Monitoring Salivary Concentrations of Tedizolid and Linezolid Using Rats.

IF 1.9 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Yuki Inoue, Yuki Sato, Hitoshi Kashiwagi, Shunsuke Nashimoto, Mitsuru Sugawara, Yoh Takekuma
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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, n = 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, p < 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.

Abstract Image

泰地唑胺和利奈唑胺大鼠唾液浓度监测。
背景与目的:治疗性药物监测(TDM)是管理使用利奈唑胺患者的有效工具。使用唾液治疗TDM比使用血浆有潜在的优势;然而,只有少数报告比较了唾液和血浆中的药物浓度。此外,尚未见类似利奈唑胺的恶唑烷类抗生素tedizolid唾液浓度的报道。本研究比较了大鼠下颌骨唾液中泰地唑胺和利奈唑胺的浓度与血浆中的浓度。方法:大鼠尾静脉给药Tedizolid (10 mg/kg, n = 6)和linezolid (12 mg/kg, n = 5)。在给药后8小时内采集下颌下唾液和血浆样本,检测泰地唑胺和利奈唑胺的浓度。结果:唾液和血浆中tedizolid浓度(r = 0.964, p max)分别为0.99±0.08µg/mL和14.46±1.71µg/mL。利奈唑胺在唾液中的Cmax为8.01±1.42µg/mL,在血浆中的Cmax为13.00±1.90µg/mL。结果显示,大鼠唾液浓度比为0.0513±0.0080,利奈唑胺浓度比为0.6341±0.0339。结论:考虑唾液与血浆中泰地唑胺和利奈唑胺浓度的相关性,以及唾液的特点,本研究结果提示唾液是TDM的有用基质。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
3.70
自引率
0.00%
发文量
64
审稿时长
>12 weeks
期刊介绍: Hepatology International is a peer-reviewed journal featuring articles written by clinicians, clinical researchers and basic scientists is dedicated to research and patient care issues in hepatology. This journal focuses mainly on new and emerging diagnostic and treatment options, protocols and molecular and cellular basis of disease pathogenesis, new technologies, in liver and biliary sciences. Hepatology International publishes original research articles related to clinical care and basic research; review articles; consensus guidelines for diagnosis and treatment; invited editorials, and controversies in contemporary issues. The journal does not publish case reports.
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