Fosfomycin Trometamol
(Synonyms: 磷霉素氨丁三醇; MK-0955 tromethamine) 目录号 : GC43698A broad-spectrum antibiotic
Cas No.:78964-85-9
Sample solution is provided at 25 µL, 10mM.
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Fosfomycin trometamol is a broad-spectrum antibiotic that is active against Gram-negative and Gram-positive bacteria with MIC90 values of 8, 32, 4, and 32 µg/mL for ESBL E. coli, carbapenemase-producing K. pneumoniae, P. mirabilis, and methicillin-resistant S. saprophyticus, respectively, in a broth microdilution assay. It is an inhibitor of uridine diphospho-N-acetyl-D-glucosamine enolpyruvyl transferase (MurA) that enters cells via the glycerol-3-phosphate and hexose-6-phosphate transporters. Formulations containing fosfomycin trometamol have been used in the treatment of urinary tract infections.
Cas No. | 78964-85-9 | SDF | |
别名 | 磷霉素氨丁三醇; MK-0955 tromethamine | ||
Canonical SMILES | C[C@H]1[C@@H](P(O)(O)=O)O1.OCC(CO)(N)CO | ||
分子式 | C4H11NO3•C3H7O4P | 分子量 | 259.2 |
溶解度 | H2O : 250 mg/mL (964.54 mM; Need ultrasonic) | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.858 mL | 19.2901 mL | 38.5802 mL |
5 mM | 0.7716 mL | 3.858 mL | 7.716 mL |
10 mM | 0.3858 mL | 1.929 mL | 3.858 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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。
Fosfomycin Trometamol for the Prevention of Infectious Complications After Prostate Biopsy: A Consensus Statement by an International Multidisciplinary Group
Eur Urol Focus 2022 Sep;8(5):1483-1492.PMID:34920977DOI:10.1016/j.euf.2021.11.007.
Context: Transrectal ultrasound-guided prostate biopsy (TRPB) has been a standard of care for diagnosing prostate cancer but is associated with a high incidence of infectious complications. Objective: To achieve an expert consensus on whether Fosfomycin Trometamol provides adequate prophylaxis in TRPB and discuss its role as prophylaxis in transperineal prostate biopsy (TPPB). Evidence acquisition: An international multidisciplinary group of experts convened remotely to discuss how to best use fosfomycin in various clinical settings and patient situations. Six statements related to prostate biopsy and the role of fosfomycin were developed, based on literature searches and relevant clinical experience. Evidence synthesis: Consensus was reached for all six statements. The group of experts was unanimous regarding fosfomycin as a preferred candidate for antimicrobial prophylaxis in TRPB. Fosfomycin potentially also meets the requirements for empiric prophylaxis in TPPB, although further clinical studies are needed to confirm or refute its utility in this setting. There is a risk of bias due to sponsorship by a pharmaceutical company. Conclusions: Antimicrobial prophylaxis is mandatory in TRPB, and Fosfomycin Trometamol is an appropriate candidate due to low rates of resistance, a good safety profile, sufficient prostate concentrations, and demonstrated efficacy in reducing the risk of infectious complications following TRPB. Patient summary: Patients undergoing transrectal ultrasound-guided prostate biopsy (TRPB) have a high risk of infectious complications, and antimicrobial prophylaxis is mandatory. However, increasing antimicrobial resistance, as well as safety concerns with fluoroquinolones, has restricted the number of antimicrobial options. Fosfomycin Trometamol meets the requirements for a preferred antimicrobial in the prophylaxis of TRPB.
Effectiveness of Fosfomycin for the Treatment of Multidrug-Resistant Escherichia coli Bacteremic Urinary Tract Infections: A Randomized Clinical Trial
JAMA Netw Open 2022 Jan 4;5(1):e2137277.PMID:35024838DOI:10.1001/jamanetworkopen.2021.37277.
Importance: The consumption of broad-spectrum drugs has increased as a consequence of the spread of multidrug-resistant (MDR) Escherichia coli. Finding alternatives for these infections is critical, for which some neglected drugs may be an option. Objective: To determine whether fosfomycin is noninferior to ceftriaxone or meropenem in the targeted treatment of bacteremic urinary tract infections (bUTIs) due to MDR E coli. Design, setting, and participants: This multicenter, randomized, pragmatic, open clinical trial was conducted at 22 Spanish hospitals from June 2014 to December 2018. Eligible participants were adult patients with bacteremic urinary tract infections due to MDR E coli; 161 of 1578 screened patients were randomized and followed up for 60 days. Data were analyzed in May 2021. Interventions: Patients were randomized 1 to 1 to receive intravenous fosfomycin disodium at 4 g every 6 hours (70 participants) or a comparator (ceftriaxone or meropenem if resistant; 73 participants) with the option to switch to oral Fosfomycin Trometamol for the fosfomycin group or an active oral drug or parenteral ertapenem for the comparator group after 4 days. Main outcomes and measures: The primary outcome was clinical and microbiological cure (CMC) 5 to 7 days after finalization of treatment; a noninferiority margin of 7% was considered. Results: Among 143 patients in the modified intention-to-treat population (median [IQR] age, 72 [62-81] years; 73 [51.0%] women), 48 of 70 patients (68.6%) treated with fosfomycin and 57 of 73 patients (78.1%) treated with comparators reached CMC (risk difference, -9.4 percentage points; 1-sided 95% CI, -21.5 to ∞ percentage points; P = .10). While clinical or microbiological failure occurred among 10 patients (14.3%) treated with fosfomycin and 14 patients (19.7%) treated with comparators (risk difference, -5.4 percentage points; 1-sided 95% CI, -∞ to 4.9; percentage points; P = .19), an increased rate of adverse event-related discontinuations occurred with fosfomycin vs comparators (6 discontinuations [8.5%] vs 0 discontinuations; P = .006). In an exploratory analysis among a subset of 38 patients who underwent rectal colonization studies, patients treated with fosfomycin acquired a new ceftriaxone-resistant or meropenem-resistant gram-negative bacteria at a decreased rate compared with patients treated with comparators (0 of 21 patients vs 4 of 17 patients [23.5%]; 1-sided P = .01). Conclusions and relevance: This study found that fosfomycin did not demonstrate noninferiority to comparators as targeted treatment of bUTI from MDR E coli; this was due to an increased rate of adverse event-related discontinuations. This finding suggests that fosfomycin may be considered for selected patients with these infections. Trial registration: ClinicalTrials.gov Identifier: NCT02142751.
Fosfomycin Trometamol: a review of its use as a single-dose oral treatment for patients with acute lower urinary tract infections and pregnant women with asymptomatic bacteriuria
Drugs 2013 Nov;73(17):1951-66.PMID:24202878DOI:10.1007/s40265-013-0143-y.
Fosfomycin Trometamol (fosfomycin tromethamine) [Monuril(®), Monurol(®), Monural(®)] is approved in numerous countries worldwide, mainly for the treatment of uncomplicated urinary tract infections (UTIs). Fosfomycin has good in vitro activity against common uropathogens, such as Escherichia coli (including extended-spectrum β-lactamase-producing E. coli), Proteus mirabilis, Klebsiella pneumoniae and Staphylococcus saprophyticus, and the susceptibility of uropathogens to fosfomycin has remained relatively stable over time. A single oral dose of Fosfomycin Trometamol 3 g (the approved dosage) achieves high concentrations in urine. Results of recent randomized trials indicate that single-dose Fosfomycin Trometamol had similar clinical and/or bacteriological efficacy to 3- to 7-day regimens of ciprofloxacin, norfloxacin, cotrimoxazole or nitrofurantoin in women with uncomplicated lower UTIs. In addition, single-dose Fosfomycin Trometamol had similar bacteriological efficacy to a 5-day course of cefuroxime axetil or a 7-day course of amoxicillin/clavulanic acid in pregnant women with asymptomatic bacteriuria, and similar clinical and/or bacteriological efficacy to a 5-day course of cefuroxime axetil or amoxicillin/clavulanic acid or a 3-day course of ceftibuten in pregnant women with a lower UTI. Single-dose Fosfomycin Trometamol was generally well tolerated, with gastrointestinal adverse events (e.g. diarrhoea, nausea) reported most commonly. In conclusion, single-dose Fosfomycin Trometamol is an important option for the first-line empirical treatment of uncomplicated lower UTIs.
Prevention of recurrent urinary tract infections
Minerva Urol Nefrol 2013 Mar;65(1):9-20.PMID:23538307doi
Urinary tract infections (UTI) are among the most frequent bacterial infections in the community and health care setting. Mostly young and, to some extent, postmenopausal women are affected by recurrent UTI (rUTI) defined as ≥3 UTI/year or ≥2 UTI/half year. In contrast, rUTI is rare in healthy men. On the other hand, rUTI are frequently found in female and male patients with complicating urological factors, e.g. urinary catheters, infection stones. Remediable predisposing factors in uncomplicated rUTI in women are rare. In complicated rUTI the success depends mainly on the possibility to eliminate or at leastimprove the complicating risk factors. Continuous antibiotic prophylaxis or postcoital prophylaxis, if there is close correlation with sexual intercourse, are most effective to prevent rUTI. Nitrofurantoin, trimethoprim (or cotrimoxazole), and Fosfomycin Trometamol are available as first-line drugs. Oral cephalosporins and quinolones should be restricted to specific indications. Antibiotic prophylaxis reduces the number of uropathogens in the gut and/or vaginal flora and reduces bacterial "fitness". Given the correct indication, the recurrence rate of rUTI can be reduced by about 90%. Due to possible adverse events and the concern of selecting resistant pathogens, according to the guidelines of the European Association of Urology antimicrobial prophylaxis should be considered only after counselling, behavioural modification and non-antimicrobial measures have been attempted. In postmenopausal patients vaginal substitution of oestriol should be started first. Oral or parenteral immunoprophylaxis is another option in patients with rUTI. Other possibilities with varying scientific evidence are prophylaxis with cranberry products, specific plant combinations or probiotics. The prophylaxis of catheter-associated UTI should employ strategies which result in a reduction of frequency and duration of catheter drainage of the urinary tract. The currently available catheter materials have only little influence on reducing catheter-associated rUTI.
[Recommendations on the diagnosis and treatment of urinary tract infection]
An Pediatr (Engl Ed) 2019 Jun;90(6):400.e1-400.e9.PMID:30979681DOI:10.1016/j.anpedi.2019.02.009.
Urinary tract infection (UTI) is defined as the growth of microorganisms in a sterile urine culture in a patient with compatible clinical symptoms. The presence of bacteria without any symptoms is known as asymptomatic bacteriuria, and does not require any treatment. In neonates and infants, fever is the guiding sign to suspecting a UTI. Classic urinary tract symptoms become more important in older children. Urine cultures collected before starting antibiotics is always required for diagnosis. Clean-catch (midstream) specimens should be collected for urine culture. In the case of non-toilet-trained children, specimens must be obtained by urinary catheterisation, or suprapubic puncture in neonates and infants. Specimens collected by urine bag should not be used for urine culture. There are no significant differences in the clinical evolution and prognosis between oral versus short intravenous followed by oral antibiotic. Empirical antibiotic therapy should be guided by local susceptibility patterns. Second-generation cephalosporin (children under 6 years) and Fosfomycin Trometamol (over 6 years), are the empiric therapy recommended in this consensus. In the case of pyelonephritis, recommended antibiotic treatment are third-generation cephalosporins (outpatient care) or, if admission is required, aminoglycosides. Ampicillin should be added in infants less than 3 months old. Antibiotic de-escalation should be always practiced once the result of the urine culture is known.