In vivo 4-androstene-3,17-dione and 4-androstene-3β,17β-diol supplementation in young men

Earnest, Conrad P.; Olson, Mark A.; Broeder, Craig E.; Breuel, Kevin F.; Beckham, Susan G.

doi:10.1007/s004210050035

Cited by 41 publications

(27 citation statements)

References 7 publications

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“…Related studies examined the acute effect of orally administered testosterone prohormones such as androstenedione and androstenediol, which did not result in uniform findings concerning the elevation of plasma testosterone concentrations of young healthy men (King et al, 1999;Brown et al, 2000;Earnest et al, 2000. In accordance to our results, an increase of plasma testosterone concentrations after sublingual androstenediol intake was reported (Brown et al, 2002), demonstrating the effectiveness of this route of drug administration.…”

Section: Discussionsupporting

confidence: 80%

Quantitative Determination of Metabolic Products of 19-Norandrostenediol in Human Plasma Using Gas Chromatography/Mass Spectrometry

Schrader

Thevis²,

Schänzer³

2006

Drug Metab Dispos

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ABSTRACT:Prohormones such as 19-norandrostenediol (estr-4-ene-3␤,17␤-diol) have been added to the list of prohibited substances of the World Anti-Doping Agency because they are metabolized to the common nandrolone metabolites norandrosterone and noretiocholanolone. So far, no studies on the metabolism and in vivo conversion of 19-norandrostenediol after oral or sublingual administration have been reported nor have had quantified data on resulting plasma nandrolone levels. In the present study, an openlabel crossover trial with eight healthy male volunteers was conducted. After application of capsules or sublingual tablets of 19-norandrostenediol plasma concentrations of 19-norandrostenediol, nandrolone as well as major metabolites (19-norandrosterone and 19-noretiocholanolone) were determined using a validated assay based on gas chromatography/mass spectrometry. The administration of 100-mg capsules of 19-norandrostenediol yielded maximum plasma total concentrations (i.e., conjugated plus unconjugated compounds) of 1.1 ng/ml (؎0.7) for 19-norandrostenediol, 4.0 ng/ml (؎2.6) for nandrolone, 154.8 ng/ml (؎130.8) for 19-norandrosterone, and 37.7 ng/ml (؎6.9) for 19-noretiocholanolone. The use of 25-mg sublingual tablets resulted in 3.3 ng/ml (؎1.0) for 19-norandrostenediol, 11.0 ng/ml (؎6.4) for nandrolone, 106.3 ng/ml (؎40.1) for 19-norandrosterone, and 28.5 ng/ml (؎20.8) for 19-noretiocholanolone. Most interestingly, the pharmacologically active unconjugated nandrolone was determined after administration of sublingual tablets (up to 5.7 ng/ml) in contrast to capsule applications. These results demonstrate the importance of prohibiting prohormones such as 19-norandrostenediol, in particular, since plasma concentrations of nandrolone between 0.3 to 1.2 ng/ml have been reported to influence endocrinological parameters.Nandrolone (NL; Fig. 1A) is an anabolic steroid usually administered as the decanoate ester in the form of oily intramuscular injections. Nandrolone has been used as an anabolic agent after debilitating illness and for the treatment of postmenopausal osteoporosis, postmenopausal metastatic breast carcinoma, anemia as a result of chronic renal failure, and aplastic anemia. In addition to these therapeutic applications, NL gained public recognition because of its abuse by athletes for the purpose of increasing muscle mass and muscular strength (Yesalis and Bahrke, 1995). As a result, NL, among others, was banned in 1974 by the International Olympic Committee. To provide evidence of NL doping, the main urinary metabolites 19-norandrosterone (NA; Fig. 1B) and 19-noretiocholanolone (NE; Fig. 1C) have been used as target analytes (Schänzer and

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Section: Discussionsupporting

confidence: 80%

Quantitative Determination of Metabolic Products of 19-Norandrostenediol in Human Plasma Using Gas Chromatography/Mass Spectrometry

Schrader

Thevis²,

Schänzer³

2006

Drug Metab Dispos

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“…Work by Earnest et al (2000) has demonstrated that oral administration of A-dione and A-diol can signi®cantly increase plasma total and free T. However, chronic administration of 300 mg/day of androstenedione for 8 weeks has also been shown to elevate serum estradiol and estrone in men, as is already known to occur in women (Gompel et al 1986;King et al 1999). Thus, one might also speculate that any anabolic eect of A-dione may be oset by the rise in plasma estrogens.…”

Section: Edione (A-dione) and Androstenediol (A-diol) T And 19-mentioning

confidence: 91%

“…Athletes ingest these particular supplements in the belief that their conversion into T will increase anabolic processes and help build up skeletal muscle mass. A study by Earnest et al (2000) examined the acute eects of oral treatment with 200 mg of 4-androstene-3,17-dione, 4-androstene-3 beta,17 beta-diol, and placebo (PL) on peripheral plasma T concentration. They found that both androstenedione and androstenediol signi®cantly increased the T concentration when compared to a placebo.…”

Section: Introductionmentioning

confidence: 99%

The effects of supplementation with 19-nor-4-androstene-3,17-dione and 19-nor-4-androstene-3,17-diol on body composition and athletic performance in previously weight-trained male athletes

Gammeren

Falk

António

2001

European Journal of Applied Physiology

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The purpose of this study was to determine the effects of 8 weeks of norsteroid supplementation on body composition and athletic performance in previously weight-trained males. Subjects were weight and percent body fat matched and randomly assigned to receive either 100 mg of 19-nor-4-androstene-3,17-dione (N-dione) and 56 mg of 19-nor-4-androstene-3,17-diol (N-diol; 156 mg total norsteroid per day), or a placebo (a multivitamin). Each subject participated in resistance training 4 days/week for the duration of the study. Body composition was assessed via dual-energy X-ray absorptiometry. Circumference measures were taken of a relaxed and flexed arm (maximum circumference of the arm), waist (level of umbilicus), and thigh (15 cm proximal to the patella). Strength was determined with a one-repetition maximum bench press, while force and power were determined with a dumbbell bench press (60% body weight) on a Stratec Galileo force platform. Profile of mood states scores were evaluated for vigor and fatigue. There were no significant changes in any of the parameters measured. In conclusion, low-dose supplementation with N-dione and N-diol does not appear to alter body composition, exercise performance, or mood states.

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“…Ingesting 100 or 200 mg doses of androstenedione Ballantyne et al 2000;Brown et al 2000b;Leder et al 2000;Rasmussen et al 2000) or androstenediol (Earnest et al 2000) does not acutely alter serum testosterone concentrations in eugonadol men. However, Leder et al (2000) observed that in 2 out of 14 healthy men who consumed a single dose of 300 mg androstenedione, serum testosterone concentrations were acutely elevated by as much as fourfold.…”

Section: Introductionmentioning

confidence: 96%

Acute resistance exercise does not change the hormonal response to sublingual androstenediol intake

Brown

McKenzie

2006

Eur J Appl Physiol

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Sublingual intake of 21.4 mg androstenediol increases serum testosterone concentrations whereas swallowing 200 mg androstenediol does not. The duration of increase in serum testosterone following sublingual androstenediol (SL-DIOL) is unknown. Resistance exercise (EX) following SL-DIOL may cause larger increases in serum estradiol concentrations than while at rest. This project evaluated the duration of change in, and the effects of acute EX on, the hormonal response to SL-DIOL. Six young resistance trained males consumed either placebo (PL) or SL-DIOL before a single session of EX or no exercise (Rest) in a random, double blind, crossover manner (for a total of four trials). Blood samples were collected before supplementation, and at 60, 120, 180, 240, 480, and 720 min post-supplementation, with the exercise occurring between 60 and 120 min. The serum [total testosterone] increased (P < 0.05) at 60 min similarly in SL-DIOL-EX and SL-DIOL-Rest by approximately 115%, and at 120 min by approximately 107% with no differences due to exercise. The serum [estradiol] increased (P < 0.05) similarly in SL-DIOL-EX and SL-DIOL-Rest by approximately 33% at 60 min and approximately 45% at 120 min, with no differences due to exercise. Serum [testosterone] returned to baseline by 240 min and serum [estradiol] returned to baseline by 720 min post-intake. These findings indicate that SL-DIOL acutely elevates serum testosterone and estradiol concentrations, that EX does not alter the endocrine response to SL-DIOL, and that the increases in serum estradiol last between 480 and 720 min while the increases in serum testosterone last <240 min following acute SL-DIOL intake.

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In vivo 4-androstene-3,17-dione and 4-androstene-3β,17β-diol supplementation in young men

Cited by 41 publications

References 7 publications

Quantitative Determination of Metabolic Products of 19-Norandrostenediol in Human Plasma Using Gas Chromatography/Mass Spectrometry

Quantitative Determination of Metabolic Products of 19-Norandrostenediol in Human Plasma Using Gas Chromatography/Mass Spectrometry

The effects of supplementation with 19-nor-4-androstene-3,17-dione and 19-nor-4-androstene-3,17-diol on body composition and athletic performance in previously weight-trained male athletes

Acute resistance exercise does not change the hormonal response to sublingual androstenediol intake

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