Relationship of Plasma Aldadiene Levels and Antimineralocorticoid Effects of Spironolactone in the Laboratory

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Abstract
Relationship of renal antimin-eralocorticoid effects with spironolactone and plasma levels of its δ6-metabolite, aldadiene, was investigated in adrenalectomized rats and in intact dogs treated with DCA. In comparative tests, spironolactone and aldadiene both given orally produced equal plasma levels of aldadiene, but unequal mineralocorti-coid-blocking effects. Potency ratios of approximately 3/1 and 5/1 were found for renal properties of spironolactone/aldadiene in rats and dogs, respectively. Interpretation of these data indicate that blocking activity of spironolactone is only partly accounted for by plasma titers of aldadiene.