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Drugs and Lactation Database (LactMed) [Internet].

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Dolutegravir

Last Revision: September 20, 2021.

Estimated reading time: 3 minutes

CASRN: 1051375-16-6

image 135268073 in the ncbi pubchem database

Drug Levels and Effects

Summary of Use during Lactation

Dolutegravir is detectable in maternal milk in low amounts. It appears that elimination by newborn infants is prolonged and the drug has been detected in infant plasma during breastfeeding. Dolutegravir has been used safely in HIV-positive mothers during breastfeeding.

Drug Levels

Maternal Levels. An HIV-positive mother took a combination tablet containing dolutegravir 50 mg, abacavir sulfate 600 mg and lamivudine 300 mg (Triumeq) once daily. Her breastmilk dolutegravir concentrations were measured periodically over a 10-month period and averaged about 100 mcg/L at 11 hours after the dose. The authors estimated a daily infant dosage of 15 mcg/kg of dolutegravir.[1]

Two HIV-positive women taking dolutegravir (dose not stated, but presumably 50 mg daily) plus 2 unspecified nonnucleoside reverse transcriptase inhibitors donated two milk samples each. At 2 weeks postpartum, steady-state breastmilk dolutegravir levels in one woman were 154.2 mcg/L at 4 hours after the dose and 40.9 mcg/L at 24 hours after a dose. In the other woman, steady-state breastmilk dolutegravir levels were 116.3 mcg/L at 3 hours after the dose and 17.7 mcg/L at 24 hours after a dose. At 2 and 9 days, respectively, after discontinuing the drug, breastmilk levels were undetectable (<10 mcg/L).[2]

Twenty-eight pregnant HIV-positive women were randomized to receive an antiretroviral regimen containing oral dolutegravir 50 mg once daily. Of these, 17 women underwent extensive postpartum sampling of breastmilk and maternal serum at a median of 10 days postpartum. Median dolutegravir peak concentration in milk was 84.6 mcg/L and minimum of 22.3 mcg/L. Only one woman had 14 mcg/L of dolutegravir in milk at 48 hours; all other milk samples at 48, 72 and 96 hours after drug discontinuation were negative for dolutegravir.[3] Data from this study were used to create a pharmacokinetic model of dolutegravir into milk. Using the model, the average concentration of dolutegravir in breastmilk over 24 hours 0.050 mg/L (range 0.029-0.10 mg/L) corresponding to an absolute infant dose of 2.2 mcg/kg daily. This corresponds to a weight-adjusted infant dosage of 0.27% of the maternal dose.[4]

Infant Levels. An HIV-positive mother took a combination tablet containing dolutegravir 50 mg, abacavir sulfate 600 mg and lamivudine 300 mg (Triumeq) once daily. Her infant had a plasma dolutegravir concentration of 100 mcg/L during the period of exclusive breastfeeding up to about 30 weeks postpartum. As supplemental feeding was introduced, the plasma concentrations dropped to about 30 mcg/L at 35 weeks, and to 0 with no breastfeeding after about 50 weeks postpartum.[1]

Two HIV-positive women taking dolutegravir (dose not stated, but presumably 50 mg daily) plus 2 unspecified nonnucleoside reverse transcriptase inhibitors breastfed their infants (extent not stated, but presumably exclusively). At 2 weeks postpartum, the plasma levels in one infant were 67.8 mcg/L and 75.5 mcg/L at 4 and 24 hours after the maternal dose, respectively. Two days after drug discontinuation, the infant had a plasma level of 58.6 mcg/L at a time when the maternal plasma level was 103.8 mcg/L. In the other infant, the plasma level was 16.3 mcg/L at 24 hours after the maternal dose.[2]

Seventeen women were receiving oral dolutegravir 50 mg daily as part of a study. Their breastfed infants had serum levels obtained at a median of 10 days postpartum. Their median dolutegravir peak serum concentration was 66.7 mcg/L and minimum was 60.9 mcg/L. After discontinuation of maternal dolutegravir, detectable concentrations were noted in 100%, 80% and 80% of breastfed infants at 48, 72 and 96 hours following final maternal dose, respectively. The ratio of paired maternal and infant serum concentrations was 0.03 at the peak and 0.08 at the trough.[3]

Twenty-one breastfed infants whose mothers were receiving dolutegravir postpartum had a total of 65 serum concentration measured postpartum. Infant serum concentrations were 4.9% of maternal plasma concentration in the first 24 hours after the final maternal dose, increasing to 11% of maternal plasma concentration when measure over the 96 hours after the final maternal dose. The increase indicates a slower drug elimination in infants compared to their mothers.[4]

Effects in Breastfed Infants

An HIV-positive mother took a combination tablet containing dolutegravir 50 mg, abacavir sulfate 600 mg and lamivudine 300 mg (Triumeq) once daily. Her infant was exclusively breastfed for about 30 weeks and partially breastfed for about 20 weeks more. No obvious side effects were noted.[1]

Effects on Lactation and Breastmilk

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

Alternate Drugs to Consider

Lamivudine, Nelfinavir, Nevirapine, Zidovudine

References

1.
Kobbe R, Schalkwijk S, Dunay G, et al. Dolutegravir in breast milk and maternal and infant plasma during breastfeeding. AIDS. 2016;30:2731–3. [PubMed: 27782968]
2.
Gini J, Penchala SD, Amara A, et al. Validation and clinical application of a novel LC-MS method for quantification of dolutegravir in breast milk. Bioanalysis. 2018;10:1933–45. [PMC free article: PMC6949129] [PubMed: 30450920]
3.
Waitt C, Orrell C, Walimbwa S, et al. Safety and pharmacokinetics of dolutegravir in pregnant mothers with HIV infection and their neonates: A randomised trial (DolPHIN-1 study). PLoS Med. 2019;16:e1002895. [PMC free article: PMC6754125] [PubMed: 31539371]
4.
Dickinson L, Walimbwa S, Singh Y, et al. Infant exposure to dolutegravir through placental and breastmilk transfer: A population pharmacokinetic analysis of DolPHIN-1. Clin Infect Dis. 2021;73:e1200–e1207. [PMC free article: PMC8423479] [PubMed: 33346335]

Substance Identification

Substance Name

Dolutegravir

CAS Registry Number

1051375-16-6

Drug Class

Breast Feeding

Lactation

Anti-HIV Agents

Antiviral Agents

Anti-Retroviral Agents

HIV Integrase Inhibitors

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.

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