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PubMed2002

Bacterial cure and somatic cell count response of dairy cows with a positive California Mastitis Test at calving to therapy with cephapirin sodium.

Cows without signs of clinical mastitis were evaluated by the California Mastitis Test at calving (Day 0). Milk samples from 117 of 184 quarters (64 cows) were positive by this test for mastitis and were submitted for bacterial culture and determination of somatic cell counts. Cows with infected quarters were randomly allocated to treatment with cephapirin sodium by intramammary infusion or to be untreated as controls. Two and 4 weeks following calving, milk was again sampled from the infected quarters and tested. By the 4-week evaluation, the quarters treated with cephapirin sodium had significantly (P < or = .05) fewer positive bacterial cultures and somatic cell counts were significantly (P < or =.05) reduced compared with untreated control quarters.

Animals↗
PubMed1987

Pharmacokinetics and serum concentrations of cephapirin in neonatal foals.

Six healthy foals, from 4 to 6 days of age, were given a single IM injection of sodium cephapirin (250 mg/ml) at a rate of 20 mg/kg of body weight. Serum concentrations of cephapirin were measured serially over an 8-hour period. The mean peak serum concentration was 21.2 micrograms/ml at 10 minutes. The overall elimination rate constant was 1.06/hr and the elimination half-life was 0.70 hour. The apparent volume of distribution at steady state was 1.06 L/kg and plasma clearance was 1,105 ml/hr/kg.

Aging↗
PubMed1980

Phlebitis associated with the intravenous use of cephapirin and cephalothin in the combination therapy of antibiotics.

Phlebitis related to antibiotic infusion is one of the most frequent causes of morbidity in the debilitated patients with severe infection. There are a number of causes of infusion-induced phlebitis such as pH of intravenous fluid, needle used, and contamination of venipuncture site. Vein used to play an important role, particularly in patients with granulocytopenia receiving intravenous infusion. Cephalothin is an effective antibiotic in the treatment of granulocytopenic infection and is widely used currently. When cephalothin was introduced commercially, the frequency of phlebitis was as high as 50%. The main reason was thought to be acidity of the antibiotic solution. The cephalothin solution used currently is neutral in pH, but prevention of phlebitis is still not perfect. In contrast, cephapirin recently developed cephalosporin antibiotic, which resembles cephalothin in the antimicrobial activity and pharmacological properties caused less phlebitis than cephalothin in initial clinical studies. The patients receiving chemotherapy for malignant diseases frequently die of infections. A cephalosporin antibiotic is administered intravenously for a prolonged time in the presence of thrombocytopenia, and under such circumstances, other antibiotics such as carbenicillin (CBPC) and aminoglycoside are usually used in combination. The influence of these antibiotics injected through the same vein must be considered, but the possibility of phlebitis due to CBPC and aminoglycoside is negligible. In the present clinical study, 24 granulocytopenic patients were treated with the combination of antibiotics, cephapirin-carbenicillin-amikacin and cephalothin-carbenicillin-amikacin. Besides the clinical effect of the antibiotics, the incidence and severity of phlebitis were studied.

Agranulocytosis↗
PubMed1976

Phlebitis associated with the intravenous use of cephalothin and cephapirin.

The frequency and severity of phlebitis associated with cephalothin and cephapirin was compared in a double-blind study in 82 surgical patients with 149 different infusion sites. After treatment with the coded drug products, the status of each patient's veins was evaluated daily by i.v. therapists. Cephapirin was associated with a slightly lower rate of phlebitis, but the difference was not significant. For both drugs, the duration of therapy did not appear to have an effect on the rate of phlebitis. Scalp vein needles were associated with a lower rate of phlebitis than plastic catheters, but the difference was not significant.

Cephalosporins↗
PubMedDate not supplied

Determination of cephapirin and ceftiofur residues in bovine milk by liquid chromatography with ultraviolet detection.

A method capable of quantitating cephapirin at a level fo 20 ng/mL and ceftiofur at a level of 50 ng/mL was developed for raw bovine milk. Raw bovine milk is deproteinated with acetonitrile. The supernatant is collected and then acetonitrile is removed under reduced pressure while warming in a water bath at 40 degrees-50 degrees C. The extract is mixed with water and loaded onto a conditioned C18 solid-phase extraction column. Analytes are eluted with acetonitrile, which is removed completely under a stream of nitrogen gas. Analytes are separated from coextractives by gradient elution with an ion-pair mobile phase on a reversed-phase column and are detected by ultraviolet absorbance at 290 nm. Mean recoveries from fortified milk samples ranged from 79 to 87% for cephapirin and from 76 to 86% for ceftiofur, with intralaboratory coefficients of variation ranging of 6-10% and 7-14%, respectively.

Animals↗
PubMed1977

Spectrophotometric determination of cephapirin, a cephalosporin antibacterial.

A simple and specific method for the quantitative determination of cephapirin, a cephalosporin antibacterial, in finished bulk and dosage forms is reported. The method is based on reproducible degradation under controlled conditions to an unidentified species, which is measured spectrophotometrically at 375 nm. The procedure can be performed manually on a short series of samples in about 15 min or can be automated for large runs. Precursors and related substances show minimal interference. The coefficient of variation of the automated system is about 1% within days and 1.3% among days.

Autoanalysis↗
PubMed1998

Assay for cephapirin and ampicillin in raw milk by high-performance liquid chromatography--integrated pulsed amperometric detection.

The FDA has issued guidelines governing the use of antibiotics in cattle and routinely tests for the presence of antibiotics in milk. Unfortunately, these compounds are often difficult to detect by direct methods because they often lack a chromophore or fluorophore. Integrated pulsed amperometric detection (IPAD) following reversed-phase liquid chromatography is well-suited for this analysis because it is selective, sensitive, and direct; i.e., derivatization is not required. This work involves the development of a simple, rapid assay for the determination of beta-lactam antibiotic residues in milk using HPLC-IPAD, specifically, ampicillin and cephapirin. Since the analyst studied here are detectable by UV detection, a comparison between IPAD and UV detection will be made. Sample preparation schemes that involve the extraction of antibiotics of interest from the milk matrix and subsequent cleanup are an important aspect of this project. These procedures will be discussed in detail. In addition, analytical figures of merit and IPAD wave form optimization will be addressed.

Ampicillin↗
PubMed1976

Effectiveness of two new cephalosporins, cephazolin and cephapirin, administered intermittently in acute and chronic osteomyelitis in children.

Ten patients were treated, most of pre-school age, with acute osteomyelitis, produced by Staphylococcus aureus and Salmonella, having evolved for approximately one week, with sodium cephazolin at doses of 60 mg/kg/day intramuscularly in two daily injections for the first seven days and then in a single dose every twenty-four hours for four to seven weeks. Nine of ten patients were asymptomatic six months after this treatment. The patient who manifested chronic signs at the end of six weeks of therapy continued to be treated with three weekly injections of the same drug at an equal dose until the completion of six months, at the end of which he was asymptomatic. Ten patients with chronic osteomyelitis having evolved for two months to five years, due to penicillin-resistant Staphylococcus aureus, were treated with cephapirin at the dose of 30 mg/kg in one daily injection intramuscularly for three to four weeks and then the same dose on Mondays, Wednesdays and Fridays until the completion of six months. Eight patients who required it were sequestrectomized. Seven of the ten patients improve and remained asymptomatic for the same period of observation. The three patients who did not show marked clinical improvement did exhibit an appreciable radiological recovery. We have presented these regimens of treatment with a view of encouraging research into the intermittent administration of bactericidal antibiotics for pyogenic infections; in spite of the good results, we do not dare to recommend them in daily practice.

Acute Disease↗
PubMedDate not supplied

Charm Safe-Level beta-Lactam Test for amoxicillin, ampicillin, ceftiofur, cephapirin, and penicillin G in raw commingled milk.

The Charm Safe-Level beta-Lactam Test was evaluated by a U.S. Food and Drug Administration (FDA) test protocol administered by the AOAC-Research Institute. The sensitivity and selectivity of the test were evaluated with >800 negative raw commingled and drug-fortified milk samples by the manufacturer and an independent laboratory. Probit analysis by the independent laboratory determined the following 90% positive levels with 95% confidence: amoxicillin, 5.6 ppb; ampicillin, 8.5 ppb; cephapirin, 13.7 ppb; ceftiofur, 46.2 ppb; and penicillin G, 3.6 ppb. These values were within a range of +/- 20% of the manufacturer's data. Selection of negative samples met confidence specifications. Ruggedness parameters were studied and defined, and the stability of frozen milk was verified. There were no interferences from somatic cells (1,000,000 somatic cell count/mL) or bacteria (300,000 colony-forming units/mL), or from 27 other non-beta-lactam animal drugs. Test performance with raw milk samples containing incurred penicillin, ampicillin, and amoxicillin was consistent with the dose responses determined with fortified milk samples. Incurred cephalosporin in raw milk samples was detected at lower levels than was cephalosporin in fortified milk samples, presumably because of the presence of metabolite, as verified by other test methods. Quality control data support consistency in manufacture between batches and the stability of refrigerated test reagents for up to 1 year. Successful fulfillment of these criteria led to FDA certification of the test when used with a reader in U.S. milk testing programs.

Amoxicillin↗
PubMed1975

Serum levels and urinary excretion of parent antibiotics and desacetyl forms after parenteral administration of cephalothin and cephapirin.

When the antibacterial substances of cephalothin and cephapirin in the serum and urine after intramuscular injection were separated and assayed, desacetyl metabolities of both drugs were detected. These tendencies were especially apparent in the tissue concentrations. When both the drugs were given intravenously to healthy volunteers, the amounts of their desacetyl metabolites were not greater in man than in rats.

Animals↗
PubMed1986

[A study of the disc sensitivity test for cephapirin].

Susceptibility of 203 strains of 34 bacterial species or subspecies to cephapirin (CEPR) was determined by the 2-fold agar dilution method in parallel with the determination of inhibition zone diameter in the single-disc method. These experiments demonstrated a significant correlation between the MIC by the dilution method and the diameter of inhibition zone determined by the conventional assay using an over-night (about 16 hours) incubation, the delayed assay (about 24 hours incubation), or the rapid assay (after 3-4 or 5-6 hours incubation), hence applicability of the single-disc assay for CEPR was confirmed. An analysis of the data obtained using CEPR discs (each containing 30 micrograms) revealed that primary regression equations were as follows: D (diameter, mm) = 25.8-9.7 log MIC (microgram/ml) in the conventional assay; D = 31.2-12.3 log MIC in the delayed assay; D = 21.7-7.1 log MIC in the 5-6-hour rapid assay and D = 17.9-5.0 log MIC in the 3-4-hour rapid assay, and especially for beta-lactamase producing Staphylococci, they were: D = 24.9-9.2 log MIC in the conventional assay, D = 20.4-7.4 log MIC in the 5-6-hour rapid assay and D = 17.5-5.8 log MIC in the 3-4-hour rapid assay.(ABSTRACT TRUNCATED AT 250 WORDS)

Agar↗
PubMed1985

[Studies on minimum antibiotic concentration of cephapirin against clinically isolated strain SMK-101 of Klebsiella pneumoniae].

Using strain SMK-101 of K. pneumoniae its nephelometric absorbencies, viable cell numbers and morphological changes were studied during the time course cultured in a broth medium containing cephapirin (CEPR), and following results were obtained. After 1 to 3 hours culture in the presence of varying concentration of the antibiotic, the absorbency increased in spite of without change in the viable cell number. Morphologically, elongation and swelling of central portion of the cells were observed though differences of the degree of these findings varied depending upon the concentration of the antibiotic. At the concentration higher than 1/4 MIC, indistinct structure was shown in cytoplasm. After 6 hours culture, 3 directions of absorbence curves, ascending, descending and no change, and 2 directions of viable cell numbers, decreasing and increasing were shown. As the morphological changes of the cells, filamentation, leaking of intracellular components were shown in rather upper concentration of the antibiotic. Fission was demonstrated around the end of cells cultured in rather lower concentration of the antibiotic. After 9 hours culture, absorbency and viable cell number were parallel. In this period, structural findings of cytoplasm became clear and fission was also demonstrated by light microscope except for the cells cultured in more than 1 MIC of the antibiotic. After 24 hours culture, both absorbency and viable cell number increased again and fission was observed in the cell which showed filamentation in 1 MIC of the antibiotic.

Cephalosporins↗
PubMed1984

[Experience in combination therapy with amikacin and cephapirin for infections complicated with acute leukemia during induction chemotherapy].

We treated infections accompanied with induction chemotherapy in 9 patients with acute leukemia by the combination of amikacin (AMK) and cephapirin (CEPR). The result was that 1 case was markedly effective, 2 cases were effective, 3 cases were marginally effective, 2 cases showed no effect and 1 case who underwent prophylactic medication had no infection. We recognized no adverse effects by AMK or CEPR. We concluded that the combination of AMK and CEPR was useful as first choice to the treatment of infections during induction chemotherapy of acute leukemia.

Acute Disease↗
PubMed1983

[Pharmacokinetics of cephapirin sodium during intravenous infusion].

Studies on absorption and excretion of cephapirin (CEPR) are described. CEPR was administered by intravenous drip infusion to 4 healthy volunteers weighing 53 kg to 61 kg, and the serum levels were measured. Pharmacokinetic parameters were calculated by one-compartment model and two-compartment model. Each model was comparatively applied to every founds. Most appropriate administration rate of intravenous drip infusion was discussed due to calculated serum levels, therapeutic AUC and effective time.

Cephalosporins↗
PubMed1983

[Comparison of side effects of intravenous cephapirin and cephalothin with special reference to the incidence of phlebitis].

The frequency and severity of side effects, above all, phlebitis, associated with an intravenous use of cephapirin (CEPR) or cephalothin (CET) was compared in 69 patients with infections. Two grams of each drug were administered intravenously twice a day with a 21-G vein needle in one of the two arms of the patients. CEPR was administered to 32 patients, and CET to 37 patients respectively. After treatment, the status of the veins was checked, and laboratory findings and other side effects were evaluated daily. Each drug appeared to be equally efficacious in the treatment of infections. The administration of CEPR was associated with a slightly lower rate of phlebitis and other side effects, but the difference between the 2 drugs was not significant (0.05 less than P less than 0.10). Phlebitis was observed in 1 patient (3.1%) of CEPR group and in 3 patients (8.1%) of CET group. Side effects, including phlebitis, were observed in 4 patients (12.5%) of CEPR group and in 12 patients (32.4%) of CET group. In CET group, drug exanthema (3 cases), drug fever (3 cases), and abnormalities in liver function (4 cases) were observed. These findings, together with the results of other reports, suggest that CEPR is a safe and useful drug in the treatment of infection as compared with CET.

Adolescent↗
PubMed1983

Determination of penicillin G, ampicillin, and cephapirin residues in tissues.

A cylinder plate microbiological method was developed for the rapid, quantitative determination of penicillin G, ampicillin, and cephapirin in animal tissues. The method uses agar plates seeded with stable spores of Bacillus stearothermophilus var. calidolactis and incubated 4 h at 64 degrees C. Standard curves were obtained for the following ranges of concentration of antibiotics in tissues: 0.02-0.32 IU penicillin G/g, 0.0125-0.2 micrograms ampicillin/g, and 0.02-0.32 micrograms cephapirin/g. The proposed method is suitable not only for penicillin residue analysis, for which the sensitivity has been greatly improved compared with the Sarcina lutea method, but also for depletion studies on these antibiotics, which are commonly used to treat diseases in food-producing animals.

Ampicillin↗
PubMed1977

[Studies on the diffusion of cephapirin into prostatic tissue].

After i.v.-application of 2 grams of Cephaprin (= Bristocef) to 13 patients with prostatic adenoma the mean serum concentrations after 30 minutes were 50 microgram/ml and 21.5 microngram/ml after 60 minutes. The corresponding tissue values were 20.8 and microgram/g respectively in prostatic tissue. The evaluated serumand tissue cncentrations are suited to the therapy of infections with cephapirin sensitive rods.

Aged↗