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Intracellular pharmacokinetics of telithromycin, a ketolide antibiotic, in alveolar macrophages

Kohei Togami1, Sumio Chono, Toshinobu Seki

  • 1Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical University, Otaru, Hokkaido, Japan.

The Journal of Pharmacy and Pharmacology
|August 21, 2010
PubMed
Abstract

Insights

Telithromycin (TEL) accumulates significantly in alveolar macrophages, with uptake dependent on temperature and cellular mechanisms. This finding is crucial for understanding antibiotic efficacy against intracellular respiratory pathogens.

Area of Science:

  • Pharmacology
  • Microbiology
  • Cell Biology

Background:

  • Telithromycin (TEL), a ketolide antibiotic, exhibits activity against intracellular pathogens.
  • Alveolar macrophages are key sites for intracellular pathogens causing respiratory infections.
  • Understanding intracellular pharmacokinetics is vital for optimizing antibiotic therapy.

Purpose of the Study:

  • To evaluate the in vitro intracellular pharmacokinetics of telithromycin (TEL) in alveolar macrophages.
  • To investigate the factors influencing TEL accumulation within these cells.

Main Methods:

  • NR8383 cultured alveolar macrophages were exposed to 50 microm of telithromycin (TEL).
  • Incubation was performed at 37°C and 4°C to assess temperature dependence.
  • Intracellular TEL concentrations were quantified post-incubation.

Main Results:

  • Telithromycin (TEL) demonstrated high intracellular accumulation in NR8383 macrophages.
  • Intracellular accumulation of TEL was significantly temperature-dependent.
  • TEL distributed to both cytosol and organelles, with notable concentration in acidic compartments like lysosomes.

Conclusions:

  • High intracellular accumulation of telithromycin (TEL) is attributed to active transport influx and trapping in acidic organelles.
  • Findings suggest lysosomes play a role in telithromycin (TEL) sequestration within macrophages.
  • This study provides essential data for tailoring antibiotic treatments for intracellular respiratory parasitic infections.

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