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依托咪酯在外科手术患者中的药代动力学

Pharmacokinetics of etomidate in surgical patients.

作者信息

de Ruiter G, Popescu D T, de Boer A G, Smeekens J B, Breimer D D

出版信息

Arch Int Pharmacodyn Ther. 1981 Feb;249(2):180-8.

PMID:7224720
Abstract

Eight adult surgical patients received a single i.v. injection of etomidate-base (mean 0.22 mg.kg(-1)). Venous blood samples were drawn at frequent intervals for up to 10 hr following drug administration. Plasma concentrations of etomidate were measured with a newly developed capillary gas chromatographic method. Plasma concentrations fitted best to an open three compartment pharmacokinetic model by a non-linear regression computer programme. The following mean parameters were computed: distribution half-life 2.8 + or - 2.3 min, half-life of the alpha-phase: 22.3 +or - 10.4 min and half-life of the beta-phase 208.8 + or - 64.9 min, distribution volume 3.68 + or - 0.66 l.kg(-1) (Vd area) and 2.16 l.kg(-1) (Vdss) and plasma clearance 879 + or - 135 ml.min(-1). High tissue uptake is indicated by the rapidity and the large volume of distribution. Etomidate is rapidly redistributed from the central to peripheral compartments and rapidly eliminated by metabolism.

摘要

八名成年外科手术患者接受了单次静脉注射依托咪酯碱(平均剂量为0.22毫克/千克)。给药后长达10小时内,频繁采集静脉血样。采用新开发的毛细管气相色谱法测定血浆中依托咪酯的浓度。通过非线性回归计算机程序,血浆浓度最适合开放式三室药代动力学模型。计算出以下平均参数:分布半衰期2.8±2.3分钟,α相半衰期:22.3±10.4分钟,β相半衰期208.8±64.9分钟,分布容积3.68±0.66升/千克(Vd面积)和2.16升/千克(Vdss),血浆清除率879±135毫升/分钟。快速性和大分布容积表明组织摄取较高。依托咪酯从中央室迅速重新分布到外周室,并通过代谢迅速消除。

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