单次静脉注射和持续静脉输注后，二氢麦角胺在比格犬体内的药代动力学。

The pharmacokinetics of dihydroergotamine in the beagle dog after a single intravenous injection and after a continuous intravenous infusion.

作者信息

Kanto J, Allonen H, Kleimola T, Mäntylä R

出版信息

Acta Pharmacol Toxicol (Copenh). 1980 Apr;46(4):241-4. doi: 10.1111/j.1600-0773.1980.tb02448.x.

DOI:10.1111/j.1600-0773.1980.tb02448.x

Abstract

The pharmacokinetics of dihydroergotamine (DHE) was studied in 6 beagles after a single 2.0 mg intravenous dose and after a continuous intravenous infusion (dose 2.0 mg, infusion time 51 min.=2.8-3.5 micrograms/min./kg). The concentrations of DHE in the plasma during 6 hours were determined by a radioimmunoassay. The mean alpha-phase T1/2 was 0.92 min. and 5.93 min., the mean beta-phase T1/2 was 104.42 min. and 115.79 min., and the mean plasma clearance value 202.88 ml/min. and 234.79 ml/min. after a single intravenous injection a continuous infusion administration, respectively. Similarly, the Vdc - values were 0.121/kg and significantly from each other. The simulated concentrations of DHE in the peripheral compartment increased rapidly explaining its fast effect on the vasculature in clinical use.

摘要

在6只比格犬中研究了双氢麦角胺（DHE）的药代动力学，静脉注射单次剂量2.0mg后以及连续静脉输注（剂量2.0mg，输注时间51分钟 = 2.8 - 3.5微克/分钟/千克）后进行研究。通过放射免疫分析法测定6小时内血浆中DHE的浓度。单次静脉注射和连续输注给药后，平均α相半衰期分别为0.92分钟和5.93分钟，平均β相半衰期分别为104.42分钟和115.79分钟，平均血浆清除率值分别为202.88毫升/分钟和234.79毫升/分钟。同样，中央室容积值分别为0.121/千克，且彼此有显著差异。外周室中DHE的模拟浓度迅速增加，这解释了其在临床应用中对脉管系统的快速作用。