HUMAN BIOCHEMISTRY - L. V. Kapilevich - 2016

PART 2. FUNDAMENTALS OF SPORTS PHARMACOLOGY

DOPING

The Use of doping is by no means a Discovery of the 20th century. Its history is much longer than one might expect. Doping has existed for as long as sports have. Apparently, it is rooted in human nature—the drive to defeat a rival and win at any cost, often even at the expense of one's own health.

The use of various stimulants to enhance physical and mental performance was documented even in antiquity. For instance, as early as the 2nd century BC, Greek athletes consumed protein, sesame seeds, and certain types of psychotropic mushrooms before competitions. Gladiators of the famous Circus Maximus in Rome (5th century BC) took stimulants to suppress fatigue and pain. In the Middle Ages, Norse berserkers intoxicated themselves before battle with an infusion of fly agaric and other psychotropic mushrooms, inducing a state of aggression that rendered them insensitive to pain and exhaustion. The 20th century "armed" humanity with such agents as anabolic Steroids, amphetamines and their derivatives, and many other milestones of pharmacological science. By the time of the first modern Olympic Games in 1896, athletes possessed a fairly wide arsenal of pharmacological support, ranging from codeine to strychnine (which, in near-lethal doses, acts as a potent stimulant). However, the true beginning of the modern doping era should be considered 1935, when injectable testosterone was isolated and subsequently synthesized by the Yugoslav chemist Leopold Ruzicka. Initially prescribed by Nazi doctors to increase aggression in soldiers (which gave rise to METABOLISM/2.html">THE CONCEPT OF "legal doping"—various stimulants used by pilots, scouts, paratroopers, and commandos), it soon found its way into sports with German athletes at the 1936 Berlin Olympics. Later, following the end of World War II, it was actively utilized in training the USSR national team for the 1952 Olympic Games.

The very term "doping" originates from the English word "dope," which means "to administer a drug." According to the definition established by the Medical Commission of the International Olympic Committee, doping is defined as the Introduction of pharmacological substances into the body of an athlete by any method (via injections, tablets, inhalation, etc.) that artificially enhances performance and athletic results. Consequently, a substance can be classified as doping only if it, or its metabolites, can be detected in the body's biological fluids (Blood, urine) with a high degree of precision and reliability.

Currently, doping agents include:

1. Stimulants (Central Nervous system stimulants, sympathomimetics, analgesics).

These include amphetamines (and their derivatives), ephedrine, and phenylpropanolamine (substances frequently found in various medications). Their effect is comparable to that of adrenaline. Every living Organism possesses innate safety mechanisms that prevent the complete depletion of its internal reserves. Stimulants override these mechanisms, enabling the athlete to draw upon their "emergency reserve" under ultra-high workloads. This group also includes beta-agonists, which occupy an intermediate position between stimulants and anabolics. They can be administered via inhalation, which is why more than half of the athletes registered for the Olympics are officially classified as asthmatics. Most of these drugs exhibit dose-dependent side effects, including headache, nausea, anxiety, Cardiac Arrhythmias, respiratory depression, and the risk of sudden death. The use of stimulants can lead to accidents resulting from the athlete's impaired situational judgment. Furthermore, stimulant abuse leads to drug dependence.

2. Narcotics (narcotic analgesics).

These include morphine and its chemical and pharmacological analogues that act on the central nervous system to relieve pain, as well as ethylmorphine, codeine, and methadone. These drugs raise the pain threshold to such an extent that the athlete fails to recognize the severity of an injury. They induce rapid habituation, leading to severe dependence.

3. Anabolic steroids and other hormonal anabolic agents.

Chemical agents that promote accelerated Muscle growth and increased muscle strength. Unlike stimulants, which allow access to the body's emergency reserves, anabolics expand these reserves, enabling athletes to withstand workloads several times greater than normal. However, Interference with normal hormonal activity triggers adverse side effects, such as tumor growth, psychiatric syndromes, and hepatic and Renal Dysfunction.

4. Beta-blockers.

A Class of drugs that act on so-called beta-receptors. Their use results in a decreased Heart rate and an anti-arrhythmic effect. Beta-blockers are utilized by athletes to induce calmness and reduce tremor in sports requiring precise coordination, such as archery, target shooting, and diving. At the same time, these drugs increase fatigue and reduce endurance.

5. Diuretics.

In certain sports, such as weightlifting, boxing, and wrestling, diuretics are used for rapid weight loss or to enhance muscle definition. Additionally, diuretics are frequently employed to lower the concentration of other prohibited substances in the urine. This Procedure is aimed at concealing the presence of doping agents in the body and is therefore strictly prohibited. Consequences of diuretic use include dehydration and muscle cramps.

In addition, doping Methods include:

1. Blood doping (withdrawing blood from an athlete a certain period before competitions and reinfusing it immediately prior to the event).

The use of blood doping can lead to allergic reactions (rashes, fever), renal dysfunction, circulatory overload, blood clot formation, and metabolic Shock.

2. Pharmacological, chemical, and mechanical manipulation of biological fluids (masking agents, addition of Aromatic Compounds to urine samples, sample substitution, suppression of renal urine excretion, and various other medical subterfuges).

Such manipulations are termed "Procedures" (i.e., any intervention capable of compromising the integrity and reliability of urine samples collected for doping control).

Administration of Doping

From the perspective of the achieved effect, sports doping agents can be broadly divided into 2 main categories:

1) substances administered directly during the competition period for the short-term enhancement of performance, as well as the athlete's mental and physical tone;

2) agents used over an extended period during training to build muscle mass and help athletes adapt to maximum physical stress.

The first group comprises various central nervous system stimulants: a) psychostimulants (or psychomotor stimulants): amphetamine, centedrin (meridil), caffeine, sydnocarb, sydnofen; closely related sympathomimetics: ephedrine and its derivatives, isadrin, berotec, salbutamol; certain nootropics: sodium oxybutyrate, phenibut; b) analeptics: corazole, cordiamine, bemegride; c) agents with a predominant stimulating effect on the Spinal Cord: strychnine. This same group includes certain narcotic analgesics with stimulating or sedative properties: cocaine, morphine and its derivatives (including promedol, omnopon, codeine, dionin), as well as fentanyl, estocin, pentazocine (fortral), tilidine, dipidolor, and others. Additionally, short-term biological stimulation can be achieved through blood transfusions (autologous or homologous) administered immediately before competition (blood transfusion, "blood doping").

The second group of doping agents includes anabolic steroids (AS) and other hormonal anabolic agents. Furthermore, there are specific types of doping agents: a) agents that reduce muscle tremor (limb twitching) and improve movement coordination (beta-blockers, alcohol); b) various diuretics used to reduce (cut) weight and accelerate The excretion of anabolic steroid breakdown products and other doping agents from the body; c) agents capable of masking traces of anabolic steroids during specialized doping control tests, such as the antibiotic probenecid and others. Among all the aforementioned preparations, anabolic steroids have become the most widespread among bodybuilders and weightlifters.

Anabolic Steroids (AS)

In biochemistry, anabolism refers to metabolic reactions that promote the synthesis of various compounds—Proteins, CARBOHYDRATES, Lipids, etc. From a chemical perspective, anabolic steroids are derivatives of a substance called cyclopentanoperhydrophenanthrene, which serves as the structural backbone of Male Sex Hormones. Thus, anabolic steroids are artificially synthesized derivatives of the male sex hormone testosterone (including testosterone itself and its esters). Testosterone affects The Human Body in two main ways: it promotes Protein Synthesis in Skeletal Muscle and, to some extent, myocardial muscle, reduces body fat and alters its distribution—this is the manifestation of testosterone's so-called anabolic activity. Testosterone also drives The Development of male sex characteristics, both primary: initial growth of the Penis, GROWTH AND DEVELOPMENT of the se

minal vesicles, growth and Development of the Prostate Gland; and secondary: density and distribution of body and facial Hair, deepening of the voice, and several others—this is the androgenic activity of testosterone. Synthetic anabolic steroids are substances with enhanced anabolic activity and proportionally reduced androgenic activity. However, anabolic steroids with zero androgenic activity do not and cannot exist. The same can be said, to an even greater extent, of testosterone, its various derivatives (esters), and their mixtures. Consequently, harmless anabolic steroids do not exist, and attempting to obtain them through friends and acquaintances is nothing more than a waste of time and effort. The primary effects of using anabolic steroids in sports during the initial period of intake include: rapid gains in muscle mass (provided the diet contains adequate protein, fats, carbohydrates, Vitamins, and Trace Elements) and the Prevention of muscle wasting during periods of heavy training loads. As a result of increased muscle mass, muscle cross-section increases, leading to a proportional increase in physical strength, faster recovery from physical exertion, and an enhanced capacity to handle training loads. Various groups of natural (endogenous) hormones and synthetic Steroid compounds exhibit anabolic effects. The main groups of anabolic agents are as follows:

1. Somatotropic hormone of the anterior Pituitary Gland—somatotropin.

2. Pituitary gonadotropic hormone—chorionic gonadotropin.

3. Androgens (male sex hormones): testosterone (testosterone propionate), testosterone enanthate (delatestryl), testonate (a mixture of testosterone propionate and testosterone enanthate), testasterone (a mixture of various testosterone esters), methyltestosterone, fluoxymesterone (halotestin), testosterone cypionate (depotestosterone), methenolone enanthate (primobolan).

4. Synthetic anabolic steroids: methandrostenolone (dianabol, nerobol, stenolon), nandrolone (nerobolil, phenobolin, durabolin, turinabol), retabolil (decadurabolin, etc.), silabolin, oxandrolone (anavar), stanozolol (winstrol), oxymetholone (anadrol-50), etc.

Anabolics can be administered orally (oral AS) or via intramuscular and subcutaneous injections. The adverse, harmful effects of anabolics are extremely diverse and dangerous. They consist of toxic effects (i.e., poisoning) on vital Organs—primarily the Liver—severe Metabolic Disorders, Impairment of the endocrine and reproductive systems, cardiovascular and urogenital diseases, and pronounced psychiatric disorders (which we will discuss in detail below). Previous claims in specialized literature regarding the safe use of AS were based on isolated short-term studies and proved to be incorrect. It is now fully established that any use of AS, even in small doses and for short periods, carries a greater or lesser degree of absolute harm. Anabolics invariably cause a certain degree of damage to an athlete's health. Several studies indicate the potential emergence of numerous negative consequences 15-20 years after discontinuing the drugs. The Nature of the side effects caused by anabolic steroids largely depends on several factors, the most important of which are: individual reaction to the drug, sex and age differences, the presence of acute or chronic diseases, dosage, and duration of use. Negative side effects develop particularly quickly and are more pronounced in children and adolescents. Their negative impact on the female body is also profound. The doses of AS used in weightlifting and athletic gymnastics significantly exceed therapeutic doses—those used to treat certain medical conditions—by 10 to 20, or even 40 times. To maximize effects and reduce the likelihood of detection during doping control, many athletes use a practice known as "staking"—a dosing regimen that involves gradually altering the dosage and alternating specific drug formulations throughout a cycle, as well as combining AS with agents from other groups (primarily testosterone and diuretics). Evidence shows that such regimens can lead to even more severe adverse consequences than the use of individual preparations.

Consequences of long-term anabolic steroid use on various organs and systems of the athlete's body

Liver and biliary tract pathology. Examinations have revealed that up to 80% of athletes using AAS suffer from hepatic dysfunction. The use of oral forms of anabolic steroids can impair the antitoxic and Excretory Functions of The Liver and lead to the development of hepatitis. Prolonged AAS intake causes biliary tract obstruction and jaundice, with fatal cases even having been reported. There is a significant body of evidence indicating an increased incidence of Liver Cancer Associated with long-term anabolic use. Effects on the Genitourinary system. Individuals using anabolic steroids over extended periods may develop Kidney tumors, renal calculi, and impaired Urine Formation. Effects on the Endocrine System. Anabolic steroids promote endocrine disorders, exerting a particularly negative impact on carbohydrate and Lipid Metabolism. The administration of testosterone in adult males suppresses the secretion of endogenous hormone. Long-term use of anabolic steroids leads to testicular atrophy, suppression of Spermatogenesis, a decrease in sperm count and fertility index, alterations in libido, etc. Furthermore, restoring normal spermatogenesis takes 6 months or more, and with prolonged steroid use, these changes can become persistent or even irreversible. In men, AAS use can induce gynecomastia—namely, significant development of breast tissue and nipples, which in severe cases may require surgical intervention. In women, the intake of even negligible doses of anabolic steroids rapidly triggers virilization: voice deepening and coarsening, facial hair growth on the chin and upper lip, male-pattern baldness, breast atrophy, clitoromegaly, generalized hirsutism, uterine atrophy, disruption or cessation of the Menstrual cycle (dysmenorrhea and Amenorrhea), acne, increased sebum secretion, and general masculinization. Menstrual irregularities and acne are reversible upon discontinuation of AAS. Facial hair growth, balding, clitoral enlargement, and voice changes are irreversible. The virilizing effects of AAS are particularly pronounced in young women and girls, in whom pseudohermaphroditism may be observed. In women, AAS use can cause Infertility, while in pregnant women it slows embryonic growth and leads to fetal demise. Such severe consequences of AAS on the endocrine system of women and girls are attributable to the androgenic activity of testosterone—a hormone normally present in the female body in minimal amounts, the artificial elevation of which in the blood leads to such extensive disorders. Thyroid and gastrointestinal dysfunctions. It has been shown that anabolic steroid use can contribute to thyroid dysfunction, gastric and intestinal disorders, and gastrointestinal bleeding. Mental and psychological disorders. AAS use is invariably accompanied by decreased sexual drive and progressive psychological alterations characterized by unpredictable mood swings, hyperexcitability, irritability, aggression, or the onset of depression. Pronounced shifts in personality and behavior often lead to serious consequences: strained friendships, broken families, and conditions conducive to socially negative or even dangerous actions. According to some observations, complete cessation of AAS use is frequently accompanied by depression, which is viewed as a manifestation of psychological dependence on anabolics, analogous to narcotic addiction. Effects on The Cardiovascular system. Anabolic steroids disrupt carbohydrate and lipid metabolism, reducing glucose tolerance, which is accompanied by a drop in blood sugar levels. The use of oral AAS increases Insulin secretion, thereby contributing to the development of diabetes. In addition, the development of atherosclerosis and other cardiovascular diseases is possible. Anabolic steroid use promotes rapid muscle mass growth that significantly outpaces the growth and development of the corresponding tendons, ligaments, and other Connective Tissues. This leads to ligament ruptures under heavy physical loads, inflammatory conditions of the bursae, and tendon degeneration. AAS causes a decrease in Muscle tissue viscosity due to Water and sodium retention, a reduction in muscle elasticity (subjectively perceived as muscle soreness or "tightness"), and an inability to generate full muscle force. All of this predisposes athletes to muscle and ligament injuries during training and competitions. Cessation of anabolic steroids is followed by a phase of decreased immuno-biological activity and heightened susceptibility to illness. The use of anabolic steroids by adolescents can cause irreversible changes: premature epiphyseal fusion (cessation of long bone growth), precocious Puberty, and symptoms of virilization and gynecomastia.

Steroid Breakdown in the Body

There are numerous Factors influencing the efficacy of medicinal compounds. One such factor—and perhaps one of the most critical—is the half-life of the active substance. In medicine, the term "half-life" refers to the time required for half of a substance to break down, from the initiation of administration until its elimination from the body. To clarify, this is not half of the total duration of the substance's activity in the body, but rather the metabolism of 50% of the substance currently present in the body. For example, upon administration of 100 mg of any steroid preparation with a 4-hour half-life, subsequent blood tests yield the following data: after 4 hours, 50 mg of the given substance remains in an active form.

After another 4 hours, the drug remained in the body, but the next half-life period had elapsed, bringing the total amount of active substance down to 25 mg. The process of eliminating a drug from the body may span several such half-lives of the active substance.

The half-life is not merely cited as the total timeframe during which a substance can be detected in its active form; rather, it serves as a guideline for the optimal use of prescribed dosages, thereby avoiding undesirable peaks and valleys in steroid levels.

In the early years of steroid research, their half-life proved to be a stumbling block in the creation of synthetic analogs. Endogenous steroids—those produced by the body itself—have a very short half-life, which makes maintaining high blood levels highly challenging. For instance, the half-life of free testosterone in the blood is only a few minutes, taking less than an hour from injection to complete elimination from the body. Furthermore, it undergoes hepatic metabolism. When you take oral preparations, only tiny fractions enter the bloodstream intact. Given this drawback of oral medications, theoretically only one solution would exist: the use of frequent testosterone injections during therapy. Obviously, this is highly unpleasant and terribly inconvenient, which prompted scientists to explore ways to prolong the lifespan of testosterone and Other Hormones in the body. Two of the best-known methods for extending the half-life of steroids were ultimately developed and approved by the pharmaceutical industry.

Oral 17-alpha-alkylated steroids

Presented here are the latest Materials on steroids. 17-alpha-alkylation is a process in which an additional carbon atom is attached to the steroid molecule at the 17th position. This atom occupies the precise Location within the molecule to neutralize the 17-keto group, completely blocking its metabolism via this pathway.

17-alpha-alkylation significantly extends the half-life of steroids. Consequently, we see that the half-life of steroids can be measured in hours rather than minutes. Unfortunately, 17-alpha-alkylation can also reduce the ability of steroids to bind to androgen receptors. This modification is particularly advantageous for oral steroids. While the liver attempts to process this type of steroid, the majority of it enters the bloodstream unchanged. Nevertheless, this exerts a toxic effect on the liver, which is likewise far from ideal for the body.

Esterification of injectable steroids

The use of esterified injectable steroid combinations increases their half-Life in the body. Esterification is a process wherein a carboxylic (fatty) acid is attached to the steroid molecule at the 17-beta position; the objective here is to protect its active 17-hydroxyl group. This is the primary target in steroid metabolism that the introduced steroid esters are designed to shield. Since esterified steroid combinations are fat-soluble, this prevents sudden spikes and surges in Blood Circulation and allows for their gradual utilization by the body. As a result, the unactivated fraction of steroids remains in a depot (the injection site), slowly releasing and entering the bloodstream over the course of days and weeks, where it is subsequently cleaved into free form by Enzymes, thereby providing a constant level of steroid activity.

We can examine two phases in the half-life of injectable steroid combinations. The first is the release of steroids from the depot (injection site), which typically takes several days for most pharmaceutical preparations. In fact, The activity of most oil-based injectables is measured in weeks, sometimes several weeks. The second is their half-life within the bloodstream. Let us examine a course of nandrolone decanoate (Deca) injections through these two phases. From the moment of injection until the active substance is released takes about 6 days, which is why many people state that Deca remains practically active for over a month following injection. The half-life of the attached decanoate esters is roughly an hour or less:

✵ nandrolone - 30-40 minutes;

✵ nandrolone phenylpropionate - 1 day;

✵ nandrolone decanoate - 6 days;

✵ nandrolone laurate - 10 days.

The figures presented best reflect the half-lives of nandrolone and its two other esters following intramuscular injections.

Non-Steroidal Doping Agents

As for doping agents unrelated to anabolic steroids, a few words should be said about such a class of performance-enhancing substances as diuretics. With the holding of athletic gymnastics championships and the expansion of our athletes' participation in international competitions, the need arose to establish weight categories and appropriate weight limits during competitions. In weightlifting, this problem has been known for a long time and remains quite acute. For rapid weight loss during the competitive period, some incompetent coaches and athletes recommend taking diuretics, i.e., water pills, although it is well known that these have long been banned and included in the prohibited doping list. For instance, Bulgarian weightlifters at the 1988 Seoul Olympics were disqualified precisely for the use of diuretic agents. In addition, there is a widespread belief in the sports community that taking diuretics helps accelerate the elimination of anabolic steroid breakdown products and other medications from the body, thereby reducing their negative side effects and shortening the washout period before a competition. It should be noted that the use of diuretics even in clinical practice for medical indications requires careful laboratory and medical supervision, as it is fraught with potential complications. By removing fluid from the body along with salts essential for normal metabolism (such as potassium, which is required for normal heart Muscle Function), diuretics—when used without a compensating diet—lead to the development of heart failure. This danger increases with physical exertion and at the peak of competitive efforts, which can result in acute cardiac dysfunction. Furthermore, taking diuretics causes elevated blood sugar levels, which can exacerbate Diabetes Mellitus, gastrointestinal disorders (including nausea, vomiting, and diarrhea), allergic reactions, and the development of Skin diseases. Exacerbations of liver and kidney diseases are also possible, along with central nervous system depression accompanied by drowsiness, lethargy, and sensory disturbances.

Sports Disciplines and Doping

All types of physical activity are classified according to exercise intensity into very high, high, moderate, and low. This corresponds to the level of sports qualification of elite athletes (Olympic and world champions), international-class masters of sports, masters of sports, ranked athletes, individuals engaged in regular physical fitness, sedentary individuals, and those engaged in therapeutic physical training for the rehabilitation of certain functions through prescribed motor activity. Naturally, the requirements placed on these individuals, their level of training, Nutrition, and pharmacological support will vary completely. However, all of them have physiological limits that restrict human physical performance.

It should be borne in mind that these performance-limiting factors depend on the type of physical activity, which can be divided into five main groups in accordance with sports classifications:

1. Endurance-dominated cyclic sports (running, swimming, cross-country skiing, speed skating, all types of rowing, cycling, etc.), where the same movement is repeated cyclically, large amounts of energy are expended, and the work itself is performed at high and very high intensities. These sports require metabolic support and specialized nutrition, especially during marathon events when Energy Sources shift from carbohydrates (macroergic phosphates, Glycogen, glucose) to fats. Monitoring the hormonal system of Various metabolic pathways is essential both for prognosticating and for correcting athletic performance using pharmacological agents.

2. Speed-strength events, where the primary quality is the manifestation of explosive, short-duration, and highly intense physical activity (all sprinting events, throwing disciplines, weightlifting, etc.). In most cases, these areas depend on genetic determinants, and the energy sources required to sustain such activity differ fundamentally from those involved in endurance events.

A distinction is made between cyclic motor actions (running) and acyclic ones (throwing). It is very difficult to improve a 100-meter dash time, whereas strength and endurance are far more responsive to training stimuli. The same applies to pharmacological intervention. Natural sprinters possess a higher percentage of fast-twitch muscle fibers compared to long-distance runners. Speed is a very telling indicator that undergoes the earliest and most pronounced decline with age compared to strength and endurance. The body mass increase in all throwers and weightlifters requires special control over specialized nutrition and a shift from the catabolic to the anabolic phase of metabolism without the use of anabolic steroids and somatotropin. Uncontrolled body weight gain is equally unacceptable in sprinters, in whom Carbohydrate Metabolism and energy sources—macroergic phosphates, glycogen, and glucose—predominate. Thus, the objectives of pharmacological correction become clear.

3. Combat sports comprise a very numerous group of athletic activities (all wrestling styles, boxing, etc.). A characteristic feature of Energy Expenditure in combat sports is the intermittent, cyclic level of physical exertion, which depends on specific fighting conditions, although at times it reaches very high intensity. These sports are quite traumatic in most cases, which can cause microcirculation disorders and metabolic disturbances in the Brain; therefore, nootropic agents should be used as protective drugs.

4. Team and ball games are characterized by a constant alternation of intense muscular activity and rest periods when athletes are not directly involved in play episodes. Movement coordination and mental resilience are of great importance. The tasks of pharmacological support are associated with optimizing recovery processes, compensating for energy expenditure, and improving cerebral metabolism using vitamin complexes, nootropics, plant- and animal-derived adaptogens, as well as antioxidants.

5. Complex coordination sports rely on extremely refined movement elements, as seen in figure skating, gymnastics, diving, and shooting, which demand exceptional composure and focus. Physical loads vary within wide ranges. For example, executing a complex jump requires tremendous explosive power, whereas shooting requires extreme concentration and minimized tremor. Enhancing mental stability using calming herbal remedies (valerian, alcohol-free hawthorn extracts), nootropics, vitamin complexes, and energy-dense foods is of great significance.

Technically complex sports are largely associated with the use of technical equipment (auto racing, bobsleigh, parachuting, sailing, and many others). The level of physical exertion may not reach extreme values, but nervous tension pushes human capabilities to the limit, which determines the principles of pharmacological intervention—namely, enhancing psychological resilience.

In addition, there are A number of mixed sports involving various combined events that incorporate the aforementioned types of human physical activity. Naturally, the goals of pharmacological support differ significantly and fundamentally.

It should be added that numerous challenges arise regarding recovery and the maintenance of a high intellectual level during chess tournaments as a sport.

Thus, there is no reason to believe that universal pharmacological agents exist that could uniquely and comprehensively solve the problems of sports pharmacology.

Hence, athletic activity encompasses virtually all types of physical performance, both dynamic and static. In the following sections, we will examine pharmacological agents that influence endurance, speed, strength, and coordination, taking into account the intensity of physical exertion.

In recent years, depending on the sport, various doping agents have been used across different countries (Table 16).

Table 16. Doping use in related sports disciplines

In equestrian sports, various doping substances are used depending on specific objectives (psychostimulants, tranquilizers, etc.); therefore, anti-doping control is conducted for horses.

Doping Control: Organization and Procedures

Due to the development of international relations and the expansion of contacts among athletes from various countries, as well as the holding of national and regional competitions, the issue of familiarizing participants with the procedures and regulations of doping control has become increasingly important.

Doping control is a vital component of the comprehensive program aimed at preventing athletes from using prohibited (doping) substances. The regulations for organizing and conducting doping control currently adopted in our country fully comply with the requirements of the IOC Medical Commission. The doping control procedure consists of the following stages: collection of biological samples for analysis, physicochemical examination of the collected samples and issuance of a Conclusion, and imposition of sanctions on violators. During competitions, an athlete receives notification that, according to the rules, they must undergo doping control. Doping control is mandatory for the winners taking 1st, 2nd, and 3rd places, as well as, by decision of the commission, one or more athletes who did not place in the top three (selected by drawing lots). After their performance, the designated athletes are escorted to the doping control station. Here, the athlete personally selects a container for collecting the urine sample. Then, in the presence of a chaperone, the urine sample is provided (the chaperone monitors the procedure to prevent sample tampering). Once the sample is provided, a number chosen by the athlete themselves is affixed to the container. Afterwards, the biological sample is divided into 2 equal parts—samples A and B—which are sealed and assigned a specific code. Thus, the athlete's name is not mentioned at any of the working stages (to ensure complete anonymity). Copies of the codes are attached to the doping control form. The samples are then packed into transport containers and dispatched to the doping control laboratory. Before signing the doping control form, the athlete is required to inform the commission of the names of all medications taken prior to the competition (since certain medications contain prohibited substances in minimal quantities, such as solutan). Upon signing the doping control form, the athlete simply has to await the analysis results. According to the doping control regulations, sample A is subjected to analysis no later than 3 days after the biological sample is taken. If prohibited substances are detected in it, sample B is unsealed and analyzed. Either the athlete themselves or their authorized representative may be present during the unsealing of sample B. If prohibited substances are also detected in sample B, the athlete is subjected to appropriate sanctions. However, if no prohibited substance is found in sample B, the conclusion based on the analysis of biological sample A is deemed invalid, and no sanctions are applied to the athlete.

An athlete's refusal to undergo doping control or any attempt to falsify its result is regarded as an admission of doping use, with all ensuing consequences. Falsification of doping control results involves various manipulations aimed at distorting the outcomes. Athletes may resort to falsification attempts when they are certain of a positive result in their biological samples for doping. Such attempts may include urine substitution (catheterization and introduction into the bladder of foreign urine, known to be free of prohibited substances, or a liquid simulating urine; use of microcontainers; intentional contamination of urine with aromatic compounds that hinder the identification of doping agents). Prohibited manipulations also include special surgical procedures (such as subcutaneous implantation of placenta tissue). The Physicochemical methods of analysis used to detect doping in biological urine samples (chromatographic, mass spectrometric, radioimmunoassay, enzyme-linked immunosorbent assay, etc.) are highly sensitive and incorporate computerized identification of doping agents and their metabolites. They allow for the highly accurate detection of all substances used by the athlete, including those used over the preceding weeks and even months. In addition, methodologies have been refined to detect so-called blood doping, i.e., the transfusion of the athlete's own or someone else's blood prior to competition. While previously doping control was administered exclusively to elite athletes and only during major international and domestic competitions, today such testing is conducted not only during the competitive period but also during training sessions. Furthermore, all individuals engaged in sports are subject to doping testing, regardless of their athletic Classification.

Below is the doping control procedure conducted by both the Russian anti-doping agency and international sports organizations (such as sports federations, the International Olympic Committee, or the International Paralympic Committee). These recommendations are primarily intended for athletes, as the main goal of doping control is to protect an athlete's right to dop-free sport. Nevertheless, it is essential that coaches, medical staff, officials, and other Representatives of the athlete are also well-versed in doping control procedures.

1. Selection of Athletes for Testing

Throughout the year, you may be selected, with or without prior notice, to undergo doping control during competitions, while at training camps, at home, or anywhere else. For in-competition testing, athletes are most frequently selected based on competition results or by random draw (lots). For out-of-competition testing, the selection of athletes is typically conducted by drawing lots, although you may also be tested based on specific decisions by anti-doping authorities.

2. Athlete Notification

As a rule, an athlete is personally informed about upcoming doping control. A doping control officer or chaperone informs you of the requirement to provide a urine sample. You are also briefed on your rights and responsibilities during the doping control procedure, particularly the right to have an accompanying person, as well as the obligation to remain within the direct observation of the doping control officer from the moment of notification until the sample collection procedure is completed. After the anti-doping representative ensures that you fully understand your rights and responsibilities, you will be asked to sign a specific form.

3. Selection of Equipment

When you are ready to provide a sample, you will be offered a choice of sealed urine collection vessels. The athlete is responsible for ensuring that the sample remains within their line of sight at all times until it is sealed.

4. Provision of the Urine Sample

You are required to provide approximately 100 ml of urine in the presence of an anti-doping representative of the same sex as you. To enable the representative to observe the sample provision process, you must undress from the waist to mid-thigh.

5. Doping Sample Collection Kit

The doping control officer will ask you to select a sealed kit to be used for storing, identifying, and transporting the urine sample. Several kits will be offered for your selection. If you or your representative are not satisfied with the condition of the packaging, you have the right to request a replacement kit.

6. Sample Numbering

Once you (and your representative) have selected a kit, you must open it and remove the contents. Following this, you and your representative will be asked to verify that the identification numbers on the bottles, lids, and the transport box match. The doping control officer, in turn, will also verify that the identification numbers on the samples are identical and will enter the sample number into the doping control form.

7. Division of the Sample into «A» and «B» Specimens and Packaging

You will be required to pour the required volume of urine into bottles «A» and «B» and seal each container with a lid as instructed by the doping control officer. The officer will then ask you to invert the bottles to ensure they do not leak. Your representative must also confirm that the specimen has been properly sealed.

8. Checking Urine pH and Specific Gravity

The doping control officer checks whether the urine sample complies with specific standards by measuring its pH level and specific gravity. If the pH level or specific gravity does not meet the standards, you may be asked to provide an additional sample.

9. Declaration of Consumed Substances

The doping control officer will ask you to voluntarily provide a list of medications (prescribed by a physician and taken independently), dietary supplements, and any other substances you have consumed over the past ten days. This information will be recorded on the doping control form, which is sent to the laboratory for analysis.

10. Doping Control Form

After filling out the form, you and your representative must ensure that the recorded information is complete and accurate. You must then sign the doping control form, thereby confirming your satisfaction with the procedure. If you are unsatisfied with the doping control procedure, specify the reasons in the comments section of the form.

11. Completion of Testing

You receive copies of all forms you have signed, which must be kept for 6 weeks in the event of an adverse analytical finding.

Next steps

Your sample collection tube is sealed, placed in a specialized transport bag, and sent to a WADA-accredited laboratory. Upon arrival at the laboratory, it is checked to ensure that the samples were not damaged during transport and that the Contents of the bottles match the descriptions in the accompanying documentation. The laboratory then analyzes the 'A' sample while keeping the 'B' sample sealed. In the event of an adverse analytical finding, you must be notified within 3–4 weeks of the laboratory receiving the sample. However, in some cases, a sample may be stored for an extended period without undergoing analysis.

Sanctions for athletes found guilty of doping

Detecting doping threatens an athlete with severe penalties, up to a complete lifetime ban from sport. For a first violation involving prohibited substances (with the exception of sympathomimetic drugs such as ephedrine and its derivatives), an athlete is disqualified for 2 years; for a second violation, for life. In the case of sympathomimetics, the first offense carries a 6-month disqualification, the second a 2-year disqualification, and the third a lifetime ban. Furthermore, the coach and the physician overseeing the athlete are also subject to disciplinary action. The use of any substances officially classified as narcotics as doping agents entails corresponding administrative and criminal penalties. Currently, legislative proposals have been introduced to criminalize the use of anabolic steroids without medical indication or the incitement of others to use them.

Self-Assessment Questions

1. Define the concept of "doping".

2. What groups of substances are currently classified as doping agents?

3. What is the MECHANISM OF ACTION of stimulants?

4. What effects do narcotics have on the human body?

5. List the consequences of prolonged intake of anabolic steroids on various organs and physiological systems of an athlete.

6. What are beta-blockers used for?

7. What is the purpose of using diuretics?

8. What prohibited methods of doping exist?

9. What categories of physical activity are distinguished according to the classification of sports?

10. How is doping control organized?

11. What sanctions are applied to athletes found guilty of doping?