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[New pharmacologic approaches to macrolides: example of roxithromycin]
1Service de Microbiologie, CHU Bichat-Claude Bernard, Paris.
Presse Medicale (Paris, France : 1983)
|December 14, 1996
Summary
Newer macrolide antibiotics like roxithromycin offer improved pharmacokinetic properties, leading to higher tissue and intracellular drug concentrations. These advancements suggest potential clinical efficacy, even with limited pharmacodynamic data.
Area of Science:
- Pharmacology
- Microbiology
- Infectious Diseases
Background:
- Macrolides represent a foundational antibiotic class with extensive clinical application.
- Recent advancements focus on enhancing pharmacokinetic profiles of macrolide derivatives.
- Erythromycin serves as the parent compound for newer macrolide development.
Purpose of the Study:
- To evaluate the pharmacokinetic advantages of newer macrolide antibiotics.
- To assess the tissue and intracellular penetration of macrolides.
- To explore the potential clinical efficacy based on pharmacokinetic data.
Main Methods:
- Comparative analysis of pharmacokinetic properties of macrolides.
- Measurement of drug concentrations in serum, tissues, interstitial fluid, and macrophages.
- Evaluation of inhibitory quotient for tissue and interstitial fluid concentrations.
Main Results:
- Newer macrolides exhibit increased half-lives and prolonged tissue persistence compared to erythromycin.
- Roxithromycin demonstrates high peak serum concentrations and elevated levels in interstitial fluid and intracellularly.
- High inhibitory quotients were observed for tissue and interstitial fluid concentrations.
Conclusions:
- Enhanced pharmacokinetic properties of newer macrolides, including roxithromycin, offer significant clinical advantages.
- High drug concentrations in tissues and intracellularly suggest potent antimicrobial activity.
- Further pharmacodynamic studies are warranted, but current data indicate promising clinical efficacy for advanced macrolides.