Tubuläre Wirkungen und renale Elimination von Spirolactonen

Hollmann, G.; Senft, G.; Werner, C.

doi:10.1007/bf02308488

Cited by 14 publications

(2 citation statements)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It has been shown in rats that the activity of spironolactone relates more closely to metabolite levels in the renal tubular fluid than to those in plasma and that reduction of tubular fluid levels (by blocking active tubular secretion) reduces the anti mineralocorticoid activity of spironolactone. 9 The implication of this work is that the active metabolites of spironolactone reach their site of activity in the distal renal tubule not only from plasma but also via the renal tubular lumen. 9 Since the presumed precursors of the sulfur-containing metabolites of spironolactone have intrinsic activity5, 8 and a high renal clearance,24 we suggest that they may account for the major part of the activity of spironolactone through their efficient delivery to the distal renal tubule.…”

Section: Discussionmentioning

confidence: 97%

“…9 The implication of this work is that the active metabolites of spironolactone reach their site of activity in the distal renal tubule not only from plasma but also via the renal tubular lumen. 9 Since the presumed precursors of the sulfur-containing metabolites of spironolactone have intrinsic activity5, 8 and a high renal clearance,24 we suggest that they may account for the major part of the activity of spironolactone through their efficient delivery to the distal renal tubule. We have discussed the limitations of the information obtained in studies of this nature elsewhere 19 , 20 and would re-emphasize that the results cannot be extrapolated automatically to the clinical situation.…”

Section: Discussionmentioning

confidence: 97%

See 1 more Smart Citation

Spironolactone and potassium canrenoate in normal man

Ramsay¹,

Shelton²,

Harrison³

et al. 1976

Clin Pharma and Therapeutics

View full text Add to dashboard Cite

The pharmacological activity of single doses of the two aldosterone antagonists, potassium canrenoate and spironolactone, was examined in two studies in healthy volunteers. Both drugs were active in reversing urinary electrolyte changes induced by fludrocortisone in periods 2 to 16 hr after treatment. Potassium canrenoate was significantly less potent that spironolactone on a weight or molar basis, with best estimates of the relative potency potassium canrenoate: spironolactone of approximately 0.3:1. On a weight basis the two drugs yielded plasma levels of the metabolite canrenone which were approximately equivalent. The results indicate that canrenone is not the principal pharmacologically active metabolite of spironolactone. Our study suggests that a major part of the renal antimineralocorticoid activity of spironolactone may be attributable to minor sulfur-containing metabolites or their precursors having a high renal clearance that affords access to their site of activity via the renal tubular fluid.

show abstract

Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 97%

Spironolactone and potassium canrenoate in normal man

Ramsay¹,

Shelton²,

Harrison³

et al. 1976

Clin Pharma and Therapeutics

View full text Add to dashboard Cite

show abstract

Effect of Micronization on the Bioavailability and Pharmacologic Activity of Spironolactone

McInnes¹,

Asbury²,

Ramsay³

et al. 1982

The Journal of Clinical Pharma

View full text Add to dashboard Cite

The bioavailability and pharmacologic activity of tablets containing micronized spironolactone chemical (median particle size 2.21 micrometers) were compared to those of tablets made from standard spironolactone chemical (median particle size 78.8 micrometers) in healthy men. Apart from particle size, all features of these tablets were identical. After 200-mg single doses, the bioavailability of micronized tablets was significantly higher than that of standard tablets. Furthermore, as assessed by 24-hour urine log10 10 Na/K ratio, the pharmacologic activity of micronized spironolactone was significantly greater than that of the standard formulation. The significant influence on renal antimineralocorticoid activity of raised plasma and urinary levels of canrenone, quantitatively the major active metabolite of spironolactone in man, emphasizes the clinical importance of the bioavailability of spironolactone preparations. Since this study, the process used in the manufacture of spironolactone (Aldactone) tablets has been under review.

show abstract

Aldosteron-Antagonisten

Herken¹

1969

Diuretica

View full text Add to dashboard Cite

Tubuläre Wirkungen und renale Elimination von Spirolactonen

Cited by 14 publications

References 11 publications

Spironolactone and potassium canrenoate in normal man

Spironolactone and potassium canrenoate in normal man

Effect of Micronization on the Bioavailability and Pharmacologic Activity of Spironolactone

Aldosteron-Antagonisten

Contact Info

Product

Resources

About