Testosterone by Alexandre Hohl

Author:Alexandre Hohl
Language: eng
Format: epub
Publisher: Springer International Publishing, Cham

The creation a testosterone ester has opened new opportunities in oral therapy. The absence of hepatotoxicity significantly enhanced the effectiveness of the therapy due to the possibility of increasing the dose of the drug, as hepatotoxicity inevitably increased with the increase in the dose of the methylated derivatives. Moreover, testosterone undecanoate is absorbed from the intestine not into the blood, but into the lymph, which excludes the hepatic first-pass metabolism with generation of toxic hepatic metabolites typical of all previously used oral 17-C-methylated derivatives of testosterone [22–24].

Because testosterone undecanoate is an ester of natural testosterone, following its administration plasma levels of both testosterone and all its active natural metabolites, such as5-α-DHT and estrogens, increase due to its ability of aromatization by fat tissue (conversion to estrogens) [23, 25].

All the above beneficial properties of oral testosterone undecanoate made it widely used in many countries worldwide, although, for example, the drug has never been approved in the US for clinical use [26] (Table 10.1).Table 10.1Comparison of oral (methyltestosterone, mesterolone, testosterone undecanoate), transdermal, and injectable drugs (testosterone propionate and testosterone undecanoate)

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