Skibińska L, Daszkiewicz P, Michalewska D, Radwańska U
Department of Physical Chemistry, Medical Academy, Poznań, Poland.
Pol J Pharmacol Pharm. 1988 Mar-Apr;40(2):135-43.
Pharmacokinetics of the intrathecally given methotrexate (MTX) for protection of the central nervous system was studied in 17 children with acute lymphoblastic leukemia (ALL). MTX plasma levels were assayed by enzymatic inhibition. The first order rate constants for the absorption, distribution and elimination phases were calculated on the base of an open one or two compartment body model. The efflux of MTX from the cerebrospinal fluid compartment is sufficiently significant to worsen myelosuppression, especially in 3-7 year old children. Therefore MTX cannot be administered intrathecally to such young children unless the complete remission in the number of circulating granulocytes is achieved according to general rules.
对17例急性淋巴细胞白血病（ALL）患儿鞘内注射甲氨蝶呤（MTX）以保护中枢神经系统的药代动力学进行了研究。采用酶抑制法测定MTX血浆水平。根据开放的一室或二室体内模型计算吸收、分布和消除阶段的一级速率常数。MTX从脑脊液腔室的流出量足以显著加重骨髓抑制，尤其是在3 - 7岁的儿童中。因此，除非按照一般规则使循环粒细胞数量完全缓解，否则不能对这类幼儿进行鞘内注射MTX。
