Summary of Use during Lactation

The consensus opinion is that women taking a statin should not breastfeed because of a concern with disruption of infant lipid metabolism. However, others have argued that children homozygous for familial hypercholesterolemia are treated with statins beginning at 1 year of age, that statins have low oral bioavailability, and risks to the breastfed infant are low, especially with rosuvastatin and pravastatin.[1] Some evidence indicates that amounts of atorvastatin and its metabolites are milk are very low and it can be taken by nursing mothers with no obvious developmental problems in their infants. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.

Drug Levels

Maternal Levels. Three women who were taking atorvastatin in doses of 20, 40 and 80 mg once daily donated milk samples at 0, 1, 2, 4, 6, 8, 10, 12, and 24 hours after their dose. Aliquots of complete milk collections from both breasts were analyzed for atorvastatin and its active metabolites. The absolute infant dosages of atorvastatin was calculated at 0.066, 0.19, and 0.27 mcg/kg daily for the 20 mg, 40 mg, and 80 mg doses, respectively. The weight-adjusted relative infant dose of atorvastatin, 2-hydroxy- and 4-hydroxyatorvastatin was 0.05%, 0.09%, and 0.052% for atorvastatin doses of 20 mg, 40 mg, and 80 mg, respectively.[2]

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

Effects in Breastfed Infants

In a case series of patients with homozygous familial hypercholesterolemia, 6 patients breastfed 11 infants after restarting statin therapy postpartum. The specific statin used by these women was not reported, most of the women on statin therapy were using atorvastatin, either 40 or 80 mg, daily. Normal early child development was reported for all offspring. Children started school at the appropriate age and no learning difficulties were reported.[3]

Two women who were taking atorvastatin in doses of 20 and 40 mg daily partially breastfed their infants. Mothers reported no infant adverse effects and no concerns about their development.[2]

Effects on Lactation and Breastmilk

Gynecomastia has been reported in men taking atorvastatin.[4-6] Serum prolactin was normal in one case where it was measured.[6] In another case, possible rosuvastatin-induced gynecomastia resolved after the patient’s medication was changed to atorvastatin.[7]

Three women who were taking atorvastatin in doses of 20, 40 and 80 mg once daily donated milk samples at 0, 1, 2, 4, 6, 8, 10, 12, and 24 hours after their dose. Aliquots of complete milk collections were analyzed for cholesterol. Milk cholesterol levels were within previously established norms in the range of 10 mg/dL.[2]

Alternate Drugs to Consider

Cholestyramine, Colesevelam, Colestipol

References

1.

Holmsen ST, Bakkebo T, Seferowicz M, et al. Statins and breastfeeding in familial hypercholesterolaemia. Tidsskr Nor Laegeforen 2017;137:686-7. [PubMed: 28551957]

2.

Campbell L, Huseman K, Krutsch K, et al. Minimal transfer of atorvastatin and its metabolites in human milk: A case series. Breastfeed Med 2024;19:889-4. [PubMed: 39268678]

3.

Botha TC, Pilcher GJ, Wolmarans K, et al. Statins and other lipid-lowering therapy and pregnancy outcomes in homozygous familial hypercholesterolaemia: A retrospective review of 39 pregnancies. Atherosclerosis 2018;277:502-7. [PubMed: 30270091]

4.

Hammons KB, Edwards RF, Rice WY. Golf-inhibiting gynecomastia associated with atorvastatin therapy. Pharmacotherapy 2006;26:1165-8. [PubMed: 16863492]

5.

Bostanitis I, Tsalidou M. Atorvastatin-induced gynecomastia in a dyslipidemic patient: A case report. Hellenic J Cardiol 2019;60:194-5. [PubMed: 30145234]

6.

Famularo G, Sarrecchia C. Atorvastatin-associated gynecomastia. Ann Pharmacother 2021;55:1300-1. [PubMed: 33472378]

7.

Oteri A, Catania MA, Travaglini R, et al. Gynecomastia possibly induced by rosuvastatin. Pharmacotherapy 2008;28:549-51. [PubMed: 18363539]

Substance Name

Atorvastatin

CAS Registry Number

110862-48-1

Drug Class

Breast Feeding

Lactation

Milk, Human

Anticholesteremic Agents

Antilipemic Agents

Hydroxymethylglutaryl-CoA Reductase Inhibitors