Last update Dec. 21, 2022

Efavirenz (EFV)

Compatible

Safe product and/or breastfeeding is the best option.

Antiretroviral. It is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against HIV-1 used with other antiretrovirals for combination therapy of HIV infection and AIDS. Oral administration once a day.

It is excreted in breast milk in clinically insignificant amounts. (Aebi 2022, Oumar 2018, Palombi 2016, Olagunju 2015, Schneider 2008)

No problems have been observed in infants whose mothers have taken it. (Kapito 2021, Oumar 2018, Olagunju 2015, Cohan 2015, Schneider 2008

Plasma levels in these infants were very low, 9% to 13% of maternal plasma levels. (Aebi 2022, Oumar 2018, Palombi 2016, Olagunju 2015, Gandhi 2013, Schneider 2008)

Several medical societies and expert authors consider the use of this medication to be safe during breastfeeding. (WHO 2016 y 2014, Pandhi 2014, Hirnschall 2013)

Alternatives

We do not have alternatives for Efavirenz (EFV) since it is relatively safe.

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Efavirenz (EFV) in other languages or writings:

Group

Efavirenz (EFV) belongs to this group or family:

Tradenames

Main tradenames from several countries containing Efavirenz (EFV) in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 42 %
Molecular weight 316 daltons
Protein Binding 99.5 %
pKa 12.52 -
Tmax 3 - 5 hours
40 - 55 hours
M/P ratio 0.86 -
Theoretical Dose 0.41 (0.32–0.48) mg/Kg/d
Relative Dose 1.35 (1.07–1.61) %

References

  1. Aebi-Popp K, Kahlert CR, Crisinel PA, Decosterd L, Saldanha SA, Hoesli I, Martinez De Tejada B, Duppenthaler A, Rauch A, Marzolini C; Swiss Mother and Child HIV Cohort Study (SHCS).. Transfer of antiretroviral drugs into breastmilk: a prospective study from the Swiss Mother and Child HIV Cohort Study. J Antimicrob Chemother. 2022 Nov 28;77(12):3436-3442. Consulted on Dec. 16, 2022 Abstract Full text (link to original source)
  2. Kapito-Tembo AP, Bauleni A, Wesevich A, Ongubo D, Hosseinipour MC, Dube Q, Mwale P, Corbett A, Mwapasa V, Phiri S. Growth and Neurodevelopment Outcomes in HIV-, Tenofovir-, and Efavirenz-Exposed Breastfed Infants in the PMTCT Option B+ Program in Malawi. J Acquir Immune Defic Syndr. 2021 Jan 1;86(1):81-90. Abstract
  3. Oumar AA, Bagayoko-Maiga K, Bahachimi A, Maiga M, Cere MC, Diarra Z, Chatelut E, Sylla M, Murphy RL, Dao S, Gandia P. Efavirenz and Lopinavir Levels in HIV-Infected Women and Their Nursing Infants, in Mali. J Pharmacol Exp Ther. 2018 Sep;366(3):479-484. Abstract
  4. WHO - World Health Organization Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection: Recommendations for a Public Health Approach. Guideline. 2016 Abstract Full text (link to original source) Full text (in our servers)
  5. Palombi L, Pirillo MF, Marchei E, Jere H, Sagno JB, Luhanga R, Floridia M, Andreotti M, Galluzzo CM, Pichini S, Mwenda R, Mancinelli S, Marazzi MC, Vella S, Liotta G, Giuliano M. Concentrations of tenofovir, lamivudine and efavirenz in mothers and children enrolled under the Option B-Plus approach in Malawi. J Antimicrob Chemother. 2016 Abstract Full text (link to original source) Full text (in our servers)
  6. Olagunju A, Bolaji O, Amara A, Waitt C, Else L, Adejuyigbe E, Siccardi M, Back D, Khoo S, Owen A. Breast milk pharmacokinetics of efavirenz and breastfed infants' exposure in genetically defined subgroups of mother-infant pairs: an observational study. Clin Infect Dis. 2015 Aug 1;61(3):453-63. Abstract Full text (link to original source)
  7. Olagunju A, Bolaji OO, Amara A, Waitt C, Else L, Soyinka J, Adeagbo B, Adejuyigbe E, Siccardi M, Back D, Owen A, Khoo S. 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 Feb;70(2):555-61. Abstract Full text (link to original source)
  8. Cohan D, Natureeba P, Koss CA, Plenty A, Luwedde F, Mwesigwa J, Ades V, Charlebois ED, Gandhi M, Clark TD, Nzarubara B, Achan J, Ruel T, Kamya MR, Havlir DV. Efficacy and safety of lopinavir/ritonavir versus efavirenz-based antiretroviral therapy in HIV-infected pregnant Ugandan women. AIDS. 2015 Jan 14;29(2):183-91. Abstract Full text (link to original source)
  9. Pandhi D, Ailawadi P. Initiation of antiretroviral therapy. Indian J Sex Transm Dis. 2014 Abstract Full text (link to original source) Full text (in our servers)
  10. Hirnschall G, Harries AD, Easterbrook PJ, Doherty MC, Ball A. The next generation of the World Health Organization's global antiretroviral guidance. J Int AIDS Soc. 2013 Abstract Full text (link to original source) Full text (in our servers)
  11. Gandhi M, Mwesigwa J, Aweeka F, Plenty A, Charlebois E, Ruel TD, Huang Y, Clark T, Ades V, Natureeba P, Luwedde FA, Achan J, Kamya MR, Havlir DV, Cohan D; Prevention of Malaria and HIV disease in Tororo (PROMOTE) study.. 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 Aug 15;63(5):578-84. Abstract
  12. Schneider S, Peltier A, Gras A, Arendt V, Karasi-Omes C, Mujawamariwa A, Ndimubanzi PC, Ndayisaba G, Wennig R. Efavirenz in human breast milk, mothers', and newborns' plasma. J Acquir Immune Defic Syndr. 2008 Aug 1;48(4):450-4. Abstract

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