Cefathiamidine
(Synonyms: 头孢硫脒) 目录号 : GC38750
Cefathiamidine is the first generation of cephalosporin antibacterial used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis.
Cas No.:33075-00-2
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
Cefathiamidine is the first generation of cephalosporin antibacterial used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis.
| Cas No. | 33075-00-2 | SDF | |
| 别名 | 头孢硫脒 | ||
| Canonical SMILES | OC(C1=C(COC(C)=O)CS[C@@]([C@@H]2NC(CS/C(NC(C)C)=N\C(C)C)=O)([H])N1C2=O)=O | ||
| 分子式 | C19H28N4O6S2 | 分子量 | 472.58 |
| 溶解度 | DMSO: 250 mg/mL (529.01 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 | 2.116 mL | 10.5802 mL | 21.1604 mL |
| 5 mM | 0.4232 mL | 2.116 mL | 4.2321 mL |
| 10 mM | 0.2116 mL | 1.058 mL | 2.116 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。
Population Pharmacokinetic Study of Cefathiamidine in Infants With Augmented Renal Clearance
Front Pharmacol 2021 Mar 15;12:630047.PMID:33790793DOI:10.3389/fphar.2021.630047.
Objectives: Augmented renal clearance (ARC) of primarily renally eliminated antibacterial agents may result in subtherapeutic antibiotic concentrations and, as a consequence, worse clinical outcomes. Cefathiamidine is frequently used as empirical antimicrobial therapy in children with ARC, but pharmacokinetic studies in infants are lacking. This population pharmacokinetic study in infants with ARC was conducted to determine optimal dosing regimens of Cefathiamidine. Methods: The population pharmacokinetics was conducted in 20 infants treated with Cefathiamidine. Plasma samples of Cefathiamidine were collected using opportunistic sampling, and the concentrations were detected by UPLC-MS/MS. Data analysis was performed to determine pharmacokinetic parameters and to characterize pharmacokinetic variability of Cefathiamidine using nonlinear mixed effects modelling (NONMEM) software program. Results: The data (n = 36) from 20 infants (age range, 0.35-1.86 years) with ARC were fitted best with a 1-compartment model. Allometrically scaled weight and age as significant covariates influenced Cefathiamidine pharmacokinetics. The median (range) values of estimated clearance and the volume of distribution were 0.22 (0.09-0.29) L/h/kg and 0.34 (0.24-0.41) L/kg, respectively. Monte Carlo simulations showed that the Cefathiamidine doses of 100 mg/kg/day q12 h, 50 mg/kg/day q8 h and 75 mg/kg/day q6 h were chosen for bacteria with MIC 0.25, 0.5 and 2 mg/L, respectively. Conclusion: The population pharmacokinetic model of Cefathiamidine for infants with ARC was developed. The PTA - based dosing regimens were recommended based on the final model.
The killing effects of Cefathiamidine or ampicillin alone and in combination with gentamicin against enterococci
J Antimicrob Chemother 1983 Jul;12(1):19-26.PMID:6413484DOI:10.1093/jac/12.1.19.
The in-vitro activity of Cefathiamidine against Streptococcus faecalis and Str. faecium were studied in comparison with other beta-lactams. All the 56 strains of Str. faecalis tested were inhibited by 2 mg/l of Cefathiamidine. MICs of ampicillin were twofold higher than those of Cefathiamidine and MICs of cephaloridine and cephazolin were 8-16-fold higher. No significant inoculum effect on MICs of Cefathiamidine could be seen. Two isolates of Str. faecium showed resistance to the four antibiotics. The MBCs of Cefathiamidine and ampicillin for ten strains of Str. faecalis showed that the ratios of MBC/MIC were greater than 64. The rates of killing of Str. faecalis were reduced at concentrations of Cefathiamidine and ampicillin greater than the MIC. The most rapid killing was obtained at 2 mg/l Cefathiamidine or 4 mg/l of ampicillin. With the addition of 1 mg/l gentamicin this paradoxical bacteriocidal effect was eliminated. Time killing studies showed 99.9% of the cells were killed within 6 h by a combination of aminoglycoside and beta-lactam. The paradoxical bacteriocidal effect of Cefathiamidine and ampicillin was also demonstrated on solid media.
Population pharmacokinetics and dosing optimization of Cefathiamidine in children with hematologic infection
Drug Des Devel Ther 2018 Apr 17;12:855-862.PMID:29713143DOI:10.2147/DDDT.S160329.
Purpose: Cefathiamidine, a first-generation cephalosporin, has approval from the China Food and Drug Administration for the treatment of infections caused by susceptible bacteria in both adults and children. As pharmacokinetic data are limited in the pediatric population, we aimed to evaluate the population pharmacokinetics of Cefathiamidine in children and to define the appropriate dose in order to optimize Cefathiamidine treatment. Methods: Blood samples were collected from children treated with Cefathiamidine, and concentrations were quantified by high-performance liquid chromatography and tandem mass spectrometry. Population pharmacokinetic analysis was conducted using NONMEM software. Results: Fifty-four children (age range: 2.0-11.8 years) were included. Sparse pharmacokinetic samples (n=120) were available for analysis. A two-compartment model with first-order elimination showed the best fit with the data. A covariate analysis identified that bodyweight had a significant impact on Cefathiamidine pharmacokinetics. Monte Carlo simulation demonstrated that the currently used dosing regimen of 100 mg/kg/day q12h was associated with a high risk of underdosing in pediatric patients. To reach the target 70% fT>MIC, a dose of 100 mg/kg/day Cefathiamidine q6h is required for effective treatment against Haemophilus influenzae. Conclusion: A population pharmacokinetics model of Cefathiamidine in children with hematologic disease was established. A dosing regimen of 100 mg/kg/day Cefathiamidine q6h should be used in clinical practice against H. influenza infections.
First four failures of Cefathiamidine to treat urogenital gonorrhoea in Guangzhou, China, 2014-15
Sex Health 2017 Jun;14(3):289-292.PMID:28384434DOI:10.1071/SH16087.
Neisseria gonorrhoeae has a remarkable ability to develop resistance to all available therapeutic antimicrobials. This report describes the first four cases of verified failure to treat gonorrhoea using 1000mg Cefathiamidine intramuscularly in Guangzhou, China; for each case, the patient was clinically cured after treatment with 500mg ceftriaxone intramuscularly. Enhanced monitoring of clinical treatment failures, finding new effective treatments and updating treatment guidelines are all of utmost importance to curb the spread of drug-resistant gonorrhoea.
Penicillin acylase-catalyzed synthesis of N-bromoacetyl-7-aminocephalosporanic acid, the key intermediate for the production of Cefathiamidine
Bioresour Bioprocess 2016;3(1):49.PMID:27917366DOI:10.1186/s40643-016-0127-3.
Background: Enzymatic approaches have become promising alternatives to chemical methods for the production of semi-synthetic β-lactam antibiotics. In this work, enzymatic synthesis of N-bromoacetyl-7-aminocephalosporanic acid (N-bromoacetyl-7-ACA), the key intermediate for the production of Cefathiamidine, was reported for the first time. Results: Of the immobilized penicillin acylases (PAs) tested, PGA-750 was the best biocatalyst. Optimization of the biocatalytic process was conducted. The optimal acyl donor, molar ratio of acyl donor to 7-ACA, pH, temperature, 7-ACA concentration, and enzyme dosage were methyl bromoacetate, 3, 7.5, 20 °C, 50 mmol/L and 4 U/mL, respectively. Under the optimal conditions, enzymatic N-acylation of 7-ACA with methyl bromoacetate afforded the desired product with the yield of 85% in 2 h, where the synthesis/hydrolysis (S/H) ratio was approximately 1.5. The immobilized enzyme PGA-750 exhibited good operational stability, and the relative yields of approximately 90% and 63% were achieved, respectively, when it was reused in 7th and 11th batch. Conclusions: An enzymatic approach to N-bromoacetyl-7-ACA, the key intermediate for the industrial production of Cefathiamidine, has been developed successfully in a fully aqueous medium. The present work may open up a novel opportunity for the production of Cefathiamidine through a simple and green process.Graphical abstractEnzymatic synthesis of N-bromoacetyl-7-ACA, the key intermediate for the production of Cefathiamidine, was reported for the first time.