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Effects of Prohormone Supplementation in Humans: A Review

Publication: Canadian Journal of Applied Physiology
December 2002


Despite a relative dearth of information on their effects, supplementation with prohormones has become a popular practice. Unlike synthetic anabolic-androgenic steroids, many of these over-the-counter androgens are produced endogenously by adrenal, gonadal and peripheral steroidogenic pathways as part of the normal sexual and reproductive hormonal milieu. It has been contended that peripheral enzymatic conversion of these prohormones to testosterone or nortestosterone (via ingestion of androstenedione/androstenediol or 19-nor-androstenedione/androstenediol, respectively) might lead to anabolic and/or ergogenic effects. Existing data suggest that acute oral ingestion of >= 200 mg androstenedione or androstenediol modestly and transiently increases serum testosterone concentrations in men; however, this is accompanied by greater increases in circulating estrogen(s). At doses < 300 mg/d, oral supplementation for as long as 12-weeks with androstenedione or androstenediol has no effect on body composition or physical performance and decreases high-density lipoprotein cholesterol. Similarly, oral supplementation with norandrostenedione and norandrostenediol for up to eight weeks has no effect on body composition or physical performance. In light of these data, new products have been developed that use alternative modes of prohormone administration (sublingual/transbuccal and cyclodextrin-complexation). Future studies should critically examine the effects of these approaches. However, within the framework of the research reviewed, over-the-counter oral prohormone supplementation is ineffective at increasing muscle mass or athletic performance. As a result of the potential health concerns that have been raised, the risk to benefit ratio of using these substances orally seems unfavorable. Keywords: androstenediol, androstenedione, norandrostenedione, norandrostenediol, ergogenic aid


La supplémentation en prohormones s'avère une pratique répandue malgré le manque d'information au sujet des effets possibles. Plusieurs de ces prohormones administrées sous surveillance pharmaceutique proviennent des glandes surrénales, des gonades et d'autres systèmes stéroïdogènes; à la différence des stéroïdes anabolisants et androgènes, ces prohormones relèvent normalement du système endocrinien associé au sexe et à la reproduction. Il est admis que la conversion enzymatique de ces prohormones en testostérone ou en nortestostérone (par la consommation d'androstènedione/androstènediol ou de 19-nor-androstènedione/androstènediol, respectivement) amène des effets anabolisants et/ou ergogènes. D'après certaines études, la consommation per os de >= 200 mg d'androstènedione ou d'androstènediol augmente légèrement et temporairement la concentration sérique de testostérone chez l'homme; en même temps, il y a augmentation de la concentration des œstrogènes en circulation. Une supplémentation per os d'androstènedione ou d'androstènediol inférieure à 300 mg par jour durant 12 semaines n'entraîne aucun effet sur la composition corporelle et sur la performance physique, cependant le niveau de HDL-cholestérol diminue. De même, la supplémentation per os en norandrostènedione ou en norandrostènediol sur une durée allant jusqu 'à huit semaines n'entraîne aucun effet sur la composition corporelle et sur la performance physique. Compte tenu de ces observations, de nouvelles façons d'administrer ces prohormones ont été élaborées: par voie sublinguale/transbuccale ou par complexation au moyen de la cyclodextrine. Ces différentes modalités devraient faire l'objet d'études scientifiques. Néanmoins, d'après l'analyse de la revue de littérature, la supplémentation en prohormones sous surveillance pharmaceutique ne fait pas augmenter la masse musculaire ni améliorer la performance. À la lumière des problèmes potentiels évoqués, le risque n'en vaut pas la chandelle. Mots-clés: androstènediol, androstènedione, norandrostènedione, norandrostènediol, agent ergogène

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cover image Canadian Journal of Applied Physiology
Canadian Journal of Applied Physiology
Volume 27Number 6December 2002
Pages: 628 - 645


Version of record online: 25 January 2011


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