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Cefmetazole sodium (Sodium cefmetazole) Sale

(Synonyms: 头孢美唑钠; Sodium cefmetazole) 目录号 : GC32168

A cephamycin antibiotic

Cefmetazole sodium (Sodium cefmetazole) Chemical Structure

Cas No.:56796-39-5

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10mM (in 1mL DMSO)
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100mg
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产品描述

Cefmetazole is a cephamycin antibiotic.1 It is active against E. coli, P. mirabilis, H. influenzae, N. gonorrhoeae, S. pneumoniae, and S. pyogenes (MIC50s = 0.25-2 μg/ml). Cefmetazole (20 and 40 mg/kg per day) decreases the lesion size and the number of ulcerative lesions in a rabbit model of active syphilis.2

1.Jones, R.N., Barry, A.L., Fuchs, P.C., et al.Antimicrobial activity of cefmetazole (CS-1170) and recommendations of susceptibility testing by disk diffusion, dilution, and anaerobic methodsJ. Clin. Microbiol.24(6)1055-1059(1986) 2.Baker-Zander, S.A., and Lukehart, S.A.Efficacy of cefmetazole in the treatment of active syphilis in the rabbit modelAntimicrob. Agents Chemother.33(9)1465-1469(1989)

Chemical Properties

Cas No. 56796-39-5 SDF
别名 头孢美唑钠; Sodium cefmetazole
Canonical SMILES O=C(C(N12)=C(CSC3=NN=NN3C)CS[C@]2([H])[C@](OC)(NC(CSCC#N)=O)C1=O)[O-].[Na+]
分子式 C15H16N7NaO5S3 分子量 493.52
溶解度 DMSO : ≥ 39 mg/mL (79.02 mM) 储存条件 4°C, away from moisture and light
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1 mM 2.0263 mL 10.1313 mL 20.2626 mL
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Research Update

Cefmetazole sodium: pharmacology, pharmacokinetics, and clinical trials

Pharmacotherapy 1991;11(1):2-19.PMID:2020609doi

Cefmetazole sodium is a semisynthetic cephamycin antibiotic. It has a broad spectrum of activity comparable to that of the second-generation cephalosporins, covering gram-positive, gram-negative, and anaerobic bacteria. Unlike the second-generation cephalosporins, cephamycins such as cefmetazole are usually active against Bacteroides fragilis. Cefmetazole is also active against beta-lactamase-producing organisms that are resistant to first-generation cephalosporins or penicillins. The pharmacokinetics of cefmetazole allow parenteral administration (intravenous or intramuscular) 2-3 times daily for treatment of infection. The drug has been studied in gynecologic, intraabdominal, urinary tract, respiratory tract, and skin and soft tissue infections. Administered preoperatively, it may reduce the frequency of infection in certain clean-contaminated or potentially contaminated procedures, including cesarean section, abdominal or vaginal hysterectomy, cholecystectomy (high-risk patients), and colorectal surgery. On the basis of in vitro spectrum, pharmacokinetics, and data from a relatively small number of clinical trials, this agent may be considered when a second-generation cephalosporin is indicated.

Clinical experience with Cefmetazole sodium in the United States: an overview

J Antimicrob Chemother 1989 Apr;23 Suppl D:21-33.PMID:2656625DOI:10.1093/jac/23.suppl_d.21.

The clinical development programme for Cefmetazole sodium included over 4000 patients treated by 78 investigators. Cefmetazole therapy was compared with that of cefoxitin sodium (cefoxitin) for the treatment of urinary tract, skin and soft tissue, lower respiratory, abdominal, and gynaecological infections (with cefoxitin-sensitive pathogens) and for the prevention of postoperative wound infection in patients undergoing surgical procedures. Both cefmetazole and cefoxitin were administered intravenously in all studies. Cefmetazole was as effective as cefoxitin in the treatment of the infections studied. In the surgical wound infection prophylaxis studies, multiple-dose cefmetazole therapy was more effective than multiple-dose cefoxitin therapy in patients undergoing lower gastrointestinal surgery; this difference approached statistical significance. Both multiple-dose and single-dose cefmetazole therapy were as effective as multiple-dose cefoxitin treatment in the other types of surgery studied. Clinical laboratory findings and adverse medical events reported among cefmetazole patients were similar to those observed in patients treated with cefoxitin.

Analysis of the polymerized impurities in Cefmetazole sodium based on novel separation principle by liquid chromatography tandem ion trap/time-of-flight mass spectrometry

J Pharm Biomed Anal 2022 Jun 5;215:114790.PMID:35483231DOI:10.1016/j.jpba.2022.114790.

To effectively control the polymerized impurities in Cefmetazole sodium, novel high performance gel filtration chromatography (HPSEC) with TSK-gel G2000SWxl column and RP-HPLC method with C18 column were used in replace of classical gel filtration chromatography with Sephadex G-10 gel. By studying the chromatographic behavior of polymerized impurities in both chromatographic systems with different chromatographic separation principles, the polymerized impurities in Cefmetazole sodium were separated and detected effectively. The two-dimensional liquid chromatography tandem ion trap/time-of-flight mass spectrometry (2D LC-IT-TOF MS) was applied to characterize the structures of polymerized impurities eluted from HPSEC method, and liquid chromatography tandem ion trap/time-of-flight mass spectrometry was applied to characterize the structures of polymerized impurities and other unknown impurities eluted from RP-HPLC method. The structures of fourteen unknown impurities in Cefmetazole sodium were deduced based on the MS n data, nine of which were polymerized impurities. The corresponding relationship between impurities in the HPSEC method and RP-HPLC method was established, and the specificity of the two methods was evaluated. The RP-HPLC method for analysis of the polymerized impurities has higher column efficiency and specificity than the HPSEC method. The RP-HPLC method is suitable for quality control of the polymerized impurities in Cefmetazole sodium. The forming mechanisms of degradation impurities in Cefmetazole sodium were also studied.

The synergistic Reduning and Cefmetazole sodium treatment of severe pneumonia is mediated by the AhR-Src-STAT3 pathway

J Thorac Dis 2022 Feb;14(2):474-493.PMID:35280469DOI:10.21037/jtd-22-126.

Background: Reduning (RDN) is a common Chinese medicine preparation with antibacterial, anti-inflammatory, antiviral and immunomodulatory effects in respiratory infectious diseases. Clinically, it is used in combination with antibiotics, but its synergistic effect and mechanism in treating severe pneumonia remain unclear. Methods: A rat model of severe pneumonia and an in vitro coculture model consisting of A549 and THP-1 cells were used to observe the synergistic effect of RDN on severe pneumonia. The inflammatory cytokines were tested by enzyme-linked immunosorbent assay (ELISA). The localization of Aryl hydrocarbon receptor (AhR) in A549 cells was observed by immunofluorescence, and the interaction of AhR and signal transducer and activator of transcription 3 (STAT3) proteins was observed by co-immunoprecipitation. AhR-Src tyrosine kinase (Src)-STAT3 pathway in rats and A549 cells were examined by Western Blot. Histopathological changes were observed by Hematoxylin-eosin (HE) staining, X-ray and survival rates were used to evaluate the effects of paclitaxel on severe pneumonia rats. Results: RDN regulation of Src-STAT3-interleukin 10 (IL-10) signaling pathway activation and macrophage polarization were mediated through the nuclear receptor AhR. The expression of AhR was significantly increased after RDN treatment, and this effect was accompanied by STAT3 expression increasing. Coimmunoprecipitation confirmed an interaction between AhR and STAT3 and upregulated IL-10 expression. Silencing AhR decreased Src, STAT3, and IL-10 expression. RDN activated AhR and increased Src, STAT3, and IL-10 expression. In addition, RDN regulated the polarization of macrophages RDN combined with Cefmetazole sodium significantly reduced the pulmonary bacterial load, alleviated lung injury, and reduced o inflammatory factors expression, improving their survival. Conclusions: RDN can synergistically enhance the effect of Cefmetazole sodium treatment in severe pneumonia, and the mechanism may involve increasing the expression level of IL-10 mediated through the AhR-Src-STAT3 pathway, driving the polarization of macrophages, and attenuating the cytokine storm to control inflammation in severe pneumonia.

Compatibility of Cefmetazole sodium with commonly used drugs during Y-site delivery

Am J Health Syst Pharm 1996 Sep 15;53(18):2185-8.PMID:8879326DOI:10.1093/ajhp/53.18.2185.

The compatibility of Cefmetazole sodium and selected other drugs during Y-site delivery was evaluated. Cefmetazole 100 mg/mL (as the sodium salt) in sterile water for injection and each of 34 drugs or solutions commonly used with it were mixed together by Y-site injection. Secondary drugs were administered at selected concentrations and rates and delivered by the method (i.v. push, i.v. infusion, or syringe pump) commonly used for the drug at the institution where the study was done. Each injection set included a filter system with a 0.8-micron filter disk. Tests were done in triplicate. After each test, the Y injection site and the tubing after it were visually inspected for precipitate and color change. If no particles or color change was detected, the filter disk was observed under a microscope. Drugs were deemed compatible with cefmetazole if unaided observation detected no color change or particles and the number of particles detected by microscopic examination was below that specified in USP guidelines. A precipitate formed when Cefmetazole sodium mixed with diphenhydramine hydrochloride, droperidol, erythromycin (50 mg/mL, as the lactobionate), haloperidol lactate, prochlorperazine edisylate, promethazine hydrochloride, or vancomycin (50 mg/mL, as the hydrochloride salt). No particles or color change was detected by unaided observation of mixtures containing dobutamine or erythromycin 10 mg/mL, but the number of particles detected by microscopic examination exceeded USP limits. All other drugs tested were compatible with cefmetazole. Cefmetazole 100 mg/mL (as the sodium salt) in sterile water for injection was shown to be compatible with 25 of 34 tested drug solutions during Y-site delivery.