米索硝唑及其主要代谢物在放射治疗中的动力学研究

Kinetic aspects of misonidazole and its major metabolite in radiotherapy.

作者信息

Meering P G, Gonzalez D G, Maes R A, van Peperzeel H A

出版信息

Hum Toxicol. 1985 Jul;4(4):425-34. doi: 10.1177/096032718500400409.

Abstract

Oral doses of misonidazole between 0.75 and 1.3 g/m2 were administered during 3-5 days per week to 21 patients with various malignancies. Mean plasma levels of misonidazole and desmethylmisonidazole at the times of radiotherapy were in the range 20-50 and 2-12 mg/l respectively. Slight accumulation of misonidazole and desmethylmisonidazole in plasma was observed with a dosage interval of 24 h. In patients with anticonvulsant comedication plasma elimination half-lives of misonidazole of 4.1-8.9 h were found. Observed side-effects were nausea and vomiting (9%), exanthema or rashes (14%) and mild peripheral neuropathy (9%).

摘要

每周3至5天，给21例患有各种恶性肿瘤的患者口服米索硝唑，剂量为0.75至1.3 g/m²。放疗时米索硝唑和去甲基米索硝唑的平均血浆水平分别在20 - 50 mg/l和2 - 12 mg/l范围内。当给药间隔为24小时时，观察到米索硝唑和去甲基米索硝唑在血浆中有轻微蓄积。在同时服用抗惊厥药物的患者中，发现米索硝唑的血浆消除半衰期为4.1至8.9小时。观察到的副作用有恶心和呕吐（9%）、皮疹（14%）和轻度周围神经病变（9%）。