Percutaneous absorption of 5α‐dihydrotestosterone in man

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Abstract
The distribution of 5.alpha.-dihydrotestosterone to the blood following application of a solution of this androgen to the skin in a hydro-alcoholic gel was studied in order to evaluate the adequacy of the percutaneous route in correcting androgen deficiencies. In 14 adult men, daily percutaneous administration of 5.alpha.-dihydrotestosterone (125 mg in 5 g gel) increases, on the average, 4 to 5 times its initial concentration in plasma. On the 14th day of treatment, repeated evaluations of plasma 5.alpha.-dihydrotestosterone, between 2 and 21 h after final administration of gel, demonstrated the stability of diurnal 5.alpha.-dihydrotestosterone levels and showed the regular distribution of the steroid from a presumably cutaneous reservoir. Plasma 5.alpha.-androstane-3.alpha.,17.beta.-diol levels evolve parallel to those of 5.alpha.-dihydrotestosterone. Plasma testosterone and luteinizing hormone, on the contrary, decrease considerably. No variation of FSH is observed during treatment. The percutaneous absorption represents an interesting method for administration of a natural androgen in men, particularly because one avoids the deleterious effects of supra-physiological levels in the liver achieved with oral administration.