Cefuroxime axetil
(Synonyms: 头孢呋辛酯) 目录号 : GC39548
Cefuroxime axetil, a prodrug of the cephalosporin cefuroxime, is a second generation oral cephalosporin antibiotic with in vitro antibacterial activity against several gram-positive and gram-negative organisms.
Cas No.:64544-07-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefuroxime axetil, a prodrug of the cephalosporin cefuroxime, is a second generation oral cephalosporin antibiotic with in vitro antibacterial activity against several gram-positive and gram-negative organisms.
| Cas No. | 64544-07-6 | SDF | |
| 别名 | 头孢呋辛酯 | ||
| Canonical SMILES | O=C(C(N12)=C(COC(N)=O)CS[C@]2([H])[C@H](NC(/C(C3=CC=CO3)=N\OC)=O)C1=O)OC(OC(C)=O)C | ||
| 分子式 | C20H22N4O10S | 分子量 | 510.47 |
| 溶解度 | DMSO: 250 mg/mL (489.74 mM) | 储存条件 | 4°C, protect from light |
| 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 | 1.959 mL | 9.7949 mL | 19.5898 mL |
| 5 mM | 0.3918 mL | 1.959 mL | 3.918 mL |
| 10 mM | 0.1959 mL | 0.9795 mL | 1.959 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。
Cefuroxime axetil
Drug Intell Clin Pharm 1988 Sep;22(9):651-8.PMID:3063476DOI:10.1177/106002808802200901.
Cefuroxime axetil is a orally active prodrug formulation of cefuroxime, which upon absorption undergoes immediate deesterification to free cefuroxime. Cefuroxime axetil offers an in vitro antibacterial spectrum against many gram-positive and some gram-negative organisms. Its beta-lactamase stability makes it useful in treating a variety of infections caused by beta-lactamase-producing strains of Haemophilus influenzae, Branhamella catarrhalis, and Staphylococcus aureus. Cefuroxime axetil has good activity against the Enterobacteriaceae and moderate activity against non-Bacteroides fragilis anaerobes. Clinical studies suggest it is at least as effective as ampicillin, amoxicillin, amoxicillin/clavulanic acid, penicillin V, or cefaclor in the treatment of uncomplicated urinary tract infections, acute otitis media, upper respiratory infections, skin and soft tissue infections, and uncomplicated gonorrhea.
Cefuroxime axetil
Int J Antimicrob Agents 1994 Mar;4(1):23-36.PMID:18611587DOI:10.1016/0924-8579(94)90061-2.
Cefuroxime is the first commercially-available second-generation cephalosporine to be widely used in therapy; it is a semi-synthetic cephalosporin obtained from the 7-cephalosporanic acid nucleus of cephalosporin C. Cefuroxime axetil is the acetoxyethyl ester of cefuroxime. The majority of micro-organisms associated with respiratory infections are highly sensitive to cefuroxime. These include Haemophilus influenzae, Streptococcus pneumoniae, Streptococcus pyogenes and the other streptococci (excluding group D streptococci), and Moraxella catarrhalis. Bacteria sensitive to cefuroxime include the enterobacteria (Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, and Salmonella and Shigella and Straphylococcus aureus (methicillin-sensitive strains). The pharmacokinetic studies show that the maximum plasma concentration of cefuroxime after oral administration of 250 mg and 500 mg of Cefuroxime axetil after a meal are respectively 4.6 and 7.9 mg/l. The absolute bioavailability of tablets is 68% (extremes 63-73%) after oral administration of 500 mg Cefuroxime axetil. The protein binding is 33+/-5.7%. Tissue diffusion was studied in the interstitial fluid, the bronchial mucosa, the tonsils, and the bronchial secretions. Cefuroxime axetil is available as capsule-shaped tablets containing 125, 250 or 500 mg. An oral suspension dosage form for paediatric purposes is also available as granules in multidose bottles and sachets. Constitution gives a suspension containing 125 mg or 250 mg cefuroxime (as Cefuroxime axetil). Cefuroxime axetil is indicated for the treatment of infections caused by susceptible bacteria. Indications include: lower respiratory tract infections (e.g., acute and chronic bronchitis and pneumonia); upper respiratory tract infections (e.g., ear, nose and throat infections such as otitis media, sinusitis tonsillitis and pharyngitis); genito-urinary tract infections (e.g., pyelonephritis, cystitis and urethritis, gonorrhoea, acute uncomplicated gonococcal urethritis and cervicitis); and skin and soft tissue infections (e.g., furunculosis, pyoderma and impetigo). For most infections, a dose of 250 mg twice daily is appropriate. In some urinary tract infections, 125 mg twice daily has been shown to be effective. If pneumonia is suspected or in more severe lower respiratory tract infection, doses of 500 mg bd should be used. Uncomplicated gonorrhoea has been shown to respond to a single 1-g dose of Cefuroxime axetil. Adverse reactions to cefuroxime have generally been mild and transient in nature (gastrointestinal disturbances, including diarrhoea, nausea and vomiting).
Cefuroxime axetil: an updated review of its use in the management of bacterial infections
Drugs 2001;61(10):1455-500.PMID:11558834DOI:10.2165/00003495-200161100-00008.
Cefuroxime axetil, a prodrug of the cephalosporin cefuroxime, has proven in vitro antibacterial activity against several gram-positive and gram-negative organisms, including those most frequently associated with various common community-acquired infections. In numerous randomised, controlled trials, 5 to 10 days' treatment with oral Cefuroxime axetil (250 or 500 mg twice daily) was an effective treatment in patients with upper (URTI) and lower respiratory tract infections (LRTI) as assessed by clinical and bacteriological criteria. The drug was as effective as several other cephalosporins, quinolones, macrolides and amoxicillin/clavulanic acid. Shorter courses (5 to 10 days') of Cefuroxime axetil were at least as effective as a 10 day course. Furthermore, sequential therapy with intravenous cefuroxime (750 mg 2 or 3 times daily for 2 to 5 days) followed by oral Cefuroxime axetil (500 mg twice daily for 3 to 8 days) proved an effective treatment in adult patients with community-acquired pneumonia (CAP). This approach provided similar efficacy to intravenous ampicillin/sulbactam followed by oral amoxicillin/clavulanic acid, a full parenteral course of cefuroxime, or intravenous then oral azithromycin or clarithromycin. Additionally, Cefuroxime axetil was an effective treatment in patients with genitourinary, skin and soft-tissue infections, and erythema migrans associated with early stage Lyme disease. The drug is well tolerated by adult and paediatric patients, with adverse effects that are consistent with those of other cephalosporins. The majority of adverse events (primarily gastrointestinal disturbances) were mild to moderate in intensity and reversible upon discontinuation of treatment, with very few serious adverse events reported. Conclusions: Cefuroxime axetil is a broad spectrum antibacterial agent with a pharmacokinetic profile that permits convenient twice-daily administration. The drug is an effective and well tolerated treatment in patients with various infections, including otitis media, pharyngitis, sinusitis, CAP and acute exacerbations of chronic bronchitis. Cefuroxime axetil proved effective as a component of intravenous/oral sequential therapy in the treatment of CAP, although there are currently no dosage recommendations available for this regimen in some countries. Cefuroxime axetil may be considered as an empirical therapy for a range of community-acquired infections, including those in which beta-lactamase-producing strains of common respiratory pathogens are identified as the causative organisms. In an era of rapidly emerging bacterial resistance, empirical treatment with bacterial agents, potentially preventing the emergence of bacterial resistance to agents such as Cefuroxime axetil may ensure the appropriate use of newer antibacterial agents, potentially preventing the emergence of bacterial resistance to these newer drugs.
Cefuroxime axetil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy
Drugs 1996 Jul;52(1):125-58.PMID:8799689DOI:10.2165/00003495-199652010-00009.
Cefuroxime axetil is an oral cephalosporin which is rapidly hydrolysed to the active parent compound, cefuroxime. Cefuroxime has a broad spectrum of in vitro antibacterial activity which encompasses methicillin-sensitive staphylococci and the common respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci. Cefuroxime has broad spectrum activity against the beta-lactamase positive respiratory pathogens H. influenzae and M. catarrhalis; it is also active against penicillin-susceptible and -intermediate strains of S. pneumoniae. In clinical trials, Cefuroxime axetil (administered twice daily) has been evaluated in the treatment of upper and lower respiratory tract infections and has demonstrated similar efficacy to established antibacterial agents, including amoxicillin/clavulanic acid and cefaclor. Five days' treatment with Cefuroxime axetil was recently shown to be as effective as 10 days' treatment with either Cefuroxime axetil or amoxicillin/clavulanic acid in patients with acute otitis media or acute bronchitis. Cefuroxime axetil was at least as effective as phenoxymethylpenicillin (penicillin V) in the treatment of patients with group A beta-haemolytic streptococcal tonsillopharyngitis. A number of studies have evaluated the efficacy of Cefuroxime axetil as the oral component of intravenous to oral sequential therapy in hospitalised patients with lower respiratory tract infection. In each study patients received parenteral cefuroxime for approximately 2 days followed by Cefuroxime axetil for 5 to 10 days. In comparative studies, cefuroxime sequential therapy was as effective as amoxicillin/ clavulanic acid sequential therapy and full courses of parenteral cefuroxime, cefotiam or cefoperazone. Adults with urinary tract infections and skin infections were also effectively treated with Cefuroxime axetil, as were adults and adolescents with early stage lyme disease. Cefuroxime axetil is associated with a low incidence of adverse events, with gastrointestinal disturbances being the most frequently observed. Thus, Cefuroxime axetil is an effective and convenient treatment for a wide range of infections and may be considered a therapeutic option when empirical treatment of community-acquired infections is required. Moreover, given the promising results of several intravenous/oral sequential treatment studies, Cefuroxime axetil may also become established as an oral component of sequential treatment regimens.
Cefuroxime axetil in the treatment of sinusitis. A review
Arch Fam Med 1994 Feb;3(2):165-75.PMID:7994439DOI:10.1001/archfami.3.2.165.
Cefuroxime axetil is a beta-lactamase-stable, second-generation, oral cephalosporin that penetrates sinus tissue in concentrations exceeding the MIC90 values (the minimum concentration of drug needed to inhibit the growth of 90% of an isolate of a particular microorganism) for pathogens most commonly associated with acute sinusitis, including Streptococcus pneumoniae and Haemophilus influenzae. A review of all clinical data published to date demonstrates that Cefuroxime axetil has been evaluated in the treatment of acute sinusitis and acute exacerbations of chronic sinusitis ("acute-on-chronic sinusitis") in 18 clinical trials involving 1516 assessable patients. In 12 randomized, comparative trials, the rates of satisfactory clinical outcomes (cure or improvement, 79% to 100%) and bacteriologic eradication (84% to 100%) reported with the use of 250 mg of Cefuroxime axetil twice daily were similar to those observed with the use of amoxicillin, amoxicillin/clavulanate potassium, cefaclor, cefadroxil, cefixime, clarithromycin, and doxycycline. In these comparisons, no antibiotic demonstrated any therapeutic advantages over Cefuroxime axetil regarding time to symptom abatement. Cefuroxime axetil was at least as well tolerated as the other antibiotics. Overall, the role of Cefuroxime axetil in the treatment of sinusitis appears to be as one of the broad-spectrum antibiotics that can be used for infections due to the most commonly implicated sinus pathogens, especially those due to the increasing number of relatively penicillin-resistant strains of S pneumoniae and beta-lactamase-producing strains of H influenzae and Moraxella catarrhalis.