aldosterone_antags
Table of Contents
aldosterone antagonists (mineralocorticoid receptor antagonists (MRAs) )
see also:
Introduction
- Competitive antagonists of aldosterone (mineralocorticoids) acting on the receptor which is a soluble cytoplasmic protein thereby inhib. the synthesis of physiologically active transport proteins:
- Na-K exchange in distal tubule & collecting duct → incr. Na excretion, decr. K excretion;
- salivary glands
- colon
- may cause clinical hypoaldosteronism and potentially type IV renal tubular acidosis with hyperkalaemia and volume depletion
-
- significantly reduce mortality, hospitalizations, and cardiovascular events in Heart Failure with reduced Ejection Fraction (HFrEF)
- also used for HF with mildly reduced or preserved ejection fraction (HFmrEF/HFpEF)
Examples
spironolactone:
P/K:
- 70% absorbed, significant 1st pass metabolism & enterohepatic circulation;
- extensive plasma protein bound;
- eliminated solely by metabolism to active (canrenone) & inactive (canrenoate) metabolites;
Adverse:
- gynaecomastia, androgen-like effects; minor GIT effects; hyperkalaemia;
Interactions:
- salicylates → decreased tubular secretion canrenone → decreased activity spironolactone;
- high K intake or thiazides+renal impairment → hyperkalaemia;
eplerenone
finerenone
aldosterone_antags.txt · Last modified: 2026/03/16 03:20 by gary1