Related Experiment Video
Updated: Aug 9, 2026

Multiplex Therapeutic Drug Monitoring by Isotope-dilution HPLC-MS/MS of Antibiotics in Critical Illnesses
Published on: August 30, 2018
Transfer of probenecid and cephalexin into breast milk
Kenneth F Ilett1, L Peter Hackett, Bridget Ingle
1Pharmacology Unit, School of Medicine and Pharmacology, University of Western Australia, Crawley, Australia. kilett@meddent.uwa.edu.au
Objective:
To report a case of the transfer of probenecid and cephalexin into human milk.
Case Summary:
A breast-fed infant of a 30-year-old woman being treated with oral probenecid and cephalexin for a breast infection developed severe diarrhea and associated symptoms. To investigate whether the maternal drug treatment was causative, milk was collected over a dose interval at steady-state, and concentrations of probenecid and cephalexin were measured by HPLC. The average concentrations of probenecid and cephalexin in milk were 964 and 745 microg/L, respectively, corresponding to absolute and relative infant doses of 145 microg/kg/day and 0.7% for probenecid and 112 mug/kg/day and 0.5% for cephalexin. The infant's adverse effects were rated as possible for probenecid and probable for cephalexin based on the Naranjo probability scale.
Discussion:
On the basis of the calculated relative infant doses for both probenecid and cephalexin in milk and the notional 10% level of concern for infant exposure, neither drug would be expected to cause significant systemic effects. However, local adverse effects, notably diarrhea, were observed. The Naranjo probability scale rating suggested that cephalexin was more likely than probenecid to be the cause of the infant's diarrhea.
Conclusions:
When using cephalexin/probenecid to treat breast infections in lactating women, clinicians should anticipate the possibility of adverse gastrointestinal effects in the breast-fed infant.
Related Concept Videos
Pharmacokinetics in Pediatric Patients: Drug Excretion
Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption
Drug Elimination by Renal Route: Tubular Secretion
Pharmacokinetics in Pediatric Patients: Drug Distribution
Pharmacokinetics: Drug–Drug Interactions
Pharmaceutical Alternatives: Stability-Related Therapeutic Nonequivalence

