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PubMed1986

Detection of penicillin, cephapirin, and cloxacillin in commingled raw milk by the Spot test.

The objective of this study was to compare Spot Test results with the results of the Bacillus stearothermophilus disc assay. Commingled raw milk samples were subdivided and spiked with penicillin, cephapirin, or cloxacillin. All subsamples, including unspiked subsamples, were analyzed by the Spot Test (3 or 9 replicates) and disc assay (9 replicates). Mean zone diameter for every subsample was calculated; subsamples having a mean zone diameter greater than or equal to 16 mm were considered positive. At penicillin concentrations less than or equal to 3.7 ng/ml, agreement between the Spot Test and disc assay was 83.4%, and false positive and negative percentages were 14.4 and 2.2%, respectively. Above 3.7 ng/ml, agreement was 100%. At cephapirin concentrations less than or equal to 12 ng/ml, agreement between the two tests was 67.9%, and false positive and negative percentages were 28.8 and 3.3%, respectively. Above 15 ng/ml, agreement was 99.3% with .7% false negatives. At cloxacillin concentrations less than or equal to 50 mg/ml agreement between the two tests was 54.5 with 45.5% false positives. At cloxacillin concentrations greater than or equal to 62.5 ng/ml, agreement between the two tests was 87.2% and false positive and negative percentages were 12.6 and .2%, respectively. In a field trial consisting of 823 bulk samples, Spot Test and disc assay agreement was 100%. The Spot Test is a rapid and reliable method for detecting penicillin, cephapirin, and cloxacillin residues in raw milk at concentrations that will produce a 16-mm zone.

Animals↗
PubMed1999

Comparison of tilmicosin and cephapirin as therapeutics for Staphylococcus aureus mastitis at dry-off.

Forty-four cows (26 Jerseys and 18 Holsteins) that had at least 1 mammary quarter that was naturally (n = 12) or experimentally (n = 84) infected with Staphylococcus aureus were allotted to three treatment groups of approximately equal number at the end of lactation. Cows were dried off by abrupt cessation of milking, and dry cow therapy was administered as an intramammary infusion of cephapirin benzathine at 10 ml per quarter, an intramammary infusion of tilmicosin (solution containing 300 mg/ml) at 5 ml per quarter, or a subcutaneous injection of tilmicosin at 5 mg/kg of body weight on the day of drying off and another injection 4 d later. Mammary secretions were monitored during the dry period and postpartum for antimicrobial residues, intramammary infection (IMI) status, and somatic cell counts. Results demonstrated the following percentage cures for IMI caused by Staph. aureus at 28 d postcalving based on individual mammary quarters: cephapirin benzathine, 78.1%; tilmicosin infused, 74.2%; and tilmicosin injected, 9.1%. During the first 4 wk after drying off, the mean concentration of tilmicosin in mammary secretions from cows infused with the antibiotic remained approximately 10-fold higher than that in secretions from cows injected with the antibiotic (3.43 vs. 0.32 ppm), and, by the time of calving, concentrations for cows treated with both methods were below the dilution limit of the assay (< 0.1 ppm). Results demonstrated that intramammary infusion of tilmicosin was equally as effective as cephapirin benzathine in curing IMI caused by Staph. aureus at drying off; however, the subcutaneous injection of tilmicosin at the dose used was not effective as a dry cow therapeutic against Staph. aureus.

Animals↗
PubMed1979

Cephapirin concentrations in prostatic and seminal vesicle tissues.

A 15 min i.v. infusion supplying either 1 or 2 g of sodium cephapirin was administered preoperatively to patients about to undergo either retropubic or transvesical prostatectomy. Tissue samples were obtained 30 min after the end of the infusion. Blood samples were obtained immediately before the start of the infusion and 30 min after the end of it. Cephapirin levels in the blood averaged 25.9 +/- 4.0 microgram/ml after the 1 g dose and 47.5 +/- 5.6 microgram/ml after the 2 g dose. Drug levels in prostatic tissue averaged 24.5 +/- 7.1 and 25.8 +/- 4.4 microgram/g for the 1 and 2 g doses, respectively. Levels in tissue taken from the seminal vesicle, often the focus of infection in bacterial prostatitis, averaged 12.5 +/- 2.3 and 44.8 +/- 14.9 microgram/g for the 1 and 2 g doses, respectively. These results suggest that bactericidal levels of cephapirin against sensitive organisms can readily be achieved in the prostate and seminal vesicles.

Adolescent↗
PubMed1982

A comparative study of cephapirin, cephalothin, and methicillin in cardiovascular surgery.

An open, randomized study involving 217 patients undergoing elective cardiovascular surgery was undertaken to compare the effectiveness of cephapirin, cephalothin, and methicillin in preventing postoperative infections. One of the three antibiotics was assigned randomly to each patient and administered beginning 2 h before operation and continuing every 6 h for 5 days. There was no significant difference between the three study groups with respect to the incidence of infection (p = 0.9913). In both the cephalothin and methicillin groups, seven patients developed adverse reactions as compared with two patients in the cephapirin group. However, the difference was not statistically significant (p = 0.0788). The results from the investigation indicate that cephapirin, cephalothin, and methicillin are equally effective as prophylactic antibiotics when used perioperatively for cardiovascular surgery.

Adult↗
PubMed1980

Concentrations of cephapirin sodium in plasma and gynecologic tissue after a single preoperative dose.

The penetration of cephapirin sodium into tissues that are commonly involved in gynecologic infections was studied after administration of a single i.v. dose of 1 g of cephapirin to about 15 patients to undergo gynecologic surgery. Blood and tissue specimens were obtained either 30 or 60 min after the infusion had been completed. Blood levels averaged 16.07 +/- 3.7 and 6.29 +/- 1.6 microgram/ml and mean tissue levels were 7.87 and 6.28 microgram at these two sampling times, respectively. These results suggest that bactericidal levels of cephapirin against sensitive organisms can be achieved in gynecologic tissues.

Adolescent↗
PubMedDate not supplied

Determination of cephapirin and desacetylcephapirin in milk using automated liquid chromatographic cleanup and ion-pairing liquid chromatography.

A simple and sensitive method was developed for determination of cephapirin and its metabolite, desacetylcephapirin, in milk. For extraction/deproteinization, 2 mL 0.2M tetraethylammonium chloride and 28 mL acetonitrile are added to 10 mL milk, and 20 mL clear filtrate (= 5 mL milk) is collected. Filtrate is evaporated to 1-2 mL and made up to 4 mL with water, filtered, and transferred to 4 mL autosampler vials. For cleanup, 2 mL filtrate is loaded onto a Supelcosil LC-18 column in 0.01M KH2PO4 (A) using a Waters WISP autosampler. The column is eluted with an acetonitrile (B) gradient from 100% A (0-3 min) to 70%A:30%B (24 min). Fractions corresponding to cephapirin and desacetylcephapirin are collected. A 0.02M pH 2.26 buffer of 0.01M decanesulfonate-acetonitrile was used for cephapirin (80 + 20) and 0.02M pH 1.96 buffer of 0.01M decanesulfonate-acetonitrile was used for desacetylcephapirin (84 + 16) on a Polymer Laboratories PLRP-S column. Recoveries at 0.01-10 ppm were 91-98%; estimated detection limits were near 2 ppb and were comparable to sensitive screening tests.

Animals↗
PubMed1971

Cephapirin: in vitro antibacterial spectrum.

Cephapirin, a new semisynthetic cephalosporin derivative, was found to have an antibacterial spectrum similar to that of cephalothin. Staphylococcus aureus was inhibited by cephapirin concentrations of 0.09 to 12.5 mug/ml. S. epidermidis, S. viridans, S. pyogenes, and Diplococcus pneumonia isolates were inhibited by less than 1 mug/ml. The Enterococcus required a concentration of 25 mug of antibiotic per ml for inhibition. Approximately 65% of Escherichia coli, and all Klebsiella, indole-negative Proteus, and Salmonella strains tested were inhibited by the drug. Serratia, Pseudomonas, indole-positive Proteus, and Erwinia strains were highly resistant. Inoculum size was not an important factor in determining the level of sensitivity of S. aureus to cephapirin. The antibiotic does not appear to be significantly bound to serum protein. In vitro development of resistance to the drug was demonstrated with two isolates of S. aureus.

Bacteria↗
PubMed1979

Renal excretion of cephapirin and cephaloridine: evidence for saturable tubular reabsorption.

Drug concentrations in plasma and urine were determined in 5 healthy subjects after intravenous infusion of 1 gm cephapirin and cephaloridine. Sampling of blood and urine was frequent and prolonged. Specimens were analyzed by high-pressure liquid chromatography (HPLC). Renal clearance of cephapirin decreased to less than 5% of control in all subjects when drug concentrations in plasma and urine declined. Cephaloridine clearance decreased to a lesser extent. Our findings suggest that, besides tubular secretion and glomerular filtration, a saturable and probably active tubular reabsorption is also involved in the renal handling of these two cephalosporins. The saturable reabsorption process was characterized by its Michaelis-Menten constant Km and its maximum transport capacity Tm.

Absorption↗
PubMed1984

Cefotaxime, cephalothin, and cephapirin: antimicrobial activity and synergy studies of cephalosporins with significant in vivo desacetyl metabolite concentrations.

The desacetyl metabolites of cefotaxime, cephalothin, and cephapirin were 5-55% as active as the parent drug, depending upon the bacterial species tested. Synergy or partial synergy was demonstrated in 64% of 25 strains of Enterobacteriaceae and Staphylococcus aureus tested against cephalothin/desacetylcephalothin and cephapirin/desacetylcephapirin combinations. Some species variations were identified that influenced synergy rates, particularly among the S. aureus strains (for example, highest rates for cephapirin).

Bacteria↗
PubMed1979

Penetration of cephapirin and cephalothin into the right atrial appendage and pericardial fluid of patients undergoing open-heart surgery.

To prevent infection in 27 patients who underwent coronary artery bypass or cardiac valve replacement surgery, each patient received a single 2-g dose of either cephalothin or cephapirin intravenously before the operation (prior to opening of the chest cavity). Samples of the right atrial appendage, pericardial fluid, and serum were obtained at various intervals after injection of the antibiotic and were assayed for cephalosporin concentrations. Cephapirin consistently reached higher levels than cephalothin in the right atrial appendage and pericardial fluid; both cephalosporins, however, reach concentrations in these sites well above their minimal inhibitory concentrations (MICs) for penicillin-resistant staphylococci. Of particular interest was the brevity of the period (about 100 min) during which levels of both antibiotics were maintained above the MIC in the right atrial appendage. This finding emphasizes the need for administration of these antibiotics shortly before surgery.

Adult↗
PubMed1972

Neutropenia associated with cephapirin therapy.

A case of neutropenia associated with cephapirin therapy is described. After discontinuation of cephapirin therapy, the neutrophil count returned to normal. Bone marrow examination revealed a marked reduction of polymorphonuclear leukocytes beyond the metamyelocyte stage and eosinophilia.

Agranulocytosis↗
PubMed1978

Hemodialysis-associated infections: treatment with cephapirin.

Large doses of cephapirin (50 mg/kg) administered during the first and last half hours of routine hemodialysis produced effective antimicrobial serum concentrations for 48 h. Repetitive administration during five successive hemodialysis sessions did not result in accumulation or accelerated metabolism of cephapirin. Ten infectious episodes in nine patients were treated in this manner with good clinical results and no toxicity.

Cephalosporins↗
PubMed1979

Bacampicillin, Ampicillin, Cephalothin, and Cephapirin levels in human blood and interstitial fluid.

The diffusibility of bacampicillin, ampicillin, cephalothin, and cephapirin into human interstitial fluid was investigated by using crossover studies. We compared bacampicillin with ampicillin and found that bacampicillin was better absorbed after oral administration. Blood, interstitial fluid, and urine levels were consistently higher in volunteers who received bacampicillin. We compared cephalothin with cephapirin and found that blood and interstitial fluid levels were comparable throughout the study.

Adult↗
PubMed1975

In vitro and in vivo microbiological evaluation of Cephapirin, a new antibiotic.

The microbiological properties of cephapirin, a new semisynthetis cephalosporin, have been studied. This antibiotic, if compared with ampicillin, shows a greater activity against gram positive bacteria, a lack of sensitivity to staphlococcal beta-lactamase, and a lower sensitivity to those produced by gram-negative bacteria. Useful therapeutic of cephapirin levels can be detected in human serum 6 h after administration of 500 and 1,000 mg parenterally.

Ampicillin↗
PubMed1989

Cephapirin-induced neutropenia.

Five cases (3.5%) of reversible cephapirin-induced neutropenia were observed in 132 patients receiving this antibiotic. The disorder was severe (agranulocytosis) in 3 cases. Simultaneous maculopapular rash was observed in all of them and in 4 cases fever occurred. All the cases observed were female (p not significant). Neutropenia developed only after administration of high doses of the antibiotic for a prolonged period of time. In contrast to another 127 patients treated with cephapirin who did not develop neutropenia, neutropenic patients had received a mean daily dose, total dose, mean daily dose per kilogram and total dose per kilogram of body weight significantly larger (p = 0.05, 0.02, 0.001 and 0.001, respectively). The duration of therapy was significantly longer in the neutropenic group (p = 0.001). Neutropenia did not occur below 90 g of total dose, but when this amount was exceeded, the incidence of the disorder reached 26.3% (p less than 0.001). We conclude that when this drug must be used either for long periods of time or at high doses, a hematologic vigilance is recommendable.

Adult↗
PubMed1980

A study of the kinetics of cephapirin and cephalexin in pregnancy.

The kinetics of cephapirin and cephalexin were studied in 60 pregnant women after the administration of single 1 g doses of the antibiotics given by the intramuscular and oral route, respectively. Maternal serum, amniotic fluid and cord serum concentrations were measured at intervals after the dose by the agar diffusion method. The results showed that the mean peak concentration of cephalexin in maternal serum, after 1 hour, was significantly greater than that of cephapirin. Both antibiotics crossed the placenta barrier and reached levels in the amniotic fluid and cord serum adequate for the in vitro inhibition of pathogens involved in materno-foetal infections.

Amniotic Fluid↗
PubMed1975

Comparison of absorption and excretion of cefazolin with cephalothin and cephapirin.

Since the discovery of cephalothin in 1962, many semi-synthetic cephalosporins have appeared. To choose the most suitable drug for the clinical treatment of infections, the characteristics of these antibiotics must be sufficiently understood. When cephalosporins which are or will be commercially available are divided into two categories, one consists of cephaloridine, cefazolin and cephalexin which are comparatively stable in the living body; and the other cephalothin, cephaloglycin, cephapirin and cephacetrile which are metabolized into desacetyl compounds with low antibacterial activity. In this study, the author compared the absorption, excretion and some other properties of cefazolin and cephalothin, (widely used clinically), and cephapirin (still under study in Japan).

Animals↗
PubMedDate not supplied

Parallux beta-lactam: a capillary-based fluorescent immunoassay for the determination of penicillin-G, ampicillin, amoxicillin, cloxacillin, cephapirin, and ceftiofur in bovine milk.

An analytical system was developed for detection of antibiotic residues in bovine milk. The method is based on competitive fluorescent immunoassays in glass capillary tubes (U.S. Patent No. 5,624,850). The system consists of an assay cartridge containing 4 glass capillaries, a reagent tray with 4 wells of dried reagents, and a Parallux processor, which processes the assay, reads fluorescent output, and reports test results. Minimum sensitivity for detection of 6 beta-lactam antibiotics in bovine milk was determined to be penicillin-G, 3.2 ppb; ampicillin, 2.9 ppb; amoxicillin, 3.6 ppb; cloxacillin, 7.4 ppb; cephapirin, 16.3 ppb; and ceftiofur, 33.7 ppb. The assay system was also specific and sensitive for detection of incurred residues at U.S. Food and Drug Administration tolerance levels: penicillin-G, 5 ppb; ampicillin, 10 ppb; amoxicillin, 10 ppb; cloxacillin, 10 ppb; cephapirin, 20 ppb; and ceftiofur, 50 ppb. There was no interference in detection of minimum sensitivity levels of antibiotic by the presence of somatic cells at approximately 1 x 10(6) cells/mL. Milk containing 3 x 10(6) cells/mL bacteria commonly found in mastitic milk also showed no interference when tolerance levels of antibiotic were present. There was no detectable interference on results by a wide variety of non-beta-lactam drugs.

Amoxicillin↗