For most agents with CNS activity, there are limited data regarding their safety in breastfeeding. Any decision to institute treatment for a neurological or psychiatric disorder must weigh the benefits of maternal treatment against the potential harm to the breastfeeding mother of withholding medication which may improve her illness. For the neonate, one must balance the risk of medication exposure against the benefit of receiving breast milk. Most tricyclic antidepressants can be used in lactating women. Because of the limited data, selective serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitors should only be used with due consideration of the potential adverse effects. Breastfeeding is best avoided by women who require lithium therapy, because of both the immature excretory systems in the infant and relatively high doses received by the infant. There is little information about the safety of antipsychotic medications in breastfeeding. Concerns include toxicity and abnormal neurological development in the infant. These agents may be used with caution. Most agents which cause depression of the CNS, including opiates and sedatives, can be used in small doses and for short courses in breastfeeding mothers. Most anticonvulsants can be used in lactating women. Reference texts and consultation with experts are useful adjuncts to discussion of the risks and benefits of therapy with the patient. The scope of this review is limited to drugs with therapeutic uses, thus drugs of abuse are not discussed, nor are caffeine and alcohol (ethanol).