Drospirenone and its antialdosterone properties.
Drospirenone is a unique progestogen derived from 17alpha-spirolactone, with a pharmacologic profile very similar to that of endogenous progesterone. In contrast with other available progestins, drospirenone is a progestogen with aldosterone receptor antagonism (PARA) through its affinity for the mineralocorticoid receptor. It is thus able to act on the renin-angiotensin-aldosterone system (RAAS), which prevents excessive sodium loss and regulates blood pressure. Estrogen acts on the RAAS to stimulate the synthesis of angiotensinogen, which increases aldosterone levels and promotes sodium and water retention. When these effects are unopposed, for example during estrogen replacement therapy, they can lead to increases in weight and blood pressure. The antialdosterone properties exhibited by drospirenone promote sodium excretion and prevent water retention, conferring potential blood pressure benefits. In addition to its effects on the kidney, aldosterone has effects on the vasculature, myocardium and central nervous system, which may elicit a variety of pathophysiologic processes associated with cardiovascular disease. The antialdosterone properties of drospirenone may therefore confer additional cardiovascular benefits beyond the RAAS system. The combined actions of drospirenone on sodium and water retention and cardiovascular parameters make it a more attractive therapeutic option as a component of hormone replacement therapy than other synthetic progestins.
Genazzani
A R
AR
Department of Obstetrics and Gynecology, University of Pisa, Pisa, Italy.
Mannella
P
P
Simoncini
T
T
D000736:Androstenes / Q000494:pharmacology*; D002319:Cardiovascular System / Q000187:drug effects; D005260:Female; D006801:Humans; D000451:Mineralocorticoid Receptor Antagonists / Q000494:pharmacology*; D052250:Nitric Oxide Synthase Type III / Q000187:drug effects / Q000378:metabolism; D012084:Renin-Angiotensin System / Q000187:drug effects*
D000736:Androstenes; D000451:Mineralocorticoid Receptor Antagonists; D052250:Nitric Oxide Synthase Type III; C035144:drospirenone