异丙肾上腺素在人和犬体内经气雾剂及直接支气管内给药后的代谢情况。
Metabolism of isoprenaline after aerosol and direct intrabronchial administration in man and dog.
作者信息
Blackwell E W, Briant R H, Conolly M E, Davies D S, Dollery C T
出版信息
Br J Pharmacol. 1974 Apr;50(4):587-91. doi: 10.1111/j.1476-5381.1974.tb08593.x.
Abstract
1 Administration of isoprenaline by aerosol inhalation to man results in over 80% being metabolized to the sulphate conjugate.2 The majority of an inhaled dose is probably swallowed since the metabolic pattern resembles that after an oral dose.3 Isoprenaline, administered in aqueous solution directly into the bronchial tree in both man and dog, is rapidly O-methylated to 3-O-methyl isoprenaline, which is subsequently conjugated with sulphate.4 3-O-Methylation is the main metabolic pathway for the small part of an inhaled dose which does enter the bronchial tree.
摘要
对人体进行异丙肾上腺素气雾剂吸入给药后，超过80%的药物会代谢为硫酸酯共轭物。
吸入剂量的大部分可能会被吞咽，因为其代谢模式与口服给药后相似。
在人和狗身上，将异丙肾上腺素以水溶液形式直接注入支气管树后，它会迅速O-甲基化生成3-O-甲基异丙肾上腺素，随后与硫酸盐结合。
3-O-甲基化是吸入剂量中进入支气管树的一小部分药物的主要代谢途径。
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