Prohormones of androgens

OH OH

OH OH

OH OH

OH OH

17B-hydroxy-5a-androst-1-en-3-one 5a-Androst-1-ene-3B,17B-diol ( "1-Testosterone" )

17B-hydroxy-5a-androst-1-en-3-one 5a-Androst-1-ene-3B,17B-diol ( "1-Testosterone" )

Fig. 24.3 Structure formula of prohormones of dihydrotestosterone and prohormones with 1-ene structure.

Fig. 24.3 Structure formula of prohormones of dihydrotestosterone and prohormones with 1-ene structure.

OH

Fig. 24.4 Structure formula of prohormones of nortestosterone.

sublingual or buccal application. In contrast to such incorrect advertisements, only small amounts of the applied prohormone maybe converted to the effective steroid. Indeed, for medical treatment prohormones are useless. Therefore companies providing prohormones recommend application several times per day, especially before training or competition [high amounts (100 mg and more) of oral preparations of single prohormones, combinations of different prohormones and sublingual preparations]. Published data (Leder etal. 2000) demonstrate that in male persons e.g. androstenedione 100 mg/day orally applied for seven days yielded no significant changes in serum testosterone levels compared to the control group whereas 300 mg/day of androstenedione for seven days showed a significant increase in peak and AUC (area under curve) serum testosterone (AUC 34%), but with high interindividual variation. As prohormones are also used by females and adolescents lower amounts of prohormones may yield physiological changes in serum testosterone levels, e.g. 100 mg androstenedione applied orally to females yielded an increase in serum testosterone concentrations up to 0.8 ng/ml (Kicman 2003).

The distribution of prohormones in the United States is not restricted by the Food and Drug Administration (FDA) because these products are not marketed as medications. In Europe prohormones are considered unlicensed medications and their distribution is banned. Nevertheless, control of the misuse of prohormones is difficult, as products enter the European market via neighbour states, directly via airports and by internet or postal orders.

Additional new products are entering the market with a 1-ene structure such as androsta-1,4-diene-3,17-dione which is considered as a prohormone of the synthetic AAS boldenone (17fi-hydroxyandrosta-1,4-dien-3-one) and steroids with a 5a-androst-1-ene structure (Fig. 24.3) which are marketed as prohormones.

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