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Drugs in Lactation


One impediment to breastfeeding is the lack of information on the use of many drugs during lactation, especially newer ones. The principles of drug passage into breastmilk are well established, but have often not been optimally applied prospectively. Commonly used preclinical rodent models for determining drug excretion into milk are very unreliable because of marked differences in milk composition and transporters compared to those of humans. Measurement of drug concentrations in humans remains the gold standard, but computer modeling is promising. New FDA labeling requirements present an opportunity to apply modeling to preclinical drug development in place of conventional animal testing for drug excretion into breastmilk, which should improve the use of medications in nursing mothers.

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Area under the concentration-time curve


Total body drug clearance


Drug concentration in plasma


Cytochrome P450 2D6




U.S. Food and Drug Administration


Human immunodeficiency virus


Infant to maternal plasma concentration ratio


Milk to plasma concentration ratio


Physiologically based pharmacokinetic


Pregnancy and Lactation Labeling Rule


Population pharmacokinetics


Quantitative structure-activity relationship


Relative infant dose


World Health Organization


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Correspondence to Philip O. Anderson.

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The author thanks Edmund Capparelli, Pharm. D. for his review of the manuscript and helpful suggestions. The author declares no competing financial interests.

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Guest Editor: Sara Eyal

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Anderson, P.O. Drugs in Lactation. Pharm Res 35, 45 (2018).

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  • breast feeding
  • drug excretion
  • human milk
  • modeling
  • pharmacokinetics