Increased Serum Oestrone and Oestradiol Following Spironolactone Administration in Hypertensive Men

Abstract

The present study was undertaken to evaluate long-term effects of spironolactone on basal serum oestrone, oestradiol, testosterone, LH and prolactin concentrations in hypertensive male patients. Serum prolactin response to TRH was also evaluated. Patients were divided into two groups: a conventional-dosage group, consisting of six males with essential hypertension who took 75 to 150 mg of spironolactone daily for 12 weeks, and a high-dosage group, consisting of two males with idiopathic hyperaldosteronism who took 300 mg of spironolactone daily for more than 40 weeks. In the conventional-dosage group, serum oestrone concentrations significantly increased (P less than 0.01) at 12 weeks, serum oestradiol concentrations gradually increased throughout the study period, however, the increments were not statistically significant (P less than 0.2). Basal serum testosterone, LH and prolactin concentrations were not significantly changed throughout the study period. Enhancement of serum prolactin response to TRH was not found in any of the patients in the conventional-dosage group. In the high-dosage group, serum oestrone maintained high levels from the beginning of this study, and serum oestradiol concentrations increased with the development of gynaecomastia. Serum testosterone, LH and prolactin concentrations did not show any definite change throughout the study period. Thus, long-term spironolactone treatment increased the serum levels of oestrone and oestradiol in hypertensive men followed by the development of gynaecomastia. The elevation in circulating oestrogens could well explain the oestrogenic side-effects of spironolactone treatment.

Circadian Rhythm of Serum Testosterone and Its Relation to Sleep: Comparison with the Variation in Serum Luteinizing Hormone, Prolactin, and Cortisol in Normal Men*

“…The mean immunological potency of LER-907 was 255.0 mlU/jug in the LH assay. The intra-and interassay coefficients of variation of a pool of serum from normal men were 7.0% and 14.0%, respectively (24). The serum PRL concentration was measured by a previously described homologous double antibody RIA (25).…”

“…Serum testosterone was measured by a previously published RIA method (24). The intra-and interassay coefficients of variation of a pool of serum from normal men were 5.64% and 11.2%, respectively.…”

Acquired hemophilia as first manifestation of breast carcinoma in a man under long-term spironolactone therapy

“…Weak inhibition of androgen synthesis and increased conversion of androgens to estrogens were irregularly demonstrated and are probably minor. 10,11 Animal studies have shown an increased rate of neoplasia, including breast carcinoma, in rats on high-dose canrenoate, another aldosterone antagonist which shares a common metabolite (canrenone) with spironolactone. 12 Some cases of breast carcinoma in women under spironolactone therapy have been reported, but this association may only be fortuitous.…”

Diuretics

“…Although several explanations have been provided, the most likely mechanism of these side effects is the lack of specificity of spironolactone as it binds, as already mentioned, not only to the renal aldosterone receptor, but also to the progesterone receptor and the dihydrotestosterone receptor (MIYAKE et al 1978;CORVOL et al 1975;BONNE and RAYNAUD 1974).…”