Effects of ketoconazole on the excretion kinetics of methandienone. An in vivo study

Methandienone, a 17α-methylated, testosterone derivative, is one of the androgenic anabolic steroid (AAS) most frequently detected in sports by the WADA accredited Antidoping Laboratories. Its metabolism has been extensively investigated in the past via both in vivo and in vitro studies [1-5]. The metabolites available as reference materials and currently used as markers of methandienone misuse in doping control routine analysis are: 6β-hydroxy-methandienone, 17α-methyl-5α-androstane-3α,17β-diol (5α-tetrahydro-methyltestosterone), 17α-methyl-5β-androstane-3α,17β-diol (5β-tetrahydro-methyltestosterone), 17β-methyl-5β-androst-1-ene-3α,17α-diol (epimetendiol) and 18-nor-17,17-dimethyl-5β-androst-1,13-dien-3α-ol (18-norepimetendiol), the last two allow a long-term detection of methandienone abuse. Recently other two metabolites, 18-nor-17-hydroxymethyl,17-methylandrost-1,4,13-trien-3-one (20-hydroxy-normetandienone) and 18-nor-17-hydroxymethyl,17-methylandrost-1,4,13-trien-3-one (20-hydroxy-normetandienone) were identified by Schänzer and its collaborators as complementary markers for long-term detection of methandienone [2, 4-5].