BIOLOGICAL ACTIVITY OF MEGALOMICIN, A NEW <i>MICROMONOSPORA</i>-PRODXJCED MACROLIDE ANTIBIOTIC COMPLEX

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  • Biological activity of megalomicin,a new Micromonospora-produced macrolide antibiotic complex
  • BIOLOGICAL ACTIVITY OF MEGALOMICIN, A NEW MICROMONOSPORA-PRODXJCED MACROLIDE ANTIBIOTIC COMPLEX

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Abstract

In vitro studies with megalomicin A base demonstrated enhanced activity with increased pH, decreased activity with increasing serum content in the medium and serum binding in the range of 20-30%. There is an inoculum effect with megalomicin A. In vivo studies in mice demonstrate that megalomicins A, B, C1, and C2 as well as the complex are active in conventional protection tests and have low acute LD50's. Absorption of megalomicin A and C1 in mice like erythromycin is better after parenteral than oral administration. In rats, and dogs, megalomicin A gives higher serum levels than erythromycin after oral dosing. Megalomicin A base is not emetic in dogs. Both megalomicins A and C1 give more prolonged serum levels in dogs than does erythromycin. Megalomicin A is absorbed along the entire intestinal tract in dogs and gives a depot effect after intramuscular dosing.

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