PMID: 590311Dec 2, 1977

Improved method for comparative evaluation of aldosterone antagonists in healthy man

European Journal of Clinical Pharmacology
J Casals-StenzelW Losert

Abstract

A method of assessing the qualitative and quantitative activity of competitive aldosterone antagonists in healthy man is described. It requires intravenous infusion of aldosterone (0.5 mg/6 h), iv and oral water loading for six hours and fractionated collection of urine over eight hours. Aldosterone antagonists were administered orally 1.5 h before the start of the infusion (spironolactone 50, 200 or 800 mg) or added to the infused solution (potassium cnarenoate 300, 600 or 1000-1200 mg). The effect was assessed by changes in urinary sodium and potassium excretion and in urinary Na+/K+ ratio. The plasma levels and urinary excretion of canrenone, canrenoate and canrenoate ester glucuronide, respectively, were determined after administration of spironolactone and potassium canrenoate. Between 4-8 h (spironolactone) or 2-8 h (potassium canrenoate) after commencement of the infusion there was linear dose-dependent reversal of the mineralocorticoid-induced sodium retention and/or decrease in the Na+/K+ ratio. The plasma levels and urinary excretion of the metabolites measured were also dose-dependent. The method appears suitable for comparison of the potency of aldosterone antagonists and for defining the time course of drug action ...Continue Reading

References

Dec 29, 1976·Naunyn-Schmiedeberg's Archives of Pharmacology·U AbshagenG Luszpinski
Oct 1, 1975·Clinical Pharmacology and Therapeutics·L E RamsayM J Tidd
Feb 1, 1976·Clinical Pharmacology and Therapeutics·A KarimM Dooley
Feb 1, 1976·Clinical Pharmacology and Therapeutics·A KarimB J Baltes
Jul 3, 1974·Naunyn-Schmiedeberg's Archives of Pharmacology·W SadéeN Rietbrock
Jan 1, 1974·Naunyn-Schmiedeberg's Archives of Pharmacology·H C Erbler
May 1, 1974·Metabolism: Clinical and Experimental·D J Morris, R P Davis
Aug 1, 1974·Clinical Pharmacology and Therapeutics·W J MroczekF A Finnerty
Jul 1, 1972·Journal of Pharmaceutical Sciences·W SadéeS Riegelman
May 1, 1971·Journal of Pharmaceutical Sciences·A KarimH I Maibach
Nov 1, 1958·The Journal of Clinical Investigation·J T AUGUSTG W THORN
Mar 1, 1964·Proceedings of the Society for Experimental Biology and Medicine·C M KAGAWAM L ANDERSON
Aug 1, 1976·British Journal of Clinical Pharmacology·L E RamsayM J Tidd

Citations

Apr 6, 2004·Journal of the American College of Cardiology·J FletcherJ N Townend

Related Concepts

Aldosterone, (+-)-Isomer
Mineralocorticoid Receptor Antagonists
Spiroctan
Drug Evaluation
Potassium
Sodium
Spiro von ct

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