Reinhardt D, Richter O, Genz T, Potthoff S
Eur J Pediatr. 1982 Feb;138(1):49-52. doi: 10.1007/BF00442328.
In order to find out whether digoxin therapy of nursing mothers might produce discomfort in suckling infants we have investigated the kinetics of the transfer of digoxin from plasma to milk in 11 nursing mothers. After intravenous or oral application of a single dose of 0.5 mg or 0.75 mg digoxin simultaneous serum, fore- and hindmilk samples were taken. Obviously, a rapid equilibrium occurred between the serum and the milk compartments and there was no difference between fore- and hindmilk. All three digoxin concentration profiles ran parallel with a milk to serum ratio of 0.6 to 0.7. The curves could best be fitted by the sum of two exponential functions. For predicting the digoxin intake into the suckling infant, simulations were carried out on the basis of two coupled compartment models. When the kinetic milk data as well as the kinetic data obtained in infants were fitted by this model it could be shown that even in the case of long half-lives only about 3% of the therapeutic drug levels were reached in the baby. Thus, one can conclude that digoxin accumulation to toxic concentrations should not occur in infants of women treated with appropriate doses of digoxin.
为了确定哺乳期母亲使用地高辛治疗是否会给哺乳婴儿带来不适,我们研究了11名哺乳期母亲体内地高辛从血浆转移至乳汁的动力学情况。静脉注射或口服单剂量0.5毫克或0.75毫克地高辛后,同时采集血清、前奶和后奶样本。显然,血清和乳汁间迅速达到平衡,且前奶和后奶之间没有差异。所有三条地高辛浓度曲线走势平行,奶与血清的比值为0.6至0.7。这些曲线最适合用两个指数函数之和来拟合。为预测哺乳婴儿摄入的地高辛量,基于两个耦合房室模型进行了模拟。当用该模型拟合乳汁动力学数据以及在婴儿身上获得的动力学数据时,可以表明,即使在半衰期较长的情况下,婴儿体内也仅能达到约3%的治疗药物水平。因此,可以得出结论,接受适当剂量地高辛治疗的女性所生婴儿不应出现地高辛蓄积至中毒浓度的情况。