Benefits associated with lowered serum DHT levels after 5α-reductase inhibitor (5AR-I) therapy in men have contributed to a misconception that circulating DHT levels are an important stimulus for androgenic action in target tissues (e.g., prostate). Yet evidence from clinical studies indicates that intracellular concentrations of androgens (particularly in androgen-sensitive tissues) are essentially independent of circulating levels. To assess the clinical significance of modest elevations in serum DHT and the DHT/testosterone (T) ratio observed in response to common T replacement therapy, a comprehensive review of the published literature was performed to identify relevant data. Although the primary focus of this review is about DHT in men, we also provide a brief overview of DHT in women. The available published data are limited by the lack of large, well-controlled studies of long duration that are sufficiently powered to expose subtle safety signals. Nonetheless, the preponderance of available clinical data indicates that modest elevations in circulating levels of DHT in response to androgen therapy should not be of concern in clinical practice. Elevated DHT has not been associated with increased risk of prostate disease (e.g., cancer or benign hyperplasia) nor does it appear to have any systemic effects on cardiovascular disease safety parameters (including increased risk of polycythemia) beyond those commonly observed with available T preparations. Well-controlled, long-term studies of transdermal DHT preparations have failed to identify safety signals unique to markedly elevated circulating DHT concentrations or signals materially different from T.

中文翻译：

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二氢睾酮：血液水平升高的生物化学、生理学和临床意义。


男性接受 5α-还原酶抑制剂 (5AR-I) 治疗后，与血清 DHT 水平降低相关的益处导致了一种误解，即循环 DHT 水平是靶组织（例如前列腺）雄激素作用的重要刺激因素。然而临床研究的证据表明，细胞内雄激素浓度（特别是在雄激素敏感组织中）基本上与循环水平无关。为了评估普通 T 替代疗法引起的血清 DHT 和 DHT/睾酮 (T) 比率适度升高的临床意义，我们对已发表的文献进行了全面回顾，以确定相关数据。尽管本次综述的主要焦点是男性的 DHT，但我们也对女性的 DHT 进行了简要概述。可用的已发表数据受到限制，因为缺乏大规模、长期、控制良好的研究，这些研究有足够的动力来揭示微妙的安全信号。尽管如此，现有的大量临床数据表明，雄激素治疗引起的 DHT 循环水平适度升高不应在临床实践中引起关注。 DHT 升高与前列腺疾病（例如癌症或良性增生）风险增加无关，也似乎对心血管疾病安全参数（包括红细胞增多症风险增加）产生任何系统性影响（超出现有 T 制剂常见的影响）。对透皮 DHT 制剂进行良好控制的长期研究未能识别出循环 DHT 浓度显着升高所特有的安全信号或与 T 存在重大差异的信号。