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[Change in the sensitivity of dysentery bacteria to certain antibiotics, furazolidone and antifungal preparations when cultured together with Candida albicans].

The effect of Candida albicans (2 collection cultures and 1 freshly isolated culture) on sensitivity of dysentery bacteria (5 Zonne strains, 4 Flexner strains and 2 Newcastle strains) to antibiotics, furazolidone and their combinations with nystatin or decamine was studied by the method of serial dilutions. A total of 937 tests were performed with the use of 10 concentrations in each test. It was found that sensitivity of the Shigella to levomycetin succinate, monomycin and furazolidone decreased in the presence of Candida. Decamine increased the bactericidal effect of furazolidone on Shigella in pure cultures and in addition increased sensitivity of various Shigella species to the antibiotics tested and especially furazolidone when the cultures were grown together with Candida albicans. Nystatin combination with levomycetin succinate and especially with monomycin increased sensitivity of various Shigella species in the presence of Candida albicans. The data are useful in treatment of dysentery since Candida are often isolated from dysentery patients.

Anti-Bacterial Agents↗

[Suitability of the streptomycin furazolidone combination in the treatment of diarrhea in newborn calves].

In the treatment of diarrhoea in new-born calves in 14 herds, the clinical effectiveness of the combination of streptomycin (1,000,000 i. u.) with furazolidone (0.2 g) was compared with that of streptomycin (1,000,000 i. u.) alone and furazolidone (0.2 g) alone in the peroral application to 710 calves twice daily. The use of the combination resulted in the recovery of 97.1% of 244 calves, the use of streptomycin alone healed 99.2% of 236 calves, and the application of furazolidone healed 97.4% of 230 calves. However, these results are not statistically significant. Taking into account the costs of treatment as well as the losses due to mortality, the treatment with streptomycin alone was more economical than the use of the comdone. The furazolidone therapy was more advantageous than the use of the combination only when evaluated from the viewpoint of the purchase price of calves.

Animals↗

Clinical pathologic profiles of dogs and turkeys with congestive heart failure, either noninduced or induced by rapid ventricular pacing, and turkeys with furazolidone toxicosis.

Characteristic alterations in the serum and urine biochemical profiles of Doberman Pinschers with congestive heart failure (CHF) resulting from idiopathic dilated cardiomyopathy were determined. We compared these alterations with those observed in 2 other models of CHF: rate overload induced by rapid ventricular pacing in dogs, and biventricular hypertrophy and dilatation induced in turkey poults by furazolidone toxicosis. Serum and urine biochemical changes in both models of CHF in dogs were mild to moderate in degree, and were moderately consistent. They could be attributed to secondary neurohumoral, hepatic, and renal effects of heart failure. The most marked and consistent changes observed were mildly decreased anion gap that developed, in part, because of decreased serum sodium concentration, moderately increased catecholamine concentrations, moderate lactaciduria, hyposthenuria, and mildly increased urea concentrations and liver enzyme activities. In birds with furazolidone cardiomyopathy, we observed mild increases in serum urate concentration, liver and muscle enzyme activities, but moderately increased sodium concentration with decreased chloride concentration. In the pacing and furazolidone models, in which CHF was rapidly induced, moderate to marked hypoproteinemia was attributable to decreases in albumin and globulin concentrations. Using the avian model we found that the hypoproteinemia could be largely attributed to blood volume expansion, and to a lesser extent, inanition. Development of hypoalbuminemia during rapid ventricular pacing and furazolidone treatment may contribute to the effects of rate overload or drug toxicity in the pathogenesis of CHF, because hypoalbuminemia may contribute to altered hemodynamics and neuroendocrine system activation. Our data indicate that clinical biochemical analysis of serum and urine may be useful for assessing progression of CHF.

Animals↗

Determination of furazolidone residues in eggs by HPLC followed by confirmation with a diode-array UV/Vis detector.

A sensitive HPLC method for the determination of furazolidone residues in eggs (10-1,000 micrograms/kg) is described. Recovery is about 86%. With the aid of a UV/Vis Diode-Array detector confirmation up to the 15-ppb level was possible. In order to test this method with "real" samples, three laying hens received 30 mg each of furazolidone in feed (single dose). The eggs were collected for five days. After five days traces of furazolidone (5 micrograms/kg) could still be detected.

Animals↗

Interaction of furazolidone with DNA.

DN forms a complex with furazolidone producing thereby a quenching and a bathochromic shift of the drug absorption pattern. The binding isotherm was a non-linear one indicating involvement of more than one binding process in the formation of the furazolidone - DNA complex. The furazolidone - DNA complex inhibited digestion of DNA by DNAase and stabilized DNA against thermal strand separation by a significant degree.

Binding Sites↗

DNA damage, prophage induction and mutation by furazolidone.

Ultraviolet absorption data and thermal chromatography through hydroxyapatite (HAP) column revealed that furazolidone treatment of Vibrio cholerae cells produced more than 80% of DNA reversibly bihelical due to the formation of interstrand cross-links and the reaction obeyed a first order relation. Sensitivities of the Escherichia coli strains to the lethal action of the drug were in the order: AB 2480(uvr- rec-) greater than AB 2463(rec-) greater than AB 1886(uvr-) greater than AB 1157(repair proficient) or AB 4401(wild type). Furazolidone was 'Rec test' positive, produced dose-dependent prophage induction in E. coli cells and also dose-dependent streptomycin-resistance forward mutation in V. cholerae cells. The quantitative aspect and also the mode of furazolidone action on DNA were discussed.

DNA Repair↗

Influence of thiamin supplements on furazolidone-induced cardiomyopathy in turkey poults.

Furazolidone (700 ppm) was fed to turkey poults from 2 to 5 weeks of age. The drug produced a cardiomyopathy and reduced the feed intake and growth of the birds. Thiamin was concurrently injected into the furazolidone-fed poults to determine whether the vitamin would prevent or reduce the severity of the cardiotoxic effect of the drug. Supplemental injections of thiamin had no significant effect on feed consumption or growth of the birds nor did they protect the heart against the cardiotoxicity. The conclusion is that furazolidone-induced cardiomyopathy is not caused by a thiamin deficiency.

Animals↗

Effects of furazolidone or nitrofurazone on the concentrations of hypothalamic amines and plasma luteinizing hormone (LH) and prolactin (PRL), levels in young turkeys.

1. Furazolidone (30 mg/kg) given orally for 14 days produced significant increases in the hypothalamic concentrations of noradrenaline, adrenaline and dopa. The amine concentrations returned to normal one week after withdrawal of the drug. 2. Nitrofurazone (30 mg/kg) given orally for 14 days did not affect significantly the hypothalamic amine concentrations. 3. Nitrofurazone (30 mg/kg, 14 days) increased significantly the plasma concentration of prolactin (PRL) and decreased luteinizing hormone (LH). The concentrations of the two hormones returned to normal one week after the drug withdrawal. Furazolidone (7.5, 15 or 30 mg/kg) did not influence the concentrations of either hormone. 4. Furazolidone (30 mg/kg, 14 days) did not influence the release of LH or PRL after treatment of LHRH or TRH, respectively. Nitrofurazone at the same dose, however, reduced the increases in LH and PRL concentrations induced by LHRH and TRH, respectively.

Amines↗

The anti-diamine oxidase effect of furazolidone in rabbits.

1. Furazolidone (50 mg/kg for 5 days) given orally to rabbits produced a significant inhibition of diamine oxidase (DAO) activity in various tissues. 2. Suppression of the rabbits' gut flora by oxytetracycline treatment significantly reduced the DAO inhibitory effect of furazolidone, suggesting that the gut flora may be involved in the transformation of furazolidone into an active DAO inhibitor.

Amine Oxidase (Copper-Containing)↗

The effect of probiotics on the genotoxicity of furazolidone.

Antigenotoxic activity of probiotic bacteria against furazolidone was studied using the short-term bacterial assay SOS chromotest, with Escherichia coli PQ37 as the test organism. The supernatants from probiotic and furazolidone co-incubation exhibited rather strong suppression on SOS induction produced by furazolidone on E. coli PQ 37 (sfiA: lacZ). Genotoxicity inhibition was found for all strains of the examined bacteria belonging to three genera. The highest genotoxicity inhibition was detected for Bifidobacterium lactis Bb-12 (92.0%) and for Lactobacillus acidophilus T20 (81.9%).

Anti-Infective Agents, Local↗

Use of solid phase extraction for the isolation and clean-up of a derivatised furazolidone metabolite from animal tissues.

A method is presented for the determination of protein-bound residues of furazolidone in animal tissue. The use of furazolidone in food-producing animals has been banned in the EU. Illegal use of furazolidone can be monitored most effectively by testing for bound residues containing the 3-amino-2-oxazolidone (AOZ) moiety which, unlike the parent drug, is stable and can be detected for prolonged periods after cessation of treatment. This paper reports the development of an extraction and clean-up procedure for AOZ from liver using solid phase extraction. The method replaces solvent extraction and provides extensive sample clean-up with removal of approximately 99% of the derivatising agent, 2-nitrobenzaldehyde, which may interfere with the determination. It also offers the advantage of being suitable for automation, thereby increasing throughput of samples. The extraction procedure may be used for HPLC and ELISA screening techniques. The method has been validated in fortified and incurred pig liver samples, yielding mean recovery of AOZ in excess of 60%.

Animals↗

Effect of acid secretion blockade by omeprazole on the relative bioavailability of orally administered furazolidone in healthy volunteers.

AIMS: The administration of omeprazole may interfere with the absorption of orally administered drugs by reducing gastric pH and hence tablet dissolution. The aim of this study was to investigate the effects of a 5 day administration of omeprazole on the pharmacokinetics of furazolidone. METHODS: Eighteen healthy (nine male and nine female) volunteers were selected. The study had an open randomized two-period crossover design with a 21 day washout period between the phases. Serum concentrations of furazolidone were measured by reversed-phase h.p.l.c. with ultraviolet detection. RESULTS: Administration of omeprazole caused a significant reduction of Cmax [0.34 microg x ml(-1) (range 0.25-0.43) vs 0.24 microg x ml(-1) (range 0.15-0.34)] with no significant delay in absorption tmax [2.5 h (range 1.85-3.0) vs 2.4 h (range 2.06-2.71)]. CONCLUSIONS: Furazolidone was rapidly absorbed after oral administration. Short-term treatment with omeprazole did alter the relative bioavailability of this drug, probably through an effect on absorption kinetics or first-pass metabolism.

Administration, Oral↗

Low cure rate of Helicobacter pylori infection with omeprazole and furazolidone dual therapy for one week.

BACKGROUND: Furazolidone is an inexpensive antibiotic that has considerable anti-Helicobacter pylori activity in vitro. METHODS: Twenty-three patients with culture-proven H. pylori infection were treated for one week with a dual therapy containing omeprazole and furazolidone. RESULTS: Eradication succeeded in 10 of the first 20 evaluable patients (50%; 95% CI: 27.2-72.8%). This percentage was regarded as too low, and the study was terminated. Side-effects were mild. CONCLUSION: With the possible increase in resistance to metronidazole and clarithromycin world-wide, furazolidone may be useful alternative in the treatment of H. pylori infection. Dual therapy for one week, however, is not sufficient.

Anti-Bacterial Agents↗

Furazolidone, amoxycillin, bismuth triple therapy for Helicobacter pylori infection.

BACKGROUND: Metronidazole-resistant Helicobacter pylori are generally the rule in developing countries such as Colombia. Developing countries need an effective, simple and inexpensive non-metronidazole therapy for H. pylori infection. AIM: To evaluate the combination of bismuth, furazolidone and amoxycillin for the treatment of H. pylori infection in Colombia. METHODS: Thirty patients with histologically documented H. pylori infection received the combination of bismuth subcitrate 240 mg b.d., furzolidone 100 mg q.d.s. and amoxycillin 500 mg q.d.s. for 14 days. Four or more weeks after ending therapy patients were re-endoscoped and gastric biopsies were obtained and examined using the Genta stain. Each slide was scored for presence, absence and density of H. pylori, active and chronic inflammation, intestinal metaplasia, erosions and atrophy. Cure was defined as the absence of H. pylori. RESULTS: All patients completed the course of therapy. Twenty-five patients were cured (86%, 95% CI: 65-94%). Mild, well-tolerated side-effects were reported by six patients (20%). CONCLUSIONS: This combination of bismuth, furazolidone and amoxycillin fulfills the criteria for successful H. pylori therapy and appears particularly well suited for developing countries since it is simple, inexpensive and effective. Furazolidone-containing therapies may become especially useful in the face of a world-wide increase in H. pylori resistance to metronidazole and macrolides.

Adult↗

High cure rate of Helicobacter pylori infection using tripotassium dicitrato bismuthate, furazolidone and clarithromycin triple therapy for 1 week.

BACKGROUND: When metronidazole is used in bismuth-based or proton pump inhibitor-based triple therapy, the cure rate of Helicobacter pylori is usually high. However, metronidazole-resistant H. pylori strains, which are increasing in frequency, are a major cause of failed H. pylori eradication. AIM: To evaluate the efficacy of non-metronidazole containing bismuth-based triple therapy for H. pylori infection. METHODS: One-hundred and eighty H. pylori-positive patients with endoscopically documented peptic ulcer disease or functional dyspepsia were randomly assigned to one of three 1-week regimens containing tripotassium dicitrato bismuthate (also called colloidal bismuth subcitrate) 240 mg b.d. and two antibiotics: furazolidone 100 mg b.d. plus clarithromycin 250 mg b.d. (Group A); or clarithromycin 250 mg b.d. plus amoxycillin 1000 mg b.d. (Group B); or furazolidone 100 mg b.d. plus josamycin 1000 mg b.d. (Group C). H. pylori status was assessed by rapid urease test, histology and culture of gastric biopsy specimens taken from both the antrum and corpus, both before and at least 4 weeks after completion of therapy. RESULTS: Thirteen patients dropped out (3 in group A, 5 in group B and 5 in group C). Based on an intention-to-treat analysis, the eradication rates achieved in groups A, B and C were 88% (53/60), 58% (35/60) and 77% (46/60), respectively. These differences were significant between groups A and B (P < 0.001), as well as between groups B and C (P < 0.05). Side-effects occurred in 7 (12%) patients in group A, 3 (5%) in group B and 8 (13%) in group C, and were mild, with the exception of vomiting in one patient (group C) that resulted in withdrawal from the study. CONCLUSION: One-week triple therapy, consisting of tripotassium dicitrato bismuthate, low-dose furazolidone and low-dose clarithromycin, achieves a high cure rate of H. pylori.

Adolescent↗

Omeprazole, clarithromycin and furazolidone for the eradication of Helicobacter pylori in patients with duodenal ulcer.

AIM: To evaluate the efficacy of omeprazole plus clarithromycin and furazolidone in Helicobacter pylori eradication and duodenal ulcer healing in Brazilian patients. METHODS: Forty H. pylori-positive patients with duodenal ulcer were randomized to receive 20 mg omeprazole o.m. or b.d. for 1 month plus 500 mg clarithromycin (b.d. ) and 200 mg furazolidone (b.d.) for 1 week. RESULTS: Three months after the end of the treatment the eradication rates were 90% by intention-to-treat analysis, and 97% by per protocol analysis. Mild side-effects were observed in 25 patients, none of whom abandoned the protocol. No difference was observed between the 20 mg and 40 mg omeprazole daily doses. Cure or significant improvement of the symptoms and of the histological alterations were observed after H. pylori eradication. CONCLUSION: Our results demonstrate that clarithromycin and furazolidone in combination with omeprazole are a good alternative for H. pylori eradication in Brazilian patients with duodenal ulcer.

Adolescent↗

Clarithromycin vs. furazolidone in quadruple therapy regimens for the treatment of Helicobacter pylori in a population with a high metronidazole resistance rate.

BACKGROUND: The eradication of Helicobacter pylori plays a pivotal role in the treatment of peptic ulcer disease. Metronidazole resistance, common in Iran, is claimed to be a major reason for the failure of metronidazole-containing regimens. Both clarithromycin and furazolidone are potential alternatives for metronidazole. AIM: To assess and compare the effectiveness of clarithromycin- and furazolidone-based regimens in eradicating H. pylori in a population with a high metronidazole resistance rate. METHODS: Patients with proven duodenal ulcer and H. pylori infection were randomly assigned to one of two groups. The patients received 2 weeks of omeprazole 20 mg b.d., amoxicillin 1000 mg b.d, bismuth subcitrate 240 mg b.d. and either clarithromycin 500 mg b.d. (the OABC group) or furazolidone 200 mg b.d. (the OABF group). RESULTS: A total of 118 patients were randomized, 55 in the OABC group and 63 in the OABF group. The intention-to-treat eradication rate was 84% and 85% for the OABF and OABC groups, respectively. The per protocol eradication rates were 90% for both groups. CONCLUSIONS: OABC and OABF are both effective in eradicating H. pylori in areas where metronidazole resistance is a problem. OABF is a good alternative in the face of growing resistance to clarithromycin in developed countries, and is attractive for developing countries where clarithromycin is not readily available.

Adult↗

One-week omeprazole, furazolidone and amoxicillin rescue therapy after failure of Helicobacter pylori eradication with standard triple therapies.

AIM: To test the efficacy of omeprazole, furazolidone and amoxicillin triple therapy for the treatment of Helicobacter pylori infection after failure of standard first-line therapy recommended by the Asia-Pacific Consensus on the management of H. pylori infection. METHODS: Patients with failed H. pylori eradication received omeprazole, 20 mg, furazolidone, 100 mg, and amoxicillin, 1 g, all twice daily for 1 week. Endoscopy (CLO test, histology and culture) was performed before treatment. Post-treatment H. pylori status was determined by 13C-urea breath test 6 weeks later. RESULTS: Fifty patients were recruited. Resistance to metronidazole, clarithromycin and both drugs was in the range of 50-64%, 60-75% and 40-50%, respectively, after failure of first-line therapy. Amoxicillin resistance was not found. The intention-to-treat and per protocol H. pylori eradication rates were 52% and 53%, respectively. Patients with double resistance to metronidazole and clarithromycin showed the lowest eradication rate (38%), which was significantly lower than that of patients with sensitive strains (88%). Side-effects were minimal and compliance was excellent (98%). CONCLUSIONS: One-week omeprazole, furazolidone and amoxicillin rescue therapy achieved a high eradication rate in strains sensitive to metronidazole and clarithromycin. This is a cheap and safe rescue regimen when guided by pre-treatment sensitivity testing.

Adult↗