Lowering serum cholesterol in infants is inadvisable because cholesterol is necessary for myelinization of the central nervous system. Although it has never been shown that cholesterol-lowering drugs in milk adversely affect the infant or lower their cholesterol, most sources recommend avoiding absorbable drugs (such as statins) during breastfeeding. This concern limits the options for mothers who need to lower their serum cholesterol.¹

For more detailed information and references on specific medications, please refer to LactMed, e-lactancia, Infant Risk, or Mother to Baby.

Statins are commonly used in managing high cholesterol and after vascular events such as strokes and heart attacks. Pharmacokinetics vary between various statins, but in general they have poor oral bioavailability of 20-30% and risks to the breastfed infant appear to be low with currently available pharmacokinetic information. However, at present, expert consensus is to avoid statin use during breastfeeding due to the theoretical risks to infant lipid metabolism and development. While alternatives are preferred due to the theoretical risks to infant lipid metabolism and development, providers should engage patients in shared decision making if a statin is necessary for a lactating individual.

Pravastatin is a relatively hydrophilic (water-soluble) statin with low levels in milk based on limited available data (which showed RID of 0.13% per LactMed) and a shorter half-life of 2 hours.^1,2 Given the low oral bioavailability and short half-life, pravastatin may be the preferred statin in lactating individuals. While alternatives to statins are preferred due to the theoretical risks to infant lipid metabolism and development, providers should engage patients in shared decision making if a statin is necessary for a lactating individual.

Rosuvastatin is a relatively hydrophilic statin with low levels in milk in limited available data and relatively low oral bioavailability. Additionally, rosuvastatin has high protein binding which theoretically decreases transmission into breastmilk as well. This medication does have a long half-life of 20-30 hours.^1,2 While alternatives to statins are preferred due to the theoretical risks to infant lipid metabolism and development, providers should engage patients in shared decision making if a statin is necessary for a lactating individual.

Atorvastatin levels have not been measured in milk, but a small study of 11 breastfed infants of 6 mothers on statins (most of them on 40 mg/day or 80 mg/day of atorvastatin) did not have any adverse outcomes and had normal development in follow-up.³ Atorvastatin has high protein binding, which theoretically would reduce its milk transfer. However, it also has a long half-life of 20-30 hours.^1,2 While alternatives to statins are preferred due to the theoretical risks to infant lipid metabolism and development, providers should engage patients in shared decision making if a statin is necessary for a lactating individual.

Pitavastatin levels have not been measured in milk. It is 99% protein bound in plasma, so amounts in milk are likely quite low. However, at present, expert consensus is to avoid statin use during breastfeeding due to the theoretical risks to infant lipid metabolism and development. While alternatives to statins are preferred due to the theoretical risks to infant lipid metabolism and development, providers should engage patients in shared decision making if a statin is necessary for a lactating individual.

Niacin is a normal component of human milk. Using niacin supplements increases milk levels, but studies have not been done to assess higher doses used for cholesterol-lowering purposes.¹ Alternatives are preferred due to the theoretical risks to infant lipid metabolism and development and limited data on efficacy for lowering cholesterol.

Bempedoic acid is an adenosine triphosphate-citrate lyase (ACL) inhibitor that lowers low-density lipoprotein cholesterol (LDL-C) by inhibition of cholesterol synthesis in the liver. The drug and its metabolites are about 99% protein bound in plasma, so amounts in milk are likely quite low. However, at present, expert consensus is to avoid  most cholesterol lowering medication use during breastfeeding due to the theoretical risks to infant lipid metabolism and development. Alternatives are preferred due to the lack of data and the theoretical risks to infant lipid metabolism and development.

These agents include cholestyramine, colesevelam/Welchol, and colestipol/Colestid. These medications are not absorbed systemically.¹ There is no absolute indication to pump and dump.

Ezetimibe/Zetia is an oral cholesterol-lowering agent that inhibits absorption of cholesterol in the GI tract. It has not been studied in lactating individuals and it is absorbed systemically (albeit poorly).¹ Alternatives are preferred due to the lack of data and the theoretical risks to infant lipid metabolism and development.

Alirocumab/Praluent and evolocumab/Repatha are injectable monoclonal antibodies that target proprotein convertase subtilisin kexin type 9 (PCSK9) and ultimately increase clearance of low-density lipoprotein (LDL). They are very potent, reducing LDL levels by 40-50% on their own or up to 60% when used in combination with statins. They are known to decrease cardiovascular events. Evinacumab is an angiopoietin-like protein 3 (ANGPTL3) inhibitor that promotes very low-density lipoprotein (VLDL) processing and clearance upstream from LDL formation. All three drugs are large protein molecules (>140 kDa molecular weight) with very low milk levels expected. They are likely to be partially destroyed in the infant’s GI tract and poorly absorbed by the infant. The use of these particular monoclonal antibodies has not been studied in lactating individuals, but previous studies on other monoclonal antibodies show generally undetectable breast milk levels and undetectable infant serum levels.¹ There is no absolute indication to pump and dump.

Inclisiran is a parenteral small interfering RNA (siRNA).The effect of inclisiran on cardiovascular morbidity and mortality has not been determined. Alternatives are preferred due to the lack of data and the theoretical risks to infant lipid metabolism and development.

Lomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor that reduces low-density lipoprotein (LDL) cholesterol, total cholesterol, apolipoprotein B, and non-high-density lipoprotein (non-HDL) cholesterol in patients with homozygous familial hypercholesterolemia (HoFH). The safety and efficacy of lomitapide have not been established in patients with hypercholesterolemia who do not have HoFH. Lomitapide has a boxed warning regarding potential hepatotoxicity so regular liver monitoring is required before initiation of treatment and routinely during therapy. Due to the potential for serious adverse effects, such as hepatotoxicity and tumorigenicity, and lack of data on milk transfer, breastfeeding is not recommended during lomitapide therapy. Alternatives are preferred due to the lack of data and the potential for harm.