Urtasun R C, Chapman J D, Band P, Rabin H R, Fryer C G, Sturmwind J
Radiology. 1975 Oct;117(1):129-33. doi: 10.1148/117.1.129.
Metronidazole was administered orally to 25 patients and its maximum concentration in blood and tumor tissues, its ability to cross the blood/brain barrier and concentrate in the cerebrospinal fluid and brain tumor tissue, its immediate and long-term toxicity, and its enhancement of irradiation in normal tissue were studied. Maximum blood concentrations of 700-1,200 muM (120-220 mug/ml) were obtained at four hours with doses of 6 g/m2. Moderate and transient nausea and vomiting were the only immediate signs of toxicity. No long-term toxicity was found up to 18 months after administration of the drug. These data indicate that metronidazole can feasibly be adminstered in clinical trials of fractionated radiotherapy using dosages ranging from 9.5 to 11 g three times a week for three to four weeks.
对25名患者口服甲硝唑，并研究了其在血液和肿瘤组织中的最大浓度、穿过血脑屏障并在脑脊液和脑肿瘤组织中浓缩的能力、即时和长期毒性以及其对正常组织辐射的增强作用。剂量为6 g/m²时，4小时后血液中最大浓度达到700 - 1200 μM（120 - 220 μg/ml）。中度和短暂的恶心和呕吐是唯一的即时毒性迹象。给药后长达18个月未发现长期毒性。这些数据表明，在每周三次、持续三至四周、剂量范围为9.5至11 g的分次放射治疗临床试验中，甲硝唑可以切实可行地给药。
