Substitution therapy of hypogonadal men with transdermal testosterone over one year

Abstract

Current testosterone substitution therapy either by injectable or oral testosterone esters suffers from markedly fluctuating serum testosterone levels often far above or below the physiological range. Recently, a transdermal therapeutic system (TTS) for the delivery of testosterone was developed which, when applied to the scrotum, provides smooth serum testosterone levels. Here we report results from seven hypogonadal men treated with the TTS for 14 months by applying a new patch every day. In all patients serum testosterone and dihydrotestosterone (DHT) determined 3\p=n-\5 h after applying a new patch increased significantly and remained within the physiological range during the entire treatment period. The DHT/ testosterone ratio remained constant. In 4 of these patients and 2 others under TTS treatment serum testosterone and DHT were also determined over a 24-h period at regular intervals. In these patients serum testosterone levels in the physiological range were seen during the entire observation period, whereas an increase in the DHT/testosterone ratio occurred towards the end of the one-day treatment phase. All patients in the 14-month treatment study were clinically well substituted and responded with good compliance. Clinical chemistry showed no abnormalities during treatment.Thus, the TTS appears to be an effective and safe new modality for the treatment of male hypogonadism.

Pharmacokinetics of a new transdermal testosterone gel in gonadotrophin-suppressed normal men

“…Accordingly, supraphysiological serum concentrations of DHT were observed in patients applying scrotal testosterone patches (7,8). In the present study, mean serum concentrations of DHT were in the upper normal range.…”

“…However, after receiving the non-scrotal patches, 7% of patients experienced allergic contact dermatitis at the site of the patch application, and 32% of patients experienced moderate irritation (6). After application of scrotal testosterone patches, supraphysiological serum concentrations of dihydrotestosterone (DHT) were measured (7,8); a further disadvantage of this system is that the scrotal skin must be shaved. Therefore an improved testosterone delivery system is desirable.…”

Pharmacology and clinical uses of testosterone

“…The membranes need to be renewed every day. When applied in the morning and worn until the next morning the resulting serum testosterone levels resemble the normal diurnal variations of serum testosterone in normal men without supraphysiological peaks (Bals-Pratsch et al 1988). More pharmacokinetic details of transdermal testosterone therapy are provided by Behre et al (1990) in this book.…”

Pharmacokinetic Characteristics, Efficacy, and Safety of Buccal Testosterone in Hypogonadal Males: A Pilot Study1

“…The scrotal T delivery system (Testoderm T transdermal system, Alza Pharmaceuticals, Palo Alto, CA) mentioned above produces T concentrations within normal ranges. However, with continued daily use, serum DHT levels are elevated 4-to 10-fold (2,(17)(18)(19)(20). In contrast, the buccal T formulation produced DHT levels in the normal range for eugonadal men (25- systemic circulation (7730 pg/h⅐mL) for a 10 mg/day dose is roughly equivalent to the T level of 6960 pg/h⅐mL obtained with the scrotal patch.…”