Is Ezetimibe safe during lactation?

From the Guidelines

Ezetimibe is not recommended during lactation.

Rationale

• According to the evidence from 1, there are no adequate and well-controlled studies of ezetimibe in pregnant or lactating women, and it is recommended to avoid its use during pregnancy and lactation.
• The evidence from 1 also suggests that statins and other systemically absorbed cholesterol-lowering drugs, including ezetimibe, should be discontinued during pregnancy and lactation.
• Additionally, the guideline from 1 states that all lipid-lowering drugs, including ezetimibe, should be avoided during pregnancy and nursing or in women who may become pregnant.
• The lack of safety data in humans and the potential risk to the fetus or infant support the recommendation to avoid ezetimibe during lactation.

Key Points

• Ezetimibe is not recommended during lactation due to the lack of safety data and potential risk to the infant.
• Statins and other lipid-lowering drugs should also be avoided during pregnancy and lactation.
• Lifestyle interventions can be considered during pregnancy and nursing as general management for dyslipidaemias.
• Patients should be counseled on the potential risks and benefits of ezetimibe and other lipid-lowering therapies during pregnancy and lactation.

From the FDA Drug Label

There is no information about the presence of ezetimibe in human milk. Ezetimibe is present in rat milk (see Data). When a drug is present in animal milk, it is likely that the drug will be present in human milk. There is no information about the effects of ezetimibe on the breastfed infant or the effects of ezetimibe on milk production Ezetimibe tablets should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant.

• Ezetimibe safety during lactation: The FDA drug label states that there is no information about the presence of ezetimibe in human milk, but it is likely to be present based on animal studies.
• Recommendation: Ezetimibe tablets should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant 2.

From the Research

Ezetimibe Safety During Lactation

• The safety of ezetimibe during lactation has been studied, with one study measuring the concentrations of ezetimibe and its main active metabolite, ezetimibe-glucuronide, in human breast milk 3.
• The study found that the measured concentrations in breast milk samples were 0.17-1.02 ng/mL and 0.42-2.65 ng/mL of ezetimibe and EZE-glucuronide, respectively, suggesting minimal exposure to breastfeeding infants 3.
• A pediatric physiologically based pharmacokinetic (PBPK) model was used to predict infant exposures, and the results showed that breastfeeding infants would receive non-therapeutic exposures 3.
• Another study discussed the general issue of drug safety during lactation, highlighting the importance of assessing risks and benefits for both mother and child, and the need for reliable information on drug transfer into milk and infant exposure 4.
• A study on medications in pregnancy and lactation emphasized the importance of consulting reliable sources and choosing the safest drug available, with considerations such as milk:plasma ratio, half-life, and protein binding 5.
• A study on inhibiting cholesterol absorption during lactation found that blocking intestinal absorption of cholesterol in milk fed to newborn mice using ezetimibe had long-term effects on cholesterol metabolism in adult mice, but this study did not directly address the safety of ezetimibe during human lactation 6.
• A study on online information discrepancies regarding medicine use during pregnancy and lactation found that inconsistencies in information can result in sub-optimal treatment for pregnant and lactating women, but did not specifically address ezetimibe 7.