madman
Super Moderator
The growing interest in testosterone's effects on men's social behaviors, in particular aggressive, risk-taking, or status maintenance behaviors, is accompanied by a paucity of dose-dependent pharmacokinetic data. Examining the neurophysiological effects of transdermal testosterone typically includes a 4h delay before further brain-behavior measurements. Nevertheless, high heterogeneity regarding the timing of follow-up measurements and dosage remains. In a double-blind placebo-controlled design, we examined the short-term pharmacokinetic profile of 100-mg transdermal testosterone (Testotop®) to determine the optimal time for detecting testosterone-mediated effects. Across two studies, 35 healthy men received a single dose of testosterone and placebo in two separate sessions. In study one (n = 16), serum testosterone and cortisol were assessed serially every 30 min up to 2 h posttreatment. In study two (n = 19), we assessed serum testosterone and cortisol at baseline, 2 h, and 4.15 h (255 min) posttreatment. Relative to baseline and placebo, transdermal testosterone significantly increased total serum testosterone concentrations 90 min posttreatment, reaching maximum concentration between 2 h and 3 h post treatment. Albeit elevated, serum testosterone levels gradually decreased between 2 h and 4 h following treatment. Transdermal testosterone did not suppress cortisol release. Instead, cortisol concentrations decreased according to cortisol's known circadian rhythm. Unlike previous findings showing significant testosterone concentration increases as soon as 60 min and as late as 3 h post 150- mg testosterone treatment, our 100-mg testosterone manipulation significantly increased testosterone concentrations 90 min following treatment. These pharmacokinetic data are important in facilitating the optimization of timing parameters for future testosterone challenge studies.
In conclusion, we examined the pharmacokinetic profile of a 100-mg transdermal T formulation and found that it quickly and significantly elevated total serum T levels 90-min posttreatment. Moreover, we found no inhibitory effects of transdermal T on serum C concentrations, the latter decreasing gradually in line with cortisol's independent rhythm. Therefore, we tentatively suggest that the optimal time-point for examining the association between testosterone and brain-behavior effects with a 100-mg transdermal preparation lies between 1.5 h and 4.15 h following treatment. Our recommendations are applicable in the context of a transdermal administration route in samples with similar anthropometric characteristics (including age, gender, sexual orientation, and body mass index) as well as similar educational and ethnic backgrounds. These pharmacokinetic data provide important guidelines for the timing optimization of studies investigating the causal influence of exogenous testosterone on the brain and behavior.
In conclusion, we examined the pharmacokinetic profile of a 100-mg transdermal T formulation and found that it quickly and significantly elevated total serum T levels 90-min posttreatment. Moreover, we found no inhibitory effects of transdermal T on serum C concentrations, the latter decreasing gradually in line with cortisol's independent rhythm. Therefore, we tentatively suggest that the optimal time-point for examining the association between testosterone and brain-behavior effects with a 100-mg transdermal preparation lies between 1.5 h and 4.15 h following treatment. Our recommendations are applicable in the context of a transdermal administration route in samples with similar anthropometric characteristics (including age, gender, sexual orientation, and body mass index) as well as similar educational and ethnic backgrounds. These pharmacokinetic data provide important guidelines for the timing optimization of studies investigating the causal influence of exogenous testosterone on the brain and behavior.
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