Free Estradiol Increase with Concomitant Decrease of Free Testosterone in Plasma from Normal Men after Incubation with Spironolactone

Antiandrogens and Hirsutism

“…This pharmacological property then has been demonstrated in vitro and clini cally exploited in prostate carcinoma, and in precocious puberty. Additional data in favor of its antiandrogenic effect were reported by our group in 1983 [7], In fact, this drug is able to increase free estradiol with a concom itant decrease in free testosterone after in vitro incubation in plasma from healthy males in an equilibrium dialysis assay ( fig. 4).…”

Female Hirsutism: Pathophysiological Considerations and Therapeutic Implications*

“…Evron later expressed the opinion that the ¥ffect of SP on the binding of steroids to plasma proteins "would account for an increase of the conversion of T into 3B 2 leading to ovulation (196)(197)(198). Our findings would "not support this opinion (139).…”

“…By contrast, Biffignandi et al have recently demonstrated that SP increases free E 2 and decreases free T in an in vitro equilibrium dialysis system (Fig. 6) (139).…”

“…Whereas, in men FSH and LH were observed to rise (149), an irregular and anovulatory pattern was seen in hirsute females (188). As mentioned before, "Blffignandi et al (139) have reported an increase in free estradiol coupled with a decrease in free T after in vitro mcubation of plasma from healthy males with SP. This finding may account for the androgen/estrogen inbalance seen after the administration of the drug which enhances the peripheral blockade of androgen receptors.…”

Spironolactone therapeutic effect in the hyperandrogenism syndrome

“…Как указано выше, это скорее всего связано с повышением конверсии Т в эстрогены. Предполагают также, что СЛ может обладать потенциаль ной возможностью вытеснять Е2 из связи с ТЭСГ, таким об разом увеличивая содержание свободногобиологически активногоэстрогена [11].…”