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Recent developments in the toxicology of anabolic steroids.

Anabolic steroids are extensively abused as ergogenic aids by athletes (and others). A number of features of anabolic steroid use and toxicology have been recently reviewed in the Journal, and a large body of data has accumulated concerning their toxic nature. The lipoprotein profile induced by anabolic steroids carries a markedly adverse cardiovascular risk. Glucose metabolism is significantly altered and includes peripheral insulin resistance, hyperinsulinaemia and attenuated responses to glucagon. Hypertension has been noted. Psychiatric and psychological alterations are major toxicities of anabolic steroids, and probably constitute the major mechanism of their action. Hepatic neoplasia occurs in the setting of abuse of this class of drugs, and may be related to their use, although there is no convincing evidence that other malignancies are induced in athletes who abuse them. Gross disturbance of reproductive function occurs in both sexes: hypogonadal states are common and prolonged. The anabolic steroids are toxic drugs with both long and short term effects. Their abuse by athletes is to be decried, particularly in view of the frequent and prolonged use by the young.

Anabolic Agents↗

Anabolic steroids.

Anabolic steroids are synthetic derivatives of testosterone modified to enhance the anabolic rather than the androgenic actions of the hormone. The anabolic effects are considered to be those promoting protein synthesis, muscle growth and crythopoiesis. There are numerous side-effects to anabolic steroids, including hypertension and atherosclerosis, blood clotting, jaundice, hepatic carcinoma, tendon damage, psychiatric and behavioural effects and, in males, reduced fertility and gynaccomastia. Anabolic steroids were added to the International Olympic Committee's list of banned substances in 1975. The majority of 'evidence' concerning the efficacy of anabolic steroids as performance enhancing agents is anecdotal. In the main, experimental investigations have been poorly designed scientifically, clinically and statistically. The percentage of positive test results from IOC accredited laboratories has remained consistently low. However, athletes take their steroids during training and out-of-competition testing is not conducted in all countries, although international co-operation is now under consideration. Despite the lack of conclusive evidence, steroids users will continue to hold the view that their effects are efficacious and they are therefore unlikely to be persuaded to curtail their use.

Anabolic Agents↗

The cardiac toxicity of anabolic steroids.

Anabolic steroids are synthetic derivatives of testosterone that were developed as adjunct therapy for a variety of medical conditions. Today they are most commonly used to enhance athletic performance and muscular development. Both illicit and medically indicated anabolic steroid use have been temporally associated with many subsequent defects within each of the body systems. Testosterone is the preferred ligand of the human androgen receptor in the myocardium and directly modulates transcription, translation, and enzyme function. Consequent alterations of cellular pathology and organ physiology are similar to those seen with heart failure and cardiomyopathy. Hypertension, ventricular remodeling, myocardial ischemia, and sudden cardiac death have each been temporally and causally associated with anabolic steroid use in humans. These effects persist long after use has been discontinued and have significant impact on subsequent morbidity and mortality. The mechanisms of cardiac disease as a result of anabolic steroid use are discussed in this review.

Anabolic Agents↗

Anabolic steroids.

Anabolic steroids may be an additional mode of intervention to promote anabolism and improve clinical outcome in various acute and chronic wasting diseases. The present review discusses the rationale for anabolic steroid treatment in acute and chronic disease, their mechanistic actions, the available clinical trials in acute and chronic disease and their side-effects.

Acute Disease↗

Adverse effects of anabolic steroids.

Anabolic steroids are used therapeutically for various disorders and as ergogenic aids by athletes to augment strength, muscular development, and to enhance performance. There is a wide range of concomitant temporary and permanent adverse effects with steroid administration. Several well-documented adverse actions of these hormones may develop rapidly within several weeks or less (i.e. altered reproductive function) or require up to several years of steroid intake (i.e. liver carcinoma). More recent studies indicate that glucose intolerance, insulin resistance, increased cardiovascular disease risk profiles, cerebral dangers, musculoskeletal injuries, prostate cancer, psychosis and schizophrenic episodes, among others, accompany anabolic steroid intake. There is, at present, no evidence to support the claim that athletes are less susceptible to adverse effects than those individuals receiving hormone treatment in a clinical setting. Based on the available information which has accumulated primarily from cross-sectional, short term longitudinal, and case studies, there is a need: (a) to develop a comprehensive battery of specific and sensitive markers of adverse effects, particularly those that would be able to detect the onset of adverse actions; and (b) to conduct controlled long term longitudinal studies in order to fully understand the extensiveness and mechanisms involved in the occurrence of adverse effects.

Anabolic Agents↗

Sudden cardiac death in a 20-year-old bodybuilder using anabolic steroids.

Anabolic steroid use is widespread and has been associated with a variety of pathological conditions. The subject of this case is a 20-year-old amateur bodybuilder who died of sudden cardiopulmonary arrest. He had no previous medical complaints but had a history of anabolic steroid abuse and a hypertrophic heart (515 g) at autopsy. This case presentation will discuss the cardiovascular effects of these drugs and the possible impact of long-term abuse.

Adult↗

Anabolic steroids.

Anabolic steroids have been employed extensively in equine practice over the past 25 years. Their usefulness is largely dependent on subjective opinions, as only minimal studies have been carried out in horses. Therefore, their use will vary markedly between practitioners depending on their personal experiences and pressures by trainers to use them. They form part of rational therapy in a variety of conditions. In addition to use for increasing muscle mass, they are used to a varying extent in the raising of yearlings and in the training and racing of horses with the view of improving performance. However, in almost all countries, the latter use is largely curtailed, and the presence of these substances in postrace urine samples constitutes use of an illegal substance. To detect the use of anabolic steroids, including testosterone, sensitive ELISA tests for screening and GC/MS for confirmation have been developed. These compounds can be used safely. Risks can be encountered if too high doses are used, as horses may become difficult to manage due to increased aggressiveness and other stallion-like behavior. Reproductive efficiency in both stallions and mares may be temporarily impaired, but this is quite rapidly reversible following cessation of treatment.

Anabolic Agents↗

[Pharmacological action of anabolic steroids].

Anabolic steroids (AS) are derivatives of androgen (testosterone and its close relatives). AS have been primarily developed for clinical use as anabolic agents with the expectation that they would be relatively less androgenic than testosterone and its close relatives. Various AS are applied to clinical use, but none is free from androgenic activity. Relation between chemical structure and anabolic-androgenic potency of various AS is summarized. AS action in erythropoiesis operates through increased porphyrin formation and production of erythropoietin. Mechanism of AS action in bone formation is suggested that AS potentiate intestinal 1.25(OH)2D receptors. Identification of androgen receptors in normal human osteoblast-like cells suggest that AS act directly on receptor-mediated mechanism. The other action of AS is briefly summarized.

Anabolic Agents↗

Spontaneous rupture of the anterior cruciate ligament after anabolic steroids.

Anabolic steroids remain popular among body builders and power athletes despite numerous warning about their side effects. A case of spontaneous rupture of the anterior cruciate ligament is reported in a bodybuilder taking steroids. While there are many published reports of tendon rupture associated with steroid intake, the authors could find no report relating to ligament disruption.

Adult↗

Anabolic steroid abuse.

Anabolic steroids are capable of increasing strength and muscle bulk in certain individuals when combined with a proper diet and an intense training program. Any steroid that is anabolic is also androgenic. Anabolic steroids are fraught with numerous side effects, a few of which are potentially life threatening, and some of which are permanent. Most of the side effects are mild and reversible. Use of anabolic steroids in sports is as much a moral issue as a medical one. Drug testing has not been a very successful means to eradicate abuse in the sporting arena. Education alone is probably not the answer to stopping anabolic steroid abuse but is an essential first step in combating this problem. Use of anabolic steroids in athletes is a form of cheating, and use will likely continue, especially if the rewards for success in sports remain so high. Physicians should avoid condemning individuals who choose to use anabolic steroids and encourage discussion of use with their health providers.

Adolescent↗

Cardiovascular implications of anabolic steroid abuse.

Anabolic steroids are synthetic derivatives of the hormone testosterone. Anabolic effects such as anticatabolism, increased skeletal muscle mass, and increased aggressiveness are usually desired; however, androgenic effects also result. Decreases in high-density lipoprotein, increases in low-density lipoprotein, changes in total serum cholesterol, hematocrit, and clotting factors, and the development of hypertensive diseases have all been implicated as resulting from anabolic steroid use. Research does not directly link anabolic steroids with cardiovascular diseases, but steroid use can significantly increase risk factors for atherosclerotic cardiovascular disease.

Anabolic Agents↗

Radioimmunoassay of anabolic steroids: an evaluation of three antisera for the detection of anabolic steroids in biological fluids.

Recently developed radioimmunoassays (RIA) for the analysis of anabolic steroids and their metabolites in biological fluids were tested for cross-reactivity with other types of steroids. Results show that the degree of desirable cross-reactivity within the two classes or orally active anabolic steroids vary widely and that the antiserum for 19-Nortestosterone (the active principle of intramuscular preparations) has a very high degree of undesirable cross-reactivity with components of oral contraceptives. Single and multiple dose studies in human volunteers demonstrate that the detection level and degree of retrospectivity are likewise variable but that the test easily detects most anabolic steroids during treatment. At the present time, the combination of the three antisera for the assay of a sample appears to be a relatively rapid and economic method for screening large numbers of samples in situations where doping control of anabolic steroids is required. The importance of utilizing physico-chemical means for identification of RIA potential positives is emphasized.

Anabolic Agents↗

Dying to be big: a review of anabolic steroid use.

Anabolic steroids use is commonly perceived to be the domain of the higher echelons of competitive athletes. However, a great deal of anabolic steroid use occurs in private gymnasia (non-local authority) among non-competitive recreational athletes. Our study has attempted to give an insight into the prevalence of the use of these drugs, the hazards associated with it, and the public health responses which we have adopted.

Adult↗

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↗

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↗

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↗