Corvol P, Mahoudeau J A, Valcke J C, Ménard J, Bricaire H
Nouv Presse Med. 1976 Mar 13;5(11):691-4.
Spirolactones (spironolactone, potassium canrenoate) may produce secundary sexual effects such as gynecomastia in man and menstrual disturbances in women. The mechanism of action of the antiandrogenic effects has been studied in man and rat. Acute i.v. injection of potassium canrenoate into man results in a decrease of plasma testosterone, without any change of gonadotropins. This decrease might be due to an impaired testicular steroidogenesis. On the other hand, spirolactones have an antiandrogenic effect at the target cells level. They do not modify the prostate 5alpha-reductase activity; however, they do inhibit the binding of androgens to their receptors. Thus the spirolactones interact with both biosynthesis and peripheral action of androgens.
螺内酯类药物（螺内酯、坎利酸钾）可能会产生继发性性效应，如男性乳腺增生和女性月经紊乱。抗雄激素作用的机制已在人和大鼠身上进行了研究。对人静脉内急性注射坎利酸钾会导致血浆睾酮水平降低，而促性腺激素水平无任何变化。这种降低可能是由于睾丸类固醇生成受损所致。另一方面，螺内酯类药物在靶细胞水平具有抗雄激素作用。它们不会改变前列腺5α-还原酶的活性；然而，它们确实会抑制雄激素与其受体的结合。因此，螺内酯类药物与雄激素的生物合成和外周作用均相互作用。
