Eri L M, Haug E, Tveter K J
Department of Surgery, Ullevaal University Hospital, Oslo, Norway.
Br J Urol. 1995 Mar;75(3):335-40. doi: 10.1111/j.1464-410x.1995.tb07345.x.
To study the hormonal changes resulting from long-term use of the non-steroidal anti-androgen Casodex.
A randomized, placebo-controlled study was carried out on 27 patients with benign prostatic hyperplasia (BPH). Fourteen patients received Casodex 50 mg daily for 24 weeks and 13 received a placebo. The patients were followed up for a further 24-week period.
Serum concentrations of luteinizing hormone (LH) increased by an average of 40% while follicle-stimulating hormone (FSH) remained unchanged. Testosterone increased by 35%, oestradiol by 29% and oestrone by 23%; all changes were statistically significant. Levels of androstenedione and dihydrotestosterone increased by 11% and 15%, respectively, but these increases did not reach statistical significance. A non-significant increase was also observed for sex hormone-binding globulin. The hormonal changes were reversible upon discontinuation of therapy. Prolactin and dehydroepiandrosterone-sulphate levels did not change.
This study indicates that Casodex, due to competitive inhibition of central androgen receptors, increases LH secretion, thus causing increased production and increased metabolism of testosterone.
研究长期使用非甾体类抗雄激素药物康士得所导致的激素变化。
对27例良性前列腺增生（BPH）患者进行了一项随机、安慰剂对照研究。14例患者每日服用50毫克康士得，持续24周，13例患者服用安慰剂。患者随后又接受了24周的随访。
促黄体生成素（LH）的血清浓度平均升高了40%，而促卵泡生成素（FSH）保持不变。睾酮升高了35%，雌二醇升高了29%，雌酮升高了23%；所有变化均具有统计学意义。雄烯二酮和双氢睾酮的水平分别升高了11%和15%，但这些升高未达到统计学意义。性激素结合球蛋白也有不显著的升高。停药后激素变化是可逆的。催乳素和硫酸脱氢表雄酮水平未发生变化。
本研究表明，由于康士得对中枢雄激素受体的竞争性抑制作用，它会增加LH的分泌，从而导致睾酮生成增加和代谢加快。
