Efficacy of a novel tetracycline derivative, glycylcycline, against penicillin-resistant Streptococcus pneumoniae in a mouse model of pneumonia.

Abstract

The MIC90 of glycylcycline (< or =0.06 mg/L) against 55 strains of Streptococcus pneumoniae was 100-fold lower than that of minocycline or tetracycline. In a mouse model of penicillin-resistant S. pneumoniae (PRSP) pneumonia, glycylcycline (10 mg/kg) decreased bacterial counts in the lungs from 10(6) cfu to <10(2) cfu, whereas no apparent reduction of bacterial numbers was observed with minocycline or penicillin G. Pharmacokinetic studies showed that the half-life and area under the curve of glycylcycline were superior to those of minocycline and penicillin G in the lungs. These results show a preferential distribution of glycylcycline in the lungs and potent in vivo bactericidal activity in PRSP pneumonia.

• Authors: K Murakami, K Tateda, T Matsumoto, S Miyazaki, K Yamaguchi
• Journal: The Journal of antimicrobial chemotherapy (J Antimicrob Chemother) Vol. 46 Issue 4 Pg. 629-32 (Oct 2000) ISSN: 0305-7453 [Print] England
• PMID: 11020264 (Publication Type: Journal Article)

Chemical References

• Anti-Bacterial Agents
• Penicillins
• Tetracycline
• Minocycline
• Penicillin G

Topics

• Animals
• Anti-Bacterial Agents (blood, pharmacokinetics, therapeutic use)
• Disease Models, Animal
• Female
• Lung (metabolism)
• Mice
• Mice, Inbred CBA
• Microbial Sensitivity Tests (methods)
• Minocycline (blood, pharmacokinetics, therapeutic use)
• Penicillin G (blood, pharmacokinetics, therapeutic use)
• Penicillins (blood, pharmacokinetics, therapeutic use)
• Pneumonia, Pneumococcal (drug therapy, metabolism)
• Streptococcus pneumoniae (drug effects)
• Tetracycline (blood, pharmacokinetics, therapeutic use)