Rose L I, Underwood R H, Newmark S R, Kisch E S, Williams G H
Ann Intern Med. 1977 Oct;87(4):398-403. doi: 10.7326/0003-4819-87-4-398.
Peripheral blood levels of testosterone, estradiol, luteinizing hormone, and follicle-stimulating hormone and the metabolic clearance rates of testosterone and estradiol, as well as the peripheral conversion of testosterone into estradiol, were measured in 16 patients with hypertension. Six of these patients were treated with spironolactone and developed gynecomastia. The other 10 patients served as control subjects. The blood testosterone level in the spironolactone-treated group (2.7 +/- 0.5 ng/ml) was significantly less (P less than 0.02) than in the control group (4.4 +/- 0.4 ng/ml). On the other hand, blood estradiol levels in the spironolactone group (30 +/- 4 pg/ml) were significantly greater (P less than 0.01) than in the control group (13 +/- 2 pg/ml). These changes were primarily due to significant increases in the metabolic clearance rate of testosterone (P less than 0.02) and in the rate of peripheral conversion of testosterone into estradiol (P less than 0.001) in the spironolactone-treated group. Thus, spironolactone does alter the peripheral metabolism of testosterone resulting in changes in the ratio of testosterone to estradiol, which could contribute to the production of gynecomastia.
对16例高血压患者测定了外周血中睾酮、雌二醇、黄体生成素和卵泡刺激素的水平，以及睾酮和雌二醇的代谢清除率，还有睾酮向雌二醇的外周转化情况。其中6例患者接受螺内酯治疗并出现了男性乳房发育。另外10例患者作为对照。螺内酯治疗组的血睾酮水平（2.7±0.5 ng/ml）显著低于（P<0.02）对照组（4.4±0.4 ng/ml）。另一方面，螺内酯组的血雌二醇水平（30±4 pg/ml）显著高于（P<0.01）对照组（13±2 pg/ml）。这些变化主要是由于螺内酯治疗组中睾酮的代谢清除率显著增加（P<0.02）以及睾酮向雌二醇的外周转化率显著增加（P<0.001）。因此，螺内酯确实会改变睾酮的外周代谢，导致睾酮与雌二醇的比例发生变化，这可能促使男性乳房发育的产生。
