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PubMed1985

The history of anabolic steroids and a review of clinical experience with anabolic steroids.

Metabolism is the term employed to embrace the various physical and chemical processes occurring within the tissues upon which the growth and heat production of the body depend and from which the energy for muscular activity, for the maintenance of vital activity and for the maintenance of vital functions is derived (Best & Taylor 1950). The destructive processes by which complex substances are converted by living cells into more simple compounds are called catabolism. Anabolism denotes the constructive processes by which simple substances are converted by living cells into more complex compounds, especially into living matter. Catabolism and anabolism are part of all metabolic processes, the carbohydrate, fat and protein metabolism. The term anabolic refers only to substances that exert an anabolic effect on protein metabolism and are unlikely to cause adverse androgenic effects. They shift the equilibrium between protein synthesis and degradation in the body as a whole in the direction of synthesis, either by promoting protein synthesis or reducing its breakdown. The protein anabolic effect of anabolic steroids is not restricted to single organs but is the result of stimulated biosynthesis of cellular protein in the whole organism.

Anabolic Agents↗
PubMed1989

Studies on anabolic steroids. I. Integrated methodological approach to the gas chromatographic-mass spectrometric analysis of anabolic steroid metabolites in urine.

The analytical and methodological imperatives for large-scale and routine gas chromatographic-mass spectrometric screening of anabolic steroid urinary metabolites are described. Several aspects of their isolation, enzymatic hydrolysis, derivatization and metabolism in humans are discussed. Gas chromatographic-mass spectrometric data illustrating artifacts arising from enzymatic hydrolysis of 3 beta-ol-5-en steroids, and describing new metabolites of boldenone, methanedienone and stanozolol, as well as the conversion of norethisterone into 19-nortestosterone metabolites through de-ethylation at C-17, are presented. The analytical approach developed for gas chromatographic-mass spectrometric screening of anabolic steroids is based on the sequential selection-ion monitoring of specific and discrete ion groups characteristic to the steroids of interest under high-resolution chromatographic conditions. The major analytical and methodological requirements necessary to provide irrefutable evidence, in the case where the presence of a synthetic anabolic steroid or a testosterone to epitestosterone ratio higher than 6:1 is suspected in a given urine specimen, are also discussed.

Anabolic Agents↗
PubMed2005

Dilated cardiomyopathy and acute liver injury associated with combined use of ephedra, gamma-hydroxybutyrate, and anabolic steroids.

Anabolic-androgenic steroids are synthetic derivatives of testosterone that some athletes have used to enhance muscle mass and improve their athletic performance. Ephedrine is a potent sympathomimetic agent that can lead to cardiomyopathy similar to that seen with catecholamine excess. Adverse cardiovascular events attributed to anabolic steroid and ephedra use, such as arrhythmias, myocardial infarction, cardiomyopathy, and sudden death, are rarely reported. Bodybuilders have used gamma-hydroxybutyrate, a potent secretagogue of growth hormone, to promote muscle development. Although dilated cardiomyopathy is a known complication of excess growth hormone levels, it has not been associated with use of gamma-hydroxybutyrate. A healthy 40-year-old man was admitted to our hospital for new-onset congestive heart failure and severe acute hepatitis that developed several months after he began using anabolic-androgenic steroids, ephedra, and gamma-hydroxybutyrate supplements. Analysis with an objective causality assessment scale revealed a probable adverse drug reaction between the patient's use of anabolic steroids, ephedra, and gamma-hydroxybutyrate and the development of his cardiomyopathy and acute liver injury.

Adult↗
PubMed2005

Analysis of anabolic steroids in the horse: development of a generic ELISA for the screening of 17alpha-alkyl anabolic steroid metabolites.

Due to the potential for misuse of a wide range of anabolic steroids in horse racing, a screening test to detect multiple compounds, via a common class of metabolites, would be a valuable forensic tool. An enzyme-linked immunosorbent assay (ELISA) has been developed to detect 17alpha-alkyl anabolic steroid metabolites in equine urine. 16beta-Hydroxymestanolone (16beta,17beta-dihydroxy-17alpha-methyl-5alpha-androstan-3-one) was synthesised in six steps from commercially available epiandrosterone (3beta-hydroxy-5alpha-androstan-17-one). Polyclonal antibodies were raised in sheep, employing mestanolone (17beta-hydroxy-17alpha-methyl-5alpha-androstan-3-one) or 16beta-hydroxymestanolone conjugated to human serum albumin, via a 3-carboxymethyloxime linker, as antigens. Antibody cross-reactivities were determined by assessing the ability of a library of 54 representative steroids to competitively bind the antibodies. Antibodies raised against 16beta-hydroxymestanolone showed excellent cross-reactivities for all of the 16beta,17beta-dihydroxy-17alpha-methyl steroids analysed and an ELISA has been developed to detect these steroid metabolites. Using this 16beta-hydroxymestanolone assay, urine samples from horses administered with stanozolol (17alpha-methyl-pyrazolo[4',3':2,3]-5alpha-androstan-17beta-ol), were analysed raw, following beta-glucuronidase hydrolysis, and following solid-phase extraction (SPE) procedures. The suppressed absorbances observed were consistent with detection of the metabolite 16beta-hydroxystanozolol. Positive screening results were confirmed by comparison with standard LCMS analyses. Antibodies raised against mestanolone were also used to develop an ELISA and this was used to detect metabolites retaining the parent D-ring structure following methandriol (17alpha-methylandrost-5-ene-3beta,17beta-diol) administration. The ELISA methods developed have application as primary screening tools for detection of new and known anabolic steroid metabolites.

Anabolic Agents↗
PubMed2003

Method development for corticosteroids and anabolic steroids by micellar liquid chromatography.

A systematic optimization of the HPLC separation of a complex mixture containing urinary steroids (anabolics and corticoids), boldenone and bolasterone (synthetic anabolics) by micellar liquid chromatography has been carried out. The isocratic micellar mobile phases (from binary to quaternary) consisted of sodium dodecyl sulphate and organic modifiers such as acetonitrile, tetrahydrofuran, propanol, butanol or pentanol. The effect of the organic modifiers, surfactant concentration, temperature, ionic strength and flow-rate on the separation has been studied. A micellar mobile phase made of 5% propanol and 40 mM surfactant allowed the separation of 13 steroids in about 23 min. A bivariant optimization method for the micellar mobile phase surfactant-propanol corroborated the above results. The separations obtained show good perspectives for future developments.

Adrenal Cortex Hormones↗
PubMed1984

Alteration of hormone levels in normal males given the anabolic steroid stanozolol.

Anabolic steroids have widespread metabolic effects but, to date, their proven clinical indications have been limited. Recently the 17 alpha-alkylated steroid, stanozolol, has been shown to be of value in a variety of commonly occurring vascular diseases. Its endocrine effects have received little attention and we have investigated the effect of administering a 14 d course of stanozolol (10 mg orally per day) on a variety of important hormonal pathways in nine healthy male subjects. Significant changes occurred as follows: a 55% reduction in serum testosterone levels was noted and was accompanied by reductions in 'derived' free testosterone, sex hormone binding globulin and LH levels; total T4 and T3 levels fell in association with a decrease in thyroxine binding globulin, but no alteration was detected in TSH or free T4 levels. Changes in vitamin D status, with falls in 25-hydroxycholecalciferol and vitamin D binding globulin were also observed. These effects were reversible on stopping treatment. Stanozolol therapy therefore leads to a number of hormonal changes, probably by an action at both pituitary and hepatic levels.

Adult↗
PubMed1985

Response of serum testosterone and its precursor steroids, SHBG and CBG to anabolic steroid and testosterone self-administration in man.

The influence of high doses of testosterone and anabolic steroids on testicular endocrine function and on circulating steroid binding proteins, sex hormone binding globulin (SHBG) and cortisol binding globulin (CBG), were investigated in power athletes for 26 weeks of steroid self-administration and for the following 16 weeks after drug withdrawal. Serum testosterone and androstenedione concentrations increased (P less than 0.05) but pregnenolone, 17-hydroxypregnenolone, dehydroepiandrosterone, 5-androstene-3 beta, 17 beta-diol, progesterone and 17-hydroxyprogesterone concentrations strongly decreased (P less than 0.001) during steroid administration. Serum pregnenolone, 17-hydroxypregnenolone and dehydroepiandrosterone sulphate concentrations followed the changes of the corresponding unconjugated steroids but 5-androstene-3 beta, 17 beta-diol and testosterone sulphate concentrations remained unchanged during the follow-up time. During drug administration SHBG concentrations decreased by about 80 to 90% and remained low even for the 16 weeks following steroid withdrawal. Steroid administration had no influence on serum CBG concentrations. In conclusion, self-administration of testosterone and anabolic steroids soon led to impairment of testicular endocrine function which was characterized by low concentrations of testosterone precursors, high ratios of testosterone to its precursor steroids and low SHBG concentrations. Decreased concentrations of SHBG and testicular steroids were still partly evident during the 16 weeks after drug withdrawal. The depressed circulating levels of dehydroepiandrosterone and its sulphate may indicate that the androgenic-anabolic steroids also suppress adrenal androgen production.

17-alpha-Hydroxypregnenolone↗
PubMed1999

Male infertility due to anabolic steroids.

(1) The anabolic steroids used by some sportsmen can cause azoospermia, which usually resolves when the drugs are stopped. (2) Infertile sportsmen should be asked if they use anabolic steroids.

Anabolic Agents↗
PubMed2002

Anabolic steroids.

The term "anabolic steroids" refers to testosterone derivatives that are used either clinically or by athletes for their anabolic properties. However, scientists have questioned the anabolic effects of testosterone and its derivatives in normal men for decades. Most scientists concluded that anabolic steroids do not increase muscle size or strength in people with normal gonadal function and have discounted positive results as unduly influenced by positive expectations of athletes, inferior experimental design, or poor data analysis. There has been a tremendous disconnect between the conviction of athletes that these drugs are effective and the conviction of scientists that they aren't. In part, this disconnect results from the completely different dose regimens used by scientists to document the correction of deficiency states and by athletes striving to optimize athletic performance. Recently, careful scientific study of suprapharmacologic doses in clinical settings - including aging, human immunodeficiency virus, and other disease states - supports the efficacy of these regimens. However, the mechanism by which these doses act remains unclear. "Anabolism" is defined as any state in which nitrogen is differentially retained in lean body mass, either through stimulation of protein synthesis and/or decreased breakdown of protein anywhere in the body. Testosterone, the main gonadal steroid in males, has marked anabolic effects in addition to its effects on reproduction that are easily observed in developing boys and when hypogonadal men receive testosterone as replacement therapy. However, its efficacy in normal men, as during its use in athletes or in clinical situations in which men are eugonadal, has been debated. A growing literature suggests that use of suprapharmacologic doses can, indeed, be anabolic in certain situations; however, the clear identification of these situations and the mechanism by which anabolic effects occur are unclear. Furthermore, the pharmacology of "anabolism" is in its infancy: no drugs currently available are "purely" anabolic but all possess androgenic properties as well. The present review briefly recapitulates the historic literature about the androgenic/anabolic steroids and describes literature supporting the anabolic activity of these drugs in normal people, focusing on the use of suprapharmacologic doses by athletes and clinicians to achieve anabolic effects in normal humans. We will present the emerging literature that is beginning to explore more specific mechanisms that might mediate the effects of suprapharmacologic regimens. The terms anabolic/androgenic steroids will be used throughout to reflect the combined actions of all drugs that are currently available.

Anabolic Agents↗
PubMed1999

[Ischemic cerebral stroke and anabolic steroids (case report)].

Anabolic steroid use is widespread and has been associated with a variety of pathological conditions. The subject of this case is a 22 years old man with cerebral ischaemic stroke. He had no previous medical complaints but had a history of anabolic steroid abuse. This case presents a side effect of long term abuse of these drugs.

Adult↗
PubMed1989

Hooked on hormones? An anabolic steroid addiction hypothesis.

Widespread illicit anabolic steroid use has recently been reported. A review of available evidence suggests that elevations of serum levels of steroid hormones, including anabolic steroids, have profound psychological effects. Long-term, high-dose anabolic steroid use may lead to a preoccupation with drug use, difficulty stopping despite psychological side effects, and drug craving. Reductions in serum levels of steroid hormones appear to result in acute hyperadrenergic withdrawal symptoms that respond to steroid replacement or to agents that also ameliorate withdrawal symptoms in alcohol and opioid dependence. A delayed depression syndrome when serum steroid levels drop precipitously has been reported that appears similar to that observed in withdrawing cocaine-dependent individuals. We conclude that a proportion of anabolic steroid abusers may develop a previously unrecognized sex steroid hormone-dependence disorder and that treatment should be based on research into steroid effects on opioid and aminergic neurotransmission systems and relapse prevention.

Acute Disease↗
PubMed1993

Pharmacokinetics of anabolic steroids.

After an anabolic steroid is administered orally there is a rapid increase in its concentration in the blood in the following few hours. Excretion of the compound and its metabolites takes place via the urine and faeces, usually taking several days to completely pass through the system. Parenteral anabolic preparations, such as microcrystal suspensions, implants and solutions of nandrolone esters in a vegetable oil, are absorbed slowly. The absorption of esters from the site of injection is a logarithmic process and depends on the nature of the ester concerned. The absorption rate is slower the longer the fatty acid chain in the ester. The rate of absorption is important regarding the length of the action, and is also relevant for the compound's pharmacodynamic pattern. Metabolism of anabolic steroids takes place mainly in the liver and involves reduction, hydroxylation and the formation of conjugates. The enzymes that bring about these changes and the metabolic pathways involved are similar to endogenous steroids. The presence of high concentrations of metabolites in the bile and in the intestinal tract points to enterohepatic circulation of metabolites. After the administration of slowly-absorbed nandrolone esters the excretion of the metabolites continues for weeks or even months. It is probable that the absorption rate of the esters from the injection depot is the rate-limiting process in the pharmacokinetics of these compounds.

Administration, Oral↗
PubMed1994

Anabolic steroid use in the adolescent athlete.

Recent surveys indicate that the use of androgenic-anabolic steroids (anabolic steroids) is prevalent among adolescent athletes, particularly those in high school. The cost of clinical drug testing makes it impractical to use random testing to identify users of these ergogenic aids. The athletic trainer is often in a position to identify anabolic steroid users if he/she knows the clinical signs and symptoms. In this article, we briefly discuss the history of anabolic steroid use, how they work, their potentially dangerous side effects, evidence of increased use by adolescent athletes, and a list of clinical signs and symptoms. Finally, we suggest strategies that may help athletic trainers counsel athletes about anabolic steroid use.

Journal Article↗
PubMed1984

Anabolic steroids.

Anabolic-androgenic steroid hormones are used by athletes in an attempt to improve performance. Side effects include decreased testosterone and sperm production, acne, balding, and increased aggression. The long-term effects are not known.

Adolescent↗
PubMed1993

Anabolic steroids and fibrinolysis.

Anabolic steroids increase the activity of the fibrinolytic system by reducing plasma levels of inhibitors (plasminogen activator inhibitor type I, histidine-rich glycoprotein, alpha-2-macroglobulin) and increasing plasma levels of tissue-type plasminogen activator activity, plasminogen, and plasmin activity (B beta 15-42 fragment of fibrinogen). Plasminogen activator inhibitor levels are elevated, and tissue-type plasminogen activator activity is depressed, in a variety of disease states, including premature venous or arterial thrombosis, connective tissue disorders, and cancer. Such abnormalities can be reversed by anabolic steroids. However the clinical benefits and adverse effects of such treatment remain to be established by large, randomized controlled trials.

Anabolic Agents↗
PubMed1993

Sexual functioning of male anabolic steroid abusers.

The effects of anabolic steroid use on male sexual behavior were assessed using a structured clinical interview administered to male body builders currently using steroids, and to two comparison groups (body builders with a past but not current history of steroid use, and a group of "natural" body builders who had never used steroids). Current anabolic steroid users had a significantly higher coital and orgasmic frequency than did comparison athletes. They also reported a significantly higher incidence of erectile difficulties during the past month. Beliefs concerning the sexually stimulating effects of steroids did not correlate with the frequencies of specific sexual behaviors. The data support the contention that anabolic steroids, as androgenic compounds, enhance sexual desire.

Adult↗