Transfer of metyrapone and its metabolite, rac-metyrapol, into breast milk

Metyrapone, an inhibitor of corticosteroid biosynthesis, is used in the diagnosis and treatment of adrenocortical hyperfunction. The authors describe the excretion of metyrapone and its metabolite, rac-metyrapol, in milk from a lactating woman requiring metyrapone treatment (250 mg 4 times daily). At steady state, the average concentrations in milk and absolute and relative infant doses were 11 µg/L, 1.7 µg/kg/d, and 0.02%, respectively, for metyrapone, and 48.5 µg/L, 7.3 µg/kg/d, and 0.08%, respectively, for rac- metyrapol. The findings suggest that maternal metyrapone use during breastfeeding is extremely unlikely to be a significant risk for the breastfed infant.