Negishi Daisuke, Mitsumatsu Okimichi, Matsumura Takahiro, Mitsumatsu Hiromi, Makiguchi Miaki, Shimizu Makiko, Yamazaki Hiroshi
Showa Pharmaceutical University, 3-3165 Higashi-tamagawa Gakuen, Machida, Tokyo, 194-8543, Japan.
Kamakura Hospital, 1-8 Hase 3-chome, Kamakura, Kanagawa, 248-0016, Japan.
J Pharm Health Care Sci. 2022 Jul 1;8(1):16. doi: 10.1186/s40780-022-00248-9.
Linezolid is a new oxazolidinone antibiotic used for infections caused by methicillin-resistant Staphylococcus and other species.
Two cases of knee osteoarthritis with acute infection were successfully treated using linezolid. The plasma and synovial fluid concentrations of linezolid in two patients [women aged 69 and 73 years (cases 1 and 2)] with knee osteoarthritis infected with Staphylococcus aureus were measured after they were administered 600 mg twice daily by intravenous infusion. The plasma linezolid concentrations during knee surgery in case 1 at day 5 and in case 2 at day 2 were 19.6 and 15.6 μg/mL, respectively. The synovial fluid concentrations of linezolid in samples taken during surgery in case 1 and case 2 were 14.9 and 17.0 μg/mL, respectively; these values corresponded to ratios of synovial fluid/plasma of 76 and 109%. Possible metabolite 2-hydroxylated linezolid potentially mediated by cytochrome P450 2 J2 was not detected in the plasma or synovial fluid samples under the current clinical setting after multiple doses.
These results implied nearly equivalent concentrations of linezolid in plasma and synovial fluid of clinical patients with knee osteoarthritis acutely infected with Staphylococcus aureus.
利奈唑胺是一种新型恶唑烷酮类抗生素，用于治疗耐甲氧西林金黄色葡萄球菌及其他菌种引起的感染。
两例膝关节骨关节炎合并急性感染患者使用利奈唑胺治疗成功。对两名感染金黄色葡萄球菌的膝关节骨关节炎女性患者（69岁和73岁，病例1和病例2）每日两次静脉输注600mg利奈唑胺后，测定其血浆和滑液中的利奈唑胺浓度。病例1在第5天膝关节手术时及病例2在第2天膝关节手术时的血浆利奈唑胺浓度分别为19.6μg/mL和15.6μg/mL。病例1和病例2手术时采集的滑液样本中利奈唑胺浓度分别为14.9μg/mL和17.0μg/mL；这些值对应的滑液/血浆比值分别为76%和109%。在当前临床用药情况下，多次给药后血浆和滑液样本中未检测到可能由细胞色素P450 2J2介导的代谢产物2-羟基利奈唑胺。
这些结果表明，急性感染金黄色葡萄球菌的膝关节骨关节炎临床患者血浆和滑液中的利奈唑胺浓度几乎相当。
