Literature DB >> 7332740

Quantitative comparison of aldosterone antagonists in normal human subjects: prediction of therapeutic potency.

G T McInnes, I R Harrison, J R Shelton, R M Perkins.   

Abstract

1 The potency of single doses of the aldosterone antagonist SC8109 relative to spironolactone in reversing the urinary electrolyte effects of fludrocortisone was examined in a double-blind, balanced, crossover study in six healthy volunteers. 2 For the urinary ratio log10 10Na/K, the relative potency of SC8109; spironolactone on a weight basis was 0.08:1 (95% confidence limits 0.04--0.13:1). 3 The potency of SC8109 relative to spironolactone for natriuresis and antikaliuresis was 0.10:1 and 0.05:1, respectively. 4 The results show excellent agreement with clinical experience where SC8109 was considered to have one tenth the potency of spironolactone. We suggest that the human bioassay employed in this study provides quantitative information which should be predictive of the therapeutic potency of aldosterone antagonists.

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Year:  1981        PMID: 7332740      PMCID: PMC1401948          DOI: 10.1111/j.1365-2125.1981.tb01299.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  24 in total

1.  Human assay of electrolyte-active steroids and their antagonists.

Authors:  E J ROSS
Journal:  Clin Sci       Date:  1962-10       Impact factor: 6.124

2.  Aldosterone antagonism by 17-spirolactosteroids.

Authors:  J D SLATER
Journal:  Postgrad Med J       Date:  1960-06       Impact factor: 2.401

3.  The use of a steroidal spirolactone in the treatment of ascites in hepatic cirrhosis.

Authors:  D N KERR; A E READ; R M HASLAM; S SHERLOCK
Journal:  Lancet       Date:  1958-11-22       Impact factor: 79.321

4.  Aldosterone antagonists.

Authors:  C L GANTT
Journal:  N Y State J Med       Date:  1961-03-01

5.  Antagonism between the effect of aldosterone and a synthetic steroid lactone on the renal excretion of sodium and potassium in man.

Authors:  E J ROSS; J E BETHUNE
Journal:  Lancet       Date:  1959-01-17       Impact factor: 79.321

6.  The use of an aldosterone antagonist in patients with cirrhosis.

Authors:  M R PLAYOUST; C R BLACKBURN
Journal:  Australas Ann Med       Date:  1960-02

7.  The sodium excretion defect in hepatic cirrhosis as studied by the use of a steroidal lactone.

Authors:  S HELLMAN; W W FALOON
Journal:  J Lab Clin Med       Date:  1960-06

8.  Blocking the renal electrolyte effects of mineralocorticoids with an orally active steroidal spirolactone.

Authors:  C M KAGAWA
Journal:  Endocrinology       Date:  1960-07       Impact factor: 4.736

9.  Bioassay of adrenal cortical steroids on the basis of electrolyte excretion by rats: effects of 11-desoxy and 11-oxy-steroids.

Authors:  B B JOHNSON
Journal:  Endocrinology       Date:  1954-02       Impact factor: 4.736

10.  A comparison of the use of Aldactone and Aldactone A in the treatment of hepatic ascites.

Authors:  S SHALDON; J A RYDER; M GARSENSTEIN
Journal:  Gut       Date:  1963-03       Impact factor: 23.059

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  1 in total

1.  Spironolactone dose-response relationships in healthy subjects.

Authors:  G T McInnes; R M Perkins; J R Shelton; I R Harrison
Journal:  Br J Clin Pharmacol       Date:  1982-04       Impact factor: 4.335

  1 in total

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