Prasad V K, Corlett S A, Abaasi K, Heney D, Lewis I, Chrystyn H
Postgraduate Studies in Pharmaceutical Technology, School of Pharmacy, University of Bradford, UK.
Cancer Chemother Pharmacol. 1994;34(5):447-9. doi: 10.1007/BF00685573.
Ifosfamide, like other oxazaphosphorine drugs, is chiral and there is some evidence, mainly from animal studies, of stereo-selective differences in metabolism, excretion and cytotoxic activity between the two enantiomers. The pharmacokinetics of racemic ifosfamide (RAC-IFO), R-ifosfamide (R-IFO) and S-ifosfamide (S-IFO) were studied in five children who received intravenous therapy with racemic ifosfamide on 3 consecutive days. The clearance of S-IFO was greater than that of R-IFO. The clearance value at the end of the infusion was faster than the respective rate measured at the beginning of or during the ifosfamide regimens in four children and, therefore, suggests autoinduction of elimination of both enantiomers.
异环磷酰胺与其他氮杂磷酰胺类药物一样具有手性，主要来自动物研究的一些证据表明，两种对映体在代谢、排泄和细胞毒性活性方面存在立体选择性差异。在五名连续三天接受消旋异环磷酰胺静脉治疗的儿童中，研究了消旋异环磷酰胺（RAC-IFO）、R-异环磷酰胺（R-IFO）和S-异环磷酰胺（S-IFO）的药代动力学。S-IFO的清除率高于R-IFO。在四名儿童中，输注结束时的清除率值比异环磷酰胺治疗开始时或治疗期间测得的各自速率更快，因此表明两种对映体的消除存在自身诱导作用。
