Search results for "Cephalosporin"
showing 10 items of 44 documents
Prediction and Interpretation of Some Pharmacological Properties of Cephalosporins Using Molecular Connectivity
1991
A method of molecular connectivity was used to study the pharmacological and antimicrobial properties of 34 cephalosporin antibiotics to verify its applicability to these parameters. By using Kier and Hall connectivity indices (Xi) as well as geometric indices (GIs), good correlation equations were obtained with a low number of variables. In some cases, such as the lethal dose for 50% of group (LD50) values and minimum inhibitory concentration (MIC) values for Pseudomonas aeruginosa, better regression equations were obtained with the GIs alone, confirming their alternative nature with respect to Xi, indices.
Randomized Comparative Trial with Ceftizoxime and Cefotaxime in Urinary Tract Infections
1984
Ceftizoxime, a new, semisynthetic, beta-lactamase-resistant cephalosporin, is not metabolized in man and is excreted almost entirely as the original active compound in the urine. The efficacy and safety of ceftizoxime were assessed in 80 patients with acute and chronic urinary infections, with and without associated pathological conditions, in comparison with cefotaxime. Two dosage schedules, 1 g or 0.5 g every 12 h, i.v. or i.m. for 10 days, were adopted according to the severity of each case and to separate randomization tables for each schedule; causal agents were all sensitive to both drugs in vitro. The overall results were excellent. Safety was excellent in almost all cases. In this t…
Ceftazidime Determination in Serum by High-pressure Liquid Chromatography
2004
A rapid and sensitive high-pressure liquid chromatographic method with simple sample preparation was developed for the quantitative analysis of the beta-lactam antibiotic ceftazidime (CAS 78439-06-2, Fortum). A good linear relationship was established between the peak area and the amount of ceftazidime injected over a concentration range of 1 to 200 microg/ml. The detection limit of the method was calculated to be 0.9 microg/ml. Stability was shown at 4 degrees C and at -196 degrees C for time periods of 2 h and 84 days, respectively.
Nonlinear intestinal absorption kinetics of cefuroxime axetil in rats.
1997
Cefuroxime is commercially available for parenteral administration as a sodium salt and for oral administration as cefuroxime axetil, the 1-(acetoxy)ethyl ester of the drug. Cefuroxime axetil is a prodrug of cefuroxime and has little, if any, antibacterial activity until hydrolyzed in vivo to cefuroxime. In this study, the absorption of cefuroxime axetil in the small intestines of anesthetized rats was investigated in situ, by perfusion at four concentrations (11.8, 5, 118 and 200 microM). Oral absorption of cefuroxime axetil can apparently be described as a specialized transport mechanism which obeys Michaelis-Menten kinetics. Parameters characterizing absorption of prodrug in free solutio…
Evidence for Impaired Hepatic Vitamin K1 Metabolism in Patients Treated with N-Methyl-Thiotetrazole Cephalosporins
1984
SummaryIn 8 patients on no oral intake and with parenteral alimentation, administration of cephalosporins with N-methyl-thiotetrazole side chain (moxalactam, cefamandole), was associated with prolongation of prothrombin time, appearance in the circulation of descarboxy-prothrombin (counter immunoelectrophoresis and echis carinatus assay) and diminution of protein C. Acute administration of 10 mg vitamin Ki was followed by the transient appearance of vitamin K1 2,3-epoxide, indicating an impaired hepatocellular regeneration of vitamin K1 from the epoxide. Impaired hepatic vitamin K1 metabolism, tentatively ascribed to the N-methyl-thiotetrazole group, is one (but possibly not the only) cause…
Particulate Matter Contamination of Intravenous Antibiotics Aggravates Loss of Functional Capillary Density in Postischemic Striated Muscle
2002
Through the increased use of less expensive and counterfeit medicines, the contamination of parenteral fluids and drugs by particulate matter poses an increasing health hazard worldwide. However, the mechanism of action of such contamination has never been conclusively demonstrated. We have systemically injected the particles contained in three different 1-g preparations of the antibiotic cefotaxime into hamsters and visualized the functional capillary density in striated skin muscle, using intravital fluorescence microscopy. Injection of particles from either of the three preparations did not affect capillary perfusion in normal muscle (n = 3 hamsters, each). However, injection of particle…
Experimental Studies on the Influence of Surfactants on Intestinal Absorption of Drugs Cefadroxil as model drug and sodium taurocholate as natural mo…
2011
The influence of the natural bile acid surfactant sodium taurocholate (CAS 81-24-3) on colic and duodenal (i.e. the proximal third of the small intestine) absorption of cefadroxil (CAS 50370-12-2) was studied using the in situ rat gut technique, and compared with the effect of sodium lauryl sulfate (CAS 151-21-3), the most widely used synthetic anionic surfactant. Previously, the stability, compatibility, and micelle-solubilization characteristics of taurocholate were assessed in order to correct, when necessary, the absorption results. White the passive absorption rate constants (kf, h-1) determined in colon in the presence of increasing lauryl sulfate concentrations showed an asymptotic v…
Mechanisms of Resistance to Ceftolozane/Tazobactam in Pseudomonas aeruginosa : Results of the GERPA Multicenter Study
2020
ABSTRACT Resistance mechanisms of Pseudomonas aeruginosa to ceftolozane/tazobactam (C/T) were assessed on a collection of 420 nonredundant strains nonsusceptible to ceftazidime (MIC > 8 μg/ml) and/or imipenem (>4 μg/ml), collected by 36 French hospital laboratories over a one-month period (the GERPA study). Rates of C/T resistance (MIC > 4/4 μg/ml) were equal to 10% in this population (42/420 strains), and 23.2% (26/112) among the isolates resistant to both ceftazidime and imipenem. A first group of 21 strains (50%) was found to harbor various extended-spectrum β-lactamases (1 OXA-14; 2 OXA-19; 1 OXA-35; 1 GES-9; and 3 PER-1), carbapenemases (2 GES-5; 1 IMP-8; and 8 VIM-2), or both (1 VIM-2…
Extended-Spectrum ß-Lactamase, AmpC-Producing, and Fluoroquinolone-Resistant Escherichia coli in Retail Broiler Chicken Meat, Italy.
2015
Background: Globally, antimicrobial drug-resistant Escherichia coli is among the most common etiological agents of invasive disease in humans. In Europe, increasing proportions of infections due to third-generation cephalosporins and/or fluoroquinolone-resistant extraintestinal pathogenic E. coli (ExPEC) strains are reported. E. coli from poultry are those more closely linked to human E. coli, but lack of reliable data makes it difficult to assess the attributable risk of different food sources. In the present study, our objective was to investigate the antimicrobial resistance profile, phylogenetic background, and virulence factors of E. coli isolates from broiler chicken meat sold at reta…
Possible coumarin-like mechanism of action for cephalosporins.
1984
In three patients treated with cephalosporins (one patient with latamoxef, two patients with cefazedone) vitamin K1 was injected to investigate whether this was followed by an increase in vitamin K1 2,3-epoxide plasma concentrations as compared to controls. Such a rise in K1-epoxide concentrations in the plasma can be demonstrated following treatment with coumarins. This reflects an inhibition of the vitamin K1-epoxide reductase in the liver. Coumarins are thought to induce hypoprothrombinaemia by such a mechanism. In all three patients we found a considerable increase in the vitamin K1-epoxide plasma concentrations following injection of 10 mg vitamin K1, whereas in normal subjects only tr…