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PubMedDate not supplied

In vitro susceptibility of Yersinia kristensenii strains to beta-lactam antibiotics.

The beta-lactam antibiotic susceptibility and beta-lactamase activity of 22 Yersinia kristensenii strains were determined in order to compare these properties with those reported for Y. enterocolitica. Carbenicillin, cephaloridine, cefoxitin and cefotaxime were the most active antimicrobial agents tested against Y. kristensenii. All strains were resistant to penicillin G, cephalothin, cephapirin and cephalexin. On the other hand, ampicillin and cefazolin activity could be considerated as intermediate. The influence of incubation temperature was also evaluated. All Y. kristensenii strains were more resistant at 22 degrees C than at 37 degrees C to beta-lactam antibiotics. Susceptibility to cefazolin was not affected by the incubation temperature. All Y. kristensenii strains produce beta-lactamase. The substrate profile of this enzyme is that of a cephalosporinase: its activity was highest on cephalothin, cephapirin, cephaloridine and cefazolin, while hydrolysis of ampicillin and carbenicillin was not detected. beta-Lactamase-resistant cefoxitin and cefotaxime were not hydrolysed. A correlation between beta-lactam antibiotic susceptibility and the hydrolysis rate of these antibiotics by beta-lactamase was observed, except for cephaloridine and cefazolin; these antibiotics were very good beta-lactamase substrates, but their MIC values were low.

Ampicillin↗
PubMed1997

Antibiotic residues and prevalence of mastitis pathogen isolation in heifers during early lactation following prepartum antibiotic therapy.

The present study was conducted to determine if antibiotic treatment of heifer mammary glands earlier in the prepartum period reduced the occurrence of residues in milk without compromising efficacy in treatment of intramammary infections. Heifers were assigned randomly to two groups: 1. untreated negative control (n = 42); and 2. intramammary infusion of 200 mg cephapirin sodium (n = 40) 14 days prior to expected calving. Mammary secretions were collected before treatment and during early lactation, and were analyzed for residues by the Bacillus stearothermophilus disc assay. Only four of 127 samples (3.1%) obtained from cephapirin-treated mammary glands at 3 days after calving were positive for residues and most (three of four) were from a heifer that calved within 3 days of treatment. Mammary secretions were also collected before treatment, and at 3 and 30 days after calving for microbiological evaluation. For untreated control heifers, mastitis pathogens were isolated from 67.3% of samples obtained from mammary glands 14 days prior to expected calving, 55.6% obtained 3 days after calving and 36.4% of samples obtained 30 days postpartum. A similar percentage of samples (63.8%) was positive for mastitis pathogens at 14 days before expected calving prior to antibiotic treatment. However, only 15.1% of samples obtained at 3 days after calving and 7.9% of samples obtained 30 days postpartum from mammary glands of antibiotic-treated heifers contained mastitis pathogens. Coagulase-negative staphylococci were isolated most frequently. Intramammary infusion of antibiotics earlier in the prepartum period markedly reduced the occurrence of residues in milk during early lactation without affecting efficacy.

Animals↗
PubMed2005

Short communication: Efficacy of parenteral ceftiofur for treatment of systemically mild clinical mastitis in dairy cattle.

The objective of this study was to evaluate the effect of intramuscular (i.m.) ceftiofur (2.2 mg/kg) on important outcomes of systemically mild clinical mastitis episodes in lactating dairy cattle. Cows with clinical mastitis were randomly assigned to a treatment group: pirlimycin intramammary (i.m.m.) (n = 35), pirlimycin i.m.m. and ceftiofur i.m.m. (n = 36), cephapirin i.m.m. (n = 40), cephapirin i.m. and ceftiofur i.m. (n = 33). Sixty-nine, 22, and 9% of initial cultures were gram-negative, gram-positive, and mixed, respectively. Logistic regression analysis showed no significant associations between treatment groups and loss of quarter, recurrence, or culling. Mixed infections, positive milk culture at 7 d after leaving hospital pen, decreased rumen motility, and absence of udder firmness were associated with increased odds of mastitis recurrence. The results suggest that i.m. ceftiofur treatment has no beneficial effects on the outcome of systemically mild clinical mastitis.

Animals↗
PubMed1992

Influence of prepartum antibiotic therapy on intramammary infections in primigravid heifers during early lactation.

Jersey heifers were assigned alternately to three groups: 1) negative control (n = 41), 2) intramammary infusion of 200 mg of sodium cloxacillin (n = 38) at 7 d before expected parturition, and 3) intramammary infusion of 200 mg of cephapirin sodium (n = 36) at 7 d before expected parturition. The percentage of mammary glands infected prior to treatment was 62.2, 50.0, and 70.1 for groups 1, 2, and 3, respectively. The percentage of mammary glands infected during early lactation was 44.5, 8.6, and 2.1 for groups 1, 2, and 3, respectively. Most infections (87.1%) were due to Staphylococcus species other than Staphylococcus aureus. Thirty-six of 460 quarters were infected with major pathogens before treatment, 3 of 22 persisted following antibiotic treatment, and 9 of 14 persisted in the control group. Infusion of sodium cloxacillin resulted in antibiotic residues in 17.4% of samples obtained .5 d postpartum. All samples were negative at 3 and 10 d postpartum. Infusion of cephapirin sodium resulted in antibiotic residues in 84.7, 28.2, and 0% of samples obtained at .5, 3, and 10 d, respectively. Prepartum antibiotic therapy was effective in eliminating many IMI, especially those caused by coagulase-negative staphylococci, but there is the potential for antibiotic residues in milk.

Animals↗
PubMed1992

Potentiation of antibiotic therapy for bovine mastitis by recombinant bovine interleukin-2.

Adjunct therapy with recombinant bovine interleukin-2 and antibiotics for Staphylococcus aureus IMI was investigated in an attempt to improve the therapy of antibiotics alone. Treatment of established S. aureus IMI with Na-cephapirin or Cefa-Lak produced average cures of 32.0 and 41.8%, respectively. When Na-cephapirin treatment was combined with recombinant bovine interleukin-2 at either 3.3 or 10 mg, the therapeutic efficacy was improved by an average of 20 to 30%. When Cefa-Lak treatment was combined with recombinant bovine interleukin-2 at 10 mg, the therapeutic efficacy was improved on average by 20%. Recombinant bovine interleukin-2, formulated in the excipient of the commercial Cefa-Lak, also improved the therapeutic efficacy by 16% compared with Cefa-Lak alone. Recombinant bovine interleukin-2, formulated in Cefa-Lak, maintained biological activity at room temperature for at least 21 d. After intramammary infusion of recombinant bovine interleukin-2, no biologically active interleukin-2 was detected in milk 48 h (four milkings) after administration. These data suggest that cytokines may be used as adjunct therapy with existing mastitis antibiotics or formulations of existing commercial products to improve the therapeutic efficacy.

Animals↗
PubMed1997

Activity of selected antimicrobial agents against strains of Staphylococcus aureus isolated from bovine intramammary infections that produce beta-lactamase.

The activity of selected antimicrobial agents was determined against strains of Staphylococcus aureus that were isolated from bovine intramammary infections and that were positive or negative for beta-lactamase. A total of 107 S. aureus strains (70 that were positive for beta-lactamase and 37 that were negative for beta-lactamase) were used in the study. Production of beta-lactamase was determined using a chromogenic cephalosporin disk method. Minimum inhibitory concentrations (MIC) for each test strain were determined using a commercially available microdilution panel. The following compounds were tested: penicillin, ampicillin, oxacillin, cephapirin, ceftiofur, penicillin plus novobiocin, erythromycin, and pirlimycin. Of the five beta-lactam compounds tested, penicillin and ampicillin were most affected by beta-lactamase activity, but oxacillin, cephapirin, and ceftiofur were not affected. Penicillin plus novobiocin also demonstrated excellent activity against strains of S. aureus that were both positive and negative for beta-lactamase. Erythromycin and pirlimycin demonstrated good activity against the S. aureus strains that were negative for beta-lactamase; 90% of the isolates had an MIC of < or = 0.5 microgram/ml (MIC90). The MIC90 for erythromycin and pirlimycin for strains that were positive for beta-lactamase was > 64.0 micrograms/ml. However, 8 strains, in addition to producing beta-lactamase, were also resistant to macrolides and lincosaminides. Recalculation of the MIC90 without these 8 strains yielded equivalent values for both erythromycin and pirlimycin with strains that were positive or negative for beta-lactamase (MIC90 < or = 0.5 microgram/ml).

Ampicillin↗
PubMed1975

In vitro bacteriostatic and bactericidal activities of 7 cephalosporin antibiotics on Haemophilus influenzae.

A total of 30 recently isolated strains of Haemophilus influenzae were tested for in vitro susceptibility to seven cephalosporins. In order of bacteriostatic effectiveness, the in vitro activity of the antibiotics studied was: cephapirin (median MIC = 0.78 mcg/ml), cephalothin (median MIC = 1.56 mcg/ml), cefazolin (median MIC: 1.56 mcg/ml), cephaloridine (median MIC = 3.12 mcg/ml), cefoxitin (median MIC = 3.12 mcg/ml), cephradine (median MIC = 12.5 mcg/ml) and cephalexin (median MIC = 25 mcg/ml). The bactericidal effectiveness of the seven compounds was studied against one of these strains. No drug was able to kill the selected strain in less than 6 hrs, even at 100 mcg per ml. Cefoxitin exhibited the best bactericidal effects, closely followed by cefazolin and cephapirin.

Cefazolin↗
PubMed1986

Randomized comparison of five irrigation solutions at cesarean section.

A randomized double-blind study was undertaken to determine which irrigation solution might be best at cesarean section. A saline placebo was compared with ampicillin sodium and one each of three generations of cephalosporins: cephapirin sodium, cefamandole nafate, and moxalactam disodium. A total of 360 cesarean sections were studied, and comparisons made between antibiotic and control groups relative to demographics, possible risk factors, and multiple measures of postoperative morbidity. The total group was further divided into high- and low-risk labor and repeat cesarean groups. Post-cesarean endometritis was diagnosed in the following frequencies for the group as a whole: placebo (24.6%), ampicillin sodium (8.5%), cephapirin sodium (11.4%), cefamandole nafate (4.6%), and moxalactam disodium (16.4%). Cefamandole nafate consistently demonstrated significant decreases in endometritis and other morbidity measures versus placebo both in laboring patients and the group as a whole.

Ampicillin↗
PubMed1995

The in vitro activity of beta-lactamase inhibitors in combination with cephalosporins against M. tuberculosis.

Although there are reports that the addition of a beta-lactamase inhibitor to ampicillin or amoxicillin greatly improves their in vitro activity against M. tuberculosis, there are no written reports about the antituberculosis effects of beta-lactamase inhibitors in combination with cephalosporins against M. tuberculosis. In this report, we have determined the minimal inhibitory concentrations (MIC) of 5 cephalosporins with or without combination with beta-lactamase inhibitor against M. tuberculosis strains isolated from patients before antituberculosis treatment and checked the production of beta-lactamase by bacteria before this procedure. Four strains of M. tuberculosis were contaminated during the experiment, and all the other 16 strains hydrolyzed the nitrocefin disc, thus indicating a beta-lactamase producer. The MICs of cephalosporins alone against M. tuberculosis were 200-400 micrograms/ml for ceforanide, 100-400 micrograms/ml for cephapirin, 400-1600 micrograms/ml for cefamandole, 200-1600 micrograms/ml for cefotaxime, and 800-1600 micrograms/ml for ceftriaxone. After adding the equimolar concentrations of sulbactam, the MICs were reduced to 100-200 micrograms/ml for ceforanide, 12.5-100 micrograms/ml for cephapirin, 100-400 micrograms/ml for cefamandole, 25-200 micrograms/ml for cefotaxime, and 100-800 micrograms/ml for ceftriaxone. We concluded that sulbactam enhanced the antituberculosis effect of cephalosporins.

Cefamandole↗
PubMed2003

Confirmatory analysis of beta-lactam antibiotics in kidney tissue by liquid chromatography/electrospray ionization selective reaction monitoring ion trap tandem mass spectrometry.

Eleven beta-lactam antibiotics were analyzed in fortified and incurred beef kidney tissue using high-performance liquid chromatography/electrospray ionization/selective reaction monitoring-ion trap tandem mass spectrometry (LC/ESI-SRM-MS(n)). The analytes included: deacetylcephapirin, amoxicillin, cephapirin, desfuroylceftiofur cysteine disulfide (DCCD, a biomarker of ceftiofur), ampicillin, cefazolin, Pen G, oxacillin, cloxacillin, naficillin and dicloxicillin. Analytes were extracted with acetonitrile and water. Clean-up was performed by solid-phase extraction. Limits of confirmation in fortified tissue are as follows (tolerances or target levels in parentheses): deacetylcephapirin: 10-50 ng/g (100 ng/g); amoxacillin: 50-100 ng/g (10 ng/g); cephapirin: 10 ng/g (100 ng/g); DCCD: 500 ng/g (8000 ng/g); ampicillin: 10 ng/g (10 ng/g); cefazolin: 10 ng/g (10-50 ng/g); Pen G: 10 ng/g (50 ng/g); oxacillin: 10 ng/g (10-50 ng/g); cloxacillin: 10 ng/g (10 ng/g); naficillin: 10 ng/g (10-50 ng/g); dicloxacillin: 100-500 ng/g (10-50 ng/g). The present method was also tested on incurred kidney tissue that had previously been analyzed using a microbial assay. Good correspondence was found between the results from this new method and the bioassay. However, the present method is much more specific and, in several cases, more sensitive than the bioassay. In addition, the time of analysis is significantly shorter than the bioassay. We also found that SRM MS(n) was superior in the analysis of unknown incurred tissue than full spectrum MS(n). We also obtained an MS/MS spectrum of DCCD that is significantly at variance with previously published fragmentation spectra.

Animals↗
PubMed1979

Separation of some cephalosporin derivatives by ion-pair reversed-phase high-performance liquid chromatography.

Cephapirin, its major metabolite desacetylcephapirin, 7-aminocephalosporanic acid and some other cephalosporin derivatives are separated on a chemically bonded octadecylsilane reversed-phase column. The selectivity between cephapirin and desacetylcephapirin on the reversed-phase column is too high, resulting in a poor separation. The effect of several variations of the chromatographic conditions on the selectivity has been examined. The in situ ion-pair formation of the cephalosporins with several counter ions and the influence of the ion-pair formation on the capacity factor and on the selectivity have been investigated. Other factors, such as the temperature, combination of counter ions and nature of the organic modifier and their influence on the selectivity have also been studied.

Cephalosporins↗
PubMed2005

Voltammetric analysis of Cu (II), Cd (II) and Zn (II) complexes and their cyclic voltammetry with several cephalosporin antibiotics.

Both osteryoung square wave voltammetry and cyclic voltammetry have been utilized to elucidate and confirm the possible complexation reaction that occur between the various cephalosporin antibiotics and either the toxic, non-essential metal ion, viz. Cd (II), or the essential but toxic (when their concentration exceeds certain level in serum) metal ions, viz. Cu (II) and Zn (II). Voltammetric measurements indicated the existence of 1:1 metal-to-ligand ratio (as in cephalexin and cephapirin complexes), 1:2 ratio (such as in cefamandole, cefuroxime and cefotaxime complexes) and 2:1 ratio in case of ceftazidime complexes. Adsorption behavior was evidenced for Cu (II)-cefuroxime or ceftazidime complexes as well as for those for Zn (II)-cephalexin or cephapirin. This phenomenon could be used for the determination of either the antibiotic or the metal ion using adsorptive stripping voltammetry. Detection limits down to 7x10(-10) M have been easily achieved.

Cadmium↗
PubMed2000

Optimization of separation and migration behavior of cephalosporins in capillary zone electrophoresis.

The influences of buffer pH, buffer concentration and buffer electrolyte on the migration behavior and separation of 12 cephalosporin antibiotics in capillary zone electrophoresis using three different types of buffer electrolyte, including phosphate, citrate, and 2-(N-morpholino)ethanesulfonate (MES), were investigated. The results indicate that, although buffer pH is a crucial parameter, buffer concentration also plays an important role in the separation of cephalosporins, particularly when cefuroxime and cefazolin, cephalexin and cefaclor, or cefotaxime and cephapirin are present as analytes at the same time. The electrophoretic mobility of cephalosporins and electroosmotic mobility measured in citrate and MES buffers are remarkably different from those measured in phosphate buffer. With citrate buffer, optimum buffer concentration is confined to a small range (35-40 mM), whereas buffer concentrations up to 300 mM can be used with MES buffer. Complete separations of 12 cephalosporins could be satisfactorily achieved with these three buffers under various optimum conditions. However, the separability of 12 cephalosporins with citrate or MES buffer is better than that with phosphate buffer. As a consequence of a greater electrophoretic mobility of cephalosporins than the electroosmotic mobility with citrate buffer at pH below about 5, some cephalosporins are not detectable. The cloudiness of the peak identification and of the magnitudes of the electrophoretic mobility of cefotaxime and cefuroxime reported previously are clarified. In addition, the pKa values of cephradine, cephalexin, cefaclor, and cephapirin attributed to the deprotonation of either an amino group or a pyridinium group are reported, and the migration behavior of these cephalosporins in the pH range studied is quantitatively described.

Alkanesulfonic Acids↗
PubMed1983

Stability of single and combination antimicrobial agents in various peritoneal dialysates in the presence of insulin and heparin.

The antimicrobial activity of ampicillin, azlocillin, cefotaxime, cephapirin, clindamycin, mezlocillin, nafcillin, piperacillin, tobramycin, and vancomycin was tested in peritoneal dialysate at room temperature for 24 hours and 48 hours. All of the antimicrobial agents were active at 24 hours. The bioactivity of cefotaxime, nafcillin, and vancomycin declined 15% to 20% after 48 hours (P less than 0.001). The addition of heparin or insulin did not affect the activity of any of the study drugs. The combination of cephapirin and tobramycin remained bioactive for 24 hours at room temperature and 35 degrees C. The preparation of drug-dialysate solution every one to two days is feasible for the treatment of peritonitis in patients on continuous ambulatory or continuous cycled peritoneal dialysis.

Anti-Bacterial Agents↗
PubMed2004

Automated microarray system for the simultaneous detection of antibiotics in milk.

A parallel affinity sensor array (PASA) for the rapid automated analysis of 10 antibiotics in milk is presented, using multianalyte immunoassays with an indirect competitive ELISA format. Microscope glass slides modified with (3-glycidyloxypropyl)trimethoxysilane were used for the preparation of hapten microarrays. Protein conjugates of the haptens were immobilized as spots on disposable chips, which were processed in a flow cell. Monoclonal antibodies against penicillin G, cloxacillin, cephapirin, sulfadiazine, sulfamethazine, streptomycin, gentamicin, neomycin, erythromycin, and tylosin allowed the simultaneous detection of the respective analytes. Antibody binding was detected by a second antibody labeled with horseradish peroxidase generating enhanced chemiluminescence, which was recorded with a sensitive CCD camera. All liquid handling and sample processing was fully automated, and one analysis was carried out in milk within less than 5 min. The detection limits ranged from 0.12 (cephapirin) to 32 microg/L (neomycin). Penicillin G could be detected at the maximum residue limit (MRL); the detection limits for all other analytes were far below the respective MRLs. The PASA system proved to be the first immunochemical biosensor platform having the potential to test for numerous antibiotics in parallel, such being of considerable interest for the control of milk in the dairy industry.

Animals↗
PubMed2003

Residues of beta-lactam antibiotics in bovine milk: confirmatory analysis by liquid chromatography tandem mass spectrometry after microbial assay screening.

A procedure for the simultaneous determination of the residues of seven beta-lactam antibiotics (penicillin G, ampicillin, oxacillin, amoxicillin, dicloxacillin, cephalexin, cephapirin) in bovine raw milk using tandem liquid chromatography mass spectrometry (LC-MS/MS) is described. The antibiotics were extracted by an acetic acid solution after centrifugation and filtration. The beta-lactams were separated using reversed-phase liquid chromatography. A triple quadrupole mass spectrometer was used in positive-ion mode as a detector via a Turbo Ionspray interface for electrospray ionization (ESI). The limits of detection and quantitation of the method were below the legal tolerances, except for ampicillin. The method was used to confirm 53 samples found positive by a microbial method (Delvotest SP) at the Istituto Zooprofilattico Sperimentale per la Lombardia e l'Emilia Romagna of Brescia during 2001. Penicillin G was found in 26 samples at concentrations ranging from less than 4 to 6240+/-550 microg x l(-1). Amoxicillin was found in three samples at concentrations ranging from 8.5+/-0.1 to 53.7+/-2.3 microg x l(-1). Cephapirin was found in two samples at 5.7+/-0.1 and 6.4+/-0.3 microg x l(-1).

Animals↗
PubMed1985

Cephalosporins for surgical prophylaxis: computer projections of intraoperative availability.

Cephalosporin antibiotics are the most frequently used agents for surgical prophylaxis. Within this class are considerable pharmacokinetic variations that could have significant implications. We used a computer simulation of cephalosporin serum levels to describe concentrations achieved and maintained intraoperatively when the agents are given intravenously "on call" to the operating room or with induction of anesthesia. Intraoperative serum concentrations fall below 1 microgram/ml if an operation lasts longer than 2.3, 2.7, 3.8, or 4.0 hours when cephalothin, cephapirin, cefamandole, or cefoxitin, respectively, is given in usual doses upon induction of anesthesia. When the same agents are given intravenously on call to the operating room, intraoperative serum concentrations fall below 1 microgram/ml for operations lasting longer than 1.1, 1.5, 2.6, or 2.8 hours, respectively. If cephalothin, cephapirin, cefamandole, or cefoxitin is used, it should be given at induction of anesthesia to provide maximal intraoperative serum concentrations. The longer half-life of cefazolin, ceforanide, cefonicid, and cefuroxime is a potential advantage because serum concentrations of these agents are well above 1 microgram/ml for as long as eight to 22 hours even after on-call administration.

Anesthesia, General↗
PubMed1981

Passage of cephalosporins and amoxicillin into the breast milk.

The concentrations of five cephalosporins and amoxicillin in breast milk were studied in 42 voluntarily participating lactating mothers using standard assay methods. Each mother received one single dose of 1 g of either an orally or intravenously administered antibiotic. Amoxicillin, cephalexin, and cefadroxil were given orally, and peak milk concentrations averaged 0.81 +/- 0.33 microgram/ml at 5 hours, 0.50 +/- 0.23 microgram/ml at 4 hours, and 1.64 +/- 0.73 microgram/ml at 6 hours, respectively. Cephalothin, cephapirin and cefotaxime were given as an i.v. bolus injection, and peak milk concentrations at 2 hours averaged 0.47 +/- 0.14 microgram/ml, 0.43 +/- 0.16 microgram/ml and 0.32 +/- 0.09 microgram/ml, respectively. The high concentrations of cefadroxil can be explained by its low rate of elimination and higher fat solubility. Milk/serum ratios for all antibiotics were increasing as serum concentrations were diminishing, especially with cephalothin and cephapirin whose serum concentrations are rapidly declining. The significance of bactericidal concentrations in breast milk remains to be evaluated.

Administration, Oral↗