Maternal Transfer of Cetirizine Into Human Milk

Abstract

Introduction Cetirizine hydrochloride is a second-generation H1 histamine antagonist with Food and Drug Administration approval for treatment of allergic rhinitis and urticaria. Currently, the Food and Drug Administration does not recommend use of cetirizine during breastfeeding, as there are insufficient studies on both the transference of cetirizine into human milk and the effects of cetirizine in infants. Main issue To determine the concentration of cetirizine in human milk, samples were analyzed using high performance liquid chromatography mass spectrometry. Management Based on calculations, relative infant dose was found to be 1.77% at 24 hr. In addition, there were no reported adverse effects seen in the infants. Conclusion We suggest that transfer of cetirizine into human milk is minimal and unlikely to pose a significant risk to the breastfeeding infant. This is the first report presenting the transfer of cetirizine in human milk.

Antihistamine use during breastfeeding with focus on breast milk transfer and safety in humans: A systematic literature review

“…Only three of the studies were published after 2019. 31,33,34 The remaining studies were published between 1982 and 1995, that is, almost more than three decades ago where use of antihistamines and allergy treatment among breastfed women may not have been as common as today, particularly for secondgeneration antihistamines. Notably, few studies systematically monitored the breastfed infants for possible ADRs.…”

“…Both product labels for cetirizine stated that caution should be exercised, due to the excretion in human breast milk. In contrast, the published study on cetirizine 31 concludes that milk transfer is minimal and unlikely to pose a significant risk to the breastfeeding infant. Recent initiatives 24,25 that engage and encourage market authorization holders to perform human lactation studies hold great promise if they can be accompanied by updating and improving the lactation section of product labels.…”

“…After full-text screening, four studies were excluded due to (i) unrelated outcome, that is, studies on laboratory methods (n = 2); (ii) no reported data (n = 1); and (iii) full text not available (n = 1). The updated search on 18 January 2021 identified one case report 31 that was eligible for inclusion in this review after the screening process (Figure 1). Thus, a total of nine studies were finally included.…”

“…32 It was 0.4%-2.5% for epinastine, 34 whereas all the remaining relative infant doses were below 2% for cetirizine, ebastine, loratadine and triprolidine. 31,[35][36][37] Given the maternal doses listed in Table 3, absolute infant doses via breast milk per kilogram body weight per day are presented in Table 4. Based on these numbers, an exclusively breastfed infant weighing 5 kg would have been exposed to an absolute infant dose of 15.5 μg cetirizine, 7.5 μg clemastine, 8.8 μg ebastine, 23.0 μg of epinastine, 34.0 μg loratadine, 30.0 μg, terfenadine or 1.8 μg triprolidine 32-37 every 24 h.…”

“…Moreover, studies analysing the extent of breast milk transfer of cetirizine, clemastine, loratadine, terfenadine and triprolidine were only based on either a single-dose intake or maximum of 3 days of treatment. 31,35,37,38 Studies including women using antihistamines with long half-lives over extended periods are needed to confirm the low breast milk transfer.…”