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The advantages of breastfeeding to the mother and newborn are many. Lactating mothers frequently ask about the safety of taking medications and the risk to their newborn. It is well established that all drugs are excreted into breast milk. However, most medications appear in only small amounts within the breast milk. With the availability of numerous resources on drug use while breastfeeding, a medication can be identified as contraindicated or compatible with breastfeeding. By understanding the anatomy of the breast, principles of lactation, and drug passage into breast milk, an approach to minimize the transfer of the medications in the breast milk to the newborn can be developed. The plan should usually support and encourage the mother to continue to breastfeed her infant.