Department of Obstetrics and Gynecology, Texas Tech University Health Sciences Center, Amarillo, TX, USA.
Department of Pharmacy Practice, Texas Tech University Health Sciences Center, Amarillo, TX, USA.
Arch Womens Ment Health. 2024 Aug;27(4):619-623. doi: 10.1007/s00737-024-01445-1. Epub 2024 Feb 20.
Buspirone, an anxiolytic with minimal risk of dependence or respiratory depression, lacks extensive published data on its transfer into human milk during lactation. The objective of this study was to 1) quantify the transfer of buspirone and its active metabolite 1-pyrimidinylpiperazine (1-PP) into human milk, allowing for an estimation of maternal drug exposure to the breastfed infant, and 2) report observations of the infants exposed to buspirone via breastmilk.
Milk samples and health histories were collected from nine lactating mothers who donated milk samples to the InfantRisk Human Milk Biorepository while taking buspirone. The drug concentration-time profile of buspirone and 1-PP was determined using liquid chromatography-mass spectrometry.
Buspirone was below the detection level of 1.5 ng/mL in all milk samples with dosages ranging from 7.5 to 30 mg twice daily. However, low levels of active metabolite 1-PP were observed at 7.5 mg twice daily up to 30 mg twice daily. The relative infant dose (RID) calculated ranged from 0.21 to 2.17%, which is below the standard 10% threshold for infant safety. There were no reports of adverse effects in the exposed infants.
The levels of buspirone observed in all participants' milk samples were exceedingly low. The subsequently low relative infant dose (RID) in the range of 0.21% to 2.17% is below the 10% threshold for infant safety, suggesting that the transfer of maternal buspirone and its active metabolite (1-PP) into human milk is clinically insignificant and poses minimal risk to a breastfed infant.
苯并二氮䓬类抗焦虑药丁螺环酮的依赖性和呼吸抑制风险极小,但关于其在哺乳期进入人乳的情况,相关数据尚未广泛发表。本研究的目的是:1)定量测定丁螺环酮及其活性代谢物 1-(嘧啶-1-基)哌嗪(1-PP)在人乳中的转移情况,从而估算哺乳期婴儿的母体药物暴露情况;2)报告通过母乳暴露于丁螺环酮的婴儿的观察结果。
从 9 位正在服用丁螺环酮并向婴儿风险母乳生物库捐赠母乳样本的哺乳期母亲中收集母乳样本和健康史。使用液相色谱-质谱法测定丁螺环酮和 1-PP 的药物浓度-时间曲线。
所有剂量为 7.5-30mg 每日两次的母亲的母乳样本中,丁螺环酮均低于 1.5ng/ml 的检测下限。然而,在每日两次 7.5mg 至每日两次 30mg 的剂量范围内,可观察到低水平的活性代谢产物 1-PP。计算得出的婴儿相对剂量(RID)范围为 0.21-2.17%,低于婴儿安全性的 10%标准阈值。暴露于丁螺环酮的婴儿均未报告出现不良反应。
所有参与者的母乳样本中观察到的丁螺环酮水平极低。随后,RID 处于 0.21%至 2.17%的范围内,低于婴儿安全性的 10%阈值,表明丁螺环酮及其活性代谢物(1-PP)从母体转移到母乳中具有临床意义,对母乳喂养的婴儿风险极小。