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PubMed1978

Comparative in vitro activity of five nitrofurans.

Five nitrofurans- nitrofurantoin, nifuratel, nitrofurazone, furazolidone and and SQ 18,506--have been tested against 201 microbial strains. Escherichia coli, Streptococcus faecalis, micrococci and Staphylococcus epidermidis were sensitive to all five compounds; furazolidone and SQ 18,506 were the most active against these species. Klebsiella aerogenes was less sensitive, and Proteus spp., Providencia stuartii and Pseudomonas aeruginosa strains were resistant. Nifuratel was inhibitory for some Candida albicans strains, and SQ 18,506 was highly active against this species. Nifuratel was judged overall to have superior in vitro antimicrobial properties to nitrofurantoin.

Bacteria↗
PubMed1985

Carnitine alterations in spontaneous and drug-induced turkey congestive cardiomyopathy.

Carnitine and acylcarnitines were measured in plasma and tissues of control turkeys, turkeys with an inbred spontaneous cardiomyopathy, and turkeys with furazolidone-induced cardiomyopathy. Heart failure was evident in both types of cardiomyopathy from decreased systemic blood pressure and cardiac dilatation compared to controls. Plasma free carnitine, short-chain acylcarnitine, and long-chain acylcarnitine were significantly elevated by 76 to 614% (p less than 0.01) in the two cardiomyopathy models compared to control. The highest carnitine levels were found in the most hypotensive turkeys. Liver free carnitine and short-chain acylcarnitine levels were also elevated by 45 to 537% (p less than 0.05) in both types of cardiomyopathy. Free carnitine was elevated by 126% in left ventricle and by 54% in skeletal muscle of the furazolidone-treated turkeys (p less than 0.05). We speculate that hepatic synthesis of carnitine may be increased in response to hypotension and progressive cardiac dysfunction in cardiomyopathic turkeys. Such an increase may be useful to promote beta-oxidation of fatty acids as a cardiac energy source.

Animals↗
PubMed1989

Recent advances in the diagnosis and management of giardiasis.

Management of patients with giardiasis is often difficult because of problems related to diagnosis, lack of knowledge about pathophysiology, and a less than satisfactory chemotherapeutic armamentarium. Treatment, particularly in children, presents several problems: What drug should be used, and at what dosage? Should the patient's contacts be treated? How does one cope with treatment failures? An overview of data available in the literature is presented, and studies on the susceptibility and resistance of Giardia isolates to different drugs in in vitro and in vivo models are discussed. In such models, tinidazole, metronidazole, and furazolidone were most active in terms of susceptibility; quinacrine was least active. However, Giardia strains resistant to all four drugs were isolated. Nitroimidazoles were associated with poor compliance in children, whereas furazolidone was well tolerated. It is concluded that management of symptomatic giardiasis is complicated by a range of factors, including drug resistance, patient compliance, and the lack of an accurate, sensitive, and noninvasive diagnostic test.

Animals↗
PubMed2004

Clinical evaluation of four one-week triple therapy regimens in eradicating Helicobacter pylori infection.

AIM: To evaluate clinical efficacy of four one-week triple therapies in eradicating Helicobacter pylori infection. METHODS: In this clinical trial, 132 patients with duodenal ulcer and chronic gastritis were randomly divided into four groups, and received treatment with OAC (omeprazole 20 mg + amoxicillin 1 000 mg + clarithromycin 250 mg), OFC (omeprazole 20 mg + furazolidone 100 mg + clarithromycin 250 mg), OFA (omeprazole 20 mg + furazolidone 100 mg + amoxicillin 1 000 mg) and OMC (omeprazole 20 mg + metronidazole 200 mg + clarithromycin 250 mg), respectively. Each drug was taken twice daily for one week. The (13)C urea breath test was carried out 4-8 weeks after treatment to determine the success of H pylori eradication. RESULTS: A total of 127 patients completed the treatment. The eradication rate for H pylori infection was 90.3%, 90.9%, 70.9% and 65.6%, respectively in OAC, OFC OMC and OFA groups. CONCLUSION: A high eradication rate can be achieved with one-week OAC or OFC triple therapy. Thus, one-week triple therapies with OAC and OFC are recommended for Chinese patients with duodenal ulcers and chronic gastritis.

Adolescent↗
PubMed2006

Efficacy of one-day quadruple therapy for H pylori infection in Chinese patients.

AIM: To compare the efficacies of one-day quadruple therapy and seven-day triple therapy in Chinese patients. METHODS: Sixty consecutive patients with nonulcer dyspepsia and confirmed H pylori infection were randomized to receive either omeprazole 40 mg, amoxycillin 1 g, and furazolidone 100 mg, all twice a day for 7 d or omeprazole 20 mg (at breakfast and dinner), amoxicillin 1 g, furazolidone 200 mg, and colloidal bismuth subcitrate 220 mg four times for only one day. H pylori status was determined before and at least 5 weeks after therapy by endoscopy with antral and corpus biopsies for rapid urease test and histology. RESULTS: H pylori eradication was successful in 66.67% (20/30) patients in the 7-d group and in 36.67% (11/30) patients in the 1-d group (P = 0.037). Side effects were induced by the treatment in 13.3% (4/30) patients of each group, but these were all self-limiting, short-lasting, and did not require any specific treatment. CONCLUSION: The one-day quadruple therapy is less effective than the one-week regimen in curing H pylori infection in Chinese patients.

Adult↗
PubMed1977

Efficacy of various drugs for treatment of giardiasis. A comparative study.

A total of 172 patients with giardiasis were treated with four of the drugs most commonly used for this infection. All drugs were used in their usual posologic schedules. The cure rates achieved with furazolidone, nimorazole, metronidazole, and tinidazole were; respectively, 72%, 94%, 87%, and 97%, while in a control group given no medication stools of only 35% of the patients became negative. Side effects were of minor importance in patients treated with nimorazole and metronidazole, and were somewhat more frequent and severe in those treated with furazolidone. Tinidazole produced no side effects.

Antiprotozoal Agents↗
PubMed1975

[Typing of E. coli strains isolated from a turkey and a test of their sensitivity in relation to antibiotics].

The turkey-poults on an industrial turkey-breeding farm were studied. A total of 75 strains of Escherichia coli were isolated. Typing was performed by Sojka's method: serotype 0-2 was established in 42.2 percent of the cases, 0-71-- in 12.6 per cent, 0-78 (11.2%), and 0-1 (8.4%). The sensitivity of the typed strains was tested to 8 antibiotics and furazolidon. It was found that all strains possess certain amount of resistance to streptomycin, chloramphenicol, oxitetracycli, and spectam. The same strains proved sensitive to ampicillin, colimycin, tetraoleandomycin, and to a certain extent to kanamycin. It is concluded that prophylaxis and treatment should be carried out with the use of ampicillin, colimycin, furazolidon, and tetraloleandomycin.

Animals↗
PubMed1991

Increasing prevalence of high degree resistance amongst Salmonella to different antibiotics.

National Salmonella & Escherichia Centre situated at Central Research Institute, Kasauli receives Salmonella strains from all over the country. Eight hundred and fourteen Salmonella strains belonging to 14 serotypes received during 1986 were studied for antibiotic resistance and Minimum Inhibitory concentration (MIC) with regard to ampicillin (A), chloramphenicol (C), furazolidone (Fz) and gentamicin (G). Resistance to ampicillin was found to be highest (80%) and furazolidone the least (0.1%). Similarly a large number of strains (31%) had very high MIC values greater than 640 mcg per ml for chloramphenicol, whereas only 3.4% strains were found to have MIC values greater than 640 mcg per ml for gentamicin. The present findings have been discussed in the light of similar data published from this Centre earlier and from other sources in India.

Ampicillin↗
PubMed1991

Five-day bismuth-free triple therapy for the eradication of Helicobacter pylori and reduction of duodenal ulcer relapse.

Previous studies have demonstrated that the eradication of Helicobacter pylori (H. pylori) is associated with a significant reduction of the rate of duodenal ulcer (DU) relapse. The aim of this study was to assess the long-term effect of a bismuth-free triple therapy on the eradication of H. pylori and reduction of DU relapse. After informed consent, 61 patients with endoscopically proven DU and H. pylori infection detected on 14C-urea breath test (BT) were included in the study. All patients received a combination of furazolidone, amoxicillin, and metronidazole, three times a day, for 5 days, in addition to eventual classical antiulcer agents prescribed by their attending physicians. BT was repeated after an interval of at least 60 days to evaluate H. pylori eradication. Endoscopy and another BT were performed again at 6.5 months after therapy to detect possible recurrences. Forty-eight patients completed the trial: 26 (54%) patients were negative for H. pylori at 6.5 months after the end of treatment, and 22 (46%) persisted H. pylori positive. Ninety-two percent of the patients in whom the bacteria were eradicated showed endoscopically healed ulcers and were asymptomatic, and two that were symptomatic presented only occasional pain not requiring therapy. Among the 22 patients who persisted H. pylori positive, six (27%) showed endoscopically active ulcers (p = 0.012) and eight (36%) patients continued to be symptomatic (p less than 0.01), and were still using antiulcer drugs (p = 0.002) 6.5 months after treatment. It is concluded that combined treatment with furazolidone, amoxicillin, and metronidazole for 5 days represents a well-tolerated, inexpensive, and effective therapeutic regime for the eradication of H. pylori and abolition of DU relapse in more than 50% of the patients during a follow-up period of 6.5 months.

Adult↗
PubMed1990

[Detection of protease specifically splitting actin in revertants of Shigella flexneri L-forms].

Proteolytic activity of cell extracts from revertants of Shigella flexneri L-forms as well as biochemical properties of these strains and their sensitivity to antibiotics were studied. The protease found earlier in cells of strain E. coli A2 was shown to be synthesized by one of 8 revertants under study. This protease split actin and did not split some other proteins, its activity was inhibited by inhibitors of metalloproteases. Strain 5a2c which produced the protease was similar to the strain E. coli A2 and differed from other revertants in some biochemical properties, resistance to ampicillin and sensitivity to furazolidone. Thus the protease activity can be a marker of structural and functional transformation of Sh. flexneri under the influence of furazolidone.

Actins↗
PubMedDate not supplied

[Effect of drugs possessing antialcoholic activity on ethanol pharmacokinetics].

Furazolidone, lithium carbonate, chlorprotixen and pyrroxan exert different effects on ethanol pharmacokinetics. Furazolidone decreases clearance of ethanol, increases its half-life with a simultaneous reduction of blood acetaldehyde concentration. Pyrroxan increases clearance and maximal concentration of ethanol. Chloprotixen effect is characterized by a concurrent increase of ethanol and acetaldehyde concentrations in the first hours after ethanol administration. Lithium carbonate produces no significant changes in ethanol pharmacokinetic parameters.

Acetaldehyde↗
PubMed1976

Relation between Salmonella typhimurium biotypes and drug resistance, Teheran, Iran (1962-1973).

According to the procedure of Cordano (1971), the identification of biotypes of 118 strains of Salmonella typhimurium isolated from stools or rectal swabs of patients with sporadic cases of diarrhoea on the Central Plateau during the period 1962-1973 revealed that: From 118 S. typhimurium, 65 (55-1%) were biotype "d", 50 (42-4%) were "a" and three (2-5%) were "b". The predominant biotype was "d", followed by the "a" biotype, and "b" was rarely encountered. Biotype "d" has existed since 1965, and after that date has increased. Biotype "a" existed from the beginning of the study, but has decreased during the period 1962-1973. Sensitivity tests were performed according to Bauer (1966). Biotypes "d" and "a" showed a high degree of resistance to tetracycline, chloramphenicol, streptomycin, triple-sulfa, ampicillin, furazolidone, kanamycin, neomycin, paromomycin, cephalothin and co-trimoxazole. All isolated biotypes "d" were multiple drug-resistant, while some of the strains of biotype "a" were resistant and some sensitive. All three biotypes "b" were sensitive to all drugs examined. Resistance to drugs for biotypes "d" and "a" increased with time. The predominant pattern of resistance for all biotypes was found to be resistance to eight drugs: tetracycline, chloramphenicol, streptomycin, triple-sulfa, ampicillin, kanamycin, neomycin and paromomycin (Tc, Cm, Sm, Su, Am, K, N, Par). Considering the relationship between resistance pattern and biotypes, the predominant pattern in biotype "d" was resistance to eight drugs (Tc, Cm, Sm, Su, Am, K, N, Par) (47-7%), and in biotype "a" was resistance to nine drugs, tetracycline, chloramphenicol, streptomycin, triple-sulfa, ampicillin, furazolidone, kanamycin, neomycin, paromomycin (Tc, Cm, Sm, Su, Am, Fx, K, N, Par) (28%).

Ampicillin↗
PubMed1997

[Influence of difuracil (PAP-49) on normal intestinal microflora of rabbits. In vitro and in vivo experiments].

The influence of difuracil (PAP-49), a novel nitrofuran, on saprotrophic and normal digestive tract microflora was studied in vitro and in vivo by comparison with that of furazolidone. It was shown that the minimum inhibitory concentration of both the drugs ranged from 0.01 to 1.56 micrograms/ml. The experiments on rabbits with the use of the drugs in doses of 5 and 10 mg/ kg body weight revealed that unlike furazolidone difuracil induced no noticable qualitative or quantitative changes in the intestinal microflora composition.

Administration, Oral↗
PubMed1990

Drug resistance in Giardia intestinalis.

Evidence for drug resistance in giardiasis is reviewed and biochemical studies undertaken to determine the basis for this resistance are discussed. Metronidazole and furazolidone, which produce toxic radicals within the cell, have different biochemical mechanisms of action. Resistance to metronidazole is negatively correlated with the intracellular concentration of pyruvateferredoxin oxidoreductase leading to a concomitant decrease in the uptake of free metronidazole into the cell, while resistance to furazolidone appears to be due to an increase in thiol cycling enzymes. At the molecular level resistance to metronidazole is associated with DNA changes. DNA probes which hybridize with specific chromosomes and repetitive sequences indicate that rearrangements both at the chromosome and repetitive DNA level occurred concurrently with the development of metronidazole resistance. The problems of cross-resistance and treatment failures that occur in the absence of resistance are additional difficulties which have important implications for the management of individual patients. New drugs such as azithromycin, while showing great variation in activity against different stocks may be useful in treating some refractory cases of giardiasis. In the community, it is important to recognize the occurrence and spread of drug resistant Giardia, and markers, such as DNA probes, provide methods to monitor potential epidemics and the spread of drug resistant Giardia.

Animals↗
PubMed1992

Myocardial myoglobin deficiency in various animal models of congestive heart failure.

Myoglobin is known to protect the mechanical function of the heart from hypoxia by acting as a sarcoplasmic oxygen reservoir and shuttle. We postulated a role for myoglobin in the pathogenesis of congestive heart failure. Several models of congestive heart failure were employed to test the hypothesis, including spontaneous inherited dilated cardiomyopathy in Doberman Pinschers, and heart failure produced by rapid ventricular pacing in dogs, volume overload in chickens and furazolidone toxicity in turkeys. Myocardial myoglobin was decreased by approximately 50% for all models (P less than 0.05). In Doberman Pinschers dogs which are predisposed to the development of dilated cardiomyopathy and have mild subclinical depression of cardiac performance, myocardial myoglobin (1.05 +/- 0.22 mg/g) is approximately 50% decreased compared to healthy mongrel dogs (2.15 +/- 0.52 mg/g), approximately twice as much as dobermans with heart failure (0.47 +/- 0.25 mg/g) but similar to the concentration found in dogs paced to heart failure (1.09 +/- 0.34 mg/g). Myocardium from poultry had remarkably decreased myoglobin compared to mammals (34 +/- 4 micrograms/g) with heart failure produced either by furazolidone or salt toxicity causing a further 50% reduction. In the canine models of heart failure, myocardial myoglobin concentration was demonstrated to be correlated with biochemical and physiological indicators of myocardial performance, namely, mitochondrial and sarcoplasmic reticular ATPase activities, and cardiac output, systemic vascular resistance, pulmonary capillary wedge pressure and mean arterial pressure, respectively. Our data implicates a role for myoglobin deficiency in the pathogenesis of congestive heart failure and in the predisposition of doberman pinschers to dilated cardiomyopathy.

Animals↗
PubMed1986

On the capacity of nitroheterocyclic compounds to elicit an unusual axial asymmetry in cultured rat embryos.

A series of nitroheterocyclic compounds with antimicrobial and radiosensitizing properties was tested for embryotoxicity in cultured Sprague-Dawley rat embryos, and their effects were compared with various other five-membered heterocycles. Nifuroxime, furazolidone, nitrofurazone, niridazole, 2-nitroimidazole, and ronidazole each elicited a striking malformation characterized by asymmetrical, right-sided hypoplasia when coincubated with embryos for 26 hr. Minimum concentrations required to elicit this unusual defect ranged from 0.01 mM with nifuroxime and furazolidone to 0.5 mM with ronidazole and were roughly correlated with single electron redox potentials; i.e., agents with relatively high redox potentials were generally more effective than those with low potentials. Nitrofurantoin failed to elicit this unusual malformation but exhibited an extremely steep dose-response curve for embryolethality. Metronidazole and 4-nitroimidazole, nitroheterocyclic agents with relatively low redox potentials, did not produce the asymmetric abnormality nor were they highly embryotoxic, even at concentrations up to 2 mM. 2-Amino-5-nitrothiazole and 4'-methylniridazole also failed to evoke the asymmetric malformation but produced significant embryotoxicity as manifested by decreased growth parameters and elicitation of other kinds of malformations. Heterocyclic compounds not bearing a nitro group (furosemide, 2-aminothiazole, and 2-aminoimidazole) failed to elicit axial asymmetry at concentrations up to 1.0 mM but produced other signs of embryotoxicity at the highest concentrations tested. The results suggest that the presence of a reducible nitro group is critical for generation of the unusual malformation and that the single-electron redox potential of the nitro group plays a dominant but not exclusive role in the capacity of these chemicals to evoke axial asymmetry in cultured rat embryos.

Abnormalities, Drug-Induced↗
PubMed2001

Determination of the metabolites of nitrofuran antibiotics in animal tissue by high-performance liquid chromatography-tandem mass spectrometry.

A LC-MS-MS method is presented to analyse simultaneously the metabolites of four nitrofuran antibacterial agents, furazolidone, furaltadone, nitrofurazone and nitrofurantoin in animal muscle tissue. Sample clean-up and analyte enrichment was performed by solid-phase extraction (SPE) with a polystyrene sorbent following combined hydrolysis of the protein-bound drug metabolites and derivatisation of the homogenised tissue with 2-nitrobenzaldehyde. Limits of detection of 0.5-5 ng g(-1) tissue and limits of determination of 2.5-10 ng g(-1) tissue were achieved using electrospray ionisation in positive mode. Analyte identification and quantification was performed according to EU guidelines, using multiple reaction monitoring (MRM) with one precursor ion and two product ions as identifiers. The use of an internal standard in combination with the simplified sample preparation led to a sensitive and reliable analysis method. The yield of the derivatisation reaction was between 66 and 74% and the recovery of SPE reached 92-105% for all values between 10 and 500 ng g(-1). The developed analytical protocol has been applied to contaminated tissue samples of furazolidone- and furaltadone-treated pigs and allowed unequivocal identification and quantification of the metabolites.

Animals↗
PubMed2000

Susceptibility of Polish clinical strains of Yersinia enterocolitica serotype O3 to antibiotics.

A total of 199 clinical strains of Yersinia enterocolitica serotype O3, biotype 4 were tested for their susceptibility to antibiotics (158 strains carried the virulence plasmid pYV and 41 strains did not). A total of 114 isolates were tested by a standard disk diffusion method for 21 antibiotics. Almost all strains tested were resistant to ampicillin and cefazolin and susceptible to amoxycillin/clavulanate, cefaclor, cefamandole, cefuroxime, cefotaxime, ceftriaxone, aztreonam, imipenem, gentamicin, amikacin, netilmicin, tetracycline, doxycycline, chloramphenicol, ciprofloxacin, sulphamethoxazole, trimethoprim, co-trimoxazole and furazolidone. In addition, minimal inhibitory concentrations of 15 antibiotics were determined by the agar dilution method for all 199 strains (158 carrying plasmid pYV and 41 strains that did not). Third-generation cephalosporins such as cefotaxime and ceftriaxone and a fluoroquinolone (ciprofloxacin) were the most active antimicrobial agents tested followed by aztreonam, imipenem, trimethoprim, tetracycline, gentamicin, chloramphenicol, amoxycillin/clavulanate, cefaclor, cefuroxime, amikacin, furazolidone and sulphamethoxazole. The present study demonstrated a high susceptibility of clinical strains of Y. enterocolitica to most of the tested antibiotics. In general there was no significant difference between susceptibility to antibacterial agents of strains with or without plasmid pYV.

Drug Resistance, Microbial↗