Ceftriaxone
(Synonyms: 头孢曲松) 目录号 : GC35648
A third-generation cephalosporin antibiotic
Cas No.:73384-59-5
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
Ceftriaxone is a third-generation, broad-spectrum cephalosporin antibiotic that disrupts the synthesis of the peptidoglycan layer of bacterial cell walls.1,2,3 It has been shown to increase excitatory amino acid transporter-2 pump expression in the central nervous system and to reduce glutamatergic toxicity in both in vitro and in vivo models.4
1.Bush, K.β-Lactamase inhibitors from laboratory to clinicClin. Microbiol. Rev.1(1)109-123(1988) 2.Kalman, D., and Barriere, S.L.Review of the pharmacology, pharmacokinetics, and clinical use of cephalosporinsTex. Heart Inst. J.17(3)203-215(1990) 3.Neu, H.C.The in vitro activity, human pharmacology, and clinical effectiveness of new β-lactam antibioticsAnnu. Rev. Pharmacol. Toxicol.22599-642(1982) 4.Lee, S.G., Su, Z.Z., Emdad, L., et al.Mechanism of ceftriaxone induction of excitatory amino acid transporter-2 expression and glutamate uptake in primary human astrocytesJ. Biol. Chem.283(19)13116-13123(2008)
| Cas No. | 73384-59-5 | SDF | |
| 别名 | 头孢曲松 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC(N(C)NC3=O)=NC3=O)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)O | ||
| 分子式 | C18H18N8O7S3 | 分子量 | 554.58 |
| 溶解度 | DMSO:≥100mg/mL | 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 | 1.8032 mL | 9.0158 mL | 18.0317 mL |
| 5 mM | 0.3606 mL | 1.8032 mL | 3.6063 mL |
| 10 mM | 0.1803 mL | 0.9016 mL | 1.8032 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。
Comparison of Clinical Outcomes among Intensive Care Unit Patients Receiving One or Two Grams of Ceftriaxone Daily
Antimicrob Agents Chemother 2020 May 21;64(6):e00066-20.PMID:32205348DOI:10.1128/AAC.00066-20.
Intensive care unit (ICU) patients may experience Ceftriaxone underexposure, but clinical outcomes data are lacking. The objective of this study was to determine the impact of Ceftriaxone dosing on clinical outcomes among ICU patients without central nervous system (CNS) infection. A retrospective study of ICU patients receiving intravenous, empirical Ceftriaxone for non-CNS infections was conducted. Patients ≥18 years of age who received ≤2 g of Ceftriaxone daily for ≥72 h were included and categorized as receiving Ceftriaxone 1 g or 2 g daily. The primary, composite outcome was treatment failure, defined as inpatient mortality and/or antibiotic escalation due to clinical worsening. Propensity score matching was performed based on the probability of receiving 2 g of Ceftriaxone daily. Multivariable logistic regression determined the association between Ceftriaxone dose and treatment failure in a propensity-matched cohort. A total of 212 patients were included in the propensity-matched cohort. The most common diagnoses (83.0%) were pneumonia and urinary tract infection. Treatment failure occurred in 17.0% and 5.7% of patients receiving 1 g and 2 g daily, respectively (P = 0.0156). Overall inpatient mortality was 8.5%. Ceftriaxone 2 g dosing was associated with a reduced likelihood of treatment failure (adjusted odds ratio [aOR] = 0.190; 95% confidence interval [CI] = 0.059 to 0.607). Other independent predictors of treatment failure included sequential organ failure assessment score (aOR = 1.440; 95% CI = 1.254 to 1.653) and creatinine clearance at 72 h from Ceftriaxone initiation (aOR = 0.980; 95% CI = 0.971 to 0.999). Therefore, Ceftriaxone at 2 g daily, when used as appropriate antimicrobial coverage, may be appropriate for ICU patients with lower mortality risk.
Safety of Ceftriaxone in paediatrics: a systematic review protocol
BMJ Open 2017 Aug 21;7(8):e016273.PMID:28827252DOI:10.1136/bmjopen-2017-016273.
Introduction: Ceftriaxone is widely used in children in the treatment of sepsis. However, concerns have been raised about the safety of Ceftriaxone, especially in young children. The aim of this review is to systematically evaluate the safety of Ceftriaxone in children of all age groups. Methods and analysis: MEDLINE, PubMed, Cochrane Central Register of Controlled Trials, EMBASE, CINAHL, International Pharmaceutical Abstracts and adverse drug reaction (ADR) monitoring systems will be systematically searched for randomised controlled trials (RCTs), cohort studies, case-control studies, cross-sectional studies, case series and case reports evaluating the safety of Ceftriaxone in children. The Cochrane risk of bias tool, Newcastle-Ottawa and quality assessment tools developed by the National Institutes of Health will be used for quality assessment. Meta-analysis of the incidence of ADRs from RCTs and prospective studies will be done. Subgroup analyses will be performed for age and dosage regimen. Ethics and dissemination: Formal ethical approval is not required as no primary data are collected. This systematic review will be disseminated through a peer-reviewed publication and at conference meetings. Prospero registration number: CRD42017055428.
Ceftriaxone: a third-generation cephalosporin
Drug Intell Clin Pharm 1985 Dec;19(12):900-6.PMID:3910386DOI:10.1177/106002808501901203.
Ceftriaxone is a new third-generation cephalosporin with excellent activity against many gram-negative, and reasonable activity against most gram-positive microorganisms. Clinical studies have demonstrated its efficacy and safety in patients with bacterial meningitis; respiratory tract, urinary tract, soft tissue, bone and joint infections; and gonorrhea. Ceftriaxone has been well tolerated except for diarrhea, which in most cases has not required a change in therapy. The long elimination half-life of Ceftriaxone has allowed twice- and once-daily administration, the latter potentially resulting in substantial cost savings. Because of its documented efficacy, safety, and convenient dosing schedule, Ceftriaxone may become the preferred third-generation cephalosporin for the treatment of a variety of serious infections.
Ceftriaxone: an update of its use in the management of community-acquired and nosocomial infections
Drugs 2002;62(7):1041-89.PMID:11985490DOI:10.2165/00003495-200262070-00005.
Ceftriaxone is a parenteral third-generation cephalosporin with a long elimination half-life which permits once-daily administration. It has good activity against Streptococcus pneumoniae, methicillin-susceptible staphylococci, Haemophilus influenzae, Moraxella catarrhalis and Neisseria spp. Although active against Enterobacteriaceae, the recent spread of derepressed mutants which hyperproduce chromosomal beta-lactamases and extended-spectrum beta-lactamases has diminished the activity of all third-generation cephalosporins against these pathogens necessitating careful attention to sensitivity studies. Extensive data from randomised clinical trials confirm the efficacy of Ceftriaxone in serious and difficult-to-treat community-acquired infections including meningitis, pneumonia and nonresponsive acute otitis media. Ceftriaxone also has efficacy in other community-acquired infections including uncomplicated gonorrhoea, acute pyelonephritis and various infections in children. In the nosocomial setting, extensive data also confirm the efficacy of Ceftriaxone with or without an aminoglycoside in serious Gram-negative infections, pneumonia, spontaneous bacterial peritonitis and as surgical prophylaxis. Outpatient use of Ceftriaxone, either as part of a step-down regimen or parenterally, is a distinguishing feature of the data gathered on the agent over the last decade. The review focuses on new applications of the drug and its use in infections in which the causative pathogens or their resistance patterns have changed over the past decade. Ceftriaxone has a good tolerability profile, the most common events being diarrhoea, nausea, vomiting, candidiasis and rash. Ceftriaxone may cause reversible biliary pseudolithiasis, notably at higher dosages of the drug (>/=2 g/day); however, the incidence of true lithiasis is <0.1%. Injection site discomfort or phlebitis can occur after intramuscular or intravenous administration. Conclusions: As a result of its strong activity against S. pneumoniae, Ceftriaxone holds an important place, either alone or as part of a combination regimen, in the treatment of invasive pneumococcal infections, including those with reduced beta-lactam susceptibility. Its once-daily administration schedule allows simplification of otherwise complex regimens in a hospital setting and has also contributed to its popularity as a parenteral agent in an ambulatory setting. These properties, together with a well characterised tolerability profile, mean that Ceftriaxone is likely to retain its place as an important third-generation cephalosporin in the treatment of serious community-acquired and nosocomial infections.
Pharmacokinetics of Ceftriaxone
Hosp Pract (Off Ed) 1991 Sep;26 Suppl 5:7-13; discussion 52-4.PMID:1918224DOI:10.1080/21548331.1991.11707737.
Ceftriaxone fulfills many of the qualities of an ideal antibiotic: a prolonged elimination half-life, which results from a "restrictive" excretion pattern; saturable protein binding, which provides the theoretical basis for administering the total daily dose as a single bolus; and once-a-day dosing, which provides plasma and tissue concentrations that exceed the MIC for most susceptible pathogens for 24 hours.