Testosterone:estradiol ratio changes associated with long-term tadalafil administration: a pilot study

J Sex Med. 2006 Jul;3(4):716-722. doi: 10.1111/j.1743-6109.2006.00264.x.

Abstract

Introduction: It has been reported that lack of sexual activity due to erectile dysfunction (ED) may be associated with testosterone (T) decline.

Aim: To investigate whether the known changes in sex hormones associated with resumption of sexual activity are sustained in the long term.

Main outcome measures: Primary endpoints were variations from baseline of steroid hormones: total T, free T (f T), and estradiol (E). Secondary endpoints were variations of erectile function domain scores at International Index of Erectile Function-5 (IIEF-5).

Methods: In an open-label fashion, 20 patients (mean age 54.8 +/- 8.4 years) received tadalafil 10-20 mg on demand for 12 months. Exclusion criteria were those reported for phosphodiesterase inhibitors, including hypogonadism and hyperprolactinemia.

Results: Tadalafil assumption was safe and well tolerated (overall adverse effects in 15% of patients) and none discontinued medication. A significant decrease in E levels occurred at the end of the study (from 19.9 +/- 9.6 to 16.6 +/- 8.1 ng/dL, P = 0.042 vs. baseline), with parallel increase in the T:E ratio (26.3 +/- 15.3 to 32.6 +/- 17.7, P = 0.05), whereas no changes in T and f T serum levels were observed, respectively (411.4 +/- 131.4 to 434.2 +/- 177.1 ng/dL and 47.7 +/- 15.3 to 49.9 +/- 19.1 pmol/L, not significant). Interestingly, nonparametric subgroup analysis for related samples revealed that E decrease was detectable only in lean (N = 14) but not in obese (N = 6, body mass index > 27.5 kg/m2) subjects (17.8 +/- 10.1 vs. 13.5 +/- 6.8, P < 0.05). A net increase in IIEF-5 scores was observed at the endpoint (13.7 +/- 5.9 vs. 25.7 +/- 2.9, P < 0.0001).

Conclusions: Sustained improvement in sexual function after 12 months of tadalafil administration is associated with increased T:E ratio mainly related to reduction of E levels. We hypothesize that androgen-estrogen cross-talk and possible inhibition of aromatase activity during chronic exposure to tadalafil might have a role in the regulation of erectile function.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Carbolines / administration & dosage*
  • Carbolines / pharmacology
  • Dose-Response Relationship, Drug
  • Erectile Dysfunction / blood*
  • Erectile Dysfunction / drug therapy*
  • Estradiol / blood*
  • Humans
  • Male
  • Middle Aged
  • Patient Satisfaction
  • Penile Erection / drug effects
  • Phosphodiesterase Inhibitors / administration & dosage*
  • Phosphodiesterase Inhibitors / pharmacology
  • Pilot Projects
  • Tadalafil
  • Testosterone / blood*
  • Treatment Outcome

Substances

  • Carbolines
  • Phosphodiesterase Inhibitors
  • Testosterone
  • Estradiol
  • Tadalafil