Testosterone Therapy: Oral Androgens

«Old» oral forms of methylated testosterone (methyltestosterone, fluoxymesterone) should not be used due to their high hepatotoxicity. Modern oral forms of testosterone (testosterone undecanoate), according to their pharmacodynamic properties (absorbed from the intestine via the lymphatic route, thus circumventing the first-pass inactivation by the liver), have a good hepatic safety profile. The pharmacokinetic characteristics of oral testosterone undecanoate do not allow maintaining an adequate sufficient plasma level of testosterone during the day in men with moderate or severe symptomatic hypogonadism, so its application is limited by mild age-related hypogonadism. Oral testosterone undecanoate can be used in boys with delayed sexual and/or physical maturation given the fact that it has no impact on the gonadotropic function. An effective off-label use of oral testosterone undecanoate is possible for treatment of women with androgen deficiency. The diagnosis of female androgen deficiency has an unconditional right to exist and should be established primarily on the basis of clinical symptoms of testosterone deficiency, which are not age-dependent. The primary indication for testosterone in women is decreased libido and sexual dysfunction, regardless of age, excluding the other known causes of reduced libido, such as hypothyroidism, hyperprolactinemia, depression, etc. Taking into account a lower requirement of testosterone in women as compared to men, oral testosterone undecanoate can be effectively adapted for use in women (once every 1–2 days) based on the clinical indication of testosterone deficiency and response to therapy. Oral testosterone undecanoate therapy in women of any age is safe and well tolerated.