Cefmetazole
(Synonyms: 头孢美唑; CS 1170) 目录号 : GC47068
A cephamycin antibiotic
Cas No.:56796-20-4
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
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)
| Cas No. | 56796-20-4 | SDF | |
| 别名 | 头孢美唑; CS 1170 | ||
| Canonical SMILES | O=C(O)C1=C(CSC2=NN=NN2C)CS[C@@]([C@]3(OC)NC(CSCC#N)=O)([H])N1C3=O | ||
| 分子式 | C15H17N7O5S3 | 分子量 | 471.5 |
| 溶解度 | DMF: 20mg/mL,DMSO: 20mg/mL,DMSO:PBS (pH 7.2) (1:4): 0.2mg/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 | 2.1209 mL | 10.6045 mL | 21.2089 mL |
| 5 mM | 0.4242 mL | 2.1209 mL | 4.2418 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1209 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。
Cefmetazole (CS-1170), a "new" cephamycin with a decade of clinical experience
Diagn Microbiol Infect Dis 1989 Sep-Oct;12(5):367-79.PMID:2692950DOI:10.1016/0732-8893(89)90106-5.
In vitro and in vivo study results were reviewed from Cefmetazole, a "new" parenteral cephamycin. Cefmetazole's spectrum of activity was comparable to that of second-generation cephalosporins, which includes clinical coverage of many Enterobacteriaceae, Staphylococcus spp., streptococci, Haemophilus spp., pathogenic Neisseria, Branhamella catarrhalis, and anaerobic bacteria. Cefmetazole was generally more potent (two- to eightfold) than cefoxitin against organisms within their spectrums and was particularly active for staphylococci (MIC90, 2.0 micrograms/ml). Methicillin-resistant S. aureus strains were more susceptible to Cefmetazole alone or in combination (fosfomycin) than any other cephamycin. Cefmetazole has demonstrated excellent stability to aerobic and anaerobic organism-produced beta-lactamases. It also inhibits Type I cephalosporinases and, uniquely, some other cephalosporinases produced by the Bacteroides. This superior stability, enzyme interaction, and better penetration into bacterial cells results in a sustained bactericidal effect and a capacity for more infrequent dosing. The Cefmetazole serum elimination half-life was 1.5 hr, also justifying use at greater than or equal to 8-hr intervals. Clinical trials in the United States and Japan demonstrated an acceptably high Cefmetazole infection cure rate (88% to 100%), especially in direct comparative studies with cefoxitin. Cefmetazole was also proven very effective in minimizing infectious wound morbidity (prophylaxis) using 2 g single- or multidose regimens. Adverse drug reactions were usually minor; in the Japanese surveillance trial (118,318 patients) the rate was only 2.2% (8.8% in United States). Cefmetazole has been extensively and safely used in Japan since 1980.
Cefmetazole Resistance Mechanism for Escherichia Coli Including ESBL-Producing Strains
Infect Drug Resist 2022 Oct 10;15:5867-5878.PMID:36237294DOI:10.2147/IDR.S382142.
Purpose: Cefmetazole (CMZ), a cephamycin antibiotic, is primarily used as a definitive therapy for Extended Spectrum β-Lactamase (ESBL)-producing Escherichia coli infections. However, the mechanism of CMZ resistance in E. coli is still unknown. To elucidate the resistance mechanism and to determine combined drugs for prevention of resistance acquisition. Methods: Clinical isolates of 14 ESBL-producing E. coli and non-producing 12 isolates were used in in vitro testing of CMZ resistance acquisition. After 10-day of CMZ exposure (1st subculture), these strains were incubated in an antibacterial-free medium for 14-day. These strains were again exposed to CMZ for 10-day (2nd subculture) and confirmed for changes in MIC. For each strain detected after 1st subculture, each mRNA expression level of porin, chromosomal ampC, and drug-efflux pump was measured using real-time RT-PCR. Relebactam (REL) has the potency to recover antimicrobial activity against carbapenem-resistant Enterobacterales that has porin deficiency. REL was added to the CMZ dilution series, and MIC changes and those of porin were confirmed. Results: Of these 26 strains, 15 strains (57.7%) acquired resistance after 1st subculture, but after passage culture on the antibacterial-free medium, 11 strains recovered susceptibility. These 11 strains showed resistance after 2nd subculture. The expression levels of ompF and ompC were significantly decreased in these strains (P<0.05). When REL was added, all strains suppressed resistance acquisition after 1st subculture. The mechanism was the activation of ompF. Conclusion: Our results showed that the mRNA expression levels of genes encoding porin were decreased in the strains that acquired resistance due to CMZ exposure, and that ompF and ompC in particular were thought to be involved in the acquisition of resistance. The CMZ acquisition of resistance was also suppressed by the concomitant use of REL and actually suppressed the decrease in mRNA expression in ompF. It was confirmed that porin reactivated by REL.
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.
Hypoprothrombinemia During Cefmetazole Treatment: A Case Report
Am J Case Rep 2022 Jul 27;23:e936712.PMID:35891595DOI:10.12659/AJCR.936712.
BACKGROUND Cefmetazole (CMZ), containing an N-methyl-tetrazole-thiol (NMTT) side chain, is a therapeutic option for diverticulitis in Japan. Cephems containing an NMTT, a methyl-thiadiazol, and a thiadiazolethiol side chain are known to induce coagulation disorders. CASE REPORT A 76-year-old woman developed hypoprothrombinemia after receiving oral levofloxacin (LVFX) 250 mg q24h for 2 days followed by intravenous CMZ 2 g q8h for sigmoid diverticulitis. On day 5 of CMZ administration (after 12 doses in total), black stool was observed. On the following day (after 14 doses), prothrombin time (PT) prolongation was noted; PT and international normalized ratio (INR) were 37.1 s and 2.47, respectively. We diagnosed the patient with hypoprothrombinemia because of vitamin K deficiency caused by markedly elevated protein levels induced by vitamin K absence or antagonist-II on day 6 of CMZ administration. Intravenous vitamin K administration and CMZ cessation rapidly restored PT and led to the disappearance of black stool. CONCLUSIONS The causes of vitamin K deficiency were considered to be an impaired vitamin K cycle due to CMZ and decreased vitamin K intake because of malnutrition. These findings are consistent with CMZ's reported adverse effects. Decreased vitamin K production due to alterations in the gut bacterial flora by LVFX and CMZ was also postulated as a cause. If a bleeding tendency is noted during diverticulitis treatment with NMTT-containing cephems, switching to intravenous quinolones or carbapenems is recommended. It remains unclear how this reaction can be avoided; however, prudent monitoring of bleeding signs and PT-INR is recommended.
Errate: Hypoprothrombinemia During Cefmetazole Treatment: A Case Report
Am J Case Rep 2022 Nov 15;23:e938954.PMID:36377524DOI:10.12659/AJCR.938954.
The authors contacted the journal with the following corrections to the published article: 1. Table 1. PT-INR at 6th hospital day. 2.46 is incorrect; Correct: 2.47. 2. Table 2. Line 5, at Purpose of use of CMZ. NA is incorrect; Correct: Infection secondary to Pneumothorax. 3. Table 2. Line 11, at PT-INR, 2.46 is incorrect; Correct: 2.47. 4. References No. 22 and No. 23 are reversed. The authors apologize for these errors and state that this does not change the scientific conclusions of the article in any way. The original article has been updated. Reference: Yuichiro Haba, Hikaru Akizuki, Naoyuki Hashiguchi, Toshio Naito. Hypoprothrombinemia During Cefmetazole Treatment: A Case Report. Am J Case Rep. 2022; 23: e936712. DOI: 10.12659/AJCR.936712.