Drug insight: testosterone preparations

Abstract

Testosterone has been used for substitution therapy in testicular and hypothalamopituitary diseases for almost six decades, with injectable testosterone esters and implanted testosterone pellets being the mainstay of treatment. Growing interest in the possible use of testosterone in nonclassical situations such as male contraception, aging (late-onset hypogonadism), muscle-wasting conditions like HIV, erectile dysfunction, and female hypoactive sexual disorder has stimulated research, leading to the development of several new modes of administration of testosterone. Transdermal patches, gels, mucoadhesive sustained-release buccal tablets and long-acting testosterone esters are designed to provide testosterone levels that approximate normal physiologic levels, to improve patient acceptability, and to further increase the number of treatment options available. In this Review, we briefly describe the chemistry, mechanism of action, and metabolism of testosterone. We then discuss the pharmacokinetics, advantages, and disadvantages of various formulations and summarize the various preparations currently available.