Summary
Moxalactam (LY127935) is a new beta-lactam antibiotic which is chemically related to the cephalosporins. The agent is highly active against theEnterobacteriaceae, with most organisms sensitive to 0.1 mcg/ml or less. It is also active at low concentration against gentamicin-resistant strains ofProvidencia andSerratia. Minimal inhibitory concentrations of moxalactam forPseudomonas aeruginosa are approximately four-fold lower than those of carbenicillin for the same isolates. It is highly active againstHemophilus influenzae, including ampicillin-resistant strains, with all strains tested sensitive to 0.1 mcg/ml or less. The majority of strains ofNeisseria gonorrheae andNeisseria meningitidis are sensitive to 0.1 mcg/ml or less. Moxalactam is more active againstBacteroides fragilis than cefoxitin. However, activity of moxalactam against gram-positive cocci was uniformly less than cephalothin and other cephalosporins tested. Little effect of inoculum size was observed with moxalactam except for particular strains of gram-negative bacilli. The drug was found to be 40–43% bound to human serum proteins.
Zusammenfassung
Moxalactam (LY127935) ist ein neues Betalactam-Antibiotikum, das den Cephalosporinen chemisch verwandt ist. Die Substanz besitzt eine hohe Aktivität gegenEnterobacteriaceae, dabei sind die meisten Organismen empfindlich gegenüber 0,1 mcg/ml oder weniger. Die Substanz ist in niedrigen Konzentrationen auch wirksam gegen Gentamicin-resistente Stämme vonProvidencia undSerratia. Die minimalen Hemmkonzentrationen von Moxalactam fürPseudomonas aeruginosa sind annähernd viermal niedriger als die von Carbenicillin für dieselben Isolate. Es ist hochaktiv gegenHaemophilus influenzae, einschließlich der Ampicillin-resistenten Stämme; dabei sind alle untersuchten Stämme empfindlich gegen 0,1 mcg/ml oder weniger. Der Großteil der Stämme vonNeisseria gonorrhoae undNeisseria meningitidis sind empfindlich gegen 0,1 mcg/ml oder weniger. Moxalactam ist wirksamer gegenBacteroides fragilis als Cefoxitin. Die Aktivität von Moxalactam gegen grampositive Kokken war hingegen insgesamt geringer als die von Cephalotin oder anderen untersuchten Cephalosporinen. Der für Moxalactam beobachtete Einfluß der Inokulumgröße war nur geringgradig, ausgenommen bestimmte Stämme von gramnegativen Bazillen. Es zeigte sich, daß die Substanz zu 40–43% an menschliche Serumproteine gebunden wird.
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DeMaria, A., McCabe, W.R., Klein, J.O. et al. In vitro studies of moxalactam (LY127935), a new beta-lactam antibiotic with significant activity against gram-negative bacteria. Infection 8 (Suppl 3), S261–S267 (1980). https://doi.org/10.1007/BF01639592
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DOI: https://doi.org/10.1007/BF01639592