Summary
The chemotherapeutic properties of the new aminothiazolyl cephalosporin HR810 were investigated in experimental animals. Unlike other cephalosporins of the third generation, HR810 had good activity againstStaphylococcus aureus as well as some activity against enterococci. In murine protection tests with these strains, it was clearly superior to ceftazidime, cefotaxime, ceftriaxone, cefoperazone and latamoxef. The compounds most effective in protecting mice from infections caused byEnterobacteriaceae were HR810 and ceftriaxone followed by ceftazidime, latamoxef and cefotaxime; cefoperazone was less active. HR810 was less active againstPseudomonas aeruginosa than ceftazidime but was considerably more effective than the other cephalosporins tested. HR810 also proved effective against localised infections such as thigh lesions, as well as against meningo-encephalitis in mice and pyelonephritis in rats. These results in laboratory animals make HR810 a promising candidate for clinical studies.
Zusammenfassung
Die chemotherapeutischen Eigenschaften des neuen Aminothiazolyl-Cephalosporins HR810 wurden bei Versuchstieren geprüft. Im Gegensatz zu anderen Cephalosporinen der dritten Generation zeigte HR810 eine gute Aktivität gegenStaphylococcus aureus und war auch gegen Enterokokken wirksam. Bei systemischen Mäuseinfektionen mit diesen Stämmen war HR810 dem Ceftazidim, Cefotaxim, Ceftriaxon und Latamoxef deutlich überlegen. HR810 und Ceftriaxon zeigten die größte Schutzwirkung gegen Infektionen durchEnterobacteriaceae, gefolgt von Ceftazidim, Latamoxef und Cefotaxim, während Cefoperazon weniger aktiv war. HR810 zeigte eine geringere Aktivität gegenPseudomonas aeruginosa als Ceftazidim, war jedoch deutlich effektiver als die anderen getesteten Cephalosporine. HR810 erwies sich auch bei Lokalinfektionen, wie der Oberschenkelläsion sowie bei der Meningo-Encephalitis bei Mäusen und der Pyelonephritis bei Ratten als wirksam. Diese Befunde bei Laboratoriumstieren weisen HR810 als ein vielversprechendes Präparat für die klinische Prüfung aus.
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Klese, N., Limber, M., Schrinner, E. et al. Chemotherapeutic properties of the new cephalosporin antibiotic HR810 in laboratory animals. Infection 12, 286–292 (1984). https://doi.org/10.1007/BF01645963
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DOI: https://doi.org/10.1007/BF01645963