To elucidate the mechanism of action of aldosterone antagonists, we studied the interaction of spironolactone with the chick mineralocorticosteroid receptor (MR). Intestinal cytosol contains specific spironolactone-binding sites (Kd approximately 3 nM; max. no. of binding sites approximately 100 fmol/mg of protein) that have been identified as MRs by competition experiments with steroid ligands...

We showed that spironolactone reduced structural damage and prevented renal dysfunction in chronic cyclosporine (CsA) nephrotoxicity. These findings evidenced an aldosterone renal vascular effect under this condition. To investigate aldosterone's role in modulating renal vascular tone, renocortical vasoactive pathways mRNA levels in chronic CsA nephrotoxicity as well as spironolactone's effect ...

BACKGROUND Drospirenone/ethinyl-estradiol is an oral contraceptive (OC) that possesses unique antimineralocorticoid activity. It is conjectured that drospirenone, taken alone or concomitantly with spironolactone, may be associated with an increased risk of hyperkalemia. METHODS A retrospective cohort study was conducted evaluating women between 18-46 years of age in the Lifelink™ Health Plan ...

OBJECTIVES This study was designed to determine the adequacy of monitoring patients receiving spironolactone as well as spironolactone's relationship to hyperkalemia. BACKGROUND After the Randomized Aldactone Evaluation Study (RALES) demonstrated a 30% mortality benefit for treating severe heart failure patients with spironolactone, acceptance of this drug was overwhelming. Hyperkalemia and w...

The administration of spironolactone, a diuretic steroid, is known to cause a depletion of microsomal cytochrome P-450 in those tissues which have a high activity of steroid 17a-hydroxylase. In this paper, studies are presented to indicate that the sulfur atom located at the carbon 7-a position on the spironolactone molecule is required for the loss of the heme and apoproteins of adrenal or tes...

The spontaneous contractions of the rabbit uterine horns and the human myometrial strips were stimulated by oxytocin and buserelin acetate in isolated preparations. Spironolactone application to these models produced inhibitory effects on the contractions. It is concluded that spironolactone has inhibitory effect on the rabbit uterine horn and the human myometrial strip contractions.

Aldosterone regulates sodium homeostasis by activating the mineralocorticoid receptor (MR), a member of the nuclear receptor superfamily. Hyperaldosteronism leads todeleterious effects on the kidney, blood vessels, and heart. Although steroidal antagonists such as spironolactone and eplerenone are clinically useful for the treatment of cardiovascular diseases, they are associated with several s...

BACKGROUND/AIMS Renin-angiotensin-aldosterone system blockade with a mineralocorticoid-receptor antagonist has not yet been studied in exposure to tobacco smoke (TS) models. Thus, this study investigated the role of spironolactone on cardiac remodeling induced by exposure to tobacco smoke. METHODS Male Wistar rats were divided into 4 groups: a control group (group C, n=11); a group with 2 mon...

This study was designed to assess the effect of the addition of low-dose spironolactone on blood pressure (BP) in patients with resistant arterial hypertension. Patients with office systolic blood pressure (SBP) >140 mm Hg or diastolic blood pressure (DBP)>90 mm Hg despite treatment with at least 3 antihypertensive drugs, including a diuretic, were enrolled in this double-blind, placebo-control...

Spironolactone acts both as a diuretic and as an antihypertensive agent. It may be given alone or with other diuretic agents that act more proximally in the renal tubule. Increased levels of the mineralocorticoid, aldosterone, are present in primary and secondary hyperaldosteronism, Oedematous states in which secondary aldosteronism is usually involved include congestive cardiac failure, hepati...