Nitrofurantoin
(Synonyms: 呋喃妥因) 目录号 : GC32182
An antibiotic
Cas No.:67-20-9
Sample solution is provided at 25 µL, 10mM.
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Nitrofurantoin is an antibiotic.1 In vivo, nitrofurantoin (25-100 mg/kg, i.m.) reduces E. coli replication and abscess formation in the renal medulla of infected rats in a dose-dependent manner. It prevents kidney and bladder infection in rats following bladder inoculation with clinical isolates of P. mirabilis. Nitrofurantoin also prevents alkalization of urine as well as calculi and abscess formation in a rat model of P. vulgaris urinary tract infection.2 Formulations containing nitrofurantoin have been used to treat urinary tract infections.
1.Rocha, H., Da Silva Teles, E., and Barros, M.Site of action of nitrofurantoin in experimental urinary tract infectionAppl. Microbiol.18(4)547-549(1969) 2.Hossack, D.J.N.Proteus vulgaris urinary tract infections in rats; treatment with nitrofuran derivativesBr. J. Pharmacol. Chemother.19(2)306-312(1962)
| Cas No. | 67-20-9 | SDF | |
| 别名 | 呋喃妥因 | ||
| Canonical SMILES | O=C1NC(CN1/N=C/C2=CC=C([N+]([O-])=O)O2)=O | ||
| 分子式 | C8H6N4O5 | 分子量 | 238.16 |
| 溶解度 | DMSO : ≥ 40 mg/mL (167.95 mM) | 储存条件 | Store at 2-8°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 | 4.1989 mL | 20.9943 mL | 41.9886 mL |
| 5 mM | 0.8398 mL | 4.1989 mL | 8.3977 mL |
| 10 mM | 0.4199 mL | 2.0994 mL | 4.1989 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 | ||||||||||
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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。
Nitrofurantoin's efficacy and safety as prophylaxis for urinary tract infections: a systematic review of the literature and meta-analysis of controlled trials
Clin Microbiol Infect 2017 Jun;23(6):355-362.PMID:27542332DOI:10.1016/j.cmi.2016.08.003.
Objectives: Nitrofurantoin has been used for the prevention of urinary tract infection (UTI) for over 60 years. We conducted a systematic review and meta-analysis to assess its efficacy and safety in the prophylaxis of UTI. Methods: We performed a systematic review of all controlled trials in humans assessing Nitrofurantoin for UTI prophylaxis published from 1946 to 2015. We further reviewed population-level cohort studies evaluating Nitrofurantoin's toxicity. Meta-analyses assessing efficacy and adverse events were conducted on controlled trials. Results: Twenty-six controlled trials including 3052 patients fulfilled entry criteria for the systematic review and meta-analysis on efficacy and toxicity, and 16 population-level cohort studies were identified for review of toxicity. Overall quality was poor, with all studies at increased risk for various biases. When compared with no prophylaxis, Nitrofurantoin is effective in the prevention of UTI (risk ratio 0.38 in favour of Nitrofurantoin, 95% CI 0.30-0.48). Its prophylactic efficacy is superior to that of methenamine hippurate and comparable to that of other antibacterials. Compared with patients receiving other antibacterials, those receiving Nitrofurantoin had an increased risk of 2.24 (95% CI 1.77-2.83) for a non-severe adverse effect. In all controlled trials, only one patient experienced a severe adverse effect (interstitial pneumonia). Cohort studies reported severe adverse effect frequencies of 0.02-1.5 per 1000 Nitrofurantoin users. Conclusions: Nitrofurantoin is effective in the prevention of UTI. Its use may be associated with increased non-severe adverse effects; severe adverse effects occur infrequently. The risk of severe toxicity seems to increase with the duration of Nitrofurantoin prophylaxis.
Nitrofurantoin revisited: a systematic review and meta-analysis of controlled trials
J Antimicrob Chemother 2015 Sep;70(9):2456-64.PMID:26066581DOI:10.1093/jac/dkv147.
Objectives: Nitrofurantoin's use has increased exponentially since recent guidelines repositioned it as first-line therapy for uncomplicated lower urinary tract infection (UTI). We conducted a systematic review and meta-analysis to assess Nitrofurantoin's efficacy and toxicity in the treatment of lower UTI. Methods: We performed a systematic review of all human controlled clinical trials published from 1946 to 2014 and assessing short-term (鈮?4 days) Nitrofurantoin for lower UTI. Meta-analyses assessing efficacy and adverse events were conducted on randomized trials. Results: Twenty-seven controlled trials including 4807 patients fulfilled entry criteria; most were conducted between the 1970s and 1990s and were at increased risk for various biases. Nitrofurantoin appears to have good clinical and microbiological efficacy for UTI caused by common uropathogens, with clinical cure rates varying between 79% and 92%. The most methodologically robust studies surveyed indicate overall equivalence between Nitrofurantoin when given for 5 or 7 days and trimethoprim/sulfamethoxazole, ciprofloxacin and amoxicillin. Meta-analyses of randomized controlled trials confirmed equivalence in clinical cure, but indicated a slight advantage to comparator drugs in microbiological efficacy (risk ratio 0.93, 95% CI 0.89-0.97). If given for only 3 days, Nitrofurantoin's clinical efficacy was diminished (61%-70%). Toxicity was infrequent (5%-16% in the 17 reporting studies), mild, reversible and predominantly gastrointestinal; meta-analyses confirmed no difference between Nitrofurantoin and comparators. Hypersensitivity reactions such as pulmonary fibrosis and hepatotoxicity were not observed. Acquisition of resistance to Nitrofurantoin is still relatively rare. Conclusions: When given short term for lower UTI, Nitrofurantoin has good clinical and microbiological efficacy; toxicity is mild and predominantly gastrointestinal.
Awareness of long-term Nitrofurantoin adverse effects
Drug Ther Bull 2022 Apr;60(4):59.PMID:35121574DOI:10.1136/dtb.2022.000005.
Overview of: Speirs TP, Tuffin N, Mundy-Baird F, et al Long-term Nitrofurantoin: an analysis of complication awareness, monitoring, and pulmonary injury cases. BJGP Open 2021;5:BJGPO.2021.0083.
Nitrofurantoin--current concepts
Urology 1988 Jul;32(1):67-71.PMID:3291373DOI:10.1016/0090-4295(88)90460-8.
Bacterial drug resistance has become a major concern for urologists in the treatment of urinary tract infection (UTI). One drug which has managed to avoid such resistance problems in its thirty years of use is Nitrofurantoin. Nitrofurantoin is effective therapeutically for the treatment of acute lower tract infections, chronic UTI, and for the suppression of catheter-associated bacteria. On a prophylactic basis it is used to sterilize urine before TURP and to prevent chronic reinfection. Its unique mechanism of action, site specificity, achievement of high urinary levels and low serum concentrations, and its effectiveness against both gram-negative and gram-positive bacteria provide many advantages in UTI therapy that many of the newer agents do not. Adverse drug reactions, especially pulmonary toxicity, are extremely rare, and Nitrofurantoin maintains an excellent safety profile.
Nitrofurantoin-induced hepatotoxicity: a rare yet serious complication
South Med J 2014 Feb;107(2):107-13.PMID:24926677DOI:10.1097/SMJ.0000000000000059.
Nitrofurantoin is a commonly prescribed antibiotic for the treatment of recurrent uncomplicated urinary tract infections. Its importance has been emphasized by the current international clinical practice guidelines for the management of uncomplicated cystitis. Since its introduction into clinical practice, Nitrofurantoin has been associated with various adverse effects, including hepatotoxicity. We searched the English-language literature using PubMed and SCOPUS for the period 1961 through the end of February 2013. Key search terms included "Nitrofurantoin AND hepatotoxicity" as well as "Nitrofurantoin AND hepatitis." When studies or case reports were found, we assessed articles cited in those publications. A broad spectrum of liver toxicity associated with Nitrofurantoin use has been reported, ranging from acute hepatitis, granulomatous reaction, cholestasis, or autoimmune-mediated hepatitis to chronic active hepatitis that could lead to cirrhosis or death. The mechanism of hepatotoxicity is poorly understood, but it is believed to be the result of an immunologic process or a direct cytotoxic reaction. It has been postulated that prolonged exposure to Nitrofurantoin, female sex, advanced age, and reduced renal function increase the risk of developing hepatotoxicity. For the management of severe cases, corticosteroids have been used along with Nitrofurantoin discontinuation. Because of mixed results, the utility of corticosteroids has not been proven and should be used judiciously. Given the severity and seriousness of the adverse effect of hepatotoxicity, clinicians should weigh the risks and benefits of Nitrofurantoin before initiating therapy, especially in long-term prophylaxis in high-risk patients. Clinicians also should be well versed in recognizing and managing liver injury associated with Nitrofurantoin.