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PubMed1983

Encapsulated forms of slow-release dry cow products of rapidly absorbed antibiotics.

The persistence of chloramphenicol, cephacetrile, and clindamycin in the udders of dry cows was studied after drying-off therapy with salts of these antibiotics suspended in conventional oil bases. Antibiotic activity was not found in dry udder secretions collected 3-5 days after treatment. After equivalent doses of encapsulated formulations of chloramphenicol were suspended in the same oil bases and infused at drying-off, most of the drug remained bound within the microcapsules; chloramphenicol concentrations higher than 10 micrograms/ml secretion were maintained for 3-4 weeks, but upon release from the microcapsule, the free drug was very quickly absorbed from the udder. Microcapsulated formulations of cephacetrile and clindamycin were infused at drying-off, suspended in the same type of oil base and at similar doses to the non-capsulated preparations. The concentrations of free drug in the secretions remained constant over a period of 2-3 weeks, although total drug (bound and free) concentrations in the udder, which were much higher than free drug levels, were progressively and markedly reduced. It appeared that after infusion of the microcapsulated preparations of cephacetrile and clindamycin, rates of drug release from the depot were equal to the rates of absorption of free drug from the udder.

Animals↗
PubMed1978

Effects of various cephalosporins on the proximal tubule of the human kidney.

Cephamandol 6.0 g, cephazolin 6.0 g or cephacetrile or cephalothin 8.0 g were administered as short-term infusions on 3 consecutive days to informed volunteers, who had no history or evidence of impairment of renal function. There were 15 subjects in the cephamandol, cephacetrile and cephalothin groups and 14 subjects in the cephazolin group. Alanine-aminopeptidase, a characteristic tubule enzyme, was determined in a 24-hour urine 2 days before administration, during the 3 day administration and on the 4 subsequent days. In addition, alanine-aminopeptidase was also estimated immunologically in concentrated urine with the aid of an anti-brush border antibody. Cephamandol, cephazolin and cephalothin were completely without effect on the proximal tubule. Cephacetrile, on the other hand, showed clear reactions in 9 out of 15 subjects, in the form of elevated AAP activity in urine and in 6 of the cases membrane elimination was demonstrable immunologically. After withdrawal of the medication, the values of the responder group returned spontaneously to normal, i.e. no cumulative effect was detected. These investigations show that elimination of alanine-aminopeptidase in the urine is a very sensitive index of the action of cephalosporins on renal tubules.

Adolescent↗
PubMed1979

Comparative penetration of various cephalosporins into inflammatory exudate.

A rabbit sterile peritonitis model was used to determine the relative penetration of four cephalosporin antibiotics into exudate fluid. Male New Zealand white rabbits were given 120 ml of sterile saline intraperitoneally, and peritonitis developed over the following 8 h, with exudate fluid containing a mean of 17,188 granulocytes per mm(3) at 8 h. Each antibiotic was administered intramuscularly at a dose of 30 mg/kg 3 h after peritonitis was initiated, and serum and peritoneal concentrations were measured 0.5, 1, 2, and 4 h later. Cefamandole gave the highest mean peak serum level (26.8 mug/ml), and cephalothin, cephacetrile, and cephradine all gave peak serum levels between 13 and 15 mug/ml. When peak peritoneal exudate concentration was expressed as a percentage of peak serum concentration, cephradine developed 28.5% of the peak serum level, cephacetrile 27.7%, cephalothin 14.0%, and cefamandole 12.5%. These percentages of exudate penetration were inversely proportional to the degree of serum protein binding: cephradine 26.6%, cephacetrile 36.3%, cephalothin 50%, and cefamandole 88%.

Animals↗
PubMed2002

Method for estimation of low outer membrane permeability to beta-lactam antibiotics.

The outer membrane of gram-negative bacteria plays a major role in beta-lactam resistance as it slows down antibiotic entry into the periplasm and therefore acts in synergy with beta-lactamases and efflux systems. Up to now, the quantitative estimation of low outer membrane permeability by the method of Zimmermann and Rosselet was difficult because of the secreted and cell surface-associated beta-lactamases. The method presented here uses the acylation of a highly sensitive periplasmic penicillin-binding protein (PBP) (BlaR-CTD) to assess the rate of beta-lactam penetration into the periplasm. The method is dedicated to measurement of low permeability and is only valid when the diffusion rate through the outer membrane is rate limiting. Cytoplasmic membrane associated PBPs do not interfere since they are acylated after the very sensitive BlaR-CTD. This method was used to measure the permeability of beta-lactamase-deficient strains of Enterobacter cloacae and Enterobacter aerogenes to benzylpenicillin, ampicillin, carbenicillin, cefotaxime, aztreonam, and cephacetrile. Except for that of cephacetrile, the permeability coefficients were equal to or below 10(-7) cm/s. For cephacetrile, carbenicillin, and benzylpenicillin, the outer membrane of E. cloacae was 20 to 60 times less permeable than that of Escherichia coli, whereas for cefotaxime, aztreonam, and ampicillin it was, respectively, 400, 1,000, and 700 times less permeable. The permeability coefficient for aztreonam is the lowest ever measured (P = 3.2 x 10(-9) cm/s). Using these values, the MICs for a beta-lactamase-overproducing strain of E. cloacae were successfully predicted, demonstrating the validity of the method.

Acylation↗
PubMed1981

[Pharmacokinetic interference between furosemide and cephalosporins].

The effect of furosemid was studied on rats in comparison to that of etamid with respect to circulation in the body of some cephalosporins, such as cephalotin, cephaloridin, cephazolin, cephacetrile, cephapirin, cefradin and cefalexin. Furosemid and etamid were administered to the rats intraperitoneally in a dose of 100 mg/kg 30 minutes before exposure to the cephalosporins. Cefalexin was administered intragastrically in a dose of 100 mg/kg and the other cephalosporins were administered intramuscularly in a dose of 20 mg/kg. It was found that furosemid increased the blood levels of all cephalosporins in the rats and especially those of cephaloridine and cephacetrile, the levels being increased 5-6 times. The effect of etamid was analogous but less pronounced. Furosemid significantly decreased the renal excretion of some cephalosporins, i.e. cephaloridine, cephalotin, cephacetrile and cephazolin and had an insignificant effect on renal excretion of the other antibiotics. Etamid did not inhibit renal excretion of the cephalosporins.

Animals↗
PubMed1977

[An investigation into the influence of human serum on the in-vitro activity of various cephalosporins (author's transl)].

Cephalosporins are being given more and more frequently empirically as initial therapy, until the bacteriological findings become available. The wide selection of cephalosporins available make the choice of the most suitable one difficult for the clinician. Cephazolin, cephradine and cephacetrile were tested against three standard bacteria strains (Escherichia coli, Staphylococcus aureus, Kelebsiella pneumoniae) in normal broth and with the addition of 30% inactivated human serum; the geometric mean of the minimum inhibitory concentration (MIC) was determined by serial dilution, and the minimum bactericidal concentration (MBC) by inoculation onto solid medium. On the addition of 30% serum, cephazolin showed a reduction in effectivity of up to 360% for the MIC and up to 74% for the MBC, cephacetril up to 250% for the MIC and 100% for the MBC, and cephradin a maximum loss of 16%. Successful treatment of a severe infection requires a high drug level or a corresponding tissue titer. Due to the high tissue concentration of cephradin and the unrivalled stable antibacterial effectivity in serum, this antibiotic can be recommended for clinical use.

Blood Bactericidal Activity↗
PubMed1977

[Experimental studies on the renal tolerance of cefuroxime (author's transl)].

The potential renal tolerance of cefuroxime was investigated in 80 female albino Wistar rats and compared with that of cephacetrile. The drugs were administered i.m. in different dosages (1000, 2000, 3000 and 5000 mg/kg/day; dosage interval: 12 h) over a period of five days. The excretion of tubular cells and urinary malic dehydrogenase was assessed before, during and after administration of the antibiotics. In addition, the concentration of serum urea was analysed and the renal histology was examined. The following toxic threshold doses were estimated: cefuroxime 5000 mg/kg/day, cephacetrile 3000 mg/kg/day. In comparison with other cephalosporines cefuroxime belongs to those antibiotics with which a high degree of renal tolerance is demonstrated.

Animals↗
PubMed1978

Drug-induced lysosomal changes and nephrotoxicity in rats.

Lysosomal involvement in renal tubular lesions was studied mainly by electronmicroscopy after single and repeated administrations of cephacetrile, cephalothin, cephaloridine, gentamicin or leupeptin and combine administrations of cephalothin and gentamicin or gentamicin and leupeptin in female Wistar rats. Large cytosomes of high density were increased due probably to either reabsorption and secretion of drugs or their metabolites. These cytosomes displaying acid phosphatase activity were demonstrated histochemically and were identified as heterolysosomes. In rats treated with cephaloridine, gentamicin or leupeptin, disruption of lysosomal membrane was noted and regional cytoplasmic destruction was seen in the vicinity of the disrupted heterolysosomes. Necrotic epithelial cells and renal insufficiency were observed in these animals. On the other hand, neither destruction of lysosomes nor cell lesion was found in rats treated with cephacetrile or cephalothin. It was speculated that lysosomal destruction might be the cause of the cell lesions found in cephaloridine, gentamicin or leupeptin treated rats.

Animals↗
PubMedDate not supplied

[Antimicrobial sensitivity of coagulase-positive staphylococcal strains isolated from bovine mastitis in the central dairy catchment area of Argentina ].

The activity of antimicrobial agents frequently used for treating bovine mastitis was determined against 101 coagulase-positive staphylococci isolated from bovine mammary secretion. The isolates were obtained from 39 dairy farms located in the central dairy area of Argentina. The disk diffusion method was used and the following antimicrobial agents were tested: penicillin, ampicillin, oxacillin, cephacetrile, penicillin + novobiocin, erythromycin, pirlimycin, novobiocin and neomycin. The highest levels of resistance were observed against penicillin and ampicillin (47.6%), while the lowest against erythromycin (2%), pirlimycin (4%) and neomycin (2.9%). No resistant strains against oxacillin, cephacetrile and penicillin + novobiocin were detected.

Animals↗
PubMed1978

[Serum and joint levels of cefacetrile during its administration for septic arthritis].

Six patients, five of whom had normal and one impaired renal function, and all suffering from purulent arthritis caused by cephalosporin-sensitive germs, were given a seven-day course of 8 g cephacetrile daily. On the first day, 6 g were administered by continuous intravenous infusion at the rate of 500 mg/h, followed by 2 g over a further 45 min. On days 2 to 7, the patients received 2 short infusions of 4 g each at an interval of 12 h. In four patients with normal renal function, serum half-life ranged from 0.8 to 1.4 h, serum levels during continuous infusion from 19 to 31 microgram/ml, and total clearances from 265 to 434 ml/min. In one patients, these values were 1.6 h, 70 microgram/ml and 131 ml/min respectively (small volume of distribution). The concentrations in the synovial fluid varied from 2 to 29 mcirogram/ml; they were generally lower than the serum levels, but clearly exceeded the minimum inhibitory concentrations for germs commonly present in purulent arthritis. In five patients, the synovial fluid became germ-free and the arthritis was clinically cured. In the case presenting with renal insufficiency, the serum half-life was 5.8 h. During continuous administration, a steady state was not attained; peak serum levels amo9nted to 75 microgram/ml and the total clearance to 61 ml/min. The cephacetrile concentrations in the synovial fluid were very high (26 and 67 microgram/ml). In this case, in which the renal insufficiency associated with mycosis fungoides was present before the treatment, renal function deteriorated futher during treatment while the arthritis improved.

Adolescent↗
PubMed1983

The permeability barrier of Haemophilus influenzae type b against beta-lactam antibiotics.

An evaluation was made of the role of the outer membrane of Haemophilus influenzae type b as a permeability barrier against beta-lactam antibiotics. Sonic extracts of H. influenzae containing beta-lactamase were assayed for the rates of hydrolysis of benzylpenicillin, ampicillin, cloxacillin, cephacetrile, cefazolin, cefamandole, cephalothin, cephaloridine, cephaloglycin, and cefaclor. Benzylpenicillin was hydrolyzed most rapidly, whereas cephacetrile, cephaloridine, and cephaloglycin were the poorest substrates for the beta-lactamase. The hydrolysis of these ten beta-lactams by intact cells was also determined; it was necessary to stabilize the cells with MgCl2 to prevent lysis and thereby to maintain the beta-lactamase in the periplasm. Calculations were made of the concentration of the antibiotics which had accumulated in the periplasm. The transmembrane permeability coefficient, C, was determined for the ten beta-lactam antibiotics. All of the compounds tested were able to diffuse across the outer membrane of H. influenzae type b very efficiently. The values of the permeability coefficient were compared with the partition coefficients of the antibiotics in a two-phase isobutanol/water mixture. For a ten-fold increase in hydrophobicity, there was a ten-fold decrease in the permeability coefficient. The outer membrane of haemophilus was not an effective barrier against the penetration of penicillins or cephalosporins. The activity of these compounds could be attributed either to their low hydrolysis by beta-lactamase or to the high affinity of binding to their sensitive targets.

Anti-Bacterial Agents↗
PubMed1994

beta-Lactamase hydrolysis of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines.

The beta-lactam hydrolysis of five cephalosporin 3'-quinolones (dual-action cephalosporins) by three gram-negative beta-lactamases was examined. The dual-action cephalosporins tested were the ester Ro 23-9424; the carbamates Ro 25-2016, Ro 25-4095, and Ro 25-4835; and the tertiary amine Ro 25-0534. Also tested were cephalosporins with similar side chains (cefotaxime, desacetylcefotaxime, cephalothin, cephacetrile, and Ro 09-1227 [SR 0124]) and standard beta-lactams (penicillin G, cephaloridine). The beta-lactamases used were the plasmid-mediated TEM-1 and TEM-3 enzymes and the chromosomal AmpC. The cephacetrile-related compounds Ro 25-4095 and Ro 25-4835 were hydrolyzed by all three beta-lactamases with catalytic efficiencies (relative to penicillin G) ranging from approximately 5 (TEM-1, AmpC) to approximately 25 (TEM-3). The cephalothin-related Ro 25-2016 was also hydrolyzed by all three beta-lactamases, particularly the AmpC enzyme (relative catalytic efficiency, 110). The cefotaxime-related compounds Ro 25-0534 and Ro 23-9424 were hydrolyzed to any significant extent only by the TEM-3 enzyme (relative catalytic efficiencies, 1.2 and 4.7, respectively.

Amines↗
PubMed1984

Epileptogenic activity induced by intravenous injection of certain cephalosporins in rats.

Epileptogenic activity induced by intravenous injection of certain cephalosporin derivatives was studied. Ceftezole provided the most potent epileptogenic activity among the drugs tested. Changes in seizure patterns on electroencephalogram (EEG) tracings and behavioral signs after administration of cefotiam and cefazolin were similar to those seen after ceftezole, though the intensity and duration were less than those of ceftezole. Cephacetrile and cephaloridine elicited the spiking activity in the frontal cortex and the other regions without apparent behavioral changes. Latamoxef and cefmenoxime displayed a weak epileptogenic activity at a dose of 1000 mg/kg. On the other hand, cephapirin, cefmetazole and cefoxitin did not evoke any changes in EEG nor in behavior. Penicillin G at a dose of 200 mg/kg affected spike or spike-and-wave complex in a few cases, but at a dose of 500 mg/kg the animals died of dyspnea almost immediately after injection without showing apparent epileptogenic signs. These results suggest that some of cephalosporins such as ceftezole, cefotiam, cephacetrile and cefazolin provide epileptogenic activity at higher doses.

Animals↗
PubMed1978

Alkalimetric microassay of cephalosporins.

Alkalimetric pH-stat titrations of cephalosporin C, cephacetril and their deacetyl derivatives using an acetyl esterase and beta-lactamase are described. The esterase was used to assay highly purified samples of cephalosporin C and cephacetril, and also to prepare analytically defined solutions of the deacetyl cephalosporins. Lactamase-catalyzed hydrolysis of the parent compounds was then found to generate exactly 2 equivalents of acid per mole; that of the deacetyl derivatives exactly 1 equivalent.

Acetylesterase↗
PubMed1978

Biophotometric investigations on the influence of cephradine and related cephalosporins on the growth of beta-lactamase-producing staphylococi.

Biophotometric growth studies were conducted with clinical isolates of beta-lactamase-producing staphylococi in the presence and absence of cephradine, cephalexin, cefazolin and cephacetrile. Of the four antibiotics, cephradine was the most effective in prolonging the suppression of bacterial growth resulting from antibiotic action while cefazolin was the least effective. Cephalexin and cephacetrile were intermediate in effect. The superiority of cephradine over cephalexin was shown to be related to the more rapid destruction of cephalexin by beta-lactamase. On comparing the results of these studies with clinical experience it was concluded that biophotometric studies have clinical relevance and consequently should be used for evaluating the efficacy of beta-lactam antibiotics against pathogenic staphylococi.

Cephalosporinase↗
PubMed1979

[Comparative study of the interaction of cephalosporins with blood serum proteins and organ homogenates].

Interaction of 7 semisynthetic antibiotics (cephaloridine, cephalexin, cephradine, cephazolin, cephalotin, cephacetrile and cephapirin) with proteins of human, bovine and rabbit blood serum, as well as organ and tissue homogenates of rats was studied comparatively. The study showed that binding of the cephalosporins by the blood serum depended on both the chemical structure of the antibiotic and the species affiliation of the protein substrate. The binding lvels of cephazolin and cephalotin by the blood serum proteins (except bovine serum) were the highest, while the binding level of cephaloridine was the lowest. A significant decrease in the values of binding by the serum proteins of the drugs with high percentage of binding was observed when the drug concentrations in solution were increased. Binding of the cephalosporins by the blood serum proteins was in most cases completely reversible. The activity of the cephalosporins decreased in the presence of the rat organ and tissue homogenates. The levels of the activity decrease as compared to the theoretical ones were the highest with the use of cephalotin, cephacetrile and cephapirin. The lowest values of detection of these antibiotics were noted on their incubation with the liver, kidneys and lungs.

Animals↗
PubMed1978

[Comparative studies on the action of aminoglycosides and cephalosporins on the proximal tubule of the human kidney (author's transl)].

Tubulo-toxic effects of drugs can be recognised by the elimination of portions of brush border membrane in the urine. An integral constituent of the brush border membrane is an alanine aminopeptidas (AAP). It is measurable in the urine enzymatically and immunologically with great reliability. The AAP activity was determined in the 24-hour urine of test subjects. Fifteen subjects received 3 mg/kg gentamicin, sisomicin or tobramycin on 3 consecutive days and 10 subjects were given amikacin (15 mg/kg). In addition, 15 subjects received cephacetrile (8.0 g), cephazolin (6.0 g) or cephalothin (8.0 g) on 3 consecutive days. It was shown that all aminoglycosides have a cumulative effect on the brush border membrane, amikacin is the strongest and tobramycin the weakest. The cephalosporins cephalothin and cephazolin were indifferent to the tubule membranes and had no effect on the excretion of AAP. There were responders and non-responders to cephacetrile. The application of cephalothin and cephazolin immediately before the administration of gentamicin prevents the membrane effect of gentamicin.

Adolescent↗
PubMed1982

Permeability of Pseudomonas aeruginosa outer membrane to hydrophilic solutes.

Pseudomonas aeruginosa is usually resistant to a wide variety of antibacterial agents, and it has been inferred, on the basis of indirect evidence, that this was due to the low permeability of its outer membrane. We determined the permeability of P. aeruginosa outer membrane directly, by measuring the rates of hydrolysis of cephacetrile, cephaloridine, and various phosphate esters by hydrolytic enzymes located in the periplasm. The permeability to these compounds was about 100-fold lower than in the outer membrane of Escherichia coli K-12. Also, we found that the apparent Km values for active transport of various carbon and energy source compounds were typically higher than 20 microM in P. aeruginosa, in contrast to E. coli in which the values are usually lower than 5 microM. These results also are consistent with the notion that the P. aeruginosa outer membrane indeed has a low permeability to most hydrophilic compounds and that this membrane acts as a rate limiting step in active transport processes with high Vmax values.

Cell Membrane Permeability↗