| Intracellular pharmacokinetics of telithromycin, a ketolide antibiotic, in alveolar macrophages. | |
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MedLine Citation:
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PMID: 20723001 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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OBJECTIVES: Telithromycin, a ketolide antibiotic, has an antibacterial range that covers intracellular parasitic pathogens that survive or multiply intracellularly in alveolar macrophages. The intracellular pharmacokinetics of TEL in alveolar macrophages was evaluated in vitro. METHODS: Telithromycin (50 microm) was applied to NR8383 as cultured alveolar macrophages, followed by incubation at 37 degrees C or 4 degrees C. After incubation, the amount of telithromycin in cells was determined. KEY FINDINGS: Telithromycin exhibited high accumulation in NR8383 and its intracellular accumulation was temperature dependent. Also, telithromycin distributed to the organelles and cytosol in NR8383 and, in particular, it accumulated in the acidic organelle compartments. CONCLUSIONS: This study suggests that the high accumulation of telithromycin in NR8383 is due to its high influx via active transport systems and trapping in acidic organelles, such as lysosomes. Moreover, this study provides important information for optimizing the treatment of respiratory intracellular parasitic infections based on the intracellular pharmacokinetics of antibiotics and parasitic sites. |
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Authors:
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Kohei Togami; Sumio Chono; Toshinobu Seki; Kazuhiro Morimoto |
Publication Detail:
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Type: In Vitro; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: The Journal of pharmacy and pharmacology Volume: 62 ISSN: 2042-7158 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2010 Jan |
Date Detail:
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Created Date: 2010-08-20 Completed Date: 2010-12-14 Revised Date: 2011-09-13 |
Medline Journal Info:
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Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 71-5 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical University, Otaru, Hokkaido, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Bacterial Agents / pharmacokinetics* Biological Transport, Active Cells, Cultured Cytosol / metabolism Ketolides / pharmacokinetics* Macrophages, Alveolar / metabolism* Organelles / metabolism Rats Rats, Sprague-Dawley Temperature |
| Chemical | |
Reg. No./Substance:
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0/Anti-Bacterial Agents; 0/Ketolides; 0/telithromycin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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