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Biomedical subjects

K Seeger

Publications and source records attributed to K Seeger.

At least 37 records · Page 2Linked to original sources

Cefodizime, an aminothiazolylcephalosporin. I. In vitro activity.

Cefodizime possesses a broad antibacterial spectrum including staphylococci, streptococci and Enterobacteriaceae. Neisseria gonorrhoeae and Haemophilus influenzae are also highly susceptible to cefodizime. Because of its beta-lactamase stability cefodizime is active against bacterial strains producing especially plasmid-coded enzymes. The MICs of cefodizime are slightly higher than those of cefotaxime, but with most Gram-negative bacteria they are lower than those of cefazolin, cefotiam and piperacillin. The in vitro activity of cefodizime is not dependent on inoculum size, or on the pH and composition of the test medium. Cefodizime did not induce in vitro resistance of Staphylococcus aureus or Escherichia coli. Because of its binding properties to PBPs 1A/B and 3, cefodizime leads to filamentation of Gram-negative rods and, at only slightly higher concentrations, to bacteriolysis.

Bacterial Proteins

Cefodizime, an aminothiazolylcephalosporin. II. Comparative studies on the pharmacokinetic behavior in laboratory animals.

The pharmacokinetic properties of cefodizime, a new aminothiazolyliminomethoxycephalosporin, were studied in laboratory animals and compared with the pharmacokinetics of another long-acting cephalosporin, ceftriaxone. Both cephalosporin derivatives showed high affinity (33-99%) for serum proteins. High and prolonged blood respectively serum levels of the antibiotics were achieved following subcutaneous and intravenous injection into mice, rats, rabbits, dogs and monkeys. Cefodizime elimination half-lives ranged from 1.17 hours in mice to 3.53 hours in rabbits compared to ceftriaxone half-lives ranging from 0.73 hour in mice to 7.31 hours in rabbits. The antibiotics were well distributed in the body and penetrated into tissues and body fluids to a high degree. Particularly high and prolonged levels were detected in the lungs, liver and kidneys of the experimental animals. Large amounts, approximately 35-55% of the given dose, were recovered in the urine of rabbits and dogs, while the recovery rate in the bile of rabbits was only 0.57% for cefodizime and 1.08% for ceftriaxone.

Animals

The in vitro antimicrobial activity of desacetylcefotaxime compared to other related beta-lactams.

Like all other cephalosporins that contain an acetyl side chain in the 3' position, cefotaxime (CTX) is partially desacetylated in vivo. Desacetylcefotaxime (des-CTX) possesses a broad antimicrobial spectrum and high beta-lactamase stability. With the exception of Pseudomonas aeruginosa, Morganella morganii, Bacteroides fragilis, and Staphylococcus aureus, most strains of other species tested usually had mean MICs of des-CTX lower than 1 microgram/ml. Its activity is generally lower than that of the parent compound. It was only against some strains of P. cepacia that des-CTX surpassed the activity of CTX. The activity of des-CTX markedly exceeds the activity of many therapeutically used cephalosporins. This is especially true for Haemophilus influenzae, Neisseria meningitidis, most species of Enterobacteriaceae, and streptococci other than Streptococcus faecalis.

Anti-Bacterial Agents

[Swine dysentery].

The microbiological and serological properties of Treponema hyodysenteriae, its mediators of pathogenicity and the morphological changes in infected animals were presented. From these changes and from the disturbances of the intestinal function, the clinical symptoms could be derived. Finally problems of epidemiology, therapy and prophylaxis of swine dysentery were discussed.

Agglutination Tests

HR 810, a new parenteral cephalosporin with a broad antibacterial spectrum.

3-[(2,3-Cyclopenteno-1-pyridinium)-methyl]-7-[2-syn-methoximino-2-(2-aminothiazol-4-yl)-acetamido]-ceph-3-em-4-carboxylate (HR 810) is a new cephalosporin derivative with an extremely broad antimicrobial spectrum. It is active against all bacterial species of clinical relevance, including strains which are frequently resistant towards cephalosporins of the third generation.

Bacteria

Penetration of cefotaxime into the pancreas.

After intravenous injection of cefotaxime, higher pancreatic concentrations of the antibiotic were found in rats with experimental pancreatitis than in control animals. Also in human pancreatic pseudocysts, high and persistent concentrations of cefotaxime were found following intravenous injection. The results justify the use of cefotaxime in acute pancreatitis, whenever an antibiotic is indicated.

Animals

Cefotaxime in human lung tissue.

In the course of thoracic surgery in 79 patients lung tissue samples were taken up to around 2 and 4 h, respectively, after i.v. injection of 1 (n = 22) or 2 g cefotaxime (n = 57). In these samples cefotaxime levels were measured using a microbiological method. About 1 h after injection 1.6 and 5.1 microgram/g (median values), respectively, were found. Even later after injection cefotaxime could still be detected. These results are evaluated with respect to the problem encountered in the biological measurement of concentrations of ester cephalosporins in tissue due to desacetylation by hemolytic samples.

Adolescent

Comparative determination of cefotaxime and desacetyl cefotaxime in serum and bile by bioassay and high-performance liquid chromatography.

In rat serum as well as in human serum and bile after injection of cefotaxime (CTX), the parent compound and the active metabolite desacetyl cefotaxime (dCTX) have been demonstrated by quantitative analysis with high-performance liquid chromatography (HPLC). Simultaneous determination of CTX by bioassay using test organisms sensitive to both CTX and dCTX resulted in spuriously high concentration readings of CTX. Using dCTX insensitive test organisms concentrations of cefotaxime obtained by agar diffusion test and by assay with HPLC were highly correlated. In human serum and bile after i.v. injection of 2 g CTX, as may be administered therapeutically, high concentrations of dCTX were observed. dCTX has a longer elimination half-life than the parent molecule. It is concluded that the measurement of CTX in biological fluids should be performed by HPLC or by bioassay with a selective test organism in order to obtain correct pharmacokinetic parameters.

Adult

An enzyme immunoassay (EIA) for progesterone in horse plasma.

A simple enzyme immunoassay (EIA) for the measurement of progesterone is described. Antibody against 11-OH-hemisuccinate-BSA is bound to polystyrene tubes. 11-OH-hemisuccinyl-beta-D-galactosidase is used as enzyme-coupled antigen and methylumbelliferyl-beta-D-galactoside as substrate. Concentrations down to 0.156 ng/ml plasm or amounts of 93 pg/tube are detectable. Probit analysis gave a linear relationship between log concentration and percentage of binding. A comparison of EIA and radioimmunoassay gave a correlation coefficient of 0.81. The assay is sufficiently sensitive to estimate progesterone levels in plasma.

Animals