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PubMed1976

In vitro and in vivo comparative evaluations of injectable cephalosporin derivatives and ampicillin.

The in vitro and in vivo activity of the 5 injectable cephalosporins, cefazolin, cephaloridine, cephalothin, cephapirin, cephacetrile, and ampicillin was compared. No gram-positive organisms resistant to any of the cephalosporin derivatives were encountered. The MIC of ampicillin for gram-positive organisms was distributed over a wide range. The antibacterial activity of cefazolin, cephaloridine and ampicillin was high against gram-negative organisms. Ampicillin was potently effective especially against P. mirabilis and cefazolin especially against K. pneumoniae. The protecting effect of the 5 cephalosporins on experimental infections in mice was compared. The effect of cefazolin and cephaloridine was more marked than that of the others. These results may be explained by the fact that the other 3 cephalospoirins are rapidly metabolized in the living body.

Ampicillin↗
PubMed1976

[The cephalosporins and their clinical value].

Up to now cephalothin was the only parenteral and cephalexin the only oral cephalosporin for clinical use in the GDR. The paper deals with several newer cephalosporins. Of these cephazolin shows some advantages, especially in antibacterial activity and serum levels. There is no metabolization and a better local tolerability compared with cephalothin. Cephapirin has no and cephacetril only inessential advantages. The antibacterial activity of the also well tolerated cephradin is less than that of cephalothin. Certain favourable pharmacokinetic properties such as high lymph and tissue levels, related to serum levels, slight protein binding, high distribution volume and a better stability against beta-lactamases lead to a superiority over cephalothin and diminish the disadvantages compared with cephazolin. The oral form of cephradin very equals to cephalexin.

Abortion, Septic↗
PubMed1975

Knee joint infections with Staphylococcus aureus and Micrococcus species.

In rabbit knees 600 Staphylococcus aureus organisms produced progressive infection in 50 per cent of the knees injected, whereas 5.3 times 10-7 Micrococcus species caused only transient colonization of the joints. Methicillin, cephacetrile, and clindamycin administered before injection of the staphylococci gave protection. Stainless-steel particles in the knee did not increase susceptibility to infection from injected micrococci but did make established micrococcal infections more persistent. Knees containing steel debris failed to become infected during prolonged staphylococcal bacteremia. Injected autologous blood, either fresh or three days old, did not increase susceptibility to infection. Large doses of steroids, given systemically or intraarticularly, decreased resistance to micrococcal infection and increased the destruction caused by infection due to this organism.

Animals↗
PubMed1976

The in vitro spectrum of the cephalosporins.

The cephalosporins may currently be classified according to their relative susceptibility to beta-lactamases. Cefoxitin, cefamandole, cefatrizine, and cephanone are relatively resistant to the gram-negative beta-lactamases, whereas cephalothin, cefamandole, and cefoxitin are resistant to staphylococcal beta-lactamase. Although the inhibitory activity of cephalothin is representative of that of cephaloridine, cephalexin, cefazolin, cephapirin, cephacetrile, and cephradine, there are significant differences between its activity and that of cefoxitin, cefamandole, and cefatrizine, especially against Enterobacter, Serratia, indole-positive Proteeae, Bacteroides fragilis, and ampicillin-resistant Haemophilus influenzae.

Bacteria↗
PubMed1977

[The growth curves of enterobacteriaceae and the estimation of L-forms under the influence of cephalosporin antibiotics].

The antibacterial effectiveness of cephalothin, cefazolin, cephacetrile and cephradine was investigated on growing cultures of Klebsiella pneumoniae recording the growth curves with a biophotometer. Thereby cefazolin has a greater antibacterial activity than the other cephalosporins. By raising the dose to 100 microgram/ml after initial bactericidal effect a second growth phase was observed. Phase microscopic observation showed that this was caused by an increasing number of L-forms. This phenomenon could be observed with two other strains and seems to be a strain-specific characteristic. It occurs only using cephalosporins and isotonic nutrient media. The medical importance of the described ability of some bacteria as a factor of pathogenicity is discussed.

Cefazolin↗
PubMed1979

[Correlation between antibacterial activity of some cephalosporins and pharmacokinetic properties "in vitro" (author's transl)].

A new apparatus is described which can be used to investigate the in vitro antibacterial activity of antibiotics as a function of different concentration-time curves. The apparatus can be adjusted to simulate the biexponential serum level curves observed in vivo after oral or intramuscular administration. Preliminary studies were carried out with cefazolin against an E. coli strain simulating initial concentrations of 5, 10 and 20 micrograms/ml that decreased exponentially with half-lives of 30, 60 and 120 min. In all the situations tested there was an initial phase of rapid bactericidal activity followed by a phase of bacteriostatic activity, whose length depended on the drug elimination rate but was relactively independent of the initial concentrations. Bacterial regrowth occurred when the antibiotic concentration fell below the minimum inhibitory concentration (MIC) of the drug. The antibacterial activity of cefazolin, cephacetrile, and cephradine against an E. coli strains was also investigated, in a medium containing 4% human albumin, simulating the serum level curves observed in humans after an intramuscular dose of 1 g. The results obtained confirm that, for cephalosporins, the dosage schedule should be adjusted taking into account the potency of the drug (MIC) and its rate of elimination.

Cefazolin↗
PubMed1982

[Microbiological evaluation of the antibacterial activity of cefotaxime in comparison with other cephalosporins].

In this study we have evaluated the antibacterial activity of six cephalosporins of the first generation (cephacetrile, cephalothin, cefazolin, cephaloridin, cephalexin, cephradine) two cephalosporin of the second generation (cefoxitin and cefuroxime) and two of the third generation (cefotaxime and cefoperazone) against 66 clinical bacterial isolates. Cefotaxime has been highly active against the strains examined in this study with low MICs.

Bacteria↗
PubMed1980

[Antibiotic concentration during extracorporeal circulation (author's transl)].

In open surgery, ampicillin (Solcillin) or cephacetrile (Celtol), 2 g for patients weighing 20 kg or more, and 1 g for those below 20 kg, was administered, and the antibiotic concentrations in blood and urine were estimated during extracorporeal circulation, from the time of operation to the admission in an intensive care unit (Group A). In other group, a total circulation volume of 0.3 mg/ml of the antibiotic was administered, based on body weight of patients and priming volumes (Group B). In Group A, blood concentration of antibiotics was so variable that it was difficult to decide additional dosage. In Group B, comparatively definite concentrations were estimated in each case. In extracorporeal circulation for a long time, it is preferable to maintain the blood concentration of antibiotic at 50 micrograms/ml, by additional antibiotic administration 90 approximately 120 minutes after the beginning of the extracorporeal circulation. In patients with preoperative subacute bacterial endocarditis, the blood concentration should be kept over 100 micrograms/ml during extracorporeal circulation.

Adolescent↗
PubMed1976

[Treatment of pneumonia in childhood (author's transl)].

It is necessary to start with antibiotic treatment in infections of the lower respiratory system, especially pneumonias. The finding of the infectious agent is difficult and without security. With simple investigations, as sedimentation rate, white blood cell count and cell differentiation there is a possibility of 80% to get a diagnosis of bacterial infection. In 25 patients aged 1 1/2 to 9 years with x-ray diagnosis of pneumonia the results of treatment with cephacetril (100 mg/kg/d) are given. Clinical symptoms disappeared after 5 days, the average time of illness was 12 days. One patient got a severe pleural effusion.

Cephacetrile↗
PubMed1976

Antibiotics and chemotherapeutics in renal lymph. An experimental study in dogs.

Renal lymph concentrations of ampicillin, carbenicillin, cephacetrile, cephaloridine, and nitrofurantoin were determined in a total of 28 dogs during constant infusion of the drugs together with [125I]iothalamate and [131I]o-iodohippurate for simultaneous determination of glomerular filtration rate and effective renal plasma flow. The lymph concentrations of the radiolabeled clearance substances, serving as a standard were compared to those of the antimicrobial agents. The lymph concentrations of the four antibiotics were all significantly lower than the respective simultaneous arterial plasma concentrations. The nitrofurantoin lymph concentrations were equal to the simultaneous plasma concentrations. It is concluded that the renal lymph concentrations of antibiotics and chemotherapeutics do not exceed the simultaneous plasma concentrations unless the urine flow is obstructed.

Ampicillin↗
PubMed1991

Gly-238-Ser substitution changes the substrate specificity of the SHV class A beta-lactamases.

The SHV-type beta-lactamase SHV-2A is related to SHV-1 by a Gly-238-Ser replacement. Strains carrying SHV-2A are resistant to the third generation cephems cefotaxime and ceftizoxime, whereas those that carry SHV-1 are sensitive to these drugs. We present a kinetic analysis of a SHV-1 and SHV-2A enzymes, with the goal of gaining insight into the role of residue 238 in hydrolyzing cefotaxime and ceftizoxime. SHV-2A shows altered kinetic properties for a number of other cephems that also have heterocyclic side chains at the amino position of the 7-aminocephalosporanic acid nucleus (R1 side chain), including a significantly higher kcat/Km than does SHV-1 for cephaloridine, cephalothin, and cefotiam. Two cephems with straight chain R1 substitutions, cephalosporin C and cephacetrile, are not hydrolyzed more efficiently by SHV-2A. These results indicate that the Ser-238-Gly substitution increases the affinity toward cephems with a heterocyclic ring in the R1 side chain. In addition, the data for ampicillin and benzylpenicillin show that addition of a nitrogen to the second carbon of the R1 side chain of a penem results in a lower kcat/Km for SHV-2A relative to SHV-1. These data strongly suggest that the previously proposed hydrogen bond formation between Ser-238 and the second carbon nitrogen of cefotaxime is not an important factor in hydrolysis by SHV-2A. We propose that the Gly-238 to Ser-238 replacement in SHV-2A has altered the hydrophobic pocket so that it can better accommodate cephems with bulky R1 side chains.

Amino Acid Sequence↗
PubMed1983

The current state of cephalosporin antibiotics: microbiological aspects.

An increasing number of new cephalosporins continue to become available in the clinic so that the clinician requires something akin to Ariadne's thread to work through the labyrinth of confusing names and product claims. The parenteral cephalosporins may be grouped on the basis of structure, antimicrobial activity and metabolic stability as follows: 1. cephacetrile, cephalothin, cefapirin; 2. cefotaxime; 3. cephaloridine, cefazedone, cefazolin, cefotiam; 4. cefamandole, cefoperazone, cefsulodin, cefuroxime, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, lamoxactam. Groups 2 and 4 contain the most interesting compounds in terms of their biological activity and therapeutic significance. Even carbenicillin-resistant strains of Pseudomonas aeruginosa are inhibited by one of the recent broad-spectrum cephalosporins. In the clinic, minor differences between the highly active cephalosporins are not likely to be of therapeutic significance.

Bacteria↗
PubMed2006

Evaluation of liquid chromatographic behavior of cephalosporin antibiotics using restricted access medium columns for on-line sample cleanup of bovine milk.

Microsample deproteinization of bovine milk was carried out on-line using a series of restricted access medium (RAM) bovine serum albumin (BSA) columns: C8, C18, phenyl, and cyano. The four different columns prepared showed a high percentage of protein exclusion using water as the mobile phase and provided an appropriate retention profile for a series of five cephalosporin antibiotics (cefoperazone, cephacetril, cephalexin, cephapirin, and ceftiofur). Chromatographic conditions such as washing time, buffer pH, and type and percentage of organic modifier were fully evaluated with respect to the protein elution profile and retention of the antibiotic by RAM column. One of these columns was chosen to develop and validate a method for the determination of cefoperazone in bovine milk. The system used in this work was composed of a RAM-BSA phenyl column coupled to a C18 analytical column. The standard curve was linear over the range 0.100-2.50 microg/mL. The limits of quantification and detection were 0.100 and 0.050 microg/mL, respectively. The developed method showed high intermediate precision (CV of 2.37-2.63%) and accuracy (90.7-94.3%) with adequate sensitivity for drug monitoring in bovine milk samples.

Animals↗
PubMedDate not supplied

Effects of subminimal inhibitory concentrations of antibiotics on adhesiveness of Escherichia coli in vitro.

The adhesion of radiolabeled Escherichia coli (strain SS142) to monolayers of Intestine 407, a human epithelioid tissue culture cell line, was investigated. In this assay the adhesion of bacteria grown in the presence of subminimal inhibitory concentrations of tetracycline, clindamycin,, or trimethoprim-sulfametrole was reduced in a manner that was dose dependent. In contrast, at such concentrations nalidixic acid enhanced the adhesion of this bacterial strain, and other antibiotics-e.g., penicillin G, ampicillin, mecillinam, cephacetrile, cephalexin, cefotaxime, chloramphenicol, and streptomycin-did not affect its adhesiveness.

Adhesiveness↗
PubMed1976

Susceptibility of "enterobacteria" to penicillins, cephalosporins, lincomycins, erythromycin, and rifampin.

Agar dilution tests for susceptibility of gram-negative rods and enterococci were done with a number of penicillins, cephalosporins, lincomycin analogues, erythromycin, and rifampin. Many in the first three categories were investigational drugs. All were generally less active than aminoglycoside and tetracycline antibiotics against gram-negative rods and more active against enterococci. Cephalosporins as a group were more active than penicillins against Klebsiella pneumoniae and Escherichia coli and less active enterococci. Both groups were equally active against Enterobacter, Proteus, and Providencia but inactive against most strains of Serratia and all strains of Pseudomonas; however, ticarcillin, carbenicillin, and BL-1654 were active against most strains of Pseudomonas. Penicillins and cephalosporins were more active against Proteus mirabilis than against indole-positive Proteus. Lincomycins had little or no activity against gram-negative rods but were moderately active against enterococci. Erythromycin was more active than the lincomycins, but rifampin was much more active than either of these types of drug. Of the penicillins, ticarcillin, carbenicillin, and BL-P1654 were the most active against gram-negative rods, whereas BL-P1654, amoxicillin, and ampicillin were the most active against enterococci. The penicillinase-resistant penicillins, cyclacillin, and penicillin V were essentially inactive against gram-negative rods. Of the cephalosporins tested, cephanone and cefamandole were the most active against most gram-negative rods, whereas cephaloridine and cephacetrile were the most active against enterococci. The least active of the cephalosporins against most species were cephradine, cephalexin, and cephapirin, but cefoxitin was the least active against enterococci.

Acinetobacter↗
PubMed1978

Cephalosporin antibiotics in therapy of experimental Streptococcus pneumoniae and Haemophilus influenzae meningitis in rabbits.

Six cephalosporin antibiotics (cefamandole, cefazolin, cephacetrile, cephalothin, cephaloridine, and cephradine) and two penicillin (ampicillin and penicillin G) were evaluated in vitro and in a rabbit model of experimental meningitis due to Haemophilus influenzae or Streptococcus pneumoniae. The percentage penetration ([concentration in cerebrospinal fluid/concentration in serum] X 100%) of these antibiotics varied from 0.7% for cephalothin to 17% for cephaloridine. The penetration varied inversely with binding to serum proteins. The bactericidal rate of all of the cephalosporin antibiotics was similar in vitro and in vivo to that of penicillin G. However, as demonstrated with cephalothin, concentrations considerably above the minimal bactericidal concentration (as determined in broth) were necessary to initiate the bactericidal effect. Cefamandole was found to be as effective as ampicillin in the therapy of H. influenzae meningitis in rabbits.

Ampicillin↗
PubMed1978

Pharmacokinetics of cephalosporins in patients with normal or reduced renal function.

The pharmacokinetic distribution of 10 cephalosporin compounds, cephalothin, cephaloridine, cephaloglycine, cephalexin, cefazolin, cephapirin, cephradine, cephacentrile, cefoxitin, and cefamandole, in patients with various degrees of renal function was reviewed. The mean serum half-life (t1/2) of each cephalosporin compound was calculated from reported data in patients grouped according to their degree of renal function, as determined by the rate of creatinine clearance. Mean t1/2 values in patients with normal renal function were compared with t1/2 values for the same cephalosporin in patients with moderate renal failure and severe renal azotemia. The effect of hemodialysis and peritoneal dialysis on the mean serum t1/2 of each cephalosporin was also determined. The mean serum t1/2 of each cephalosporin progressively increased as the rate of creatinine clearance decreased. Hemodialysis decreases the t1/2 of cephaloridine, cephalexin, cefazolin, and cephacetrile but only minimally influences the t1/2 of cephalothin and cefamandole. Peritoneal dialysis reduces the t1/2 of cephalothin and cephaloridine but only minimally influences the t1/2 of cefazolin and cefamandole.

Cephalexin↗
PubMed1978

New in vitro model to study the effect of antibiotic concentration and rate of elimination on antibacterial activity.

A new apparatus is described which serves to investigate the in vitro antibacterial activity of antibiotics as a function of different concentration time curves. The apparatus can be adjusted to simulate the biexponential serum level curves observed in vivo after oral or intramuscular administration. Preliminary studies were carried out with a cephalosporin derivative, cefazolin, against Escherichia coli and Klebsiella sp. strains simulating initial concentrations of 5, 10, and 20 mug/ml that decreased exponentially with half-lives of 30, 60, and 120 min. Surviving cells were counted at 1-h intervals for 10 h. In all the situations tested there was an initial phase of rapid bactericidal activity followed by a phase of bacteriostatic activity, whose length depended on the drug elimination rate but was relatively independent of the initial concentrations. Bacterial regrowth occurred when the antibiotic concentration fell below the minimum inhibitory concentration of the drug against the strains tested. The antibacterial activity of cefazolin, cephacetrile, and cephradine against E. coli and Klebsiella strains was also investigated, in a medium containing 4% human albumin, simulating the serum level curves observed in humans after an intramuscular dose of 1 g. The results obtained suggest that, for cephalosporins, a longer half-life might be more useful than higher peak levels.

Anti-Bacterial Agents↗