STEROIDS,
a group of natural and synthetic chemical compounds - derivatives of partially or fully hydrogenated 1,2-cyclopentenophenanthrene type
Also on the topic:
MEDICINE
in the molecular skeleton of which 17 carbon atoms form 4 articulated rings A, B, C, D. Steroids are widespread in nature, they are involved in a wide variety of biological functions. Sex hormones, vitamin D, adrenal hormones, bile acids, hormones of molting and metamorphosis of arthropods, insect repellents that repel predators, and poisons in the skin of toads are of steroid nature. Both natural and synthetic steroids, with similar structures, exhibit very different physiological effects, so they are widely used in medicine as anti-inflammatory, cardiac, contraceptive and other agents.
Also on topic:
VITAMIN D
Steroids are divided into sterols, bile acids, steroid hormones, steroid saponins, cardiac glycosides and steroid alkaloids ( see also
ALKALOIDS).
Steroids are most often found in the form of sterols, found in almost all plants, fungi and animals. This, in particular, is the well-known cholesterol, which serves as the starting material for the synthesis of all steroid hormones in the body. Cholesterol can be used for the industrial production of many steroids, but it is more economical to use instead some of the readily available plant sterols (for example, stigmasterol from soybeans) that are structurally similar to the target steroids.
Steroid sex hormones
Also on topic:
ENDOCRINE SYSTEM
are steroids produced by or affecting the gonads (testes and ovaries). These include androgens, or male hormones, the main of which is testosterone, and female sex hormones - estrogens and progestins (gestagens). Progestins, including progesterone, are involved in preparing the uterus for pregnancy and in maintaining pregnancy. Synthetic progestins and estrogens are included in birth control pills ( see also
HORMONES).
Androgens, due to their anabolic activity (manifested in particular in the building of muscle and bone tissue), have become notorious among athletes, for whom the word “steroid” has come to mean specifically male sex hormones. However, the ability of androgens taken in high doses to improve athletic performance by increasing strength, endurance, and muscle mass remains a matter of debate. Moreover, excessive use of these steroids can lead to liver disease and other harmful side effects.
History of anabolic steroids[edit | edit code]
The use of anabolic steroids began even before their identification and isolation. Medical use of animal testicle extract began in the late 19th century. In 1931, Adolf Butenandt was able to isolate 15 mg of androstenone from 10,000 liters of urine. This anabolic steroid was subsequently synthesized by Leopold Ruzicka in 1934.
In the 1930s, it was already known that testicular extract contained a more powerful anabolic steroid than androstenone. Three groups of scientists, funded by three competing pharmaceutical companies from different countries: the Netherlands, Nazi Germany and Switzerland, began searching for more potent compounds.[3] Thus, in May 1935, Karoly Gyula David, E. Dingemanse, J. Freud and Ernst Laqueur managed to isolate crystalline testosterone [4]. The hormone received its name based on its origin: dough - testicle, sterol - steroid structure, and the ending -one, which indicates that the substance is a ketone.
The chemical synthesis of testosterone from cholesterol was carried out in the same year by Butenandt and G. Hanisch. Just a week after this event, the third group of Ruzicka and A. Wettstein applied for a patent on a new method for the chemical synthesis of testosterone. Ruzicka and Butenandt received the Nobel Prize for their inventions in 1939.
Clinical trials in humans, including oral methyltestosterone and injections of testosterone propionate, began in 1937.
The first mention of an anabolic steroid in the history of strength sports dates back to 1938, when it refers to testosterone propionate in a letter to the editor of Strength and Health magazine. There are rumors that in Nazi Germany anabolic steroids were used on soldiers to increase aggression and endurance, but at present these facts have no official confirmation. However, Adolf Hitler himself received injections of anabolic steroids, according to his personal physician. Anabolic steroids were used by the Nazis in experiments on concentration camp prisoners. In other countries, anabolic steroids were used to treat and restore malnourished prisoners who were released from camps. [5]
Modern history
Improvements in testosterone's anabolic properties began in the 1940s in the Soviet Union and Eastern Bloc countries such as East Germany, where anabolic steroids began to be used to improve the performance of Olympic weightlifters. In response to the success of Russian weightlifters, the US Olympic team doctor, Dr. John Ziegler, began working with chemists to develop an anabolic steroid with less androgenic activity, resulting in Methandrostenolone. The new drug was approved by the FDA in 1958. It was most often prescribed for the treatment of severe burns and the elderly, but most Methandrostenolone was consumed in bodybuilding and other strength sports. Dr. John Ziegler prescribed only small doses for athletes, but he later noticed that athletes who overdosed experienced prostate hypertrophy and testicular atrophy. [6]
In 1976, anabolic steroids were banned by the International Olympic Committee, ending the history of their legal use in sports, and 10 years after that, special tests were developed to determine anabolic steroids in urine.
Search for new anabolic steroids[edit | edit code]
Currently, the entire variety of anabolic steroids and their modifications is based on four main ideas:
- Alkylation at the alpha-17 position with a methyl or ethyl group to prevent drug degradation in the liver, allowing oral administration in tablet form.
- Esterification at the beta-17 position, which makes the drug soluble in fats and allows the creation of a tissue depot that is absorbed for a long time, thus significantly increasing the duration of action (up to several months) of the anabolic agent.
- A change in the ring structure of an anabolic steroid applies to oral and parenteral drugs and is associated with the desire to increase the anabolic index.
- A structural change that prevents the conversion of steroids to estrogens.
Also, active development of a new class of selective androgen receptor modulators is currently underway.
Corticoids.
Steroids secreted by the adrenal cortex are called corticoids or corticosteroids. About 30 different corticoids are known, divided into two broad classes: mineralocorticoids and glucocorticoids. The former regulate mineral, water-salt metabolism (for example, chemical processes involving sodium), the latter regulate carbohydrate (glucose) and protein metabolism.
The function of corticoids is mainly to maintain homeostasis (a constant, stable internal state of the body), especially in stressful situations (during inflammatory processes, desalination or fasting). Thus, during fasting, corticosteroids, by stimulating the formation of glucose from body tissues, protect the vital functions of the brain, which depend on glucose as an energy source. One of the glucocorticoids involved in maintaining homeostasis is cortisone, which is widely used in the treatment of arthritis and other diseases as an anti-inflammatory agent. However, long-term massive use of cortisone leads to harmful side effects, so doctors now routinely prescribe related synthetic steroid compounds for the same diseases. see also
ADRENAL GLANDS.
Indications for use
Anabolic steroids are widely used in clinical practice. The ability of these drugs to enhance synthetic processes in protein metabolism allows them to be used to stimulate weight and improve the general condition in diseases that occur with symptoms of exhaustion, in the preoperative and postoperative periods, during radiation therapy, in acute and chronic infections, in the stage of convalescence after serious illnesses , with interstitial pituitary insufficiency, toxic goiter. When moderate doses of anabolic steroids are used, the absence of virilization in female patients and increased libido in male patients, the absence of noticeable progression of skeletal differentiation and ossification allows the successful use of anabolic steroids to stimulate the growth and physical development of premature children and patients with hypoplastic forms of short stature.
The use of anabolic steroids has also proven to be very beneficial for pituitary and cerebral-pituitary dwarfism.
Anabolic steroids have a positive effect in case of myocardial infarction, accelerating reparative processes in the heart. When they were included in the complex of therapeutic agents, positive ECG dynamics were noted, the number of aneurysms, myocardial ruptures, and so on was lower than before their use.
Anabolic steroids for rheumatism improve the condition of the myocardium and increase the indicators of nonspecific immunity. The improvement in renal function and reduction in residual nitrogen in the blood under the influence of anabolic steroids makes them a useful symptomatic remedy for renal failure, as well as nephrotic hypoproteinemia. Anabolic steroids improve the trophism of the vascular wall, increase capillary permeability, which is used in the treatment of diabetic angiopathy: nephropathy and retinopathy. Under their influence, an increase in the glomerular filtration of the kidneys and, in some cases, an improvement in the condition of the fundus of the eye were noted: resorption of exudates while maintaining, and sometimes increasing, visual acuity.
The anti-catabolic properties of anabolic steroids determine the effectiveness of their use in endogenous hyperglucocorticism (Cushing's disease, steroid diabetes) and long-term therapy with corticosteroids.
The ability of anabolic steroids to enhance protein synthesis in the bone matrix and retain calcium, phosphorus, sulfur and other minerals allows them to be successfully used in various forms of osteoporosis, long-term non-healing fractures, and osteogenesis imperfecta. To achieve an effect when treating with anabolic steroids, patients must receive adequate amounts of proteins, fats, carbohydrates, vitamins and minerals from food.
The antigonadotropic effect explains the activity of anabolic steroids in breast cancer and menopausal angioneurosis in women, and the progesterone-like effect explains the effect in functional metrorrhagia and mastopathy.
Cardiac glycosides
– very toxic substances of plant origin, but in small doses they stimulate cardiac activity. Used to treat heart and other diseases. Under the influence of acids, they break down into sugars and aglycone (steroid). Free aglycones of cardiac glycosides (genins) are strong poisons that are not used in medicine; Among them, strophanthidin (convallate oxygenin) is the most well studied; it is contained in lily of the valley, hemp lily, and wallflower. Other aglycones are also known, for example, digitoxigenin, dioxygenin, gitoxigenin, periplogenin, sarmentogenin, adonitoxigenin, etc. see also
GLYCOSIDES.
Links[edit | edit code]
- https://www.psypost.org/2017/03/study-suggests-sexual-competition-among-men-influences-steroid-use-48014
- https://journals.sagepub.com/doi/abs/10.1177/1359105317692145
- Hoberman JM, Yesalis CE (1995). "The history of synthetic testosterone". Scientific American 272(2):76–81. doi:10.1038/scientificamerican0295-76 (inactive 2010-01-05).
- David K, Dingemanse E, Freud J, Laqueur L (1935). "Uber krystallinisches mannliches Hormon aus Hoden (Testosteron) wirksamer als aus harn oder aus Cholesterin bereitetes Androsteron." Hoppe Seylers Z Physiol Chem 233:281
- Taylor, William N (January 1, 2002). Anabolic Steroids and the Athlete. McFarland & Company. p. 181.
- Justin Peters The Man Behind the Juice, Slate Friday, Feb. 18, 2005, Accessed 29 April 2008
- Lavery DN, McEwan IJ (2005). "Structure and function of steroid receptor AF1 transactivation domains: induction of active conformations." Biochem. J. 391(Pt 3): 449–64
- Singh R, Artaza J, Taylor W, Gonzalez-Cadavid N, Bhasin S (2003). "Androgens stimulate myogenic differentiation and inhibit adipogenesis in C3H 10T1/2 pluripotent cells through an androgen receptor-mediated pathway." Endocrinology 144(11):5081–8.
- George P. Chrousos, The gonadal hormones and inhibitors, in Bertram G. Katzung (Ed.), Basic and Clinical Pharmacology, McGraw-Hill Professional, 2006, ISBN 0-07-145153-6, p. 674–676
Toad poisons and sea onion aglycones
(Scilla maritima
). Toad poisons are secreted by skin glands. They are used in medicine. They have the same effect on the mammalian heart as cardiac glycosides due to the steroidal bufogenins present in them. Related compounds are also present (in the form of glycosides) in sea onions, which have been used since ancient times as medicine (Ancient Egypt, Ancient Rome). The most important of the bufogenins, bufalin and bufotalin, were isolated from the skin of the Chinese toad. Scillarene A has been isolated from sea onion glycosides, the saponification of which produces the aglycone scillaridine A.
Introduction
Finally, we come to the most difficult, and for some, perhaps the most interesting topic. It is interesting mainly for one single reason - many, if not everyone, talk about it, but almost no one can correctly explain what it is. The topic of using anabolic steroids has become especially popular among beginners who mistakenly believe that such drugs are the only and irreplaceable remedy that can turn “scraggy” into a mountain of muscles in the shortest possible time.
This category of means cannot be considered either absolute good or absolute evil. This categorization is generally incorrect in its formulation. Their use can be called expedient or inappropriate only in a specific individual case. In general, whether to accept or not is neither good nor bad, it’s just a choice. And this choice must be deliberate. It is precisely in order to have something to think about that this material was created.
IMPORTANT. This article is based on materials from the book by the author Davidenko F. Yu. “ ANABOLISM PROFILES ” .
What is the rollback phenomenon
The rebound phenomenon is the process of loss of muscle volume after stopping the use of anabolic steroids. The duration of this process is usually about 1 month. The rollback manifests itself especially clearly after prolonged use of inflated dosages, and also, which is also not uncommon, after illiterately designed courses. Now let us explain how this process occurs and what is the immediate reason for the decrease in volume and strength indicators.
The body always strives for balance and constancy of the internal environment, and taking AS takes it out of this balance. As soon as the intake of steroids into the body stops, all their positive effects on it also immediately end. Training no longer stimulates the active formation of new myofibrils in such large quantities as before, and the formation of new ones no longer occurs in such favorable conditions. In other words, when you stop taking AS, the growth of muscle volume stops to a large extent. But what happens to the muscles that you have already built up?
It is not difficult to guess that the number of myofibrils begins to decrease. This occurs due to the completely natural process of aging. Aged and no longer needed structures are subsequently replaced by new ones. At the moment when the level of anabolic hormones sharply decreases, the formation of new myofibrils slows down significantly, and the process of replacing old myofibrils with new ones no longer proceeds so actively. This happens due to the fact that new myofibrils no longer come to replace old myofibrils. At this moment the so-called rollback begins. The volume of muscle cells is reduced to such an amount that the current level of testosterone can be maintained, and since it is strongly suppressed by the use of anabolic steroids, you can not only “deflate”, but even lose what you had before the start of the course.
Exiting the course is usually accompanied by a number of procedures that are aimed at maximizing the preservation of health and full functioning of all body systems. This series of procedures is called post-cycle therapy. During this period, all physical activity is usually reduced, the caloric intake of the diet is reduced, and in general it is recommended to allow the body to recover so that it can return to its original vital signs. This rehabilitation period, depending on the complexity of the course and its duration, can sometimes reach several months.
