The excretion of chloroquine and the major metabolite, desethylchloroquine, in breast milk was investigated in eleven lactating mothers following a single oral dose of chloroquine (600 mg base). The average milk to plasma concentration ratio at the 24th hour was 6.6 +/- 2.4 for chloroquine and 1.5 +/- 0.6 for desethylchloroquine in five of the volunteers. In five other volunteers the elimination half-life of chloroquine in milk was 8.8 +/- 4.7 days which was longer than that in saliva (3.9 +/- 1.0 days) from the same volunteers. The maximum daily dose of the drug that the infant can receive from breastfeeding was about 0.7% of the maternal start dose of the drug in malaria chemotherapy. It is, therefore, suggested that it is safe for mothers to breastfeed their infants when undergoing treatment for malaria with chloroquine.