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PubMed1979

Effect of cephapirin on formation of D-alanine carboxypeptidase in growing Bacillus subtilis cells.

Cephapirin was utilized to examine the interaction of beta-lactam antibiotics with growing Bacillus subtilis cells and the biological effects simultaneously produced. Saturation binding and quantitative cell death were observed at the cephapirin concentration of 0.1 mug/ml. Cephapirin bound to all penicillin-binding proteins except the d-alanine carboxypeptidase. A specific [(14)C]benzylpenicillin-binding assay was developed for the d-alanine carboxypeptidase. At the lowest saturating concentration of antibiotic (0.1 mug/ml), cephapirin inhibited formation of the d-alanine carboxypeptidase. Upon incubation with cephapirin, 18% of the membranous d-alanine carboxypeptidase was released into the media. The data suggest that beta-lactam antibiotics may affect the formation of bacterial cytoplasmic membranes in addition to their effect on cell wall synthesis.

Bacillus subtilis↗
PubMed2002

Use of antimicrobial susceptibility testing of bacterial pathogens isolated from the milk of dairy cows with clinical mastitis to predict response to treatment with cephapirin and oxytetracycline.

OBJECTIVE: To determine whether results of antimicrobial susceptibility testing of bacterial pathogens isolated from the milk of dairy cows with clinical mastitis were associated with duration of clinical signs or bacteriologic cure rate following treatment with cephapirin and oxytetracycline. DESIGN: Observational study on a convenience sample. ANIMALS: 58 dairy cows with 121 episodes of clinical mastitis. PROCEDURE: Cows that only had abnormal glandular secretions were treated with cephapirin alone. Cows with an inflamed gland and abnormal glandular secretions were treated with oxytetracycline and cephapirin. Cows with systemic signs of illness, an inflamed gland, and abnormal glandular secretions were treated with oxytetracycline and flunixin meglumine and frequent stripping of the affected glands. The Kirby-Bauer method was used for antimicrobial susceptibility testing, and current guidelines were used to categorize causative bacteria as susceptible or resistant to the treatment regimen. RESULTS: Median durations of episodes of clinical mastitis caused by susceptible (n = 97) and resistant (24) bacteria were not significantly different. Bacteriologic cure rates at 14 and 28 days were similar for episodes caused by susceptible and resistant bacteria; however, for 56 episodes of clinical mastitis caused by gram-positive bacteria and treated with cephapirin alone, bacteriologic cure rate at 28 days was significantly higher for susceptible than for resistant bacteria. CONCLUSIONS AND CLINICAL RELEVANCE: Results suggest that antimicrobial susceptibility testing was of no value in predicting duration of clinical signs or bacteriologic cure rate in dairy cows with mastitis, except for episodes caused by gram-positive organisms treated with intramammary administration of cephapirin alone.

Animals↗
PubMed1984

Stability of cephapirin sodium admixtures after freezing and conventional or microwave thaw techniques.

The freeze-microwave thaw technique has important advantages compared with conventional piggyback delivery systems. A requirement for the implementation of this technique, however, is the documentation of antibiotic stability following freezing and microwave thawing. The purpose of this study was to assess the stability of a commonly used cephalosporin, cephapirin sodium, following freezing and conventional or microwave thawing. This data was not previously available. Cephapirin sodium was admixed with either 5% dextrose injection or 0.9% sodium chloride injection in polyvinylchloride minibags at concentrations of 10 and 40 mg/ml and then frozen for 14 days. Admixtures were then thawed conventionally or by microwave heating. Cephapirin concentrations were determined spectrophotometrically after reconstitution, immediately after thawing, and 6, 12, and 24 hours after thawing. No significant differences in admixture potency after reconstitution, immediately after thawing, or at 6, 12, and 24 hours after thawing were observed when thaw techniques were compared. All admixtures retained at least 90% of labeled content regardless of thaw technique, type of diluent, or initial concentration. In addition, all admixtures retained at least 90% potency 24 hours after thawing when compared with the actual concentration determined immediately after reconstitution. The rate of cephapirin degradation was not influenced by thaw technique, type of diluent, or initial admixture concentration. The results of this study suggest that cephapirin sodium may be added to the list of drugs capable of withstanding freeze-microwave thaw treatment.

Cephalosporins↗
PubMed2005

The effect of a single administration of cephapirin or cloprostenol on the reproductive performance of dairy cows with subclinical endometritis.

This study examined the effect of a single administration of cephapirin iu or cloprostenol im on the reproductive performance of dairy cows with subclinical endometritis. Cows (n = 228) at 20-33 days in milk (DIM) from two commercial dairy farms, determined to be normal for clinical endometritis (based on absence of abnormal uterine discharge on vaginoscopic examination) were enrolled. At enrollment, a thorough reproductive examination was performed, including rectal palpation, ultrasonography (US) and endometrial cytology (EC). The case definition for subclinical endometritis was the presence of >18% neutrophils on EC examination or fluid in uterus (FIU) on US examination. All cows were randomly assigned to receive one of three treatments: 500 mg benzathine cephapirin iu, 500 microg cloprostenol im, or control (no treatment). Reproductive performance was monitored for a minimum of 8 months after treatment. Cows with subclinical endometritis treated with cephapirin or cloprostenol had a significantly increased relative pregnancy rate compared to control [hazard ratios 1.89 (P = 0.01) and 1.70 (P = 0.05), respectively]. In conclusion, a single treatment with cephapirin or cloprostenol at 20-33 DIM significantly improved the reproductive performance of cows with subclinical endometritis.

Animals↗
PubMed1981

A comparison of the penetration characteristics of cephapirin and cephalothin into right atrial appendage, muscle, fat, and pericardial fluid of pediatric patients undergoing open-heart operation.

Thirty-two pediatric patients having open-heart operation received a single dose of either cephalothin or cephapirin intravenously, 30 mg per kilogram of body weight, in the operating room, for prophylaxis before the chest cavity was opened. Samples of right atrial appendage, pericardial fluid, muscle, fat, and plasma were obtained at various time intervals after injection of the antibiotics, and assayed for cephalosporin concentration. The concentration-time profiles of cephalothin and cephapirin in atrial appendage, muscle, fat, and plasma were identical. Cephapirin produced higher total and free concentrations in pericardial fluid compared with cephalothin. This presumably was due to the lower protein binding of cephapirin. Antibiotic concentrations above the minimal inhibitory concentration for Staphylococcus aureus and S. epidermidis were present in myocardial tissue for at least 90 minutes after the dose was administered. These data support the need to administer these antibiotics shortly before surgical intervention and, if the operation is prolonged, the need to administer a second dose of antibiotic.

Adipose Tissue↗
PubMed1987

Distribution of cephapirin into a tissue chamber implanted subcutaneously in horses.

The pharmacokinetics of cephapirin sodium and its distribution into a tissue chamber implanted subcutaneously in the neck of mature horses are described. Cephapirin was administered as an intravenous bolus dose of 20 mg/kg. The serum concentration vs time curve was best described by a two-compartment open model. Cephapirin disappeared from serum rapidly (t1/2 beta = 18.8 min), and had only a modest volume of distribution (Vd(area) approximately equal to 346 mg/kg, Vd(ss) approximately equal to 204 ml/kg). Total clearance was also rapid (approximately equal to 13 ml/min.kg). Concentrations of the antibiotic in tissue chamber fluid, however, were quite constant from 30 min to 3 h post-injection, and did not decay in parallel with either the concentration of the drug in serum or the estimated concentration of drug in the peripheral compartment. The ratio of area under the curve (AUC0-3 h) for serum: chamber fluid was 13.8 : 1, while that for peripheral compartment : chamber fluid was 11 : 1. The slow rate of cephapirin transport into, and out of, the chamber may be related to its hydrophilic nature. The lack of parallelism between the chamber fluid decay curve and that of serum is characteristic of drugs with a very short half-life.

Animals↗
PubMed1991

Development of an analytical method for cephapirin and its metabolite in bovine milk and serum by liquid chromatography with UV-VIS detection and confirmation by thermospray mass spectometry.

Metabolites of the cephapirin beta-lactam antibiotic have not previously been reported in bovine milk. The principal metabolite was tentatively identified as desacetylcephapirin by liquid chromatography with UV-VIS photodiode array (LC/UV-VIS PDA), and liquid-chromatography-mass-spectrometric (LC-MS) detection. Synthetic desacetylcephapirin was prepared by incubation of cephapirin in bovine milk and serum at 37 degrees C. Also, a method for determining cephapirin in bovine milk and serum was developed. The detection limits for cephapirin and desacetylcephapirin were estimated to be 10 and 50 micrograms/kg, respectively, for LC/UV-VIS PDA, and 100 and 500 micrograms/kg for LC-MS.

Animals↗
PubMed1991

Efficacy of a cephapirin dry cow product for treatment of experimentally induced Staphylococcus aureus mastitis in heifers.

A dry cow product containing 300 mg of cephapirin benzathine was evaluated in pregnant and nonpregnant Jersey heifers for its effect on experimentally induced Staphylococcus aureus mastitis. Cephapirin was detectable in mammary secretion of nonpregnant heifers for up to 5 wk and in tissue for 1 wk after intramammary infusion. Staphylococcus aureus was not detectable in tissue and secretion of treated quarters at 1 and 3 wk but was not eliminated from two quarters of one heifer tested at 6 wk posttreatment. Histologic evaluation of mammary tissue from nonpregnant heifers revealed significant differences in leukocytosis between uninfected and S. aureus-infected quarters but no differences in epithelium, lumen, and stroma, indicating no difference in secretion potential or glandular development. Twenty-five pregnant Jersey heifers were experimentally infected in two quarters with S. aureus 12 to 14 wk prepartum. After 1 to 3 wk, 13 heifers were infused in 21 S. aureus-infected quarters with a commercial cephapirin dry cow product. Nine infected quarters were left untreated. All treated quarters were bacteriologically negative both at calving and through 2 mo after calving. Of the 9 infected quarters not treated prepartum, 1 spontaneously cured and 2 became non-functional. The remaining quarters were treated at calving with a commercial cephapirin lactating cow product. Of these, 3 cured and 3 failed to resolve.

Animals↗
PubMed1979

[Effect of combination of hetacillin, cephapirin and amikacin (author's transl)].

With the investigations of the effect of combination of hetacillin, cephapirin and amikacin, following experimental results were obtained; 1. Effect of combination of amikacin, cephapirin and hetacillin was differed depending upon the genus and species of bacteria. However, in general, in the cases showing effective results there was a relation in the concentration of these antibiotics. With strains of Escherichia coli amikacin and cephapirin was cooperative, but not with other combinations and strains of Proteus showed similar tendencies to those strains. In the strains of Pseudomonas, no effect was observed with these antibiotics. However, significant cooperative effect was shown in strains of Klebsiella pneumoniae. In penicillin-resistant strains of Staphylococci cooperative effect was represented only a combination of amikacin and hetacillin. 2. Amikacin was resistant against penicillinase isolated from penicillin-resistant strain of Staphylococcus and cephalosporinase extracted from cephalosporin-resistant strain of Escherichia coli. 3. When a strain of K. pneumoniae, showing cooperative effect with amikacin and cephapirin, was examined by electronmicroscopy, enlargement of cells and destruction of the cell walls were observed.

Amikacin↗
PubMed1991

Pharmacokinetics and synovial fluid concentrations of cephapirin in calves with suppurative arthritis.

Six calves with suppurative arthritis were given a single IM injection of sodium cephapirin at a dosage of 10 mg/kg of body weight. Cephapirin concentrations were serially measured in serum and in normal and suppurative synovial fluid over a 24-hour period. Mean peak serum concentration was 6.33 microliters/ml at 20 minutes after injection. The highest cephapirin concentrations in normal and suppurative synovial fluid were 1.68 and 1.96 micrograms/ml, respectively, 30 minutes after injection. Overall mean cephapirin concentration in normal synovial fluid for the first 4 hours (1.04 +/- 0.612 micrograms/ml) was not significantly different from that in suppurative synovial fluid (0.88 +/- 0.495 micrograms/ml; P greater than 0.05). Elimination half-life was 0.60 hours and clearance was 1,593 ml/h/kg.

Animals↗
PubMed1972

Relative incidence of phlebitis caused by continuous intravenous infusion of cephapirin and cephalothin.

In a single-blinded study, two groups of 10 healthy subjects were given cephapirin or cephalothin by continuous intravenous infusion for 5 days, 0.5 g every 6 hr for the first day and then 1.0 g every 6 hr for 4 days. Eight of the cephalothin subjects and two of the cephapirin subjects developed phlebitis. Phlebitis was more severe in the cephalothin group and developed more rapidly, necessitating vein changes six times more often than in the cephapirin group. The less irritating properties of cephapirin demonstrated in this study indicate it may be the more useful cephalosporin analogue for intravenous therapy.

Acetamides↗
PubMed2000

Conversion of cephapirin to deacetylcephapirin in milk and tissues of treated animals.

Cephapirin is one of six beta-lactam antibiotics approved for use in the treatment of food-producing animals in the United States. When used for treatment of mastitis by intramammary infusion, it is partially converted to a microbiologically active metabolite identified as deacetylcephapirin (DACEP). The degradation was followed in four cows with naturally acquired mastitis which were treated with cephapirin. DACEP persisted longer than the parent compound in the milk. When a calf was treated with cephapirin by intramuscular injection, the compound was almost completely converted to DACEP in tissues. The deacetyl form must be considered in the determination of residues in treated animals.

Animals↗
PubMed1983

Cephapirin therapy in infective endocarditis.

Ten patients, eight of them heroin addicts, with infective endocarditis were treated with cephapirin. Causative organisms included Staphylococcus aureus in six patients and viridans streptococci, S bovis, and S pneumoniae in one patient each. In one of the patients with endocarditis, both S aureus and an organism of the beta-Streptococcus group were simultaneously isolated. All patients except two, both with monomicrobial S aureus endocarditis, were cured. All isolates were inhibited by less than or equal to 0.5 micrograms/ml of cephapirin. Peak serum bactericidal activity greater than or equal to 32 times the minimal inhibitory concentration (MIC) of the causative organism was achieved in all cases after giving 2 gm IV every four hours. After using large inoculums of staphylococci for in vitro tests, we found that twofold to eightfold increases in MIC occurred. Cephapirin was well tolerated intravenously and high levels in serum were achieved without toxicity or accumulation of the drug.

Adult↗
PubMed1976

Comparative pharmacokinetics and metabolism of cephapirin in laboratory animals and humans.

Comparative drug disposition studies in mice, rats, dogs, and humans indicate that cephapirin, a new semisynthetic cephalosporin antibiotic that exhibits broad-spectrum antimicrobial activity, is metabolized to desacetylcephapirin in these species. Pharmacokinetic analyses of the concentrations of cephapirin and desacetylcephapirin in plasma and urine reveal that the rate and extent of deacetylation decreases from rodents to dogs to humans. The kinetic analyses also suggest that the kidney performs a role not only in the excretion but also in the metabolism of cephapirin to desacetylcephapirin.

Animals↗
PubMed1976

Comparative pharmacokinetics of cefamandole, cephapirin, and cephalothin in healthy subjects and effect of repeated dosing.

Cefamandole nafate, cephapirin, and cephalothin were administered intravenously in crossover fashion to 12 volunteers, in dosages of 2 g every 6 h for 16 doses. Mean peak levels of cefamandole were approximately 50% higher than those of the other agents. The serum concentration curves appeared to decline bi-exponentially, suggesting that a two-compartment model was most applicable for pharmacokinetic analysis; accordingly, the t((1/2)) of cefamandole was significantly longer when the serum peak was omitted from the analysis (0.86 versus 0.73 h, P < 0.05). The half-lives of cephalothin and cephapirin, 0.34 and 0.36 h, respectively, were probably underestimates reflecting the inclusion of distribution-phase values in the calculation. Repeated dosing had no effect on the peak serum levels, half-life, serum clearance, or apparent volume of distribution with one exception: peak serum levels of cephapirin were significantly lower after the sixteenth than after the first dose. Marked variations within a given subject were noted in the half-life and apparent volume of distribution of cefamandole in several instances. Renal clearances of cefamandole exhibited saturation kinetics similar to those of penicillin G.

Cephalosporins↗
PubMed1982

Anion-exchange extraction of cephapirin, cefotaxime, and cefoxitin from serum for liquid chromatography.

An anion-exchange column technique for extraction of antibiotics from serum proteins has been developed for use in the assay of cephapirin, cefotaxime, and cefoxitin by high-pressure liquid chromatography. Anion-exchange extraction of cephapirin from serum samples by this technique was compared with protein precipitation methods, using 6% trichloroacetic acid or absolute ethanol. Column extraction gave improved quantitative drug recovery and reduced background serum interferences in the resultant chromatograms when evaluated against protein precipitation. Comparisons of this method with microbiological assay gave statistically equivalent results. Twelve patient samples were assayed for cephapirin, and no interferences were encountered from the 22 systemic agents these subjects were receiving. The anion-exchange technique for antibiotic extraction provides a rapid, precise, and quantitative antibiotic assay when used with liquid chromatography.

Bacillus subtilis↗
PubMed1976

Comparative incidence of phlebitis due to buffered cephalothin, cephapirin, and cefamandole.

Buffered cephalothin, cefamandole, and cephapirin were compared with respect to their tendency to produce phlebitis. Two grams of each agent was administered every 6 h for 4 days to 12 healthy volunteers in a double-blind crossover fashion. Approximately 50% of intravenous sites developed mild (grade 1) phlebitis and 25% developed moderate (grade 2) phlebitis. The frequency of grade 1 inflammation did not differ significantly among the three cephalosporins. The proportion of individuals eventually exhibiting grade 2 phelebitis was highest with cefamandole, lowest with cephalothin (P = 0.07), and intermediate with cephapirin; however, cephapirin required a substantially greater number of doses to produce grade 2 phelebitis than did the other two drugs. These findings, together with the results of other reports, suggest that interpretation of the phlebitogenic potential of these antibiotics must be made with caution.

Adolescent↗