Wang S X, Sutfin T A, Regårdh C G
Astra Hässle AB, Mölndal, Sweden.
Eur J Drug Metab Pharmacokinet. 1992 Oct-Dec;17(4):263-8. doi: 10.1007/BF03190158.
Felodipine, a vasoselective dihydropyridine calcium antagonist, has been given i.v. (0.2 mumol/kg) to anaesthetized and conscious male rats. There was no effect of pentobarbital anaesthesia on bile flow over a 6 h observation period. Felodipine increased the 6 h recovery of bile by approximately 25% in the conscious rat but in the anaesthetized rat there was a 20% decrease in bile flow following i.v. felodipine. A positive effect of Na-taurocholate infusion (1 mumol/min/100 g body weight) on bile flow in conscious rats was reinforced by concomitant felodipine dosing. Accumulated 6 h recoveries were 2.32 +/- 0.80 g/100 g body weight (control), 3.09 +/- 0.91 g/100 g body weight (taurocholate) and 5.00 +/- 0.80 g/100 g body weight. (taurocholate plus felodipine). The excretion of felodipine in the bile was significantly reduced during anaesthesia and during infusion of 2% bovine serum albumin (0.01 ml/min/100 g body weight) to conscious rats.
非洛地平是一种血管选择性二氢吡啶类钙拮抗剂，已对麻醉和清醒雄性大鼠静脉注射（0.2 μmol/kg）。在6小时的观察期内，戊巴比妥麻醉对胆汁流量没有影响。非洛地平使清醒大鼠胆汁的6小时恢复量增加约25%，但在麻醉大鼠中，静脉注射非洛地平后胆汁流量下降了20%。同时给予非洛地平可增强牛磺胆酸钠输注（1 μmol/分钟/100克体重）对清醒大鼠胆汁流量的积极作用。6小时的累积恢复量分别为2.32±0.80克/100克体重（对照组）、3.09±0.91克/100克体重（牛磺胆酸钠组）和5.00±0.80克/100克体重（牛磺胆酸钠加非洛地平组）。麻醉期间以及向清醒大鼠输注2%牛血清白蛋白（0.01毫升/分钟/100克体重）期间，非洛地平在胆汁中的排泄显著减少。
