Carruthers S G, Dujovne C A
Clin Pharmacol Ther. 1980 Feb;27(2):184-7. doi: 10.1038/clpt.1980.28.
The effects of oral cholestyramine 4 gm 8 times daily and spironolactone 300 mg daily, given independently and in combination, on the elimination rate of digitoxin were studied in 6 healthy subjects pretreated with 0.1 or 0.15 mg oral digitoxin daily for 30 days before each intervention. The mean pretreatment digitoxin concentrations for the group ranged from 21 +/- 2.9 (SD) ng/ml to 28.5 +/- 6.9 ng/ml. The mean control digitoxin half-life (t 1/2) was reduced from 141.6 to 84.4 by treatment with cholestyramine alone. Treatment with spironolactone alone prolonged the mean digitoxin t 1/2 to 192.2 hr. The mean digitoxin t 1/2 after both active drugs was intermediate at 102.9 hr. Spironolactone did not fulfill the expectation from animal studies that it would enhance the clearance of digitoxin by cholestyramine. The prolongation of digitoxin elimination after spironolactone may contraindicate this drug in digitoxin intoxication.
在6名健康受试者中研究了每日8次口服4克消胆胺和每日口服300毫克螺内酯单独及联合使用对洋地黄毒苷消除率的影响。在每次干预前,受试者每天口服0.1或0.15毫克洋地黄毒苷,持续30天进行预处理。该组预处理洋地黄毒苷浓度的平均值范围为21±2.9(标准差)纳克/毫升至28.5±6.9纳克/毫升。单独使用消胆胺治疗可使洋地黄毒苷平均对照半衰期(t1/2)从141.6小时降至84.4小时。单独使用螺内酯治疗可使洋地黄毒苷平均t1/2延长至192.2小时。两种活性药物联合使用后,洋地黄毒苷平均t1/2处于中间水平,为102.9小时。螺内酯未达到动物研究中预期的它会增强消胆胺对洋地黄毒苷清除率的效果。螺内酯后洋地黄毒苷消除时间的延长可能表明在洋地黄毒苷中毒时不宜使用该药。