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Biomedical subjects

M Nishida

Publications and source records attributed to M Nishida.

At least 577 records · Page 32Linked to original sources
PubMed1977

Laboratory evaluation of FR10024 a new cephalosporin derivative.

FR10024 is a broad-spectrum antibiotic. The in vitro antibacterial activity of FR10024 against clinical isolates of Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis is greater than that of any of the cephalosporins developed to date. Indole-positive Proteus, Enterobacter, and Citrobacter are resistant to FR10024, as is true for the other cephalosporins. However, more than half of the strains of Enterobacter and Citrobacter tested were susceptible to FR10024 at an inoculum of 10(6) cells/ml. A single subcutaneous injection of FR10024 to mice with peritoneal infections due to S. aureus and several species of gram-negative bacilli gave a protective effect inferior to that of cefazolin but appeared to be superior to that of cephalothin. When given in two divided doses, however, the protective effect of FR10024 was enhanced and almost equaled that of cefazolin. The serum levels and rates of urinary recovery of FR10024 varied in different animal species. The mean peak serum level of FR10024 in humans after a single intramuscular injection of 500 mg was two times higher than that of cephalothin. The serum half-life after intramuscular injections of 250 and 500 mg was slightly shorter than that of cephalothin. After receiving 250 mg of FR10024 intramuscularly the urinary recovery rate was 87.7% in healthy volunteers. The biliary excretion rate of FR10024 was particularly high. The 24-h excretion of FR10024 in rats was 63.3%, this being six to seven times higher than that for cefazolin, which has the highest biliary excretion of the other known cephalosporins. When FR10024 was injected intramuscularly (20 mg/kg), it was found that the hepatic levels of FR10024 in rats were the highest of all the cephalosporins, including cefazolin, but the levels of FR10024 in other tissues were not as high as those of cefazolin.

Adult↗
PubMed1977

Exudate levels and bactericidal activity of cefazolin in a new local infection system using rat granuloma pouches.

An experimental local infection system has been developed in which exudates are induced with croton oil in granuloma pouches of rats. This system provided a suitable model for the evaluation of the therapeutic effect of two antibiotics, cefazolin and cephalothin. Exudate levels of cefazolin were found to be higher than those of cephalothin, and these levels correlated with the higher serum level of cefazolin. The therapeutic effect of cefazolin, after intramuscular injection of 20 mg of each antibiotic per kg, was superior to that of cephalothin in eradicating both Staphylococcus aureus and Escherichia coli.

Animals↗
PubMed1977

Enterohepatic circulation of a new oral cephalosporin, FR10612, and its effect on serum and tissue levels in rats.

Serum levels of FR10612 given orally to rats persisted significantly longer than did those of cephalexin. Since the elucidation of this phenomenon observed in rats is considered to be pertinent to the understanding of the drug kinetics of FR10612 in other animals including man, the present study was undertaken. From the dose-response curve of the serum levels of FR10612 in rats, it is apparent that the maximum oral absorption is obtained in the range of 100-400 mg/kg. Even when the doses were increased from 100 to 1,000 mg/kg, the tissue levels with the exception of the kidneys, did not increase significantly. However, the persistence of the tissue levels was enhanced. The serum and tissue levels of FR10612 in rats after repeated massive dosings did not increase accumulatively. From the experimental results of FR10612 in rats with ligated bile ducts and the results obtained after intravenous injection, it seems clear that the prolonged in vivo levels of FR10612 in rats after oral dosing are closely related to its enterohepatic circulation.

Administration, Oral↗
PubMed1977

Five cases of absence of iodide concentrating mechanism.

Five cases, 2 males and 3 females, with absence of iodide concentrating mechanism are reported. Three of the five subjects are siblings and the eldest sister has no symptom to account for the cretinism. All 5 cases have improved clinically following the administration of potassium iodide and 4 cases are still in a euthyroid state without any adverse effects during a half to more than 4 years. This study suggests that the absence of iodide concentrating mechanism might be erroneously diagnosed as athyroidal cretinism or adolescent non-toxic diffuse goitre, and may at times not show any clinical symptoms.

Adolescent↗
PubMed1977

Nocardicin A, a new monocyclic beta-lactam antibiotic III. In vitro evaluation.

Nocardicin A, a new monocyclic beta-lactam antibiotic, exerts a comparatively potent antimicrobial activity against gram-negative organisms, especially Pseudomonas aeruginosa, the indole-positive and indole-negative Proteus groups (except Pr. morganii), Serratia marcescens and the Neisseria groups. The in vitro antimicrobial activity of nocardicin A against clinical isolates of Ps. aeruginosa was about twice that of carbenicillin. The mean MICs of nocardicin A for Pr. mirabilis, Pr. rettgeri and Pr. inconstans ranged from 3.13 to 12.5 microgram/ml and were 25 similar to 50 microgram/ml for Pr. vulgaris. Nocardicin A in concentrations of 12.5 similar to 50 microgram/ml inhibited 30 strains (48 percent) of S. marcescens usually resistant to beta-lactam antibiotics. However, nocardicin A had no significant in vitro activity against Staphylococci and Escherichia coli. No cross-resistance was seen between nocardicin A and other beta-lactam antibiotics. This antibiotic was stable to beta-lactamase. The in vitro activity of nocardicin A against Ps. aeruginosa and Pr. mirabilis was greatly influenced by the assay media used. Nocardicin A was bactericidal and appeared to act synergistically with serum bactericidal factors against Ps. aeruginosa and with polymorphonuclear leukocytes against Ps. aeruginosa, E. coli and Pr. vulgaris. The bactericidal activity of nocardicin A against the above 3 organisms, therefore, increased markedly in the presence of fresh serum and polymorphonuclear leukocytes.

Animals↗
PubMed1977

Nocardicin A, a new monocyclic beta-lactam antibiotic IV. Factors influencing the in vitro activity of Nocardicin A.

Factors influencing the in vitro antimicrobial activity of nocardicin A against Pseudomonas aeruginosa and Proteus mirabilis were investigated. Sodium chloride was identified as a major inhibitor. Some of the amino acids, sugars and divalent cations were found to be minor inhibitors. The presence of potassium phosphates enhanced nocardicin A activity against P. aeruginosa, but antagonized the activity against P. mirabilis.

Amino Acids↗
PubMed1977

Nocardicin A, a new monocyclic beta-lactam antibiotic V. In vivo evaluation.

Nocardicin A is a new monocyclic beta-lactam antibiotic which provides a potent therapeutic effect in mice experimentally infected with gram-negative bacilli. When given subcutaneously to mice, the therapeutic effect of the drug was stronger than had been anticipated from in vitro studies. Nocardicin A was more potent in therapeutic effect than carbenicillin against infections due to Pseudomonas aeruginosa, Proteus mirabilis, Pr. vulgaris, Pr. rettgeri and Pr. inconstans, and was similar in effect to carbenicillin against infections due to Escherichia coli in mice. In addition, nocardicin A proved to be active against infections due to Serratia marcescens and other organisms resistant to beta-lactam antibiotics. When nocardicin A was given subcutaneously to mice, blood and hepatic levels of the drug were higher than those of carbenicillin.

Ampicillin↗
PubMed1977

Nocardicin A, a new monocyclic beta-lactam antibiotic VI. Absorption, excretion and tissue distribution in animals.

The absorption, excretion and tissue distribution of nocardicin A, a new monocyclic beta-lactam antibiotic, were studied in various animals. When nocardicin A was given intramuscularly in single doses of 20 mg/kg to rats, rabbits, and dogs, the peak serum levels of nocardicin A were about 1.6 similar to 2.8 times higher than those of carbenicillin in all animals though the levels varied among the species tested. The serum half-life of nocardicin A in these animals was about twice that of carbenicillin. The 24-hour urinary recovery rate of nocardicin A after intramuscular injection was 68.5 percent in rabbits and 77.0 percent in dogs, but was low in rats; i.e., 0.7 percent. When nocardicin A was given intravenously in single doses of 20 mg/kg to these animals, the peak serum levels varied widely among the test species; i.e. about 3 times higher than those of carbenicillin in rabbits and dogs, similar to those in rats. The peak serum and tissue levels of nocardicin A after intramuscular to intravenous injection were the highest in the kidneys, followed by the liver, serum, lungs, heart and spleen. The levels in the liver were prolonged. Nocardicin A, and traces of unknown substances less active than nocardicin A were observed as active substances in the urine recovered after injection of nocardicin A.

Administration, Oral↗