The steady-state pharmacokinetics of two doses of a transdermal testosterone cream: 5 and 10 mg was investigated after daily application for 21 days by Fooladi and colleagues in a two-way, cross-over study conducted for 6 weeks . Seven healthy postmenopausal women (mean age 59.3 years) were randomly allocated to 5 or 10 mg of transdermal testosterone cream applied daily to the upper arm. Serum total testosterone (TT), free testosterone (fT), sex hormone binding globulin, and metabolite concentrations were measured. Baseline-corrected and uncorrected serum TT and fT pharmacokinetic parameters (AUC[-]0-24[/-], C[-]avg[/-], C[-]max[/-], and T[-]max[/-]) were calculated using a standard model-independent approach. After the single-dose application of 5 mg of the transdermal testosterone cream on day 22, the median uncorrected TT C[-]avg[/-] was found to be 0.54 ng/ml (range 0.43–1.31 ng/ml), and the median uncorrected fT C[-]avg[/-] was found to be 4.14 pg/ml (range 2.41–9.72 pg/ml). Doubling of the dose only resulted in a 30% increase in baseline-corrected TT C[-]avg[/-] (0.52 vs. 0.69 ng/ml for 5 and 10 mg, respectively) and a 31% increase in baseline-corrected fT C[-]avg[/-] (4.75 vs. 6.24 pg/ml for 5 and 10 mg, respectively). Neither dose resulted in any meaningful variation in dihydrotestosterone, estrone, estradiol, or sex hormone binding globulin across the post-dose sampling period. It was concluded that the 5-mg dose of transdermal testosterone cream restores TT and fT levels to levels above and within the reference range, respectively, for premenopausal women.
Fooladi E, Reuter SE, Bell RJ, et al. Pharmacokinetics of a transdermal testosterone cream in healthy postmenopausal women. Menopause 2014, May 19. Epub ahead of print
Davis SR. Androgen therapy in women, beyond libido. Climacteric 2013;16(Suppl l):18-24.
El Hage G, Eden JA, Manga RZ. A double-blind, randomized, placebo-controlled trial of the effect of testosterone cream on the sexual motivation of menopausal hysterectomized women with hypoactive sexual desire disorder. Climacteric 2007;10:335-43
Shifren JL, Braunstein GD, Simon JA, et al. Transdermal testosterone treatment in women with impaired sexual function after oophorectomy. N Engl J Med 2000;343:682-8.
Tamimi RM, Hankinson SE, Chen WY, et al. Combined estrogen and testosterone use and risk of breast cancer in postmenopausal women. Arch Intern Med 2006;166:1483-9.
Haring R, Hannemann A, Ulrich J, et al. Age-specific reference ranges for serum testosterone and androstenedione concentration in women measured by liquid chromatography-tandem mass spectrometry. J Clin Endocrinol Metab 2012;97;408-15.