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儿童中环磷酰胺的血浆半衰期及尿排泄情况。

PLasma half-life and urinary excretion of cyclophosphamide in children.

作者信息

Sladek N E, Priest J, Doeden D, Mirocha C J, Pathre S, Krivit W

出版信息

Cancer Treat Rep. 1980 Oct-Nov;64(10-11):1061-6.

PMID:7459891
Abstract

The plasma half-life and urinary excretion of cyclophosphamide were determined in 13 children who had various malignancies and/or who were being prepared for bone marrow transplantation. Disappearance from the plasma following iv infusion over a 1-2 hour period was first-order. Urinary excretion was maximal during the first 8 hours after administration and was essentially complete in 24 hours. The plasma half-life in children not receiving known inducers of hepatic microsomal mixed-function oxygenase activity or cyclophosphamide in the 3-week period prior to each determination ranged from 145 to 390 minutes. These values are lower than those ordinarily found in adult patients. The fraction of the total dose excreted in the urine as the parent compound ranged from 4% to 27%. Repeated administration of cyclophosphamide at approximately 30-60 day intervals did not appear to alter its plasma half-life but did appear to increase its urinary excretion. Daily administration of cyclophosphamide (approximately 50 mg/kg/day x 2 or 4) significantly decreased its plasma half-life and urinary excretion suggesting that it may reversibly induce its own metabolism.

摘要

对13名患有各种恶性肿瘤和/或正准备进行骨髓移植的儿童测定了环磷酰胺的血浆半衰期和尿排泄情况。静脉输注1 - 2小时后,血浆中环磷酰胺的消除呈一级动力学。给药后最初8小时尿排泄量最大,24小时基本排泄完毕。在每次测定前3周内未接受已知肝微粒体混合功能氧化酶活性诱导剂或环磷酰胺的儿童,其血浆半衰期为145至390分钟。这些值低于成年患者通常的数值。以母体化合物形式经尿液排泄的总剂量分数为4%至27%。以约30 - 60天的间隔重复给予环磷酰胺似乎并未改变其血浆半衰期,但确实增加了其尿排泄量。每日给予环磷酰胺(约50mg/kg/天×2或4)显著降低了其血浆半衰期和尿排泄量,提示它可能可逆地诱导自身代谢。

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