Objective: Analyze the serum levels of DHEA (prasterone) and its metabolites after daily intravaginal 0.50% (6.5 mg) DHEA in postmenopausal women with vulvovaginal atrophy (VVA).
Methods: Serum samples were obtained at baseline and after 12, 26 and 52 weeks of treatment. The serum levels of DHEA, DHEA-sulfate (DHEA-S), androstene-3β, 17β-diol (5-diol), androstenedione (4-dione), testosterone, dihydrotestosterone (DHT), estrone (E1), estradiol (E2), E1-sulfate (E1-S), androsterone glucuronide (ADT-G) and androstane-3α,17β-diol 17-glucuronide (3α-diol-17G) were measured by validated liquid chromatography-tandem mass spectrometry.
Results: A total of 435 women were exposed for 52 weeks. All serum steroids remained within normal values with no significant differences between lengths of treatment. For the most relevant estrogen-related compounds, namely E1, E2, and E1-S, a reliable marker of total estrogen exposure, the values in the DHEA-treated group at 52 weeks were -3.4%, -9.1% and +1.8%, respectively, compared to the normal postmenopausal values, thus clearly confirming the absence of significant systemic estrogen exposure.
Conclusion: While confirming that all serum sex steroids originating exclusively from DHEA after menopause are maintained within the normal postmenopausal values, the present data show that the dose of intravaginal DHEA used is free from systemic exposure with no detectable change in metabolism up to 52 weeks of treatment.