Pharmacokinetics of high-dose methylprednisolone in children.

S Ito, Y Kusunoki, T Oka, Y Ito, A Okuno, H Yoshioka
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引用次数: 22

Abstract

Disposition of methylprednisolone was characterized in 11 children receiving the high-dose therapy (26.0 mg/kg on average). After intravenous infusion, methylprednisolone hemisuccinate was rapidly converted to methylprednisolone with a half-life of about 20 min. Methylprednisolone in serum, eliminated monoexponentially in 8 patients and biexponentially in the remaining three, had the mean residence time of about 3 h, and a terminal half-life of 2.5 h. The volume of distribution at steady state, and the clearance were 1.3 liters/kg and 0.5 liters/kg/h, respectively. Although these average pharmacokinetic parameters were comparable to those determined in other studies with conventional low doses, the clearance values in our data were characterized by 5-fold interindividual difference, suggesting large variations in exposures to methylprednisolone among children on the high-dose pulse therapy.

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大剂量甲基强的松龙在儿童体内的药代动力学。
在接受高剂量治疗(平均26.0 mg/kg)的11名儿童中,甲基强的松龙的处置具有特征。经静脉输注半乙酰甲基强的松龙后迅速转化为甲基强的松龙,半衰期约为20 min。血清中甲基强的松龙8例呈单指数消除,其余3例呈双指数消除,平均停留时间约为3 h,终末半衰期为2.5 h,稳定分布体积为1.3升/kg,清除率为0.5升/kg/h。尽管这些平均药代动力学参数与其他常规低剂量研究中确定的参数相当,但我们数据中的清除率值具有5倍的个体差异,这表明在接受高剂量脉冲治疗的儿童中,甲基强的松龙暴露的差异很大。
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