Summary of Use during Lactation

Data from 2 mothers indicate that levels of ezetimibe and its active metabolite are very low in milk and predicted serum levels in infants were considerably lower than in adults. Ezetimibe appears to be acceptable during breastfeeding. Ezetimibe in combination with a statin (e.g., atorvastatin, simvastatin) should be avoided in nursing mothers.

Drug Levels

Maternal Levels. Two nursing mothers taking ezetimibe 10 mg daily donated a total of 15 milk samples for analysis of ezetimibe and ezetimibe glucuronide. In one mother, the highest drug concentrations were found in hindmilk at 2.08 hours after a dose. The ezetimibe concentration was 0.95 mcg/L and the glucuronide concentration was 1.39 mcg/L. In the second mother, the highest ezetimibe concentration of 0.98 mcg/L occurred 5.22 hours after a dose between feedings and the highest ezetimibe glucuronide concentration of 2.65 mcg/L occurred 8.47 hours after a dose just after feeding. These values result in a total ezetimibe plus ezetimibe glucuronide relative infant dosages of about 0.16% and 0.25%, respectively. A computer model of ezetimibe during nursing was consistent with the observed levels and indicated that predicted serum levels in infants were considerably lower than in adults.[1]

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

Cholestyramine, Colesevelam, Colestipol

References

1.

Yeung CHT, Autmizguine J, Dalvi P, et al. Maternal ezetimibe concentrations measured in breast milk and its use in breastfeeding infant exposure predictions. Clin Pharmacokinet 2024. [PubMed: 38278872]

Substance Name

Ezetimibe

CAS Registry Number

163222-33-1

Drug Class

Breast Feeding

Lactation

Milk, Human

Anticholesteremic Agents

Antilipemic Agents