Haustein K O
Eur J Clin Pharmacol. 1981 Jan;19(1):45-51. doi: 10.1007/BF00558383.
Patients suffering from congestive heart failure received maintenance doses of digitoxin (N = 10) or digoxin (N = 8). The plasma glycoside concentration was determined, and after a single dose of 3H-digitoxin or 3H-digoxin, the decline and excretion of radioactivity were measured over a period of 7 (digitoxin) and 3 days (digoxin). Plasma radioactivity declined with a T1/2 beta between 77 and 234 h (mean 138 h) in the case of digitoxin and with a T1/2 beta between 9.2 and 38.6 h (mean 23.5 h) for digoxin. A close correlation between T1/2 beta and excreted radioactivity and T1/2 beta and total plasma level was found for digitoxin. In 4 patients TLC of urine showed that interindividual variations in digitoxin elimination could possibly be attributed to variation in metabolism, resulting in the production of different metabolites. Predicted digitoxin plasma levels agreed well with measured values. The maintenance dose could be calculated from the total body clearance (VCl) and a presumed plasma glycoside level. The recommended technique facilitates dosage calculations in patients treated with digitoxin.
患有充血性心力衰竭的患者接受了洋地黄毒苷（N = 10）或地高辛（N = 8）的维持剂量治疗。测定了血浆糖苷浓度，在单次给予3H-洋地黄毒苷或3H-地高辛后，在7天（洋地黄毒苷）和3天（地高辛）的时间段内测量了放射性的下降和排泄情况。洋地黄毒苷的血浆放射性以77至234小时（平均138小时）的β半衰期下降，地高辛的β半衰期在9.2至38.6小时（平均23.5小时）之间。发现洋地黄毒苷的β半衰期与排泄放射性以及β半衰期与血浆总水平之间存在密切相关性。在4名患者中，尿薄层层析显示洋地黄毒苷消除的个体间差异可能归因于代谢差异，导致产生不同的代谢产物。预测的洋地黄毒苷血浆水平与测量值吻合良好。维持剂量可根据总体清除率（VCl）和假定的血浆糖苷水平计算得出。推荐的技术有助于洋地黄毒苷治疗患者的剂量计算。
