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丙吡胺在近期发生至中度心力衰竭患者中的药代动力学。

Pharmacokinetics of disopyramide in patients with imminent to moderate cardiac failure.

作者信息

Landmark K, Bredesen J E, Thaulow E, Simonsen S, Amlie J P

出版信息

Eur J Clin Pharmacol. 1981 Feb;19(3):187-92. doi: 10.1007/BF00561947.

Abstract

The parmacokinetics of disopyramide (DP) in 10 patients with imminent to moderate cardiac failure has been studied and compared with the results in normal volunteers. The biological half life of rapid distribution (T1/2 alpha) and of elimination (T1/2 beta) were increased (11.1 +/- 4.4 min and 9.7 +/- 4.2 h, respectively). Total body clearance (Clt) was decreased (0.467 +/- 0.215 ml . min-1 . kg-1), and the volume of distribution (Vd) was slightly reduced (0.610 +/- 0.1361 . kg-1), probably due to the lower cardiac index. After oral administration, the time of peak serum concentration was increased (139 +/- 89 min), and the mean peak serum concentration (2.4 +/- 0.8% dose . 1-1) was also higher than reported in normal subjects. Comparison of the areas under the concentration versus time curves after intravenous and oral administration (AUC i. v. and AUC oral) showed that DP was almost completely absorbed, its bioavailability being 97.5 +/- 15.0%.

摘要

对10例重度至中度心力衰竭患者的丙吡胺(DP)药代动力学进行了研究,并与正常志愿者的结果进行了比较。快速分布生物半衰期(T1/2α)和消除生物半衰期(T1/2β)均延长(分别为11.1±4.4分钟和9.7±4.2小时)。总体清除率(Clt)降低(0.467±0.215毫升·分钟-1·千克-1),分布容积(Vd)略有减少(0.610±0.136升·千克-1),这可能是由于心脏指数较低所致。口服给药后,血清浓度达峰时间延长(139±89分钟),平均血清峰浓度(2.4±0.8%剂量·升-1)也高于正常受试者的报道。静脉注射和口服给药后浓度-时间曲线下面积(AUCiv和AUC口服)的比较表明,DP几乎完全吸收,其生物利用度为97.5±15.0%。

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