Piperaquine use while Breastfeeding

Summary of Use during Lactation

Piperaquine is not approved for marketing in the United States by the U.S. Food and Drug Administration, but is available in other countries. Amounts in milk are very low and should not affect the breastfed infant.

Drug Levels

Maternal Levels. Twenty-seven women received 3 doses containing 320 mg of piperaquine combined with dihydroartemisinin or sulfadoxine-pyrimethamine. Breastmilk was sampled on days 1, 2, 3 to 5, 7 to 11, and 14 to 17 after delivery. Serum concentration data were analyzed using a population pharmacokinetic model (NONMEM) and breastmilk concentrations were estimated from plasma concentrations using the milk-to-plasma ratio. The estimated absolute daily infant dosage was 0.41 mcg/kg, which corresponds to a relative infant dose of 0.004%. The maximum simulated relative infant dosage from any dosing scenario was 2.5%.[1]

A physiologically based pharmacokinetic model has been developed that adequately predicts piperaquine excretion into breastmilk.[2]

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

Atovaquone and Proguanil, Chloroquine, Doxycycline, Mefloquine

References

1.

Moore BR, Salman S, Benjamin J, et al. Pharmacokinetics of piperaquine transfer into the breast milk of Melanesian mothers. Antimicrob Agents Chemother 2015;59:4272-8. [PMC free article: PMC4468664] [PubMed: 25963980]

2.

Almond LM, Abduljalil K, Pansari A, et al. PBPK-led assessment of antimalarial drug concentrations in breastmilk: A strategy for optimal use of prediction methods to guide decision making in an understudied population. CPT Pharmacometrics Syst Pharmacol 2025;14:738–50. [PMC free article: PMC12001273] [PubMed: 39930940]

Substance Name

Piperaquine

CAS Registry Number

4085-31-8

Drug Class

Breast Feeding

Lactation

Milk, Human

Anti-infective Agents

Antiparasitic Agents

Antimalarials

Antiprotozoal Agents