Cefotaxime
(Synonyms: 头孢噻肟酸,Cefotaxim; HR-756) 目录号 : GC60685
Cefotaxime是一种具有广谱抗菌活性的第三代头孢菌素类抗生素。它最常用于治疗革兰氏阳性菌或革兰氏阴性菌引起的传染病。
Cas No.:63527-52-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
Cell lines | Human fibrosarcoma HT1080 cells |
Preparation Method | HT1080 cells were seeded on glass plates and treated with the indicated concentrations (200, 400, 600, or 1000μg/mL) of Cefotaxime for 24h. After stimulation, cells were treated with 10µM DCFH-DA for 30min at 37°C. After washing with PBS, the intracellular ROS generation was observed under laser confocal microscope. |
Reaction Conditions | 200, 400, 600, or 1000μg/mL; 24h |
Applications | Cefotaxime significantly promotes ROS generation in HT1080 cells. |
| Animal experiment [2]: | |
Animal models | Pneumonia model in leukopenic mice |
Preparation Method | Amoxicillin (AMO) and Cefotaxime (CTX) were administered at 8-h intervals with a total of nine injections, and Ceftriaxone (CRO) was given at 12-h intervals with a total of six injections. The dose of each antibiotic varied with the infective strain. Mice infected with strain P40422 were treated with AMO or CTX at 200 or 400mg/kg or with CRO at 100mg/kg. Mice infected with P40984 were treated with AMO at 200 or 400mg/kg, CTX at 400mg/kg, or CRO at 100 or 200mg/kg. Each dose was administered subcutaneously (s.c.) in 0.5ml of sterile water. Control animals received the same volume of isotonic saline. |
Dosage form | 200 or 400mg/kg/8h, 9 injections, subcutaneous injection |
Applications | Cefotaxime significantly increased bacterial clearance from the pneumonia model in leukopenic mice. |
References: | |
Cefotaxime is a third-generation cephalosporin antibiotic with broad-spectrum antibacterial activity. It is most commonly prescribed for the treatment of infectious diseases induced by Gram-positive or Gram-negative bacteria[1].
Cefotaxime (200, 400, 600, or 1000μg/mL; 24h) significantly promotes ROS generation in HT1080 cells[1]. Cefotaxime (0.02-2µg/ml, 5h) combined with Mecillinam could eliminate both cephalosporin-resistant bacteria harbouring CTX-M-15WT and mecillinam-resistant bacteria harbouring the mutant CTX-M-15N135D, thereby constraining resistance evolution of β-lactamase CTX-M-15[2].
Cefotaxime (200 or 400mg/kg/8h, 9 injections, subcutaneous injection) significantly increased bacterial clearance from the pneumonia model in leukopenic mice[3]. Cefotaxime (100mg/kg/4h, 24h, subcutaneous injections) combined with Amoxicillin-Clavulanate significantly reduces bacterial counts and achieves kidney sterilization in in a Murine Urinary Tract Infection Model[4].
References:
[1] Yamada M, Suzuki M, Noguchi T, et al. The antibiotic cefotaxime works as both an activator of Nrf2 and an inducer of HSP70 in mammalian cells. BPB reports. 2020;3(1):16-21.
[2] Rosenkilde CE, Munck C, Porse A, et al. Collateral sensitivity constrains resistance evolution of the CTX-M-15 β-lactamase. Nature communications. 2019 Feb 6;10(1):618.
[3] Sauve C, Azoulay-Dupuis E, Moine P, et al. Efficacies of cefotaxime and ceftriaxone in a mouse model of pneumonia induced by two penicillin-and cephalosporin-resistant strains of Streptococcus pneumoniae. Antimicrobial agents and chemotherapy. 1996 Dec;40(12):2829-34.
[4] Rossi B, Soubirou JF, Chau F, et al. Cefotaxime and amoxicillin-clavulanate synergism against extended-spectrum-β-lactamase-producing Escherichia coli in a murine model of urinary tract infection. Antimicrobial Agents and Chemotherapy. 2016 Jan;60(1):424-30.
Cefotaxime是一种具有广谱抗菌活性的第三代头孢菌素类抗生素。它最常用于治疗革兰氏阳性菌或革兰氏阴性菌引起的传染病[1]。
Cefotaxime（200、400、600或1000μg/mL，24小时）显著促进HT1080细胞中的ROS生成[1]。Cefotaxime（0.02-2µg/ml，5h）与Mecillinam联合应用，可以同时消灭携带CTX-M-15WT的头孢菌素耐药菌和携带突变体CTX-M-15N135D的Mecillinam耐药菌，从而抑制β-内酰胺酶CTX-M-15的耐药性进化[2]。
Cefotaxime（200或400mg/kg/8小时，9次注射，皮下注射）显著增加白细胞减少小鼠的肺炎模型中的细菌清除率[3]。Cefotaxime（100mg/kg/4h，24h，皮下注射）与Amoxicillin-Clavulanate联合使用，在小鼠尿路感染模型中显著降低细菌数量并实现肾脏消毒[4]。
| Cas No. | 63527-52-6 | SDF | |
| 别名 | 头孢噻肟酸,Cefotaxim; HR-756 | ||
| Canonical SMILES | O=C(C(N12)=C(COC(C)=O)CS[C@]2([H])[C@H](NC(/C(C3=CSC(N)=N3)=N\OC)=O)C1=O)O | ||
| 分子式 | C16H17N5O7S2 | 分子量 | 455.47 |
| 溶解度 | DMSO: 250 mg/mL (548.88 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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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1955 mL | 10.9777 mL | 21.9553 mL |
| 5 mM | 0.4391 mL | 2.1955 mL | 4.3911 mL |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1955 mL |
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Cefotaxime is extensively used for surgical prophylaxis
Am J Surg 1992 Oct;164(4A Suppl):28S-38S.PMID:1443358DOI:10.1016/s0002-9610(06)80055-3.
Cefotaxime, a broad-spectrum third-generation cephalosporin, has been extensively used worldwide for chemotherapy of serious infections. Based on the characteristics of its antimicrobial spectrum, low incidence of allergy, and lack of adverse effects, Cefotaxime has been used successfully for prophylaxis of a number of different surgical procedures. Extensive data have been accumulated for single-dose or short-course Cefotaxime prophylaxis regimens. These Cefotaxime regimens have been demonstrated to be very effective and inexpensive. For this article, over 11,500 published Cefotaxime prophylaxis cases are reviewed (10,500 control cases) and 98 references are cited. Single-dose Cefotaxime was clearly indicated for hysterectomies, cesarean sections, upper gastrointestinal cases, bone and joint operations, biliary tract procedures, transurethral resections, open urologic surgeries, and some vascular procedures. Short-course (3-4 doses) may be required for colorectal resections, cardiac surgeries, head and neck surgeries, organ transplants, specific pediatric surgical cases, and for some patients with compromised immune function, regardless of origin. Cefotaxime has reduced wound morbidity of contaminated abdominal operations to < 10%. This change from multiple-dose regimens to the single-dose or short-course regimens, enabled by Cefotaxime use, decreases the risk of inducing or selecting bacterial resistance; the change would generate a significant reduction in hospital costs. Surgeons should not hesitate to employ Cefotaxime and other third-generation cephalosporins with proven limited-dose indications to greatly benefit their patients and the hospital environment.
Cefotaxime. An update of its pharmacology and therapeutic use
Drugs 1990 Oct;40(4):608-51.PMID:2083516DOI:10.2165/00003495-199040040-00008.
Cefotaxime was the first 'third generation' cephalosporin to be marketed and is administered intramuscularly or intravenously. Similar to other agents of this class, it has a broad spectrum of in vitro activity, particularly against Enterobacteriaceae, including beta-lactamase-producing strains. Cefotaxime forms a metabolite, desacetylcefotaxime, which is antibacterially effective against many bacteria per se and acts additively or synergistically with Cefotaxime against many strains. Since the first review of Cefotaxime in the Journal, further studies have confirmed its value in the treatment of various infections: complicated urinary tract infections, lower respiratory tract infections, bacteraemia, meningitis, uncomplicated gonorrhoea, infections of skin and soft tissue and of bone and joints, and obstetric and gynaecological infections. Cefotaxime is effective as an empirical treatment of suspected infection due to susceptible organisms in immunocompromised patients and is of proven efficacy in serious, life-threatening infections in general. Cefotaxime reduces the incidence of postsurgical infection but the role of third generation cephalosporins in prophylaxis remains to be determined. The indications for which Cefotaxime and other 'third generation' cephalosporins would be considered the most appropriate therapy remain largely dependent upon such factors as varied as cost, local medical custom, decisions of regulatory agencies and geographical patterns of bacterial resistance. Cefotaxime nevertheless represents a valuable 'third generation' cephalosporin of great clinical value in certain infectious conditions, in particular those which are serious and life-threatening and where resistance to therapies is creating a clinical problem.
Cefotaxime: microbiology, pharmacology, and clinical use
Clin Pharm 1982 Mar-Apr;1(2):114-24.PMID:6309465doi
The microbiological activity, pharmacology, and clinical efficacy of the third-generation cephalosporin Cefotaxime are reviewed. Cefotaxime has greater activity than other available first- and second-generation cephalosporins against Enterobacteriaceae. It is more active than older cephalosporins against Pseudomonas aeruginosa and Acinetobacter spp., but most strains are still considered resistant. Cefotaxime is also active against some gram-negative bacilli that are resistant to aminoglycosides, including amikacin. Cefotaxime has activity comparable with other cephalosporins against gram-positive cocci, except staphylococci and enterococci, which are resistant. Cefotaxime in combination with penicillins or aminoglycosides may be synergistic against selected gram-negative bacilli. Cefotaxime is metabolized in vivo to the desacetyl derivative, which is also microbiologically active. Cefotaxime appears to penetrate most body tissues and fluids, including cerebrospinal fluid. Clinical use of Cefotaxime has resulted in response rates between 70 and 95% in most infections. The ultimate role of Cefotaxime and other third-generation cephalosporins is not established since controlled clinical comparisons with standard antimicrobial regimens are lacking. Possibilities include the empiric and specific therapy of serious gram-negative bacillary infection probably in combination with a penicillin or an aminoglycoside. Cefotaxime appears to be potentially useful in the management of gram-negative bacillary meningitis.
Cefotaxime in urinary tract infections
Infection 1989 Nov-Dec;17(6):425-8.PMID:2693361DOI:10.1007/BF01645565.
According to available studies the experience with Cefotaxime in the treatment of urinary tract infections (UTI) is presented. Because of its broad spectrum antibacterial activity Cefotaxime is active against most of the causative organisms, including multiresistant strains (except enterococci). Of 400 isolates cultured from 400 urological inpatients with complicated and/or hospital acquired UTI 90.2% of the gram-negatives and 87.7% of the staphylococci were inhibited by concentrations of less than or equal to 8 mg/l. As with other antibiotics in uncomplicated UTI, high cure rates could be achieved by single dose or short-term treatment. According to six non-comparative and nine comparative studies it could be demonstrated that treatment with Cefotaxime achieved favorable results in patients with complicated and hospital acquired UTI even if caused by multiresistant strains. In general, in these studies Cefotaxime was superior to gentamicin, cefoxitin, cefazolin and cefuroxime, but as effective as other third generation cephalosporins and aztreonam and as the combination of ampicillin and netilmicin. A good tolerance of Cefotaxime was reported in all studies.
Cefotaxime. A review of its antibacterial activity, pharmacological properties and therapeutic use
Drugs 1983 Mar;25(3):223-89.PMID:6303743DOI:10.2165/00003495-198325030-00001.
Cefotaxime is a new 'third generation' semisynthetic cephalosporin administered intravenously or intramuscularly. It has a broad spectrum of activity against Gram-positive and Gram-negative aerobic and anaerobic bacteria, and is generally more active against Gram-negative bacteria than the 'first' and 'second generation' cephalosporins. Although Cefotaxime has some activity against Pseudomonas aeruginosa, on the basis of present evidence it cannot be recommended as sole antibiotic therapy for pseudomonal infections. However, Cefotaxime has been effective in treating infections due to other 'difficult' organisms, such as multidrug-resistant Enterobacteriaceae. Like other cephalosporins, Cefotaxime is effective in treating patients with complicated urinary tract and lower respiratory tract infections, particularly pneumonia caused by Gram-negative bacilli. High response rates have also been achieved in patients with Gram-negative bacteraemia. Although favourable clinical results have been obtained in patients with infections caused by mixed aerobic/anaerobic organisms (such as peritonitis or soft tissue infections), the relatively low in vitro activity of Cefotaxime against Bacteroides fragilis may restrict its usage in situations where this organism is the suspected or proven pathogen. In preliminary studies, males and females treated with a single intramuscular dose of Cefotaxime for uncomplicated gonorrhoea caused by penicillinase-producing strains of Neisseria gonorrhoeae responded very favourably. Encouraging results have also been reported in open studies in children including neonates, treated with Cefotaxime for meningitis and various other serious infections. In some situations, Cefotaxime has been given in combination with another antibiotic such as an aminoglycoside, but the merits of such a combination have not been clearly established. Whether Cefotaxime alone is appropriate therapy for conditions previously treated with aminoglycosides (other than pseudomonal infections) also needs additional clarification, but if established as equally effective in such conditions Cefotaxime offers potentially important clinical and practical advantages in its apparent lack of serious adverse effects and freedom from the need to undertake drug plasma concentration monitoring.