甲基麦角新碱（甲基麦角新碱）在兔和人体中的药代动力学。

Pharmacokinetics of methylergometrine (methylergonovine) in the rabbit and man.

作者信息

Mäntylä R, Kleimola T, Kanto J

出版信息

Acta Pharmacol Toxicol (Copenh). 1977 May;40(5):561-9.

Abstract

Methylergometrine concentrations in human and rabbit plasma were determined by a new radioimmunoassay after a single intravenous injection (0.2 mg in man and 0.05, 0.1 and 0.2 mg/kg in rabbits). Both in man and in the rabbit methylergometrine disappeared quickly from the plasma with a mean T1/2alpha of 1.8 and 1.2-1.7 min. respectively. Similarly, the T1/2beta-values were 32.1 and 27.3-93.2 min. tthe mean maximal response in the rabbit uterus in situ after 0.05, 0.1 and 0.2 mg/kg intravenously dose was found at 40 sec., 26 sec., and 26 sec. after the drug administration, respectively, and the dose response curve was quite steep. A significant correlation was found between the dose and response.

摘要

单次静脉注射后（人类注射0.2毫克，兔子分别注射0.05、0.1和0.2毫克/千克），采用一种新的放射免疫分析法测定了人类和兔子血浆中的甲基麦角新碱浓度。在人类和兔子体内，甲基麦角新碱均迅速从血浆中消失，平均α半衰期分别为1.8分钟和1.2 - 1.7分钟。同样，β半衰期值分别为32.1分钟和27.3 - 93.2分钟。静脉注射0.05、0.1和0.2毫克/千克后，兔子原位子宫的平均最大反应分别在给药后40秒、26秒和26秒出现，且剂量反应曲线相当陡峭。剂量与反应之间存在显著相关性。