The concentration of canrenone, a principal metabolite of spironolactone, was determined in human serum and milk. The milk to serum concentration ratios of this metabolite were 0.72 at 2 hr and 0.51 at 14.5 hr after ingestation of spironolactone. It was estimated that the maximum quantity of canrenone ingested daily by a human infant via its mother's milk would be approximately 0.2% of the daily dose of spironolactone given to the mother.