Ma Xiaoqing, Zhang Ruoying, Cai Xinjun, Lang Yuying, Wang Huaichong, Li Jinmeng
Department of Pharmacy, Hangzhou Red Cross Hospital, Hangzhou, People's Republic of China.
Infect Drug Resist. 2024 Jul 15;17:3047-3056. doi: 10.2147/IDR.S468543. eCollection 2024.
As a new generation of oxazolidinone antibacterial drugs, contezolid has been shown to have comparable or even stronger activity than linezolid and has a low risk of adverse reactions such as bone marrow suppression toxicity. However, there are currently very few clinical reports and pharmacokinetic data of contezolid on the anti-tuberculosis therapy. Therefore, we report a case study of the pharmacokinetic study of contezolid in elderly patients with renal insufficiency and tuberculosis. The patient's condition improved after receiving an anti-tuberculosis regimen containing contezolid, with significant absorption of pleural effusion and lung plaques and nodules reduced. During the treatment, the patients' platelet and white blood cell levels fluctuated within normal ranges, but hemoglobin levels significantly decreased and did not recover after discontinuation of contezolid. The trough concentration of contezolid and the concentration at 2, 4, 6, and 10 h after administration were 1.27µg/mL, 3.88µg/mL, 6.32µg/mL, 8.99µg/mL, and 3.14µg/mL, respectively. The plasma concentrations of bedaquiline and cycloserine during the treatment were also monitored. This study demonstrated the efficacy and safety of contezolid in the treatment of multidrug-resistant tuberculosis and analyzed its pharmacokinetic changes in elderly patients with renal insufficiency, providing a reference for the clinical use of contezolid.
作为新一代恶唑烷酮类抗菌药物，康替唑胺已被证明具有与利奈唑胺相当甚至更强的活性，且骨髓抑制毒性等不良反应风险较低。然而，目前关于康替唑胺抗结核治疗的临床报告和药代动力学数据非常少。因此，我们报告了一例康替唑胺在老年肾功能不全合并结核病患者中的药代动力学研究案例。患者接受含康替唑胺的抗结核方案治疗后病情改善，胸腔积液明显吸收，肺部斑片及结节减少。治疗期间，患者血小板及白细胞水平在正常范围内波动，但血红蛋白水平显著下降，停用康替唑胺后未恢复。康替唑胺的谷浓度及给药后2、4、6和10小时的浓度分别为1.27µg/mL、3.88µg/mL、6.32µg/mL、8.99µg/mL和3.14µg/mL。治疗期间还监测了贝达喹啉和环丝氨酸的血药浓度。本研究证明了康替唑胺治疗耐多药结核病的有效性和安全性，并分析了其在老年肾功能不全患者中的药代动力学变化，为康替唑胺的临床应用提供参考。
