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环磷酰胺属于烃化剂,是氮芥的衍生物。口服吸收良好,服药后经1小时血药浓度达峰值、t1/2约5～7小时,经别嘌呤醇作前处理可延长t1/2。用~3H标记的环磷酰胺静注后,药物本身在血中停留不太久,迅速分布到各组织中。环磷酰胺尚可透过血脑屏障。脏器中以肝脏分布较多。肿瘤组织的药物浓度比相应的正常组织为高。在体外几无烃基化活性,进入人体后在肝中受到微粒体混合功能酶催化,在细胞色素P—450等存在下,经氧化、裂环,生成具有活化作用型的醛磷酰胺。其代谢途径如下图所示。图:环磷酰胺的代谢途径
Cyclophosphamide belongs to the class of alkylating agents and is a derivative of nitrogen mustard. Oral absorption of good, after taking the drug peak concentration 1 hour, t1 / 2 about 5 to 7 hours, after allopurinol pretreatment can be extended t1 / 2. ~ 3H labeled cyclophosphamide after intravenous injection, the drug itself stays in the blood not too long, quickly distributed to various tissues. Cyclophosphamide is still permeable to the blood-brain barrier. Organ in the liver to distribute more. Tumor tissue drug concentrations higher than the corresponding normal tissue. In vitro few hydrocarbon-based activity into the human body in the liver by microsomal mixed function enzyme catalysis, in the presence of cytochrome P-450 and so on, by oxidation, split ring, with the formation of activation-type aldosterone. The metabolic pathway as shown below. Figure: cyclophosphamide metabolic pathway