J Sex Med. 2006 May;3(3):541-9.
Vaginal application of
testosterone: A study on pharmacokinetics and the sexual response in healthy
volunteers.
Apperloo M,
Midden M,
van der Stege J,
Wouda J,
Hoek A,
Weijmar Schultz W.
Department of Gynecology,
University Hospital Groningen, Groningen, The Netherlands. m.j. A. Apperloo@og.umcg.nl
Introduction:
Androgen substitution
is advocated to improve sexual functioning in women with androgen
insufficiency. Nevertheless, the role of androgens in female sexual
functioning is not yet unraveled. Even less is known about changes in
androgens and the female sexual response.
Aim:
The aim of the study is to
describe the pharmacokinetics of a single dose of vaginally applied
testosterone. In addition, the study aims to gain more insight into the
relation between acute changes in testosterone levels and the sexual
response in women.
Methods:
A randomized, double-blind, crossover study
design was used to compare a single vaginal dose of testosterone propionate
(2 mg) with placebo. Ten healthy premenopausal women participated. Serum
levels of testosterone, free testosterone, and estradiol were measured. The
sexual response was measured before application of medication and 4 and 8
hours after application. Erotic video fragments and erotic fantasies were
used as stimuli. The genital sexual response was measured using vaginal
plethysmography. The subjective sexual response was measured using a visual
analog scale.
Results:
Vaginal administration of testosterone propionate
induced a significant rise in serum testosterone levels and free
testosterone levels, but not in serum estradiol levels. Peak levels were
reached after 5.5 hours (range 2-12 hours). Mean peak levels of testosterone
were 7.71 nmol/L after testosterone propionate and 2.99 nmol/L after placebo
(P< 0.005). Mean peak levels of free testosterone were 0.12 nmol/L after
testosterone propionate and 0.04 nmol/L after placebo (P< 0.005). Despite
marked elevated levels of androgens this study was unable to detect a direct
effect on the genital or subjective sexual response.
Conclusions:
A single
dose of vaginally applied testosterone propionate elevates serum levels of
testosterone and free testosterone within 6 hours. Nevertheless, this acute
rise in androgens has no effects on the female sexual response.

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