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Indacrinone: Natriuretic and Uricosuric Effects of Various Ratios of Its Enantiomers in Healthy Men
Author(s) -
Vlasses Peter H.,
Rotmensch Heschi H.,
Swanson Brian N.,
Irvin John D.,
Johnson Cynthia L.,
Ferguson Roger K.
Publication year - 1984
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1984.tb03374.x
Subject(s) - hydrochlorothiazide , uricosuric , enantiomer , diuretic , chemistry , endocrinology , natriuresis , placebo , uric acid , medicine , pharmacology , kidney , hyperuricemia , blood pressure , stereochemistry , alternative medicine , pathology
Indacrinone is an investigational loop‐acting diuretic. To evaluate the natriuretic and uricosuric effects of varying ratios of its enantiomers, 10 healthy men, on a controlled Na (100 mEq) and K (80 mEq) diet, participated in a double‐blind, randomized, balanced incomplete block, multiple‐dose (one week) study of a fixed daily dose (10 mg) of (–) enantiomer combined with increasing doses (40, 90 and 140 mg) of (+) enantiomer versus 50 mg hydrochlorothiazide and placebo. On day 1, mean 24‐h urinary Na increased (p < 0.01) comparably (–285 mEq) after each enantiomer combination and hydrochlorothiazide; however, the enantiomer combinations had marked uricosuric and hypouricemic effects that were enhanced with increased (+) enantiomer doses. By day 7, while enantiomer combinations and hydrochlorothiazide demonstrated comparable natriuretic activity, mean serum uric acid levels (mg/dl), in comparison to placebo, were increased (p < 0.05) with hydrochlorothiazide but progressively decreased with increases in (+) enantiomer. Thus varying the ratio [(+, uricosuric):(–, natriuretic)] of the enantiomers of indacrinone caused natriuresis similar to hydrochlorothiazide, but had an opposite effect on serum uric acid.