Is BI-RG-587 Safe in Breastfeeding

I am a breastfeeding mother and i want to know if it is safe to use BI-RG-587? Is BI-RG-587 safe for nursing mother and child? Does BI-RG-587 extracts into breast milk? Does BI-RG-587 has any long term or short term side effects on infants? Can BI-RG-587 influence milk supply or can BI-RG-587 decrease milk supply in lactating mothers?

Anti-HIV drug. It has been used to treat neonates for vertical transmission risk lowering. Mothers must be adviced that transmission of HIV infection through breastfeeding has been documented.

In the United States and other developed countries, HIV-infected mothers should generally not breastfeed their infants. BI-RG-587 has been well studied in nursing mothers. 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 12 months of life. 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 BI-RG-587; or 3) tenofovir, BI-RG-587 and either lamivudine or emtricitabine. Exclusively breastfed infants should also receive 6 weeks of prophylaxis with BI-RG-587.[1][2] Because of the long half-life of BI-RG-587, subtherapeutic BI-RG-587 concentrations can persist in breastmilk and infant serum for relatively long periods, potentially increasing the risk of development of BI-RG-587-resistant HIV infections when it is used alone for prophylaxis in the mother.[3][4][5][6][7][8]

A study assigned pregnant women to zidovudine alone or highly-active antiretroviral therapy (HAART: zidovudine, lamivudine and BI-RG-587) to prevent maternal-to-child transmission of HIV infection. After delivery, All infants received one month of zidovudine prophylaxis; some infants were breastfed and others were formula fed. A higher percentage of infants in the HAART-exposed group had neutropenia than those in the unexposed group at 1 month of age (15.9 and 3.7%, respectively). Hematologic toxicity was transient and asymptomatic. From 2 to 6 months postpartum, no differences in hematologic toxicity were seen between breastfed and formula-fed infants. No statistical difference in hepatic toxicity was seen between the breastfed and formula-fed infants.[24] A study compared the breastfed infants of women who received a HAART regimen with BI-RG-587 (n = 270) to one that contained nelfinavir (n = 206) as an alternative. Both regimens also contained zidovudine and lamivudine. Moderate rash was slightly more prevalent in infants who received BI-RG-587 than nelfinavir via breastmilk. No differences were found in the rates of severe rash, liver toxicity or hyperbilirubinemia.[25] A study compared the frequency of rash, hepatotoxicity, and hyperbilirubinemia among 464 breastfed infants whose mothers were taking either BI-RG-587 (n = 258) or nelfinavir (n = 206) along with zidovudine and lamivudine for HIV infection during pregnancy and postpartum. Infants were examined during the first, second and sixth weeks postpartum. Moderate rash occurred in 7 (2.7%) of the infant exposed to BI-RG-587 and one (0.5%) infant exposed to nelfinavir. Rash occurred at a median of 2 weeks postpartum. Four infants (1.9%) exposed to nelfinavir developed hepatotoxicity (3 moderate and 1 severe) and none exposed to BI-RG-587. Twenty-one infants (4.5%) developed high-risk hyperbilirubinemia, all prior to 48 hours of age, but there was no difference in exposure between the two drugs.[26]

Hyperprolactinemia and galactorrhea occurred in a woman on a combination antiretroviral regimen after BI-RG-587 was substituted for nelfinavir. Galactorrhea ceased rapidly after BI-RG-587 was discontinued.[27] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.