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Antibacterial activity of roxithromycin: a laboratory evaluation
The Journal of Antibiotics
|May 1, 1986
Summary
Roxithromycin, a new macrolide antibiotic, shows comparable in vitro activity to erythromycin but superior in vivo efficacy and bioavailability. This novel antibiotic demonstrates excellent tissue penetration, particularly in the lungs.
Area of Science:
- Microbiology
- Pharmacology
- Infectious Diseases
Background:
- Roxithromycin (RU 28965) is a novel 14-membered semisynthetic macrolide antibiotic.
- It exhibits antibacterial activity against Gram-positive cocci and bacilli, Gram-negative cocci, and some Parvobacteriaceae.
Purpose of the Study:
- To compare the in vitro antibacterial activity of roxithromycin with erythromycin and spiramycin.
- To evaluate the in vivo efficacy and pharmacokinetic properties of roxithromycin.
Main Methods:
- In vitro comparison using 2-fold broth macro-dilution tests against 275 clinical isolates.
- In vivo studies in laboratory animals to assess antibacterial potency and pharmacokinetic parameters like bioavailability and tissue distribution.
Main Results:
- Roxithromycin and erythromycin demonstrated qualitatively similar antibacterial spectra, though erythromycin had lower minimal inhibitory concentrations except for Corynebacterium sp. and Bacteroides fragilis.
- Roxithromycin showed significantly superior in vivo antibacterial activity, being up to six times more potent than erythromycin in animal models.
- Roxithromycin exhibited high blood levels, long elimination half-lives, and excellent oral bioavailability (72% in mice, 85% in rats), with extensive tissue distribution, especially in the lungs.
Conclusions:
- Roxithromycin possesses a favorable pharmacokinetic profile, including high bioavailability and extensive tissue penetration.
- Its superior in vivo efficacy suggests potential advantages over erythromycin for treating bacterial infections, particularly those involving lung tissue.