Objective: To study the transfer of carbetocin into human breast milk.
Methods: Five healthy nursing women, 7-14 weeks postpartum, emptied t
heir breasts using a breast pump and then received 70 mug carbetocin b
y intramuscular injection. Using a radioimmunoassay, the concentration
s of carbetocin were measured in plasma and breast milk samples obtain
ed before carbetocin administration and at 15, 30, 60, 90, 120, and 24
0 minutes after drug administration. Results: For plasma, the mean (+/
- standard deviation) area under the curve (AUC) of carbetocin versus
time was 1119.3 +/- 315.9 pg/mL, a value about 50 times higher than th
e mean AUC for carbetocin in breast milk (18.6 +/- 13.7 and 29.0 +/- 2
3.8 pg/mL for the right and left breast, respectively). The ratio of m
ilk to plasma AUC was low: 1.7 +/- 0.9 and 3.1 +/- 2.8% for the left a
nd right breast, respectively. No serious adverse reactions occurred a
nd no clinically significant changes in vital signs were found. Conclu
sion: Very little carbetocin is transferred into human breast milk, pr
esenting little risk to breast-fed infants.