Progestogen preparations themselves do not produce a feminizing effect, but they are often included in the combination therapy of patients with transsexualism, mainly as part of estrogen-gestogenic drugs. In the literature, there are quite contradictory data on the effect of progestins on increasing and breast development in transgender patients. Thus, there is evidence of the proliferative effect of progestins on breast tissue, but the nature of this effect is defined as carcinogenic [Druckmann R., 2003; VON Schoultz B., 2002]. It is proved that natural progesterone does not produce any effect on the mammary glands [de Lignieres V., 2002].
We believe that the targeted administration of progesterone drugs is not appropriate for treating patients with M / W transsexualism due to their lack of a main target organ for progesterone, the uterus, but the presence of progestins in combination oral medications is acceptable and does not have undesirable effects.
In some cases, when it is not possible to use cyproterone acetate, it can be replaced by the progestogen medroxy-progesterone acetate, which has a similar effect to cyproterone acetate, but a less weak antiandrogen. The recommended dose for the treatment of M / F-transgender 5-10 mg / day. Some researchers attribute medroxyprogesterone acetate to drugs of choice.
There is evidence of a positive experience with didrogesterone (20 mg / day) in cases where medroxyprogesterone acetate has a virilizing effect, while patients noted an increase in sexual desire and breast enlargement [A. Lev et al., 2003]. We do not have our own experience of using gestagens in patients with transsexualism.
Flutamide. There are few data on the use of flutamide as a component of transgender-M / F substitution therapy, and for the most part they are based on isolated observations.
Flutamide is an antiandrogenic drug of non-steroid structure. Its mechanism of action is associated with inhibition of androgen uptake and / or inhibition of androgen binding in the nuclei of target tissue cells. Flutamide is used mainly in combination with LH-releasing hormone agonists for prostate cancer in case of failure of other therapies. Its ability to inhibit the action of testosterone at the cellular level is in addition to the drug castration caused by LH-releasing hormone agonists. The target organs of pharmacological action of flutamide are the prostate gland and seminal vesicles. Flutamide does not possess estrogenic, antiestrogenic, progestogenic and anti-progestogenic activity.
This drug is characterized by a fairly wide range of side effects, its use in the treatment of M / F-transsexuals seems to be inappropriate.
Spironolactone. This drug is intended for use as an antihypertensive and diuretic agent. In addition, spironolactone has a weak antiandrogenic effect, less effective when compared with drugs cyproterone acetate. We believe that the use of spironolactone in M / F-transsexuals can be justified only in the case of hypertension or fluid retention in the body. According to various researchers, the dose of spironolactone used in transsexuals can vary from 100 to 400 mg / day.
Side effects of this drug are nausea, spasticity in the gastrointestinal tract, diarrhea, hyperkalemia, increased blood concentrations of urea, creatinine, uric acid, dizziness, headache, drowsiness, ataxia.