去甲基米索硝唑在人体肿瘤组织和脑脊液中的浓度。
The concentration of desmethylmisonidazole in human tumours and in cerebrospinal fluid.
作者信息
Dische S, Saunders M I, Riley P J, Hauck J, Bennett M H, Stratford M R, Minchinton A I
出版信息
Br J Cancer. 1981 Mar;43(3):344-9. doi: 10.1038/bjc.1981.54.
The concentration of desmethylmisonidazole (DESMISO) was determined in 60 biopsy samples taken from 13 human tumours and in cerebrospinal fluid (CSF) from 8 patients after oral administration. In comparison with misonidazole (MISO), peak concentrations in plasma were reached at earlier times and half-lives were shorter, so that the area under the curve of plasma concentration with time (AUC) was reduced by 45%; the AUC of CSF concentration with time was reduced by 67%. Between 1 and 2 h after administration of DESMISO, concentrations in tumours were generally 85-90% of those of MISO estimated approximately 4 h after it was given. The two drugs when tested in equimolar concentrations have been found in laboratory experiment to be equally potent as hypoxic cell radiosensitizers. Recognizing the lower mol. wt of DESMISO and the trend to higher concentrations in the more necrotic areas of the tumours studied equal doses by weight of the two drugs given orally may give equal radiosensitization of hypoxic cells in human tumours.
在口服给药后，测定了取自13例人类肿瘤的60份活检样本以及8例患者脑脊液（CSF）中的去甲基米索硝唑（DESMISO）浓度。与米索硝唑（MISO）相比，血浆中的峰值浓度在更早时间达到，且半衰期更短，因此血浆浓度随时间变化的曲线下面积（AUC）降低了45%；脑脊液浓度随时间变化的AUC降低了67%。在给予DESMISO后1至2小时，肿瘤中的浓度通常为给予MISO约4小时后估计浓度的85 - 90%。在实验室实验中发现，当以等摩尔浓度进行测试时，这两种药物作为乏氧细胞放射增敏剂的效力相同。鉴于DESMISO的分子量较低，且在所研究肿瘤的坏死程度更高的区域有浓度升高的趋势，口服给予两种药物等重量的剂量可能会使人类肿瘤中的乏氧细胞获得同等的放射增敏效果。
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