide/water, basic medium of pH 9.4 (ammonium chloride/ammonia) and a time of irradiation of 15 s are selected. Calibration graphs are established, with the percentage of decrease of absorbance as analytical signal, in the range 2-10 microg ml(-1). To analyze mixtures of the three compounds the partial least-squares (PLS) multivariate analysis method is used with the spectra obtained by subtracting the spectra after irradiation to the original spectra. Good results have been obtained in the analysis of synthetic samples and a formulation containing all these compounds.

Furazolidone↗
PubMed1997

Application of the bivariate spectrophotometric method for the determination of metronidazole, furazolidone and di-iodohydroxyquinoline in pharmaceutical formulations.

The bivariate calibration algorithm was applied to the spectrophotometric determination of metronidazole, furazolidone and di-iodohydroxyquinoline in pharmaceutical dosage forms. The results obtained were compared with the results of derivative spectrophotometry. The statistical evaluation of method bias was carried out, and it was shown that the proposed procedure may be competitive with commonly used first-derivative spectrophotometry. The advantage of the bivariate calibration is its simplicity, and the fact that there is no need to use the derivatization procedures.

Amebicides↗
PubMed1999

Simultaneous determination of tinidazole, furazolidone and diloxanide furoate in a combined tablet preparation by second-derivative spectrophotometry.

A second-derivative spectrophotometric procedure has been developed for the simultaneous determination of tinidazole (TD), furazolidone (FD) and diloxanide furoate (DF) in a commercial preparation. The method consists of the utilization of second-derivative absorption spectra of tablet extract in distilled water and then determination of the analyte concentration in the mixture was carried out using zero-crossing (ZC) and ratio-compensation (RC) techniques. Calibration graphs constructed at their wavelengths of determination were linear in the concentration range of TD (5-20 microg ml(-1)), FD (2.5-10 microg ml(-1)) and DF (7.5-15 microg ml(-1)). The results were found to be accurate and free from interference. The details of the statistical treatment of analytical data are also presented.

Antiprotozoal Agents↗
PubMed2000

Plasma and hepatic lipid profiles in furazolidone-treated rats.

Rats were treated orally with furazolidone (FZ) at doses of 50, 100, and 200 mg/kg body weight for three consecutive days. The parameters determined in plasma included: total cholesterol, high density (HDL) cholesterol, low-density (VLDL+LDL) cholesterol, triglycerol (TAG), phospholipids (PL), and lipoprotein lipase. In the liver, cholesterol, TAG and phospholipid concentrations were measured. At the lowest dose used, no statistically significant effect on any of these parameters in plasma or liver was observed. The drug, dose-dependently, increased the concentrations of total cholesterol, VLDL cholesterol, TAG and PL in plasma. The activity of lipoprotein lipase was significantly decreased by FZ by about 45%. The hepatic cholesterol concentration was not significantly affected by any of the doses used. However, doses of 100 and 200 mg/kg produced fatty infiltration in the liver and significantly increased TAG level. The highest dose also decreased PL concentration.

Administration, Oral↗
PubMed1999

Pharmacological, therapeutic and toxicological properties of furazolidone: some recent research.

Some of the recent publications on the pharmacological, therapeutic and toxicological properties of the antimicrobial agent furazolidone (FZ) are briefly reviewed. In animals, most of the recently published papers focus on (1) the methodology of measuring the residues of the drug and its metabolites in edible tissues; (2) the carcinogenicity and genotoxicity of FZ; (3) the cellular and molecular basis of FZ-induced cardiomyopthy, and the action of different cardioprotectant drugs thereon; and (4) hormonal effects. In humans, the use of FZ as an anti-ulcer drug and in controlling infectious diseases, especially opportunistic infections in AIDS patients, is described.

Animals↗
PubMed2004

Invasive characteristics of apathogenic Shigella flexneri 5a2c mutant obtained under the effect of furazolidone.

Apathogenic Shigella flexneri 5a2c mutant treated with furazolidone can infect eucaryotic cells. These bacteria contain no virulence genes responsible for Sh. flexneri invasion, which seems to be the cause of their apathogenicity. The capacity of bacteria to penetrate into eucaryotic cells correlates with the appearance of ECP 32 protease specifically cleaving actin.

Antigens, Bacterial↗
PubMed1997

Furaltadone cytotoxicity on three cell lines in the presence or absence of DMSO: comparison with furazolidone.

Nitrofuran drugs have been studied on cellular systems in order to develop in vitro tests for safety assessment of food contaminants. In the present study we have tested furaltadone on three cell lines (HEp-2, Caco-2 and V79), using the same toxicity endpoints as in a previous study with furazolidone, namely cell viability and growth, colony-forming ability, LDH release, and O2 consumption. One of the aims of this investigation was to compare the two compounds in order to determine whether our models are able to discriminate among structurally related molecules. The other aim was to study the influence of the solvent used on the observed toxicity, because furaltadone is soluble both in water and in DMSO. The results show that the three cell lines used as differently affected by the two compounds, and that, at least in the case of furaltadone, the solvent is not relevant for the observed toxicity.

Animals↗
PubMed2004

Evaluation of the carcinogenic effects of furazolidone and its metabolites in two fish species.

The major metabolite from the use of furazolidone (FZD) in mammals, birds and fish is 2,3-dihydro-3-cyanomethyl-2-hydroxy-5-nitro-1alpha, 2-di(2-oxo-oxazolidin-3-yl)iminomethyl-furo[2,3-beta]furan, also called 3-amine-2-oxazolidone (AOZ). A minor metabolite was identified as N-(5-amine-2-furfuryliden)-3-amine-2-oxazolidone (FOZ). To assess the potential carcinogenicity of FZD and the metabolic mixture of AOZ/FOZ, 11 mg FZD/kg feed/day was fed for 12 weeks to mollies (Poecilia formosa), an ornamental fish species prone to develop tumors. The rate of tumors was quantified and defined both in mollies and their offspring. Then, some fish was made into fishmeal and incorporated into fish food at 500 g of meal/kg of food and fed to other mollies for 12 weeks. The rate of tumors was assessed. A similar trial design was carried out in tilapia fish (Oreochromis niloticus) by adding 50 mg FZD/kg to the feed for 90 days. All animals were placed in glass fishponds under controlled laboratory conditions. Each week, a significant biomass was collected from both groups to assess the macroscopic and histopathological changes. All mollies developed melanohistiocytomic tumors in the liver and other organs. Offspring from surviving mollie females stimulated to breed showed no changes compared to control animals. None of the mollies fed with the mollie-meal food contaminated with AOZ/FOZ developed tumors. Neither tilapia medicated with FZD nor tilapia fed with tilapia-meal contaminated with AOZ/FOZ developed tumors. These results do not support the established viewpoint that FZD must be banned from trophic chains based on its potential carcinogenic properties.

Animals↗
PubMed1986

The effect of furazolidone on some clinical and biochemical parameters in goats.

Furazolidone (FZ) administered to goats orally at the recommended therapeutic dose (10 mg/kg body weight for 5 days) resulted in significant decreases in heart rate, pulse rate, and rectal temperature. No change was observed in respiratory rate or body weight, although a tendency towards a decrease in the latter was observed. An increase in the number of the erythrocytes was found. FZ also produced significant decreases in the pseudocholinesterase activity and plasma concentrations of total protein and ascorbic acid. A significant increase in the adrenal cholesterol concentration was observed while the weight of adrenal glands and their ascorbic acid concentration and content were unaffected. No significant histopathological changes were observed in treated goats.

Adrenal Glands↗
PubMed1990

Postmortal degradation of furazolidone and furaltadone in edible tissues of calves.

Rapid and complete postmortal degradation of furazolidone and furaltadone occurred in liver, kidney and muscle tissues of veal calves. Different degradation half-lives were observed between these tissues, the mean ranging from less than 7 minutes to 63 minutes. At 24 h after slaughter the parent nitrofurans were no longer detectable in edible tissues. For residue monitoring purposes plasma and/or urine can be used, if these matrices are treated in a specific way immediately after slaughter; muscle tissues and organs are unsuitable for residue monitoring of parent nitrofurans.

Animals↗
PubMedDate not supplied

Binding of 14C-furazolidone metabolites to the muscular and hepatic proteins of trout.

A high level of 14C was found to bind irreversibly with the liver proteins of rainbow trout (Oncorhyncus mykiss) exposed to 135 mg/kg bodyweight of 14C-labelled furazolidone (14C-FZ) in fish feed daily for 10 days. After the cessation of 14C-FZ treatment, hepatic protein-bound 14C in trout stayed high for at least 30 days. The chemical identity of protein-bound 14C remained to be elucidated. However, a part of the protein-bound 14C in the liver and muscle could be released as 3-amino-2-oxazolidinone by acid hydrolysis. The formation of protein-bound 14C in the liver was investigated further with trout dosed intravenously with different 14C-FZ doses at 10 degrees C or with 5 mg/kg FZ at different water temperatures. 14C binding to the liver proteins was found to increase with increasing FZ dose or water temperature. Results of these studies indicate that protein-bound 14C in the muscle and liver of trout is related to the formation of reactive intermediates from FZ. However, additional studies on the identities of the protein-bound FZ residues are required before they can serve as useful biomarkers to monitor FZ exposure in farm fish.

Administration, Oral↗
PubMed2000

Antibiotic resistance patterns of aerobic coryneforms and furazolidone-resistant Gram-positive cocci from the skin surface of the human axilla and fourth toe cleft.

Samples of skin surface bacteria from 28 healthy subjects plated directly on to selective and non-selective media revealed that the proportion of aerobic coryneforms and furazolidone-resistant Gram-positive cocci (FURECs) resistant to erythromycin was significantly greater in the fourth toe cleft than in the axilla (P < 0.05). There were more erythromycin-resistant bacteria than tetracycline-resistant bacteria at both sites (P = 0.001 for the toe cleft; P < 0.01 for the axilla). In total, 160 distinct isolates were obtained, of which 42 were FURECs and 118 were aerobic coryneforms. Of these, 153 (96%) were resistant to erythromycin and 66 (41%) to tetracycline. All except seven of the tetracycline-resistant strains were also resistant to erythromycin. The resistant isolates belonged to a variety of species. CDC group ANF corynebacteria were most numerous and composed 31% of all isolates. The majority (76%) of FURECs were identified as Micrococcus luteus. MIC determinations on selected strains revealed that tetracycline-resistant FURECs were sensitive to doxycycline and minocycline, as were most tetracycline-resistant coryneforms. Nine coryneform isolates were cross-resistant to all three tetracyclines. Only a minority of erythromycin-resistant FURECs (21%) demonstrated a macrolide-lincosamide-streptogramin type B (MLS)-resistant phenotype with inducible or constitutive cross-resistance to clindamycin and the type B streptogramin, pristinamycin IA. Twenty-nine erythromycin-resistant FURECs had a novel phenotype distinct from MLS and macrolide-streptogramin type B resistance. In contrast, most coryneforms (79%) were MLS resistant. Among the remainder, two unusual erythromycin resistance phenotypes were apparent, both of which differed from the unusual phenotype in FURECs. This study has revealed that the non-staphylococcal aerobic flora of skin contains a considerable reservoir of tetracycline and erythromycin resistance determinants. The three unusual macrolide resistance phenotypes may be associated with novel resistance mechanisms.

Actinomycetales↗
PubMed1985

Furazolidone concentrations in plasma, milk and some tissues of Nubian goats.

The concentrations of furazolidone (FZ) in plasma and milk were measured in goats treated orally with the drug at a dose of 10 mg kg-1 daily for 5 days. The maximum plasma concentrations obtained were 1.57 +/- 0.52 micrograms ml-1 (n = 5) 8 h after the first dose, and 2.13 +/- 0.11 micrograms ml-1 (n = 4) 6 h after the fifth dose. The maximum milk concentration was 0.88 +/- 0.32 micrograms ml-1 (n = 4) 8 h following the administration of a single dose. Using a colorimetric method, FZ was not detectable in goats' liver or muscle after the recommended therapeutic dose (10 mg kg-1, 5 days). However, using an HPLC method, the drug was detected 24 h after the treatment in the gluteal muscle and liver at concentrations of 0.26 +/- 0.01 microgram g-1 (n = 5) and 0.10 +/- 0.02 microgram g-1 (n = 5), respectively. The drug concentrations decreased significantly (P less than 0.05-0.01) at 3, 5 and 7 days after treatment, and no measurable concentrations were found after 10 days.

Animals↗
PubMed1988

Effect of furazolidone and nitrofurazone on brain gamma-amino butyric acid and glutamate concentrations in chickens.

1. The concentrations of gamma-amino butyric acid (GABA) and glutamate were measured in the brains of chickens which were treated with furazolidone (FZ) or nitrofurazone (NF) at oral doses of 12.5, 25 or 50 mg/kg for 5 days. 2. At the end of the treatment, birds on the small dose of FZ or NF lost about 9% of their bodyweight, and those on the high doses lost about 18%. 3. Both drugs produced dose-dependent increases in the concentrations of GAA and glutamate which were statistically significant at doses of 25 and 50 mg/kg of NF and 50 mg/kg of FZ.

Animals↗
PubMed1989

Effect of furazolidone and nitrofurazone on brain gamma-amino butyric acid and glutamate concentrations in chickens.

1. The concentrations of gamma-amino butyric acid (GABA) and glutamate were measured in the brains of chickens which were treated with furazolidone (FZ) or nitrofurazone (NF) at oral doses of 12.5, 25 or 50 mg/kg for 5 days. 2. At the end of the treatment, the birds lost about 9% of their bodyweight when on the small dose of FZ or NF and about 18% when on the high doses. 3. Both drugs produced dose-dependent increases in the concentrations of GABA and glutamate which were statistically significant at doses of 25 and 50 mg/kg of NF, and 50 mg/kg of FZ.

Animals↗
PubMedDate not supplied

Treatment of peptic ulcer disease with furazolidone.

Furazolidone (FZ) has been used in China as a treatment of peptic ulcer disease for about 20 years. Clinical and experimental studies suggest that it has good short-term and long-term effects on both human and animal ulcers. The ulcer healing rate is related to the dosage and course of treatment. The healing rate of a high dose, 2 week course is about 70-75% and the relapse rate after 3 years is 9.5%. The adverse reactions to FZ are not severe, and are well tolerated in most patients. However the mutagenic studies of several biological systems indicate that it has a mutagenic effect, but the mutagenic and carcinogenic effects on humans and animals remain questionable, because FZ has been biotransformed into other metabolites. The mechanisms of FZ in the treatment of peptic ulcer disease are not fully understood, perhaps partly due to the monoamine oxidase (MAO) inhibitory reaction and partly to the antibacterial activity to Helicobacter pylori (HP). The long-term effects of FZ are still not clear.

Animals↗
PubMed1978

Characterization of glycogen in selected tissues of turkey poults with spontaneous round heart disease and furazolidone-induced cardiomyopathy.

Furazolidone (FZ) at 700 ppm was added to feed mixtures fed turkey poults 2--5 weeks after hatching to induce acute experimental cardiomyopathy. Poults in the control pen received the same ration but without FZ. From EKG data obtained at weekly intervals, poults were selected for sacrifice at 5 and 10 weeks of age. Poults were sacrificed by cervical dislocation and appropriate samples of tissue from the left ventricle, liver, pectoralis and tibialis cranialis muscles were removed for glycogen assays. Character of glycogen, as determined by percent of branching and number of glucose units per segment, was not significantly altered in poults with spontaneous round heart disease or FZ-induced cardiomyopathy. This suggests that the glycogen accumulation noted in these conditions most closely resembles type II glycogenosis.

Animals↗