Department of Pediatrics, Texas Tech University Health Sciences Center, Amarillo, Texas.
Department of Obstetrics and Gynecology, Texas Tech University Health Sciences Center, Amarillo, Texas.
Breastfeed Med. 2020 Jan;15(1):41-43. doi: 10.1089/bfm.2019.0124. Epub 2019 Sep 18.
Rivaroxaban (Xarelto) is a reversible direct factor Xa inhibitor used for the treatment and prevention of coagulation in numerous syndromes. There is very limited information available on the transfer of rivaroxaban into human breast milk. This study determined the drug concentration-time profile of rivaroxaban in milk samples collected from two lactating mothers consuming 15 mg twice daily. After 21 days, each mother transitioned to 20 mg once daily. Levels in milk were measured using liquid chromatography mass spectrometry and analysis was done for both dosages. The maximum concentration of rivaroxaban observed for the 15 mg dose was 0.3 ± 0.02 μg/mL and that for the 20 mg dose was 0.26 ± 0.01 μg/mL. The relative infant dose (RID) was calculated to be 5% and 4%, respectively. This relatively low infant dose is probably explained by the high plasma protein binding of rivaroxaban and its subsequent poor penetration into human milk. The results indicate that rivaroxaban receded to minimum concentration over a period of 12 hours. In these two cases, we found the levels of rivaroxaban in milk to be quite low, and the RID to be 5% of the maternal dose. Although the levels detected were low, rivaroxaban does transfer into breast milk. Caution should be exercised until further studies are conducted and report the safety profile of rivaroxaban in breastfeeding infants.
利伐沙班（拜瑞妥）是一种可逆的直接 Xa 因子抑制剂，用于治疗和预防多种综合征中的凝血。关于利伐沙班转移到人乳中的信息非常有限。本研究旨在确定两名每日服用两次 15 毫克利伐沙班的哺乳期母亲的乳汁样本中利伐沙班的药物浓度-时间曲线。21 天后，每位母亲转换为每日一次 20 毫克。使用液相色谱-质谱法测量乳汁中的水平，并对两种剂量进行分析。观察到 15 毫克剂量的利伐沙班最高浓度为 0.3 ± 0.02 μg/ml，20 毫克剂量的利伐沙班最高浓度为 0.26 ± 0.01 μg/ml。相对婴儿剂量（RID）分别为 5%和 4%。相对较低的婴儿剂量可能是由于利伐沙班与血浆蛋白的高结合率及其随后在人乳中较差的渗透所致。结果表明，利伐沙班在 12 小时内消退至最低浓度。在这两种情况下，我们发现乳汁中的利伐沙班水平相当低，RID 为母亲剂量的 5%。尽管检测到的水平较低，但利伐沙班确实会转移到母乳中。在进一步研究报告利伐沙班在母乳喂养婴儿中的安全性概况之前，应谨慎使用。
