Effect of cephapirin on formation of D-alanine carboxypeptidase in growing Bacillus subtilis cells.
(1/21)
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. (+info)
Influence of cephalosporin antibiotics on blood coagulation and platelet function.
(2/21)
Administration of cephalothin to normal volunteers in maximal doses of 300 mg/kg per day resulted in a combined defect of platelet function and blood coagulation. No such abnormalities were evident after infusion of cefazolin or cephapirin at a maximal dosage of 200 mg/kg per day. The observed thrombocytopathy was similar to but less severe than that induced by carbenicillin or ticarcillin and was not reflected by a prolonged bleeding time test or impaired prothrombin consumption. Moreover, it was not a consistent finding in those persons receiving cephalothin. A separate defect involving blood coagulation appeared to result from delayed fibrinogen-fibrin polymerization and was evidenced by extended values of the activated partial thromboplastin and thrombin time tests. It remains uncertain whether the abnormalities described may constitute clinically important hemostatic disorders in patients with normal renal function receiving large doses of cephalosporin antibiotics. (+info)
In vitro activity of BL-s640 against gram-negative bacilli and Staphylococcus aureus compared with activity of four other semisynthetic cephalosporins.
(3/21)
The in vitro activity of BL-S640 (cefatrizine) was determined against 674 recent clinical isolates of Staphylococcus aureus and Enterobacteriaceae. Activity against S. aureus was less than that of cephapirin, cephalothin, and cefazolin, but greater than that of cephalexin. Activity against gram-negative isolates was variable: BL-S640 was slightly less potent than cefazolin against Escherichia coli and Klebsiella, but more active than the other compounds. As for the more resistant gram-negative genera, BL-S640 was significantly superior to the control cephalosporins. The effect of inoculum size on the antibacterial activity was moderate for most organisms except Enterobacter, Providencia stuartii, and indole-positive Proteus, the median minimal inhibitory concentrations of which were 6 to 27 times lower when determined with a 10(-4)-diluted culture compared with the undiluted one. The stability in aqueous solution at 37 C was remarkably high at the lower pH values, but low at the neutral point. (+info)
Comparison of phlebitis produced by cephapirin and cephalothin.
(4/21)
In a single-blinded study involving 120 patients neither the incidence nor severity of phlebitis observed with cephapirin and cephalothin was significantly different. (+info)
Structural determinants of substrate binding to Bacillus cereus metallo-beta-lactamase.
(5/21)
Binding and hydrolysis of the beta-lactams cefotaxime, cephapirin, imipenem, and benzylpenicillin by the metallo-beta-lactamase from Bacillus cereus were studied by presteady state kinetic measurements. In all cases, the substrate was unmodified in the most populated reaction intermediate, and no chemically modified substrate species accumulated to a detectable amount. The cephalosporins tested showed similar formation rate constants for this intermediate, and they differed mostly in their decay rates. Formation of a non-productive enzyme.substrate complex was detected for imipenem. The substrate binding differences can be accounted for by considering the structural features of each substrate. The apoenzyme could not bind any of the substrates, but binding was restored when the apoenzyme was reconstituted with Zn(II), revealing that the metal ions are the main determinants of substrate binding. This evidence is in line with the lack of an optimized substrate recognition patch in B1 and B3 metallo-beta-lactamases that provides a broad substrate spectrum. (+info)
Treatment of pneumonia and other serious bacterial infections with cephapirin.
(6/21)
Nineteen patients with pneumonia due to Streptococcus pneumoniae, Staphylococcus aureus, Klebsiella pneumoniae, or Escherichia coli were treated with 4 to 18 g of cephapirin daily. There were three treatment failures. One patient each with pneumonia due to E. coli or S. pneumoniae died despite apparent eradication of the pathogen. Lobar pneumonia due to K. pneumoniae progressed during therapy in a third patient to lung gangrene, necessitating pneumonectomy. Five additional patients with pneumococcal pericarditis or septic bursitis, empyema, cannula-associated bacteremia, and thoractomy wound infection due to S. aureus were cured. All isolates of S. aureus, S. pneumoniae, and group A Streptococcus were inhibited by 0.8 mug of cephapirin per ml; minimal inhibitory concentrations of cephalothin were similar. Ninety percent of K. pneumoniae, 85% of Proteus mirabilis, 73% of E. coli, and 30% of Enterobacter were inhibited by 12.5 mug cephapirin per ml. All isolates of Pseudomonas, Serratia and indole-positive Proteus had a cephapirin minimal inhibitory concentration of [Formula: see text] 100 mug/mg. Serum concentrations after intravenous and intramuscular injection were similar to those reported for cephalothin. The intramuscular injections were moderately painful, and intravenous infusions caused phlebitis in three of nine patients treated with doses up to 18 g per day. Cephapirin appears comparable to cephalothin in vitro and is an effective agent in treatment of infection due to S. aureus and S. pneumoniae. (+info)
Impact of experimental trauma and niflumic acid administration on antimicrobials' concentration in serum and mandible of rats.
(7/21)
Administration of antibiotics and analgesics in surgery or trauma is of great importance for an effective treatment. Trauma, as stress stimulus, causes alterations in various functions of the organism as well as in drug pharmacokinetics. The aim of this study was to determine the effect of trauma upon the serum and bone levels of the antimicrobial ampicillin and cefapirin, with and without co-administration of a non-steroidal anti-inflammatory analgesic (NSAIDs). Fifty-six male Wistar rats were divided into two groups A (control) and B (experimental). Each group consisted of 4 subgroups (n=7) receiving ampicillin, ampicillin with niflunic acid, cefapirin, and cefapirin with niflunic acid. In group B traumatic injury was performed by incision (7 mm length) in the right cheek. The levels of the antibiotics were estimated by the inhibition zone of B. subtilis. An increase in antibiotic levels was observed in group B, being statistically significant only for cefapirin level in the mandible. Upon niflumic acid co-administration a statistically significant rise in serum ampicillin and mandible cefapirin levels was observed in both control and experimental groups (student t-test). It can be concluded that the combination of antibiotics and non-steroid antiinflammatory drugs (NSAIDs) may enhance the antibacterial drug concentration. (+info)
Efficacy of a 5-day extended therapy program during lactation with cephapirin sodium in dairy cows chronically infected with Staphylococcus aureus.
(8/21)
This study determined the efficacy of a 5-day extended therapy with cephapirin sodium in dairy cows chronically infected with Staphylococcus aureus. Chronically infected cows selected from 14 dairy herds in the St-Hyacinthe region, Quebec were randomly allocated to a group of 31 cows treated for 5 consecutive days with 200 mg of cephapirin per quarter BID or a group of 30 untreated control cows. Bacteriological cure was determined by 3 negative bacterial cultures at 10, 24, and 31 days after treatment. The cow cure rates were 25.8% (8/31) in the treated cows and 3.3% (1/30) in the control group (P = 0.013). The quarter cure rates at first sampling post-treatment were 77.6% (38/49) and 18% (9/50) in the treated and the control groups, respectively (P < 0.0001). A 5-day extended therapy with cephapirin is effective in treating cows chronically infected with S. aureus. (+info)