Thompson F D, Joekes A M, Foulkes D M
Br Med J. 1972 May 20;2(5811):434-6. doi: 10.1136/bmj.2.5811.434.
The pharmacodynamics of propranolol were studied in patients with renal functional impairment. (14)C-labelled propranolol was given either intravenously or by mouth and the disappearance rates of propranolol, 4-hydroxypropranolol, and total radioactive metabolites measured. The renal clearance of total radioactive compounds is directly related to renal function. The half-life of total radioactivity is greatly lengthened in the presence of severe renal failure while the half-lives of the pharmacologically active propranolol and 4-hydroxymetabolite are slightly reduced. There is a suggestion that the absorption of propranolol is delayed in renal failure. No known pharmacological action or side effects from the other metabolic products of propranolol have been recognized. There is still too little well-documented evidence concerning the beta-blocking activity of the unidentified major metabolites of propranolol to suggest any alteration in the dosage regimen used in renal failure.
对肾功能损害患者进行了普萘洛尔的药效学研究。静脉注射或口服给予(14)C标记的普萘洛尔,并测定普萘洛尔、4-羟基普萘洛尔和总放射性代谢物的消失率。总放射性化合物的肾清除率与肾功能直接相关。在严重肾衰竭时,总放射性的半衰期大大延长,而具有药理活性的普萘洛尔和4-羟基代谢物的半衰期略有缩短。有迹象表明肾衰竭时普萘洛尔的吸收延迟。尚未认识到普萘洛尔其他代谢产物有已知的药理作用或副作用。关于普萘洛尔未鉴定的主要代谢物的β受体阻断活性,仍有太少充分记录的证据,无法建议改变肾衰竭时使用的给药方案。