Topic
Ceftezole
About: Ceftezole is a research topic. Over the lifetime, 36 publications have been published within this topic receiving 382 citations.
Papers
TL;DR: Ceftezole, a new cephalosporin derivative, was compared with cefazolin, Cephaloridine, and CEPhalothin this article.
Abstract: Ceftezole, a new cephalosporin derivative, was compared with cefazolin, cephaloridine, and cephalothin. Data obtained indicate that it is a broad-spectrum antibiotic, with almost identical antimicrobial activity against pathogenic organisms isolated from patients. The therapeutic effect of ceftezole on experimental infections in mice was similar to that of cefazolin and was superior to that of cephalothin. The binding of ceftezole to serum proteins was somewhat less than that of cefazolin. The concentrations of ceftezole in the sera of test animals and human volunteers were determined after intramuscular injection of 20 mg/kg and after a single dose of 500 mg, respectively. The concentration of ceftezole in the serum of volunteers peaked at 24.9 μg/ml 15 min after injection and remained effective (about 2.6 μg/ml) at 4 h. The half-life in serum under the same conditions was 56 min, i.e., about one-half that of cefazolin. The 24-h urinary recovery rate was 87.5%. Most of the administered ceftezole was excreted unchanged mainly through the urinary tract. The biliary excretion rate in SD strain rats after intramuscular injection of 20 mg/kg was about 4.4%. As compared with commercially available cephalosporins, ceftezole was second only to cefazolin in biliary excretion rate. Various tissue levels of ceftezole in animals were higher than cephalothin but, with the exception of renal levels in the early stage after administration, were lower than cefazolin.
27 citations
TL;DR: In this paper, a simple and sensitive procedure for the simultaneous determination of cephacetrile and ceftezole in a mixture is presented, which can be profitably applied to the quantitation of these drugs in injectable dosage forms.
Abstract: A simple and sensitive procedure for the simultaneous determination of cephacetrile and ceftezole in a mixture is presented. First and second derivative spectrophotometry, with a ‘zero - crossing’ technique of measurement, has been used. The methods give linear calibration graphs, with zero intercept on y-axis, for up to 36 μg/ml of cephalosporins. Detection limits of cephacetrile and ceftezole, at p=0.05 level of significance, were calculated to be 0.39 and 0.46 μg/ml in the first derivative mode, and 0.26 and 0.19 μg/ml in the second derivative mode, respectively. The method can be profitably applied to the quantitation of these drugs in injectable dosage forms.
25 citations
TL;DR: In this article, the solubility data of ceftezole in seven pure solvents and two binary solvent systems were experimentally measured via a static gravimetric method in the temperature range from 278.15 to 313.15 K under atmospheric pressure.
16 citations
TL;DR: In vivo and in vitro results suggest that ceftezole may be a clinically useful anti-diabetic compound.
Abstract: Using a high throughput-compatible assay to screen for potential alpha-glucosidase inhibitors, we found that the beta-lactam antibiotic ceftezole exhibited potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Using an in vivo streptozotocin-induced mouse model, we confirmed that blood glucose levels decreased by 30% 20 min after ceftezole treatment (10 mg/kg/day). Expression levels of glycogen synthase kinase-3, peroxisome proliferator-activated receptor-gamma, and uncoupling protein-3 mRNA were also slightly decreased compared to controls following ceftezole treatment. Taken together, these in vivo and in vitro results suggest that ceftezole may be a clinically useful anti-diabetic compound.
15 citations
TL;DR: The results suggest that some of cephalosporins such as ceftezole, cefotiam, cephacetrile and cefazolin provide epileptogenic activity at higher doses.
Abstract: Epileptogenic activity induced by intravenous injection of certain cephalosporin derivatives was studied. Ceftezole provided the most potent epileptogenic activity among the drugs tested. Changes in seizure patterns on electroencephalogram (EEG) tracings and behavioral signs after administration of cefotiam and cefazolin were similar to those seen after ceftezole, though the intensity and duration were less than those of ceftezole. Cephacetrile and cephaloridine elicited the spiking activity in the frontal cortex and the other regions without apparent behavioral changes. Latamoxef and cefmenoxime displayed a weak epileptogenic activity at a dose of 1000 mg/kg. On the other hand, cephapirin, cefmetazole and cefoxitin did not evoke any changes in EEG nor in behavior. Penicillin G at a dose of 200 mg/kg affected spike or spike-and-wave complex in a few cases, but at a dose of 500 mg/kg the animals died of dyspnea almost immediately after injection without showing apparent epileptogenic signs. These results suggest that some of cephalosporins such as ceftezole, cefotiam, cephacetrile and cefazolin provide epileptogenic activity at higher doses.
14 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2020 | 1 |
| 2019 | 3 |
| 2015 | 3 |
| 2013 | 2 |
| 2012 | 3 |
| 2011 | 4 |