The Basics
What is Efavirenz?
Used along with other medications to treat HIV infection.
Brand names for Efavirenz
Sustiva
How Efavirenz is classified
Anti-Infective Agents, Anti-HIV Agents, Antiviral Agents, Anti-Retroviral Agents, Reverse Transcriptase Inhibitors
Efavirenz During Pregnancy
Efavirenz pregnancy category
Category DNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.
What we know about taking Efavirenz while pregnant
Early animal data indicated a possible association between in utero efavirenz exposure and neural tube defects. However, data in humans to date do not support this association
Taking Efavirenz While Breastfeeding
What are recommendations for lactation if you're taking Efavirenz?
In the United States and other developed countries, HIV-infected mothers should generally not breastfeed their infants. Published experience with efavirenz during breastfeeding is limited. In countries in which no acceptable, feasible, sustainable and safe replacement feeding is available, World Health Organization guidelines recommend that all women with an HIV infection who are pregnant or breastfeeding should be maintained on antiretroviral therapy for at least the duration of risk for mother-to-child transmission. Mothers should exclusively breastfeed their infants for the first 6 months of life; breastfeeding with complementary feeding should continue through at least 12 months of life up to 24 months of life.[1] The first choice regimen for nursing mothers is tenofovir, efavirenz and either lamivudine or emtricitabine. If these drugs are unavailable, alternative regimens include: 1) zidovudine, lamivudine and efavirenz; 2) zidovudine, lamivudine and nevirapine; or 3) tenofovir, nevirapine and either lamivudine or emtricitabine. Exclusively breastfed infants should also receive 6 weeks of prophylaxis with nevirapine.[2][3] Treatment of mothers of HIV+ mothers with efavirenz as part of Option B+ therapy does not appear to affect growth of their HIV-negative breastfed infants.
Maternal / infant drug levels
In the United States and other developed countries, HIV-infected mothers should generally not breastfeed their infants. Published experience with efavirenz during breastfeeding is limited. In countries in which no acceptable, feasible, sustainable and safe replacement feeding is available, World Health Organization guidelines recommend that all women with an HIV infection who are pregnant or breastfeeding should be maintained on antiretroviral therapy for at least the duration of risk for mother-to-child transmission. Mothers should exclusively breastfeed their infants for the first 6 months of life; breastfeeding with complementary feeding should continue through at least 12 months of life up to 24 months of life.[1] The first choice regimen for nursing mothers is tenofovir, efavirenz and either lamivudine or emtricitabine. If these drugs are unavailable, alternative regimens include: 1) zidovudine, lamivudine and efavirenz; 2) zidovudine, lamivudine and nevirapine; or 3) tenofovir, nevirapine and either lamivudine or emtricitabine. Exclusively breastfed infants should also receive 6 weeks of prophylaxis with nevirapine.[2][3] Treatment of mothers of HIV+ mothers with efavirenz as part of Option B+ therapy does not appear to affect growth of their HIV-negative breastfed infants.
Possible effects of Efavirenz on milk supply
Gynecomastia has been reported among men and at least one woman receiving efavirenz therapy.[12][13] Efavirenz appears to be much more likely to cause gynecomastia than other antiretroviral agents. Gynecomastia is unilateral initially, but can progress to bilateral. Spontaneous resolution usually occurred within one year, even with continuation of the regimen. The relevance of these findings to nursing mothers is not known. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
Possible alternatives to Efavirenz
List of References
Lactation sources: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK501922/1. Anon. Guideline: Updates on HIV and infant feeding: The duration of breastfeeding, and support from health services to improve feeding practices among mothers living with HIV. Geneva: World Health Organization. 2016. PMID: 27583316
2. World Health Organization. HIV and infant feeding: update. 2007. http://whqlibdoc.who.int/publications/2007/9789241595964_eng.pdf
3. World Health Organization. Consolidated guidelines on the use of antiretroviral drugs for treating and preventing HIV infection. Geneva: World Health Organization. 2013. http://www.who.int/hiv/pub/guidelines/arv2013/en
4. Schneider S, Peltier A, Gras A et al. Efavirenz in human breast milk, mothers’, and newborns’ plasma. J Acquir Immune Defic Syndr. 2008;48:450-4. PMID: 18614925
5. Olagunju A, Bolaji OO, Amara A et al. Development, validation and clinical application of a novel method for the quantification of efavirenz in dried breast milk spots using LC-MS/MS. J Antimicrob Chemother. 2015;70:555-61. PMID: 25326089
6. Olagunju A, Bolaji O, Amara A et al. Breast milk pharmacokinetics of efavirenz and breastfed infants’ exposure in genetically defined subgroups of mother-infant pairs: An observational study. Clin Infect Dis. 2015;61:453-63. PMID: 25882300
7. Palombi L, Pirillo MF, Marchei E et al. Concentrations of tenofovir, lamivudine and efavirenz in mothers and children enrolled under the Option B-Plus approach in Malawi. J Antimicrob Chemother. 2016;71:1027-30. PMID: 26679247
8. Oumar AA, Bagayoko-Maiga K, Bahachimi A et al. Efavirenz and lopinavir levels in HIV-infected women and their nursing infants, in Mali. J Pharmacol Exp Ther. 2018;366:479-84. PMID: 29986950
9. Gandhi M, Mwesigwa J, Aweeka F et al. Hair and plasma data show that lopinavir, ritonavir, and efavirenz all transfer from mother to infant in utero, but only efavirenz transfers via breastfeeding. J Acquir Immune Defic Syndr. 2013;63:578-84. PMID: 24135775
10. Cohan D, Natureeba P, Koss CA et al. Efficacy and safety of lopinavir/ritonavir versus efavirenz-based antiretroviral therapy in HIV-infected pregnant Ugandan women. AIDS. 2015;29:183-91. PMID: 25426808
11. Kapito-Tembo AP, Wesevich A, Bauleni A et al. Growth in infants exposed to EFV and TDF through breastmilk: Malawi PMTCT option B+. Top Antiviral Med. 2017;25:333s-4s. Abstract.
12. Jover F, Cuadrado JM, Roig P et al. Efavirenz-associated gynecomastia: report of five cases and review of the literature. Breast J. 2004;10:244-6. PMID: 15125753
13. Rahim S, Ortiz O, Maslow M, Holzman R. A case-control study of gynecomastia in HIV-1-infected patients receiving HAART. AIDS Read. 2004;14:23-4, 29-32, 35-40. PMID: 14959701
Disclaimer: This material is provided for educational purposes only and is not intended for medical advice, diagnosis, or treatment. Consult your healthcare provider with any questions.
