Ebastine and Breastfeeding

Summary of use during lactation

Ebastine is a nonsedating antihistamine that is not available in the United States, but is available in other countries. Preliminary evidence indicates that the amounts in milk are unlikely to affect a breastfed infant.

Drug levels in milk and infant serum

Ebastine is a pro-drug that is metabolized to the active metabolite, carebastine, which has a much longer half-life than ebastine. Maternal Levels. A woman with chronic urticaria was taking ebastine 10 mg daily during pregnancy and postpartum. On day 5 postpartum, the highest measured ebastine concentration in breastmilk was 6.3 mcg/L at 3.9 hours after the dose. The highest measured breastmilk carebastine concentration of 5.4 mcg/L occurred at 11.3 hours after administration. At 24.3 hours after the dose, the ebastine concentration was 1.1 mcg/L and the carebastine concentration was 4.4 mcg/L. Based on milk samples obtained at 11.3 hours after the dose, the authors estimated that a fully breastfed infant would receive daily dosages of 0.3 mcg/kg of ebastine and 0.2 mcg/kg of carebastine.[1] Infant Levels. A woman with chronic urticaria was taking ebastine 10 mg daily during pregnancy and postpartum. At 24 hours after birth, her breastfed infant had an undetectable serum (<0.2 mcg/L) ebastine concentration and a carebastine concentration of 46.8 mcg/L, probably obtained via placental transfer. At 2 days postpartum, both ebastine and carebastine were undetectable in the infant’s serum.[1]

Effects in breastfed infants

A woman with chronic urticaria was taking ebastine 10 mg daily during pregnancy and postpartum. Her infant was exclusively breastfed until the age of 6 months. He showed normal development at 1 and 3 months of age.[1]

Effects on lactation and breastmilk

Antihistamines in relatively high doses given by injection can decrease basal serum prolactin in nonlactating women and in early postpartum women.[2,3] However, suckling-induced prolactin secretion is not affected by antihistamine pretreatment of postpartum mothers.[2] Whether lower oral doses of antihistamines or ebastine have the same effect on serum prolactin or whether the effects on prolactin have any consequences on breastfeeding success have not been studied. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternative drugs to consider

Cetirizine, Desloratadine, Fexofenadine, Levocetirizine, Loratadine

References

1. Saito J, Yakuwa N, Sandaiji N, et al. Ebastine during pregnancy and lactation in a patient with chronic urticaria: Ebastine and carebastine levels in maternal serum, cord blood, breast milk, and the infant's serum. J Eur Acad Dermatol Venereol 2020;34:e496-e97.32249465 PubMed
2. Messinis IE, Souvatzoglou A, Fais N, et al. Histamine H1 receptor participation in the control of prolactin secretion in postpartum. J Endocrinol Invest 1985;8:143-6.3928731 PubMed
3. Pontiroli AE, De Castro e Silva E, Mazzoleni F, et al. The effect of histamine and H1 and H2 receptors on prolactin and luteinizing hormone release in humans: Sex differences and the role of stress. J Clin Endocrinol Metab 1981;52:924-8.7228996 PubMed