Testosterone Replacement With Transdermal Therapeutic Systems

Abstract

Testosterone was administered transdermally to hypogonadal men under three protocols. In the first protocol, it was shown that peak levels of testosterone were achieved three to eight hours after scrotal application of a transdermal therapeutic system containing 5, 10, or 15 mg of testosterone, and values at 22 hours were greater than 60% of peak values. In the second protocol, patients were treated with 10-mg systems for four weeks followed by 15-mg systems for eight weeks. Serum samples were obtained three to five hours after application of the transdermal therapeutic system. Testosterone increased from a pretreatment level (mean +/- SE) of 1.5 +/- 0.4 nmol/L to 15.2 +/- 3.4 nmol/L at four weeks, 18.6 +/- 3.3 nmol/L at eight weeks, and 17.3 +/- 2.8 nmol/L at 12 weeks. The serum testosterone/dihydrotestosterone (DHT) ratio fell from 4.53 to 2.47 at four weeks and was similar at eight and 12 weeks, reflecting a greater rise in DHT with this route of treatment (normal testosterone/DHT ratio, 9/1 to 12/1). Eight patients were treated with the 15-mg systems for an additional year. Seven of the eight were compliant and maintained serum testosterone levels (at six time points from two to 12 months [mean +/- SE] ) ranging from 11.5 +/- 1.2 to 44.9 +/- 2.4 nmol/L. It was possible to achieve physiological serum levels of testosterone by transdermal administration of testosterone in two thirds of our hypogonadal men.

An update on male hypogonadism therapy

“…The first transdermal preparations are the scrotal patches, which are not currently available because of the need to shave or cut scrotal hair to maintain adequate patch adhesion to the skin [115]. In addition, some individuals complained of scrotal itching or discomfort.…”

Evolution of delivery systems for testosterone administration

“…In 1983, based on the finding that scrotal skin was more efficient at transporting testosterone, scientists at ALZA Corporation (Mountain View, CA) developed a scrotal patch (Testoderm) for ART [30][31][32]. Periodic scrotal shaving was required and men used either 40 or 60 cm 2 patches daily, which delivered approximately 10 or 15 mg testosterone.…”

Testosterone Replacement Therapy

“…Appli- cation of a patch results in a physiological curve of serum testosterone that imitates the circadian pattern serum levels of the hormone [4,5,20,61,74]. Two transdermal testosterone systems are now commercially available: a scrotal testosterone patch and a permeation-enhanced nongenital patch.…”

“…Two transdermal testosterone systems are now commercially available: a scrotal testosterone patch and a permeation-enhanced nongenital patch. The scrotal transdermal system, when applied daily on the scrotal skin, can produce midnormal serum testosterone levels in hypogonadal men 4-8 h after application of the patch followed by gradual decrease in serum testosterone levels over the next 24 h [20]. The patches are available in two sizes, 40 and 60 cm', which deliver 4 and 6 mg of testosterone per day, respectively.…”