US EPA

517327 

Journal Article 

Safety aspects of androgen treatment with 5 alpha-dihydrotestosterone 

Sakhri, S; Gooren, LJ 

2007 

Yes 

Andrologia
ISSN: 0303-4569
EISSN: 1439-0272 

39 

6 

216-222 

English 

5 alpha-Dihydrotestosterone (DHT), the most powerful naturally occurring androgen, is commercially available since 1982 as a gel. In view of its considerably higher biopotency (three to six times) than of testosterone, side effects, particularly on the main target organ of androgens, the prostate, are anticipated. In fact, DHT appears to be a prostate-sparing androgen for two reasons. Unlike testosterone, it does not undergo any further amplification in biopotency through 5 alpha reduction in the prostate. Secondly, it is likely to lead to less aromatisation of testosterone to oestradiol in the prostate, thus reducing local oestradiol concentrations. Oestrogens have been implicated in the aetiology of benign prostate hyperplasia and prostate cancer. However, aromatisation of testosterone has appeared to be essential for the maintenance of bone mineral density. Administration of DHT reduces circulating oestradiol levels, but the levels remain above the levels critical for the antiresorptive effect of oestrogens on bone. Effects of DHT on erythropoiesis and on lipids are very similar to those of testosterone. Safety concerns regarding androgen treatment with DHT are similar to those of treatment with testosterone, while the effects of DHT on the prostate are likely to be less biopotent. 

androgen treatment; dihydrotestosterone; drug safety; prostate; congenital estrogen deficiency; hypogonadal men; transdermal; dihydrotestosterone; testosterone gel; therapeutic implications; percutaneous-absorption; prostatic hyperplasia; replacement therapy; double-blind; elderly-men