Testosterone undecanoate and testosterone enanthate injections are both effective and safe in transmen over 5 years of administration.

OBJECTIVE: To retrospectively evaluate and compare safety and efficacy of short and long-acting testosterone (T) parenteral formulations over 5 years in transmen. DESIGN AND METHODS: Fifty transmen between 21 and 42 years of age were enrolled. Twenty-five received T undecanoate 1000 mg IM (weeks 0 and 6 then every 12-16 weeks), and 25 received T enanthate 250 mg IM (every 3-4 weeks). Hormonal and biochemical parameters, anthropometric characteristics and blood pressure were assessed at baseline and then every 12 months. Body composition was evaluated at baseline and then after 1, 3 and 5 years of T treatment. Global satisfaction was assessed at baseline and after 1 and 5 years. RESULTS: Both T formulations led to amenorrhoea in all subjects within 1 year of T administration. Both T treatments led to a similar increase in haemoglobin and haematocrit which always remained within the physiological range. T administration was associated with an increase in total cholesterol, low-density lipoprotein cholesterol and triglycerides and a slight reduction in high-density lipoprotein cholesterol. Coagulative and glucidic profiles and blood pressure did not change significantly in either group. Body weight and BMI showed a slight but not significant increase in both groups, while lean mass rose significantly in both groups. Global satisfaction was increased at years 1 and 5 in both groups. CONCLUSIONS: Preliminary results from this pilot study suggest that administration of either TU or TE for 5 years in young transmen is both effective and safe. Our study presents the longest follow-up published so far reporting no adverse events and these data are consistent with previous reports with a shorter follow-up.

Cyproterone acetate vs leuprolide acetate in combination with transdermal oestradiol in transwomen: a comparison of safety and effectiveness.

OBJECTIVE: To retrospectively compare the effectiveness and safety of 1-year administration of transdermal oestradiol (TE) with cyproterone acetate (CPA) or leuprolide acetate (Leu) in transwomen. DESIGN, PATIENTS AND MEASUREMENTS: Forty transwomen received 50 mg of CPA daily orally (n = 20; CPA+E group) or Leu at a dose of 3·75 mg i.m. monthly (n = 20; Leu+E group) in combination with TE at a dose of 1 or 2 mg daily for 1 year. Reproductive hormones, biochemical parameters, body composition and bone mineral density were assessed. RESULTS: LH, FSH and total testosterone levels were significantly decreased by month three of hormone administration in both groups and continued to decrease until month 12; the decrease in LH levels in the first 12 months was significantly faster in the Leu+E group. Prolactin was significantly increased at month 12 in the CPA+E group only. Bone metabolism parameters and bone mineral density as detected at DEXA did not significantly change in either group, apart from a statistically significant increase in parathyroid hormone after 52 weeks of Leu administration. Total cholesterol and HDL-cholesterol were significantly increased in the Leu+E group and reduced in the CPA+E group. No major adverse effects were registered in either group. Psychological well-being parameters did not differ between the two groups. CONCLUSIONS: Preliminary results from this retrospective observational pilot study suggest that CPA and Leu in combination with TE are equally effective in the suppression of gonadotrophins and testosterone levels over 1 year. Whether the different effects on HDL-cholesterol may lead to long-term different cardiovascular safety profiles remains to be defined.

A prospective study on sexual function and mood in female-to-male transsexuals during testosterone administration and after sex reassignment surgery.

Testosterone administration in female-to-male transsexual subjects aims to develop and maintain the characteristics of the desired sex. Very little data exists on its effects on sexuality of female-to-male transsexuals. The aim of this study was to evaluate sexual function and mood of female-to-male transsexuals from their first visit, throughout testosterone administration and after sex reassignment surgery. Participants were 50 female-to-male transsexual subjects who completed questionnaires assessing sexual parameters and mood. The authors measured reproductive hormones and hematological parameters. The results suggest a positive effect of testosterone treatment on sexual function and mood in female-to-male transsexual subjects.

Effect of long-term testosterone administration on the endometrium of female-to-male (FtM) transsexuals.

INTRODUCTION: Long term safety of testosterone (T) administration in women is still unknown. In particular few and discordant data exists on the effects of T on the endometrium. AIM: The aim of this study was to investigate the effects of long-term T treatment on endometrium histology and proliferation in female to male transsexual subjects (FtM). We compared these endometria with those of young women in the proliferative phase (PM) of the cycle and with those of post menopausal women (M). METHOD: Endometrial samples from 27 FtM treated with T (intramuscular injection of 100 mg Testoviron Depot /10 days for at least one year), 30 M undergoing vaginal hysterectomy, and 13 PM undergoing hysteroscopy for infertility problems were collected. Endometrial proliferation was evaluated on the basis of histopathology and expression of the proliferation marker Ki-67. Both M and PM women had not received any hormonal treatment for at least one year. MAIN OUTCOME MEASURE: Circulating total testosterone (TT), estradiol (E), progesterone (P), insulin and glucose levels were measured in FtM and PM subjects. RESULTS: FtM had received T for 33.6 +/- 21.3 months (mean +/- SD). In FtM subjects, histological analysis found inactive endometrium similar to the atrophic menopausal endometrium. The expression of Ki-67 in the glands, stroma and glands and stroma together was significantly (p < 0.0005) lower in FtM than in PM women and was similar in the FtM and M groups. Small polyps were detected in 5 of the 27 FtM subjects. CONCLUSIONS: In conclusion our data suggest that exogenous T administration does not stimulate endometrial proliferation in FtM transsexuals and indeed may have atrophic effects.

Pharmacokinetics of testosterone undecanoate injected alone or in combination with norethisterone enanthate in healthy men.

Long-acting injectable testosterone undecanoate (TU) is a promising androgen for male hormonal contraception. As a prerequisite for a planned multicenter male contraceptive efficacy study, we studied the pharmacokinetics of 2 doses of TU alone or in combination with norethisterone enanthate (NETE) in a prospective 2-center study, randomized for TU dose in each center. Twenty healthy male volunteers in each center were administered intramuscular injections of 750 or 1000 mg TU alone or in combination with 200 mg of NETE IM every 8 weeks for 3 injections. There were no significant differences in maximum concentration and area under the curve (AUC) for serum total and free testosterone (T) between the TU 750 and 1000 mg groups, irrespective of whether TU was administered with 200 mg of NETE. TU 1000 mg IM alone or with NETE at 8-weekly intervals resulted in linear increases in average concentration and AUC of serum total and free T with each injection. Accumulation ratios of serum total and free T levels (calculated as 8 weeks post- to preinjection levels) for each period showed significant increases in the TU+ NETE groups. Serum gonadotropins levels and sperm concentration were more consistently suppressed in the TU 1000 mg + NETE group. We conclude that despite some accumulation of T, TU 1000 mg + NETE 200 mg administered every 8 weeks may be preferable for the future contraceptive efficacy study because of more complete suppression of gonadotropins and spermatogenesis.