新陈代谢的阿替洛尔的人。
文章的细节
-
引用
-
Reeves公关,McAinsh J,麦金托什哒,Winrow乔丹
新陈代谢的阿替洛尔的人。
Xenobiotica。1978; 8 (5): 313 - 20。doi: 10.3109 / 00498257809060956。
- PubMed ID
-
27019年(在PubMed]
- 文摘
-
1。1 -的性格和新陈代谢(4-carbamoyl [14 c] methylphenoxy) 3-isopropylaminopan-2-ol(阿替洛尔、Tenormin)研究了在人后口服给药和静脉注射的剂量。2。大约50%的口服剂量是消除尿液;阿替洛尔(约的主要放射性标记组件。90%)。粪便提取物也包含阿替洛尔基本未变,有少量的极性代谢物。阿替洛尔的胆汁排泄及其代谢物不是消除的主要路线的人。化合物的代谢是不广泛的代谢和route-dependent模式不出现复杂的位置。3所示。 Atenolol appeared to be the only major radiolabelled component in blood. 4. Oral doses of atenolol are incompletely absorbed (range 46-62%), even when formulated as a solution. 5. 1-[4-(C-Carbamoylhydroxymethyl)phenoxy]-3-isopropylaminopropan-2-ol was a minor urinary metabolite, which has only one tenth the activity of the parent compound as a beta-adrenergic blocking agent in the rat. 6. Pharmacological activity in man appears to be due to atenolol alone.