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Erschienen in: European Journal of Drug Metabolism and Pharmacokinetics 4/2023

27.06.2023 | Original Research Article

Monitoring Salivary Concentrations of Tedizolid and Linezolid Using Rats

verfasst von: Yuki Inoue, Yuki Sato, Hitoshi Kashiwagi, Shunsuke Nashimoto, Mitsuru Sugawara, Yoh Takekuma

Erschienen in: European Journal of Drug Metabolism and Pharmacokinetics | Ausgabe 4/2023

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Abstract

Background and Objective

Therapeutic drug monitoring (TDM) is an effective tool for the management of patients who are administered linezolid. The use of saliva for TDM has potential advantages over the use of plasma; however, only a few reports have compared drug concentrations in the saliva and plasma. Moreover, there are no reports on the salivary concentration of tedizolid, an oxazolidinone antibiotic similar to linezolid. In the present study, the concentrations of tedizolid and linezolid in rat submandibular saliva were compared with those measured in the plasma.

Methods

Tedizolid (10 mg/kg, n = 6) and linezolid (12 mg/kg, = 5) were administered via the rat tail vein. Submandibular saliva and plasma samples were collected for up to 8 h after the initiation of drug administration, and assayed for the concentrations of tedizolid and linezolid.

Results

A strong correlation was found between the saliva and plasma concentrations of tedizolid (r = 0.964, < 0.001) and linezolid (r = 0.936, p < 0.001). The value of tedizolid maximum concentration of drug (Cmax) was 0.99 ± 0.08 µg/mL in the saliva and 14.46 ± 1.71 µg/mL in the plasma. Meanwhile, the Cmax of linezolid was 8.01 ± 1.42 µg/mL in the saliva and 13.00 ± 1.90 µg/mL in the plasma. According to these results, the saliva/plasma concentration ratios of tedizolid and linezolid in rats were 0.0513 ± 0.0080 and 0.6341 ± 0.0339, respectively.

Conclusions

Considering the correlation between saliva and plasma concentrations of tedizolid and linezolid, as well as the characteristics of saliva, the results of this study suggest that saliva is a useful matrix for TDM.
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Metadaten
Titel
Monitoring Salivary Concentrations of Tedizolid and Linezolid Using Rats
verfasst von
Yuki Inoue
Yuki Sato
Hitoshi Kashiwagi
Shunsuke Nashimoto
Mitsuru Sugawara
Yoh Takekuma
Publikationsdatum
27.06.2023
Verlag
Springer International Publishing
Erschienen in
European Journal of Drug Metabolism and Pharmacokinetics / Ausgabe 4/2023
Print ISSN: 0378-7966
Elektronische ISSN: 2107-0180
DOI
https://doi.org/10.1007/s13318-023-00836-6

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