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PubMed1974

Cephapirin.

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Acetamides↗
PubMed1984

Twice-daily intramuscular ceforanide therapy of Staphylococcus aureus endocarditis in parenteral drug abusers.

Twice-daily intramuscular ceforanide therapy of Staphylococcus aureus endocarditis in parenteral drug abusers was compared in a randomized prospective trial with intravenous cephapirin therapy. Dosage regimens were ceforanide, 1 g every 12 h, and cephapirin, 2 g every 4 h. Mean minimal inhibitory and bactericidal concentrations of ceforanide for S. aureus treated with ceforanide were 0.78 and 1.56 microgram/ml compared to cephapirin for patient isolates of 0.08 and 0.14 microgram/ml, respectively. Serum killing levels with ceforanide were 1:5.7 and 1:1.5 at peak and trough levels, compared to 1:134 (peak) and 1:4.2 (trough) with cephapirin. Despite this apparent in vitro advantage of cephapirin, patients treated with ceforanide did as well as those with cephapirin. Of 16 ceforanide-treated patients, all responded initially to therapy, and 15 were cured with 28 days of therapy. One patient relapsed at the end of therapy. Of 16 cephapirin-treated patients, 1 was a clinical and microbiological failure, and 3 other relapsed at the end of therapy. In addition, one ceforanide-treated patient and two cephapirin-treated patients developed central nervous system abscesses. These were cured with drainage and continuation of antibiotic therapy. Ceforanide was well tolerated by the intramuscular route. Cost analysis suggests that therapy with intramuscular ceforanide would result in an approximate 70% decrease in drug therapy cost when compared to intravenous cephapirin. Ceforanide appears to be a safe, efficacious, convenient, and relatively inexpensive drug for treating staphylococcal endocarditis in parenteral drug abusers.

Adult↗
PubMed1980

Use, misuse, and cost of parenteral cephalosporins at a county hospital.

We reviewed total usage of parenteral cephalosporins at a county hospital during 1978 with regard to appropriateness, pattern of use, and cost. In addition, we determined the impact of replacing cephalothin with cephapirin in the hospital formulary. During the 12-month study 366 patients received 409 courses of parenteral cephalosporins: 167 received cefazolin, 160 received cephapirin, and 35 received a combination of cefazolin and cephapirin. The surgical service prescribed 87% of the cephapirin and 92% of the cefazolin. Parenteral cephalosporins were used 62% of the time for prophylaxis and 38% of the time for therapy. Usage was judged inappropriate in 47% of all courses based on our criteria; 25% of the therapeutic courses were judged inappropriate, compared to 60% of the prophylactic courses. Pharmacy costs of cefazolin used as prophylaxis were more than twice the cost for cephapirin. Cost of a mean therapeutic course for cefazolin was 43% higher than for cephapirin. Antibiotic audits and continued education combined with judicial substitution of therapeutic equivalents should limit the inappropriate use and expense of parenteral cephalosporins for large as well as small hospitals.

Cefazolin↗
PubMed1998

Recombinant bovine interleukin-2 and dry cow therapy: efficacy to cure and prevent intramammary infections, safety, and effect on gestation.

Cows from eight commercial dairies were randomly assigned to intrammamary infusions of cephapirin or cephapirin plus interleukin-2 at the end of lactation. During the first phase of the trial, interleukin-2 was administered to 159 cows at a dose of 1 mg per gland by intracisternal infusion immediately after 300 mg of cephapirin were administered. One hundred sixty-one cows received infusions of a placebo (phosphate-buffered saline; PBS) immediately after cephapirin. In the second phase of the trial, 70 cows received 2 mg of interleukin-2 per gland, and 78 cows received the placebo. Cows were observed daily by the participating farmer for 72 h after infusion and also during routine feeding and care during the dry period and at calving. Potential side effects from udder infusions, particularly gross abnormalities of the udder and signs of systemic side effects were monitored. During the first phase, cure rates for intramammary infections caused by Staphylococcus aureus that were present at the end of lactation were 33.3% for quarters treated with cephapirin and 53.6% for quarters treated with cephapirin and interleukin-2. Cure rates did not differ between treatment groups for all other pathogens or during the second phase of the trial. The incidence of new intramammary infections during the dry period was not affected by intramammary infusion of interleukin-2. Eighteen of 229 (7.9%) cows treated with interleukin-2 aborted within 49 d of treatment compared with 4 of 239 (1.7%) cows treated with PBS. Eleven of the 18 (61.1%) abortions by cows treated with interleukin-2 occurred 3 to 7 d after infusion; none of the abortions by cows treated with PBS occurred until wk 7 after infusion.

Abortion, Veterinary↗
PubMed1981

[Cephalosporin pharmacokinetics in rabbits].

The kinetics of the blood serum and urine levels of cephalotin, cephaloridine, cephazolin, cephacetrile, cephapirin, cefalexin and cefradin was studied on rabbits treated with the antibiotics administered intravenously. The pharmacokinetic constants of the cephalosporins were calculated on the basis of the one-compartmental mathematical model. It was shown that cephalotin and cephapirin had the highest blood elimination rates. These antibiotics had higher constants of the elimination rate and lower time values of a two-fold decrease in the blood level. The elimination rates of the other cephalosporins were almost the same. The drugs did not differ in renal clearance. Cephapirin, cephalotin and cephacetrile had the lowest values of excretion with the urine. It was found that the tubular secretion took part in the renal excretion of all cephalosporins. Its proportion was especially high in renal excretion of cephalotin, cephapirin, cephazolin. The value of the "apparent" distribution was much higher for cephalotin, cephacetrile, cefradin and cephapirin as compared to the other drugs. The highest values of the total clearance were observed with respect to cephalotin, cephacetrile and cephapirin, as well as higher values of the extrarenal clearance.

Animals↗
PubMed1994

Efficacy of intramuscular oxytetracycline as a dry cow treatment for Staphylococcus aureus mastitis.

To determine the efficacy of intramuscular oxytetracycline as a supplemental dry cow treatment for Staphylococcus aureus mastitis, 37 Holstein cows were randomly assigned to two treatment groups: intracisternal infusion with a commercial preparation of cephapirin benzathine at drying off (20 cows) and infusion with cephapirin benzathine at drying off and intramuscular oxytetracycline at 11 mg/kg once daily on d 7, 8, 9, and 10 after drying off (17 cows). Milk samples collected 7, 14, 30, and 60 d after calving were plated for bacterial isolation within 24 h after collection and after 24 to 72 h of storage at -20 degrees C. Quarters were defined as infected if S. aureus was isolated from the fresh and frozen cultures from any one sample collected before drying off. An infected quarter was defined as cured if S. aureus was not isolated from the fresh or frozen culture from milk samples obtained following calving. The rate of cure by 30 d after calving for systemic oxytetracycline (in combination with cephapirin treatment) was 29.4% for infected quarters and 29.4% for infected cows, compared with 27.5 and 25.0%, respectively, for the cephapirin treatment only. Results including the culture at 60 d after calving were 21.2 and 22.5%, respectively, for combination therapy and cephapirin therapy only. Systemic oxytetracycline, in combination with intramammary dry cow treatment, did not improve the rate of cure for S. aureus mastitis.

Animals↗
PubMed1986

In vitro activity of antibiotics alone and in combination against Actinobacillus actinomycetemcomitans.

The MICs for 90% of the organisms tested (MIC90S) of 11 antibiotics against 24 clinical isolates of Actinobacillus actinomycetemcomitans were determined by the MIC 2000 system. The lowest MIC90S (16 micrograms/ml) were observed with ceftriaxone and rifampin. The next lowest MIC90S were found with cephapirin, tetracycline, and chloramphenicol (3.12 micrograms/ml). The MIC90S of penicillin, ampicillin, ticarcillin, piperacillin, and amikacin were each greater than or equal to 12.5 micrograms/ml. Antibiotic synergy was studied by the killing curve method and was defined as a greater than or equal to 2 log10 reduction in CFU when two antibiotics were used in combination at one-fourth the MBC for each compared with the effect of each antibiotic alone at one-half the MBC. Synergism between rifampin and penicillin, cephapirin, or ceftriaxone was tested for with 12 A. actinomycetemcomitans strains. In 7 of 37 instances, synergism was demonstrated for the combinations rifampin plus ceftriaxone (n = 3) or rifampin plus penicillin (n = 4); in 9 instances, an additive effect was noted, and impaired killing with drug combinations compared with the effect of a single antibiotic was suggested in 4 strains. The majority of strains were indifferent to the combinations. Similarly, variable results were observed when the combination of trimethoprim and cephapirin was tested against eight A. actinomycetemcomitans strains. Our data suggest that rifampin and cephapirin are the most active of the 11 antibiotics studied against A. actinomycetemcomitans. In addition, in vitro synergism between rifampin and other antibiotics or between trimethoprim and cephapirin was not consistently demonstrable.

Actinobacillus↗
PubMed1975

The formation of functional penicillin-binding proteins.

A method was developed which permitted determination of the [14C]benzylpenicillin and [14C]Cephapirin binding capacity of rapidly growing Bacillus subtilis cells in liquid culture. Over the concentration range of the binding plateau (0.1 to 0.8 mug/ml), [14C]benzylpenicillin significantly inhibited formation of functional penicillin-binding proteins, but had comparatively little effect on total bacterial protein synthesis. The data suggest that penicillin covalently bound to the cells in a chemically stable manner alone is not sufficient to inhibit formation of functional binding proteins and that unbound penicillin in the growth medium is necessary. The concentration of unbound antibiotic in the culture medium, in turn, is a function of the cell-bound penicillinase activity whose significance increases with cell density. [14C]Cephapirin, a cephalosporin resistant to this cell-bound penicillinase almost completely inhibited the formation of functional Cephapirin-binding proteins, but had relatively little effect on total protein synthesis. At concentrations 250-fold higher than that required to inhibit formation of functional binding proteins. Cephapirin did not inhibit particulate D-alanine carboxypeptidase activity and presumably did not bind covalently to this penicillin-binding protein.

Alanine↗