“高剂量”甲硝唑的人体研究：一种低氧细胞的无毒放射增敏剂。
Human studies with "high dose" metronidazole: a non-toxic radiosensitizer of hypoxic cells.
作者信息
Deutsch G, Foster J L, McFadzean J A, Parnell M
出版信息
Br J Cancer. 1975 Jan;31(1):75-80. doi: 10.1038/bjc.1975.9.
Abstract
The serum concentrations of the radiosensitizer metronidazole have been determined in mice for both oral and intraperitoneal doses of the drug and these have been related to radiosensitization studies in murine tumour systems. In preliminary work before a possible clinical trail the serum metronidazole concentration/time curves have been determined in 7 patients using single doses of metronidazole of up to 15 g. The data suggest that a linear relationship exists between the metronidazole dose expressed in mg/kg and the peak serum concentration. The possibility of achieving radiosensitization of tumours in patients after tolerable doses of metronidazole is discussed in relation to enhancement ratios determined for in vitro and in vivo systems. It is concluded that predictions from in vitro systems give values that are probably too optimistic.
摘要
已测定了小鼠口服和腹腔注射放射增敏剂甲硝唑后的血清浓度，并将这些浓度与小鼠肿瘤系统中的放射增敏研究相关联。在可能进行临床试验之前的初步工作中，已对7名患者使用高达15 g的单剂量甲硝唑测定了血清甲硝唑浓度/时间曲线。数据表明，以mg/kg表示的甲硝唑剂量与血清峰值浓度之间存在线性关系。结合体外和体内系统测定的增强率，讨论了在患者耐受剂量的甲硝唑后实现肿瘤放射增敏的可能性。得出的结论是，体外系统的预测值可能过于乐观。
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Letter: "High-dose" metronidazole: a preliminary pharmacological study prior to its investigational use in clinical radiotherapy trials.信函：“高剂量”甲硝唑：在临床放射治疗试验中进行研究性使用之前的初步药理学研究。
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