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.     

Metabolism of anabolic androgenic steroids

Anabolic androgenic steroids (AAS) are misused to a high extent in sports by athletes to improve their physical performance. Sports federations consider the use of these drugs in sports as doping. The misuse of AAS is controlled by detection of the parent AAS (when excreted into urine) and (or) their metabolites in urine of athletes. I present a review of the metabolism of AAS. Testosterone is the principal androgenic steroid and its metabolism is compared with that of AAS. The review is divided into two parts: the general metabolism of AAS, which is separated into phase I and phase II metabolism and includes a systematic discussion of metabolic changes in the steroid molecule according to the regions (A-D rings), and the specific metabolism of AAS, which presents the metabolism of 26 AAS in humans.     

Treatment of myasthenic patients with anabolic steroids

The authors report of their observations over 52 patients with severe and moderate myasthenia who after diverse forms of therapy (thymusectomy, x-ray therapy, prolonged use of anticholesterase preparations, etc.) did not demonstrate a stable therapeutical effectiveness. However, treatment by retabolil proved to be effective with minimal side effects. The paper contains theoretical prereqisites to therapy by anabolic hormones and the approximate scheme of its use.     

Azoospermia in 2 body-builders after taking anabolic steroids

During investigations for infertility azoospermia was diagnosed in two men who were concomitantly using anabolic steroids for body-building. Following cessation of anabolic steroid use the semen quality was normalized. Suppression of spermatogenesis during treatment with testosterone and derivatives hereof is wellknown. Usage of anabolic steroids should be remembered as a cause of oligo- and azoospermia and asked about in cases of sperm counts approaching or at zero.     

Intrasynovial injection of steroids uses and abuses

Intra-articular injection of steroids is a valuable method of treatment, but selection of the appropriate clinical setting is required to obtain maximal benefits and to minimize the complications. All intra-articular injections must be performed under strict aseptic technique. The rheumatoid patient with one or two joints that resist systemic therapy and the patient with an occasional osteoarthritic joint with an acute inflammation are amenable to this treatment. The patient who has acute attacks of tendinitis, pseudogout, or bursitis will obtain significant benefits. Selected patients with traumatic and acute gouty arthritis also may benefit. Repetitive injections appear to be contra-indicated as they may create an environment conducive to joint destruction.     

The action of anabolic steroids on bone in experimental animals

Anabolic steroids are currently used in the treatment of established osteoporosis. It has been demonstrated that, at least partly, anabolic steroids increase bone density by stimulating bone formation. Very little is known about how anabolic steroids affect bone in experimental animals. Because bone studies in animals have been performed only with the anabolic steroid nandrolone, or its long-acting ester nandrolone decanoate (ND), we present a general overview in this paper of the effect of these anabolic agents in various steroid-affected animal models for osteoporosis, viz. gonadectomized rats, heparin-treated mice and intact or ovariectomized dogs. In rats and mice these agents increase longitudinal and periosteal bone growth and bone mass, thus demonstrating their anabolic action. They also decrease trabecular bone resorption in ovariectomized and orchidectomized rats, which indicates that they have anti-catabolic effects. In ovariectomized rats, ND was found to increase the mechanical strength of cortical bone, which is an important property in a drug that is intended to be used in treating established osteoporosis. In elderly dogs, ND was found to stimulate endosteal bone formation. These findings indicate that nandrolone and ND have beneficial effects on bone in both oestrogen and androgen-deficient animals.     

The use of anabolic steroids by athletes to increase body weight and strength

Over the past 20 years the taking of anabolic steroids by healthy athletes for the purpose of increasing body weight and strength has become very widespread. The ability of these agents to cause potentially serious side effects is discussed. In a series of 20 subjects studied over 18 months, no side effects of significance were recorded, and marked increases in strength and body weight were achieved.     

Lipoprotein (a) and cholesterol in body builders using anabolic androgenic steroids

A 67-year-old Taiwanese woman with multilocular hydatid cysts of the liver presented with a 5-month history of intermittent right upper abdominal discomfort. Abdominal ultrasonography and computed tomography showed multiple cysts in both lobes of the liver. Subsequent selective celiac angiography revealed an avascular space-occupying lesion in the right lobe. She underwent a radical excision of the cyst by total closed (without opening the wall) cystopericystectomy over segments 4, 5 and 6. Histologic study of the lesions showed three structural components: 1) an outer acellular laminated membrane, 2) a thin nucleated germinal membrane and 3) several protoscolices with Echinococcus granulosus suckers. The patient has been well for 5 years since her discharge. Although hydatid cysts of the liver are extremely rare in Taiwan, they may cause life-threatening complications and mortality. Making a preoperative diagnosis is important and is only possible if this rare disease is kept in mind.     

The effects of anabolic steroids on driving performance as assessed by the Iowa Driver Simulator

The effect of physiologic (100 mg/wk) and supraphysiologic (250 and 500 mg/wk) doses of testosterone cypionate (TC) on automobile driving were studied using the Iowa Driver Simulator. Six normal subject volunteers were studied off TC and on TC once steady-state concentrations were achieved after at least three weeks of dosing. Despite the administration of supraphysiologic testosterone doses, an increase in aggressive driving behavior was not detected. Likewise, corresponding psychometric testing using the Buss-Durkee Hostility Inventory to assess aggression was unable to detect any change in aggression in the test subjects. Although aggressive driving behavior may be increased by testosterone administration, the drug itself may not be responsible for these effects. Supraphysiologic doses greater than 500 mg/wk and a semi-controlled research environment may be necessary to produce this effect since case reports of AAS abuse causing altered driving behavior may be multifactorial in nature.     

The role of anabolic steroids on baseline and stress heart rate in cynomolgus monkeys.

This investigation examined the role of anabolic steroids on baseline heart rate (HR) and HR responses to the threat of capture in Macaca fascicularis. Ten cynomolgus monkeys were randomly assigned either to a steroid or to a sham control group. Steroid-treated animals were given testosterone injections biweekly for 10 weeks, whereas sham controls received injections of sesame oil on an identical schedule. Pretreatment and posttreatment HRs were evaluated to establish both baseline and acute-stress responses. Results revealed that animals given testosterone experienced a statistically significant increase in baseline HR when contrasted with the sham controls. No difference between the groups was detected in response to the threat of capture. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Two cases of acute myocardial infarction associated with aplastic anemia during treatment with anabolic steroids

Thrombosis is a rare complication in patients with aplastic anemia because of the presence of coincidental thrombocytopenia. We have recently treated two cases, a 61-year-old male and a 59-year-old female, with acute myocardial infarction associated with aplastic anemia. Although their platelet counts were lower than normal in spite of treatment with anabolic steroids for aplastic anemia, the coronary angiographic findings strongly suggested coronary thrombosis in both cases. Anabolic steroids, which have been commonly used for the treatment of aplastic anemia, are a possible risk factor for coronary thrombosis because they have an accelerating effect on thrombus formation. We report two very rare but clinically important cases.     

Clenbuterol and anabolic steroids: a previously unreported cause of myocardial infarction with normal coronary arteriograms

During the last 10 years, several cases of myocardial infarction associated with anabolic steroid use have been reported. Postulated mechanisms to explain this association have included changes in lipid levels, the fibrinolytic system, and platelet aggregation. Clenbuterol is a beta 2-agonist with anabolic properties that has not been seen previously with myocardial infarction. We report a case of myocardial infarction in an otherwise healthy 26-year-old body-builder who recently used clenbuterol and anabolic steroids. In this case, synergistic effects of the two agents seem likely to have played a role in the infarct. The normal coronary arteriograms before any anticoagulant or thrombolytic therapy strongly suggest coronary spasm as the mechanism of the infarct.     

Miscellaneous lesions of bone

There are several tumors and tumorlike entities of bone that do not easily fit into the specific classifications provided elsewhere in this issue. In this article, several seemingly unrelated entities are discussed, including cystic diseases of bone (simple bone cysts and aneurysmal bone cysts), Langerhans' cell histiocytosis, benign and malignant vascular tumors of bone, and adamantinoma of long bone and its relationship to osteofibrous dysplasia.     

Epidural steroids

Although perhaps only controversial internationally, epidural steroids have become the focus of litigation in Australia. The literature provides endorsement but offers little compelling data on rationale and efficacy. Steroid preparations appear to be chemically safe, provided they are accurately injected into the epidural space. Hazards occur if intrathecal penetration is not recognized. Conventional techniques do not guarantee that injectates reach the desired target nerve.     

Sulphonylureas--action and uses

Although sulphonylureas have been of great value in the treatment of diabetics for the last 20 years, there has been some suggestion that when used in treating the maturity onset diabetic, they would be responsible for an increased death rate from cardiovascular disease. This article discusses the factors involved in the use of sulphonylureas with regard to indications, mode of action and side effects.