Tissue distribution of 3H-canrenoate potassium in rabbits.

Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenone. Both were eliminated from plasma and other tissues with a half-life of about 1 hr. Plasma concentrations of both drugs were equal as early as 10 min after intravenous drug administration. Canrenone was concentrated about 10-fold in organ tissues when compared to plasma, while no such preferential uptake was found with canrenoate. Total 3H-activity declined slowly in all tissues with a half-life of approximately 15 hr, indicating extensive metabolism and metabolite retention in the rabbit.