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环孢素A不同给药途径对骨髓移植患者血药浓度的影响。

Effects of different routes of cyclosporin A administration on blood levels in patients undergoing bone marrow transplantation.

作者信息

Capone D, De Marino V, Fontana R, Notaro R, De Marino V, Pisanti N

机构信息

Department of Neurosciences, School of Medicine, Federico II University, Naples, Italy.

出版信息

Bone Marrow Transplant. 1997 Feb;19(4):369-72. doi: 10.1038/sj.bmt.1700660.

Abstract

This follow-up study has been carried out on 15 bone marrow transplant recipients treated intravenously with cyclosporin A (CsA) as a bolus (1.25-2.5 mg/kg/12 h) or by continuous infusion (1-3 mg/kg/24 h) from -2 until the 21st day after transplantation. All patients were subsequently treated with CsA orally at a starting dose of 6.25 mg/kg/12 h; this starting dose was then adjusted on the basis of CsA blood levels until the 60th day after transplantation, followed by progressive reduction and withdrawal within 6-12 months. In whole blood, trough levels of polyclonal (P) and monoclonal (M) CsA were monitored by a FPIA method and the polyclonal/monoclonal ratio (P/M) was calculated. This ratio was lower during CsA administration as a bolus or by continuous infusion than during oral administration; the decrease was statistically significant. This difference was probably due to first-pass metabolism which occurs in the liver and gut after oral administration.

摘要

本随访研究对15例骨髓移植受者进行,这些受者在移植后第 -2天至第21天接受静脉注射环孢素A(CsA),给药方式为大剂量推注(1.25 - 2.5 mg/kg/12小时)或持续输注(1 - 3 mg/kg/24小时)。所有患者随后口服CsA,起始剂量为6.25 mg/kg/12小时;该起始剂量随后根据CsA血药浓度进行调整,直至移植后第60天,之后在6 - 12个月内逐渐减量并停药。采用荧光偏振免疫分析(FPIA)法监测全血中环孢素A的多克隆(P)和单克隆(M)谷浓度,并计算多克隆/单克隆比值(P/M)。与口服给药期间相比,静脉大剂量推注或持续输注CsA期间该比值较低;差异具有统计学意义。这种差异可能是由于口服给药后在肝脏和肠道发生的首过代谢所致。

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