Furazolidone
(Synonyms: 呋喃唑酮) 目录号 : GC32138
A nitrofuran antiprotozoal and antibacterial agent
Cas No.:67-45-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Furazolidone is a nitrofuran antiprotozoal agent and antibacterial agent.1,2,3 It is active against G. lamblia trophozoites (IC50 = 2.9 ?M), as well as metronidazole-susceptible and -resistant T. vaginalis clinical isolates with minimum lethal concentration (MLC) values of less than 3.1 ?g/ml.1,2 Furazolidone is also active against clinical isolates of Salmonella, Shigella, E. coli, and V. parahaemolyticus (MICs = ≤0.5-4 ?g/ml).3 In vivo, furazolidone (50 mg/kg per day) reduces splenic and hepatic parasite burden in a golden hamster model of L. chagasi infection.4 Formulations containing furazolidone have been used in the treatment of bacterial and protozoal infections.
1.Campanati, L., and Monteiro-Leal, L.H.The effects of the antiprotozoal drugs metronidazole and furazolidone on trophozoites of Giardia lamblia (P1 strain)Parasitol Res.88(1)80-85(2002) 2.Narcisi, E.M., and Secor, W.E.In vitro effect of tinidazole and furazolidone on metronidazole-resistant Trichomonas vaginalisAntimicrob. Agents and Chemother.40(5)1121-1125(1996) 3.Carlson, J.R., Thornton, S.A., Dupont, H.L., et al.Comparative in vitro activities of ten antimicrobial agents against bacterial enteropathogensAntimicrob. Agents Chemother.24(4)509-513(1983) 4.Tempone, A.G., Mortara, R.A., de Andrade, H.F., Jr., et al.Therapeutic evaluation of free and liposome-loaded furazolidone in experimental visceral leishmaniasisInt. J. Antimicrob. Agents36(2)159-163(2010)
| Cas No. | 67-45-8 | SDF | |
| 别名 | 呋喃唑酮 | ||
| Canonical SMILES | O=C1OCCN1/N=C/C2=CC=C([N+]([O-])=O)O2 | ||
| 分子式 | C8H7N3O5 | 分子量 | 225.16 |
| 溶解度 | DMSO : 10 mg/mL (44.41 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4413 mL | 22.2064 mL | 44.4129 mL |
| 5 mM | 0.8883 mL | 4.4413 mL | 8.8826 mL |
| 10 mM | 0.4441 mL | 2.2206 mL | 4.4413 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Furazolidone treatment for Helicobacter Pylori infection: A systematic review and meta-analysis
Helicobacter 2018 Apr;23(2):e12468.PMID:29480532DOI:10.1111/hel.12468.
Antibiotic resistance is a major cause of Helicobacter pylori (H. pylori) treatment failures. Because the resistance rate of H. pylori to Furazolidone is low, we aimed to assess the efficacy and safety of Furazolidone. We searched the PubMed, Web of Science, Cochrane Library, and Embase databases and included randomized controlled trials (RCT) that either compared Furazolidone to other antibiotics or changed the administered dose of Furazolidone. A total of 18 articles were included in the meta-analysis. According to the intention-to-treat (ITT) analysis, the total eradication rates of furazolidone-containing therapy were superior to those of other antibiotic-containing therapies (relative risk [RR] 1.07, 95% confidence interval [CI] 1.01-1.14) (13 RCTs). Specifically, the eradication rates of furazolidone-containing therapy were better than those for metronidazole-containing therapy (RR 1.10, 95% CI: 1.01-1.21 for ITT). The eradication rate of furazolidone-containing bismuth-containing quadruple therapy was 92.9% (95% CI: 90.7%-95.1%) (PP). In addition, a higher daily dose of Furazolidone increased the eradication rate (RR 1.17, 95% CI: 1.05-1.31). And the incidence of some adverse effects, such as fever and anorexia, was higher in the Furazolidone group than in the control group, the overall incidences of total side effects and severe side effects showed no significant differences between the groups. Furazolidone-containing treatments could achieve satisfactory eradication rates and did not increase the incidence of total or severe adverse effects, but the incidence of milder side effects, such as fever and anorexia, should be considered when prescribing furazolidone-containing treatments to patients.
Furazolidone-based therapies for Helicobacter pylori infection: a pooled-data analysis
Saudi J Gastroenterol 2012 Jan-Feb;18(1):11-7.PMID:22249086DOI:10.4103/1319-3767.91729.
Background/aim: Furazolidone-based therapies are used in developing countries to cure Helicobacter pylori infection due to its low cost. The low bacterial resistance toward Furazolidone may render appealing the use of this drug even in developed countries. However, some relevant safety concerns do exist in using Furazolidone. Patients and methods: This was a systematic review with pooled-data analysis of data regarding both eradication rate and safety of furazolidone-based therapies for H. pylori infection. Intention-to-treat (ITT) and per-protocol (PP) eradication rates were calculated. Results: Following furazolidone-based first-line therapy, H. pylori eradication rates were 75.7% and 79.6% at ITT and PP analysis, respectively (P<0.001). The overall incidence of side effects and severe side effects were 33.2% and 3.8%, respectively. At multivariate analysis, only high-dose Furazolidone was associated with increased therapeutic success (OR: 1.5, 95% CI: 1.3-2.7; P<0.001), while occurrence of side effects was relevant following treatment for a long duration (OR: 2.9, 95% CI: 2.2-4.1; P<0.001), high-dose Furazolidone (OR: 2.3, 95% CI: 1.7-3.2; P<0.001) and bismuth-containing regimens (OR: 2.1, 95% CI: 1.5-2.8; P<0.001). Conclusions: Furazolidone-based regimens usually achieve low eradication rates. Only a high-dose regimen improves the cure rate, but simultaneously increases the incidence of severe side effects. Therefore, we suggest that patients have to be clearly informed about the possible genotoxic and carcinogenetic effects for which Furazolidone use is not approved in developed countries.
Furazolidone-induced pulmonary hypersensitivity
Ann Pharmacother 2005 Feb;39(2):377-9.PMID:15644484DOI:10.1345/aph.1E080.
Objective: To report a case of pulmonary hypersensitivity associated with Furazolidone use and review the literature on this topic. Case summary: A 43-year-old white female presented with fever and dyspnea. She had recently completed a course of Furazolidone 125 mg 4 times daily for 10 days for enteritis. Investigations revealed bibasilar interstitial infiltrates on chest X-ray, hypoxia, and 21% eosinophilia. Her fever, hypoxia, and dyspnea rapidly abated following discontinuation of Furazolidone and administration of corticosteroids. Discussion: Furazolidone is a bactericidal agent used to treat infectious enteropathies. It is chemically similar to nitrofurantoin, which is well known to cause pulmonary hypersensitivity reactions. Application of the Naranjo probability scale suggests that a Furazolidone adverse reaction in this patient was probable. A MEDLINE search from 1966 to October 2004 revealed 2 previously reported cases suggestive of Furazolidone pulmonary hypersensitivity. All published reports closely resemble each other and descriptions of nitrofurantoin-associated pulmonary hypersensitivity reactions. Conclusions: Furazolidone may induce pulmonary hypersensitivity reactions; clinicians should be aware of this potentially serious adverse effect.
Some pharmacological and toxicological properties of Furazolidone
Vet Res Commun 1983 Jan;6(1):1-11.PMID:6346666DOI:10.1007/BF02214890.
The pharmacological and toxicological properties of Furazolidone have been briefly reviewed. Among the most important pharmacological actions of Furazolidone is the inhibition of mono- and diamine oxidase activities, which seem to depend, at least in some species, on the presence of the gut flora. The drug also seems to interfere with the utilization of thiamin, which is probably instrumental in the production of anorexia and loss of body weight of the treated animals. Furazolidone is known to induce a condition of cardiomyopathy in turkeys, which could be used as a model to study alpha 1-antitrypsin deficiency in man. The drug is most toxic to ruminants. The toxic signs observed were of nervous nature. Experiments are in progress in this laboratory to try to explain the mechanism(s) by which this toxicity is brought about. It is uncertain whether the use of Furazolidone at the recommended therapeutic dose would result in drug residues in tissues of treated animals. This is a matter of public health importance as the drug has been shown to possess a carcinogenic activity. It is important that a simple and reliable method of identification and estimation of Furazolidone residues be devised. More work is needed to elucidate the mode of action and biochemical effects caused by the drug in both the host and the infective organisms.
Furazolidone and Nitrofurazone Metabolic Studies in Crucian Carp by Ultra-Performance Liquid Chromatography Tandem Mass Spectrometry
J Chromatogr Sci 2022 Dec 13;60(10):963-969.PMID:35428881DOI:10.1093/chromsci/bmac024.
In this work, the detection of the Furazolidone (FZD) and nitrofurazone (NFZ) metabolites residuals in crucian carp are focused. Crucian carps of identical size were exposed to the mixed nitrofuran antibiotics under optimized bath conditions at a concentration of 50 mg/L, 26 ± 0.5°C for 24 h. Then, liquid chromatography-electrospray ionization-triple quadrupole mass spectrometry (LC-ESI-MSMS) was performed after the drug exposure experiments when the nitrofuran metabolites were enriched in organisms. During the period of 0-144 h, residue levels of the 3-amino-2-oxazolidinone (AOZ) gradually decreased with a prolonged sampling time. The changing trend in semicarbazide (SEM) with the sample collection duration is divided into two stages, and its concentration showed a trend of rising first and then falling. The metabolite concentration-time curve demonstrates that 24 h was used as a sampling time, and fish muscle was selected as tissue samples in the further quantitative study. A novel crucian carp-enrichment procedure coupled to LC-ESI-MSMS quantitative method was further explored based on much metabolite data. According to the exponential curve of the SEM-to-AOZ concentration ratio at a precisely designed FZD-to-NFZ mass ratio, the final FZD content of the veterinary NFZ antibiotics was 0.069 ± 0.005% (in terms of mass).