Primaquine Pharmacokinetics in Lactating Women and Breastfed Infant Exposures

Clin Infect Dis. 2018 Sep 14;67(7):1000-1007. doi: 10.1093/cid/ciy235.

Abstract

Background: Primaquine is the only drug providing radical cure of Plasmodium vivax malaria. It is not recommended for breastfeeding women as it causes hemolysis in glucose-6-phosphate dehydrogenase (G6PD)-deficient individuals, and breast milk excretion and thus infant exposure are not known.

Methods: Healthy G6PD-normal breastfeeding women with previous P. vivax infection and their healthy G6PD-normal infants between 28 days and 2 years old were enrolled. Mothers took primaquine 0.5 mg/kg/day for 14 days. Primaquine and carboxyprimaquine concentrations were measured in maternal venous plasma, capillary plasma, and breast milk samples and infant capillary plasma samples taken on days 0, 3, 7, and 13.

Results: In 20 mother-infant pairs, primaquine concentrations were below measurement thresholds in all but 1 infant capillary plasma sample (that contained primaquine 2.6 ng/mL), and carboxyprimaquine was likewise unmeasurable in the majority of infant samples (maximum value 25.8 ng/mL). The estimated primaquine dose received by infants, based on measured breast milk levels, was 2.98 µg/kg/day (ie, ~0.6% of a hypothetical infant daily dose of 0.5 mg/kg). There was no evidence of drug-related hemolysis in the infants. Maternal levels were comparable to levels in nonlactating patients, and adverse events in mothers were mild.

Conclusions: The concentrations of primaquine in breast milk are very low and therefore very unlikely to cause adverse effects in the breastfeeding infant. Primaquine should not be withheld from mothers breastfeeding infants or young children. More information is needed in neonates.

Clinical trials registration: NCT01780753.

Publication types

  • Research Support, American Recovery and Reinvestment Act
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Antimalarials / blood
  • Antimalarials / chemistry
  • Antimalarials / pharmacokinetics*
  • Antimalarials / therapeutic use*
  • Area Under Curve
  • Breast Feeding
  • Child, Preschool
  • Female
  • Humans
  • Infant
  • Infant, Newborn
  • Lactation
  • Malaria, Vivax / drug therapy*
  • Male
  • Milk, Human / chemistry*
  • Primaquine / analogs & derivatives
  • Primaquine / blood
  • Primaquine / chemistry
  • Primaquine / metabolism
  • Primaquine / pharmacokinetics*
  • Primaquine / therapeutic use*
  • Young Adult

Substances

  • Antimalarials
  • 8-(3-carboxy-1-methylpropylamino)-6-methoxyquinoline
  • Primaquine

Associated data

  • ClinicalTrials.gov/NCT01780753