Lofexidine use while Breastfeeding

Summary of Use during Lactation

No data are available in nursing mothers on the excretion into milk or safety of lofexidine in nursing mothers. A computer model predicted a maximum relative infant dose of about 3%, which should be acceptable. Although it is not contraindicated during breastfeeding, lofexidine should be used with caution until more data are available. An alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug Levels

Maternal Levels. A pharmacokinetic model was designed using in vitro-in vivo techniques that were then used to create a physiologically based pharmacokinetic model of lofexidine. A simulation of administering a dose of lofexidine to nursing mothers resulted in peak milk levels of about 4 mcg/L with a single 1.2 mg dose and 6 mcg/L with a single 2 mg dose assuming milk pH to be 6.8. Excretion was pH-sensitive, with levels dropping by over 90% at a pH of 7.[1] Using the peak level from a 2 mg maternal dose, the worst-case relative infant dose would be about 3%.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

Alternate Drugs to Consider

Buprenorphine, Methadone

References

1.

Dash SK, Rahman MA, Yi B, et al. Microfluidic blood-milk barrier and physiologically based pharmacokinetic model to predict lofexidine secretion into breast milk. J Pharm Sci 2025;114:103767. [PubMed: 40113090]

Substance Name

Lofexidine

CAS Registry Number

31036-80-3

Drug Class

Breast Feeding

Lactation

Milk, Human

Adrenergic Alpha-2 Receptor Agonists,

Narcotic Antagonists