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Bactericidal activity and induction of cell volume alterations of cephalosporins in Escherichia coli.

The bactericidal efficacy of cefuroxime and cephacetril on Escherichia coli cultures was measured by killing curves. Simultaneously bacterial cell volumes were analysed by electronic particle counting using a Coulter Counter Channelanalyser system in order to study the relationship between bactericidal activity and bacterial cell volume alterations. Various concentrations (2-120 mg/l cefuroxime and 16-120 mg/l cephacetril) and different exposure times (over a time period of 12 h) were used. Growth medium was human plasma ultrafiltrate. The bactericidal activity of cefuroxime, as measured by the rate of killing of the E. coli culture, was independent of the concentration and constant in the range 4-120 mg/l. The characteristic cefuroxime-induced change in bacterial cell volume was a marked volume increase up to a maximum of 5-fold after 160-200 min exposure with a low-grade bacteriolysis following. The cefuroxime-induced bacterial volume changes were, in accordance with the bactericidal testing, almost independent of the concentration. In contrast, the killing curves for cephacetril strongly depended on the drug concentration. However, this effect was short-lived and regrowth of the E. coli culture followed. The typical cephacetril-induced volume distribution curves were also highly concentration-dependent. With increasing drug levels bacterial cell volume increased up to 20-fold, and regrowth of a persisting bacterial population occurred at lower antibiotic concentrations. Bacteriolysis started earlier than with cefuroxime. The relationship between loss of viability and cell volume increase was more marked with cefuroxime than with cephacetril.

Autoanalysis↗

[Sensitivity of agents of mastitis to various antibiotics].

Studied was the sensitivity to antibiotics of a total of 328 strains of mastitis-causative agents, employing the agar-diffusion method. Staphylococcus aureus proved most sensitive to cephacetril (100%), gentamycin (85.3%), and erythromycin (75.2%). Of the pathogenic streptococci Str. agalactiae was most sensitive to cephacetril (100%), chloramphenicol (100%), and tetracycline (92,8%), while Str. uberis and Str. dysgalactiae ranked second - cephacetril (88,2%), tetracycline (77.4%), and gentamycin (74.5%). Coliform bacteria were found to be most sensitive to streptomycin (75-77%), gentamycin (69-74%), and chloramphenicol (66-73%), and completely resistant to penicillin and ampicillin. Corynebacteria were sensitive to most of the antibiotics - cephacetril (100%), chloramphenicol (83.8%), erythromycin (78.3%), gentamycin (75.6%), and ampicillin (72.9%). Usually, the mastitis causative agents showed polyresistance at one and the same time mostly to three (36.3%) and four (19%) antibiotics.

Animals↗

[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↗