Attribution Statement: LactMed is a registered trademark of the U.S. Department of Health and Human Services.
NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.
Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006-.
CASRN: 163222-33-1
Drug Levels and Effects
Summary of Use during Lactation
Data from 2 mothers indicate that levels of ezetimibe and its active metabolite appear in very low amounts in milk and serum levels in infants predicted by a pharmacokinetic model are 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
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;63:317-32. [PubMed: 38278872]
Substance Identification
Substance Name
Ezetimibe
CAS Registry Number
163222-33-1
Disclaimer: Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.
- User and Medical Advice Disclaimer
- Drugs and Lactation Database (LactMed) - Record Format
- LactMed - Database Creation and Peer Review Process
- Fact Sheet. Drugs and Lactation Database (LactMed)
- Drugs and Lactation Database (LactMed) - Glossary
- LactMed Selected References
- Drugs and Lactation Database (LactMed) - About Dietary Supplements
- Breastfeeding Links
- PubChem SubstanceRelated PubChem Substances
- PubMedLinks to PubMed
- Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia).[Drug Metab Dispos. 2004]Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia).Ghosal A, Hapangama N, Yuan Y, Achanfuo-Yeboah J, Iannucci R, Chowdhury S, Alton K, Patrick JE, Zbaida S. Drug Metab Dispos. 2004 Mar; 32(3):314-20.
- Fungal biotransformation of ezetimibe.[Biotechnol Biotechnol Equip. 2...]Fungal biotransformation of ezetimibe.Pervaiz I, Ahmad S, Khaliq FH, Arshad A, Imran M, Khan BA, Ullah A, Ali U, Iqbal K, Usman M, et al. Biotechnol Biotechnol Equip. 2014 Sep 3; 28(5):934-940. Epub 2014 Nov 17.
- Dose-comparison study of the combination of ezetimibe and simvastatin (Vytorin) versus atorvastatin in patients with hypercholesterolemia: the Vytorin Versus Atorvastatin (VYVA) study.[Am Heart J. 2005]Dose-comparison study of the combination of ezetimibe and simvastatin (Vytorin) versus atorvastatin in patients with hypercholesterolemia: the Vytorin Versus Atorvastatin (VYVA) study.Ballantyne CM, Abate N, Yuan Z, King TR, Palmisano J. Am Heart J. 2005 Mar; 149(3):464-73.
- Review Paroxetine.[Drugs and Lactation Database (...]Review Paroxetine.. Drugs and Lactation Database (LactMed®). 2006
- Review Ezetimibe: a novel option for lowering cholesterol.[Expert Rev Cardiovasc Ther. 2003]Review Ezetimibe: a novel option for lowering cholesterol.Davidson MH. Expert Rev Cardiovasc Ther. 2003 May; 1(1):11-21.
- Ezetimibe - Drugs and Lactation Database (LactMed®)Ezetimibe - Drugs and Lactation Database (LactMed®)
Your browsing activity is empty.
Activity recording is turned off.
See more...