Das G P, Talmers R N, Weissler A M
Clin Pharmacol Ther. 1977 Sep;22(3):280-5. doi: 10.1002/cpt1977223280.
The positive inotropic effects and serum glycoside levels following intravenous and oral administration of betamethyl digoxin (BMD) were measured and compared with those of digoxin in normal adults. The cardiac inotropy was assessed noninvasively in the abbreviation of the electromechanical systolic index (QS2I) obtained by serial measurements of systolic time intervals. Following 0.8 mg BMD intravenously, the QS2I abbreviation occurred within 3 min and reached a maximum at 4 hr. The time-course and the magnitude of the response were essentially the same as those obtained with 0.8 mg digoxin given intravenously in the same subjects. The serum glycoside levels were also similar for both drugs. When administered orally the QS2I abbreviation to 0.8 mg BMD appeared at 40 min and reached a maximum at 4 hr. The time-course and the magnitude of the effects were similar to those observed following oral digoxin. The blood digitalis levels following the drug ingestion, however, were significantly higher for BMD than for digoxin which suggests greater gastrointestinal absorption of BMD. Based on our observations, the inotropic effects of BMD are similar to those of digoxin. Our results, however, do not demonstrate greater cardiac activity after oral administration of BMD despite higher blood levels.
对正常成年人静脉注射和口服β-甲基地高辛(BMD)后的正性肌力作用和血清糖苷水平进行了测量,并与地高辛的相关指标进行了比较。通过连续测量收缩期时间间期获得的机电收缩指数(QS2I)缩短来无创评估心脏收缩力。静脉注射0.8mg BMD后,QS2I在3分钟内缩短,并在4小时达到最大值。反应的时间进程和幅度与同一受试者静脉注射0.8mg地高辛时基本相同。两种药物的血清糖苷水平也相似。口服0.8mg BMD时,QS2I缩短在40分钟出现,并在4小时达到最大值。作用的时间进程和幅度与口服地高辛后观察到的相似。然而,服药后BMD的血洋地黄水平显著高于地高辛,这表明BMD的胃肠道吸收更好。基于我们的观察,BMD的正性肌力作用与地高辛相似。然而,我们的结果并未显示口服BMD后尽管血药水平较高但心脏活性增强。