Rampono Jonathan, Hackett L Peter, Kristensen Judith H, Kohan Rolland, Page-Sharp Madhu, Ilett Kenneth F
Department of Psychological Medicine, Women's and Children's Health Service, Subiaco, Australia.
Br J Clin Pharmacol. 2006 Sep;62(3):316-22. doi: 10.1111/j.1365-2125.2006.02659.x.
To investigate the transfer of escitalopram and its demethyl metabolite into milk, the absolute and relative infant doses via milk and to assess any unwanted effects in the breastfed infant.
Multiple samples of blood and milk were obtained over a dose interval at steady state from eight women who were taking escitalopram for postnatal depression. Drug concentrations in plasma and milk were measured by high-performance liquid chromatography and milk/plasma ratio (M/P(AUC)), absolute infant dose and relative infant dose were estimated by standard methods. Their breastfed infants were also examined clinically and in five infants a blood sample was taken for drug analysis.
The median dose taken by the women was 10 mg day(-1). The mean (95% confidence interval) M/P(AUC) was 2.2 (2.0, 2.4) for escitalopram and 2.2 (1.9, 2.5) for demethylescitalopram. Absolute infant doses were 7.6 microg kg(-1) day(-1) (5.2, 10.0) for escitalopram and 3.0 microg kg(-1) day(-1) (2.4, 3.6) for demethylescitalopram. The total relative infant dose for escitalopram plus its demethyl metabolite was 5.3% (4.2, 6.4) as escitalopram equivalents. All of the infants had met normal developmental milestones and no adverse effects were seen. Compared with average maternal plasma concentrations (24 microg l(-1)), the concentrations of the parent drug and its metabolite in plasma from five infants were most commonly below the limit of detection (</=3 microg l(-1)).
The study shows that escitalopram is safe for use during breastfeeding. Because its absolute infant dose is lower than that for an equivalent antidepressant dose of rac-citalopram, it may be preferred over rac-citalopram in treating depression in lactating women. Nevertheless, each decision to breastfeed should always be made on the basis of an individual risk:benefit analysis.
研究艾司西酞普兰及其去甲基代谢产物向乳汁中的转移情况、通过乳汁摄入的绝对婴儿剂量和相对婴儿剂量，并评估对母乳喂养婴儿的任何不良影响。
在稳态下的一个给药间隔内，从八名因产后抑郁而服用艾司西酞普兰的女性身上采集多份血液和乳汁样本。采用高效液相色谱法测定血浆和乳汁中的药物浓度，并通过标准方法估算乳汁/血浆比率（M/P(AUC)）、绝对婴儿剂量和相对婴儿剂量。对她们的母乳喂养婴儿也进行了临床检查，并且对五名婴儿采集了血样进行药物分析。
这些女性服用的中位剂量为10毫克/天。艾司西酞普兰的平均（95%置信区间）M/P(AUC)为2.2（2.0，2.4），去甲艾司西酞普兰为2.2（1.9，2.5）。艾司西酞普兰的绝对婴儿剂量为7.6微克/千克/天（5.2，10.0），去甲艾司西酞普兰为3.0微克/千克/天（2.4，3.6）。以艾司西酞普兰等效物计算，艾司西酞普兰及其去甲基代谢产物的总相对婴儿剂量为5.3%（4.2，6.4）。所有婴儿均达到正常发育里程碑，未观察到不良反应。与母亲平均血浆浓度（24微克/升）相比，五名婴儿血浆中母体药物及其代谢产物的浓度最常见的是低于检测限（≤3微克/升）。
该研究表明，艾司西酞普兰在母乳喂养期间使用是安全的。由于其绝对婴儿剂量低于等量消旋西酞普兰抗抑郁剂量的绝对婴儿剂量，在治疗哺乳期妇女抑郁症时，它可能比消旋西酞普兰更受青睐。然而，每次母乳喂养的决定都应始终基于个体的风险效益分析。
