Pharmacokinetics of caffeine in breast milk and plasma after single oral administration of caffeine to lactating mothers

Abstract

Six healthy lactating women ranging in age from 28 to 35 years were selected to participate in the study. The women had been nursing their infants from 3 1/2 weeks up to 17 weeks. On the morning of the study each participant received 100 mg dose of caffeine. The oral dose of caffeine was taken with a glass of water on an empty stomach. Blood samples were collected from zero time to 24 h after caffeine administration. Each subject aseptically collected breast milk from the right and left breasts by manual expression or using a mechanical breast pump, from zero time to 24 h after caffeine administration. Caffeine in plasma and breast milk was determined by gas liquid chromatography using nitrogen phosphorous detection. Caffeine was rapidly absorbed producing plasma time to peaks ranging from 0.50 to 1.00 h, with values for peak concentrations between 3.60 and 6.15 micrograms ml-1 in plasma. In breast milk, time to peak ranged from 0.75 to 2.00 h and concentration values between 1.98 and 4.30 micrograms ml-1. No significant differences were found between attainment of the time of the peak in plasma and breast milk, p greater than 0.05. In addition, peak concentration for the right and left breast were not statistically different, p greater than 0.05. However, significant differences, p less than 0.05, between plasma and both breasts in regards to the peak concentrations were found. The overall breast milk/plasma ratio obtained from the respective area under the curves were 0.815 +/- 0.0521 and 0.809 +/- 0.202 for the right and left breast, respectively, and no statistical differences were observed between the right and left breasts, p greater than 0.05. In summary, caffeine is rapidly transferred to breast milk. Multiple dose studies are needed to provide more information about caffeine concentration in breast milk of women who receive multiple doses of caffeine or who chronically consume caffeine.

The physiology of the normal human breast: an exploratory study

“…In serum, caffeine levels and kinetic profile were comparable to literature values, where levels are typically between 1.5 and 6.2 μg/mL and are highest approximately 30-60 min after ingestion (Fig. 1a, b) [24,30,32,33].…”

“…These levels in ductal fluid differ dramatically from reported caffeine levels in breast milk, where milk/serum ratios are typically between 0.5 and 0.9 (Fig. 1a) [3,30,32,33]. Although our population was diverse in regard to parity and menopausal status, we were unable to analyze the influence of these factors due to the small number of women studied.…”

Liquid chromatography/electrospray ionization tandem mass spectrometry assay for determination of nicotine and metabolites, caffeine and arecoline in breast milk

“…Caffeine (CAF) is known to be consumed by pregnant and lactating mothers in large quantities in beverages and in prescription and non‐prescription drugs despite the suggestion that its consumption should be reduced during pregnancy 16, 17. The elimination of CAF is surprisingly slow in the newborn due to an immaturity in the hepatic N‐demethylation metabolic pathway, implying that the breast‐fed newborns with a significant daily intake of CAF via maternal breast milk could potentially accumulate toxic concentrations of CAF with consequent adverse reactions 18, 19…”

Breast Milk and Hair Testing to Detect Illegal Drugs, Nicotine, and Caffeine in Donors to a Human Milk Bank

“…The low correlation between the 2 different matrices regarding the presence of caffeine may be due to the narrow exposure window in donor milk (5 or 6 hours after having the drink [16][17][18] ) compared with the wider detection window in hair (months, depending on hair length). It may also be due to potential interindividual variability in caffeine metabolism among the donors.…”