Pharmacokinetics of testosterone and estradiol gel preparations in healthy young men

Abstract

The paucity of pharmacokinetic data on testosterone gel formulations and absence of such data on estradiol administration in healthy young men constitutes a fundamental gap of knowledge in behavioral endocrinological research. We addressed this issue in a double-blind and placebo controlled study in which we applied a topical gel containing either 150mg of testosterone (N=10), 2mg of estradiol (N=8) or a respective placebo (N=10) to 28 healthy young men. We then assessed serum concentrations of estradiol and testosterone in one hour intervals up to seven hours after drug application, measured LH, SHBG and cortisol levels once at baseline and three, four as well as six hours after gel administration. Treatment with testosterone gel resulted in maximum total serum testosterone concentration three hours after administration and did not suppress LH, cortisol and SHBG levels at any time point. Administration of estradiol gel led to maximum estradiol serum concentration two hours after administration. There was no suppression of cortisol, SHBG and absolute LH levels. We report here, for the first time, pharmacokinetic data on both high dose testosterone and estradiol gel application in healthy young males. The proposed model will assist in the design of future studies that seek to establish causality between testosterone and estradiol gel administration and behavioral as well as neurophysiological effects.