HUMAN BIOCHEMISTRY - L. V. Kapilevich - 2016
PART 2. FUNDAMENTALS OF SPORTS PHARMACOLOGY
NON-DOPING PHARMACOLOGICAL AGENTS
To date, a clear understanding has been established regarding the groups of non-doping pharmacological agents that can be employed in sports medicine to address its core objectives. It should be noted that the ability of these agents to influence numerous performance-limiting mechanisms allows them to be used as prophylactic preparations to enhance the quality of life in healthy individuals (athletes, fitness enthusiasts, and occupational medicine), as well as in clinical practice during the physical Rehabilitation of patients undergoing sports training regimens.
Summarizing the literature data, it can be noted that the main groups of non-doping pharmacological preparations include medicinal substances listed in the Register of Medicines of Russia for 2001 (Table 9).
Adaptogens as Promising BIOLOGICALLY ACTIVE SUBSTANCES
Adaptogens have a history spanning millennia; they were quite widely represented in the pharmacopoeias of the Far East (Japan, China, Korea) and Southeast Asia. Until recently, Europe knew nothing of them, and even now, judging by publications, knowledge remains relatively scarce. Proceedings of the 1996 Olympic Congress in Atlanta featured the first serious studies on the effects of Siberian ginseng on the physical performance of elite U.S. athletes, whereas in the USSR, as early as 1960, I. I. Brekhman published a book on Siberian ginseng as a novel stimulating and tonic remedy.
Class="center">Table 9. Non-doping pharmacological preparations
Pharm. group No. per RLM |
Name of pharmacological group |
Pharmacological preparations |
8.8 |
General tonics, adaptogens |
Ginseng, schisandra chinensis, golden ROOT (rhodiola rosea), maral root (rhaponticum carthamoides), spiny eleutherococcus, Manchurian aralia, zizania (echinopanax), solasodine, escuzin, dibazol, aloe, apilak, milife, FiBS, Bittner balsam, pantocrine, gerimax, etc. |
8.10 |
Nootropics |
Aminalon, ginkgo biloba, Glycine, glutamic acid, picamilon, actovegin, nootropil, piracetam, encephabol, phenibut, pantogam |
7.2 |
Antihypoxants and antioxidants |
Bemithyl, levocarnitine, mildronate, oliphen, preductal, cytochrome C, mexidol, reamberin, succinic acid, ceruloplasmin, superoxide dismutase, dibunol, tocopherol, essentiale, actovegin |
7.4 |
Vitamins and vitamin-like agents |
Complex preparations: aevit, ascorutin, aerovit, one-a-day maximum, vitamin 15 solco, vitamcur, vitrum, hexavit, decamevit, duovit, quadevit, calcinova, macrovit, multi-tabs, sana-sol, supradyn, undecвит (undevit), unical, gerimax, calcium D3, etc. |
5.5 |
Immunomodulators |
Proleukin, interferon, levamisole, wobenzyme, immunal, ribomunyl, echinacea, T-activin, thymogen |
13.8 |
Agents for enteral (including dietary supplements) and parenteral Nutrition |
Alanine, aspartame, sorbitol, fructose, aminosol, bodyform, detox +, lifeppak, aminon, alvesin |
2.5, 7.1 |
Plastic and energy-action agents (metabolics) |
Potassium orotate, methyluracil, ekdisten and leuzea preparations, riboxin (inosine), L-carnitine, adenosine monophosphate AMP, nooton, panangin (asparkam), mildronate, actovegin, Lipoic Acid, sodium succinate (succinic acid salt) |
The most studied plant-derived adaptogen preparations include: ginseng, schisandra, golden root (rhodiola rosea), maral root (rhaponticum carthamoides), spiny eleutherococcus, Manchurian aralia, plane-tree sterculia, devil's club (echinopanax elatus), Dahurian cimicifuga, solanine, solasodine, escuzin preparation (horse chestnut extract), preparations from various Algae (sterculin, morinil-sport), and many others. These active principles are incorporated into combination remedies produced as medications and dietary supplements, for example, elton, leveton, phytoton, adapton, and numerous others. Most frequently, the pharmaceutical industry produces them in the form of tinctures, extracts, dragees, tablets, and other dosage forms for enteral (tablets, dragees, capsules, powders, extracts, tinctures, decoctions) and parenteral administration (ampoule solutions), as well as dietary supplements. In recent years, there has been a clear trend toward creating combination preparations containing adaptogens, vitamins, apicultural products, marine ingredients, and other components. It is hypothesized that these constituent components potentiate each other's effects.
Animal-derived adaptogens include: lipocerebrin (cattle Brain tissue preparation), pantocrine, pantohaematogen (extract from unossified antlers of the maral, wapiti, or sika deer), rhinoceros horn (in Africa), tiger and bear bone powder, fresh and preserved Blood, the meat of snakes and other reptiles (in Southeast Asia), bee products — bee bread, flower pollen, royal jelly, comb honey from multi-year harvesting frames, preparations from marine and oceanic fauna — sea cucumbers, sea lions, mussels, scallops, sea turtles, etc.
Adaptogens are medicinal agents that increase the body's nonspecific resistance to adverse environmental stressors. This group encompasses remedies of PLANT AND ANIMAL origin or those synthesized chemically. I. I. Brekhman posits that:
1) adaptogens must be entirely harmless to the Organism, possess a wide therapeutic index, induce minimal shifts in normal bodily Functions (or none at all), and manifest their adaptogenic action only against an appropriate Background;
2) the nonspecific action of an adaptogenic agent is defined by an increased resistance to the harmful impact of a very broad spectrum of physical, chemical, and biological factors;
3) adaptogens are characterized by a normalizing effect regardless of the direction of preceding physiological shifts.
According to A. V. Lupandin, the action of an adaptogen must be nonspecific and universal; that is, its influence should enhance resistance to major natural (physical exertion, Hypoxia, cold, etc.) and technogenic (motion sickness, vibration) extreme factors. The positive effects of its application should be mediated not by stimulating arbitrary processes, but by optimizing metabolic pathways and protecting tissue structures from degradation. The optimization of its effect should manifest under altered Homeostasis and reach its maximum under comfortable conditions. Repeated administration should lead to The formation of a systemic structural memory trace of adaptation.
METABOLISM/2.html">THE CONCEPT OF non-specifically increased organismal resistance, formulated by N. V. Lazarev, served as the theoretical foundation for The Doctrine of adaptogens. It was established that repeated exposure of experimental animals to small doses of certain toxins, as well as physical training and the administration of specific pharmacological substances, enhances animal resistance to various damaging insults. The author believes that with the aid of an adaptogen, the organism can be induced into a special state characterized by increased work capacity and heightened resistance to a wide range of adverse factors.
Among the medicinal agents of this group, ginseng was the first to be studied, and subsequently, the high efficacy of eleutherococcus preparations and other plant adaptogens was demonstrated when combined with bee products and with each other. They enhance athletes' performance levels, allowing for a reassessment of their indications in sports and general medicine.
The main pharmacological properties of adaptogens are presented in Table 10.
As can be seen from the table, adaptogens possess a complex chemical Structure, and their action cannot be attributed to a single component alone. For instance, while the anabolizing effect of leuzea can be interpreted as a consequence of the phytoecdysteroid ecdysteren, its tonic effect is entirely unrelated to it. Therefore, one should not seek to dissect the active principles of herbal remedies into isolated constituents, as many of their properties may consequently be lost.
Table 10. Structure, pharmacological action, and Practical Application of major plant-derived adaptogens
Name |
Active principles |
Action in the organism |
Asian ginseng Panax ginseng C. A. Mey. |
Triterpene Glycosides (panaxosides A, B, C, D, E, F), essential oil (panaceas), panaxic acid, pectin substances, panaquilon, CARBOHYDRATES, daucosterol, mucilage, resins, Alkaloids, potassium, manganese, zinc, aluminum, boron, panaxin, ginsenosides, etc. |
Stimulating, tonic, general strengthening; increases stress resistance, physical and mental performance; reduces fatigue; exhibits antioxidant and immunomodulatory effects. Infusions, decoctions, tinctures, and micro-powder are used for 2-3 weeks. Ginseng root tincture and "Bioginseng" at 20-30 drops 3 times a day. Keep in mind that alcohol is considered doping in certain sports federations |
Golden root (rhodiola rosea) Rhodiola rosea L. |
Pyrogallol-group Tannins, anthraglycosides, essential oil, organic acids, sugars, Proteins, fats, stearins, Waxes, tertiary alcohols, unsaturated compounds, phenolic substances, glycosides, Flavonoids, manganese, oxyphenyl-beta-ethanol, tyrosol, rhodoloside, etc. |
Enhances adaptation to extreme factors, exerts stimulating and tonic effects, increases the volume of dynamic and static work, accelerates recovery processes, and improves mental performance. Liquid extract is used at 5-10 drops per day throughout the course |
Manchurian aralia Aralia mandshurica Rupr. et Maxim. |
Aralosides A, B, C, triterpene saponins, alkaloids, minerals, Essential Oils, carbohydrates, starch, proteins, etc. |
Increases mental and physical performance, tones and stimulates The Nervous system; provides antihypoxic, antioxidant, immunomodulatory, and stress-protective effects. Tincture administered at 30-40 drops per day. Preparations saparal and safinor (combination tablet preparation) are prescribed for one month |
Devil's club (echinopanax elatus) Echinopanax elatus Nakai |
In roots and rhizomes: essential oils, triterpene glycosides, Phenolic Compounds, alkaloids, minerals, etc. |
Tones the nervous system, enhances physical performance, and exerts general excitatory, antioxidant, and immunomodulatory actions. Tincture is used in a course of up to 30 drops for up to 30 days |
Maral root (rhaponticum carthamoides) Rhaponticum carthamoides |
In rhizomes: phytoecdysteroid ecdysterone, organic acids, resins, essential oils, tannins and coloring agents, alkaloids, vitamins, carotene, inulin, etc. |
Excitatory, tonic effect on the Central Nervous System; anabolic influence on Muscles; increases PROTEIN AND NUCLEIC acid synthesis; exerts antioxidant and antihypoxic actions; normalizes immune system function; enhances physical performance and recovery. Leuzea extract is used at 20 drops, course — 20 days. Ecdysterone — 1 tablet 3 times a day for 20 days |
Siberian ginseng Eleutherococcus senticosus Rupr. et Maxim. |
In roots: eleutherosides A, B, C, D, E, essential oils, glucose, sugars, starch, wax, resins, Pectins, coumarin derivatives, Trace Elements, etc. |
Accelerates athletes' recovery, tones the CNS. Extract is taken at 2 ml daily for one month |
Chinese magnolia vine Schisandra chinensis Baill. |
Fruits: Lignans (gomisins A, B, C, D, E, H, schisandrin, deoxyschisandrin, etc.), sesquiterpenoids (gelangen, alpha- and beta-chamigrene, etc.), tannins, vitamins C, P, E, potassium, Se, etc. |
Accelerates adaptation to extreme factors (physical exertion, heat, cold, climatic-zone adaptation), exerts stimulating and tonic effects on the CNS, provides immunomodulatory and antioxidant actions, and normalizes metabolism. Prescribed as a course of 20 drops of tincture 3 times a day during intense physical loads. |
Echinopanax preparation containing echinopanax |
Micro-powder of echinopanax, vitamins E and C, excipients |
Accelerates recovery processes after exhausting physical exertion, tones the CNS. Taken for 30 days, 1 tablet 3 times a day |
Leuzea preparation containing leuzea |
Micro-powder of leuzea roots, vitamins E and C, excipients |
Enhances physical performance and recovery in athletes when taken as a 20-day course of 2 tablets 3 times a day. A new, user-friendly dosage form has been introduced |
Apivit — preparation containing flower pollen |
Complex of all fat- and Water-Soluble Vitamins, Nucleic Acids, proteins, Enzymes, Plant HORMONES, electrolytes and trace elements, energy-rich carbohydrates, etc. |
Accelerates recovery processes in athletes, helps replenish energy reserves in The Liver and muscles, and exerts immunomodulatory and antioxidant effects when taken as a course of 3 tablets for 20-30 days |
Elton Eltonum |
Micro-powder of eleutherococcus roots, vitamins E and C, flower pollen, propolis, excipients in a single 0.42 g tablet |
Accelerates recovery processes after physical exertion, possesses tonic action. Normalizes depleted antibody titers, acts as an antioxidant when taken as a course of 3 tablets 3 times a day for 20 days |
Leveton Levetonum |
Micro-powder of leuzea roots, vitamins E and C, flower pollen, propolis, excipients in a single 0.42 g tablet |
Anabolic effect due to ecdysterone. Central tonic action. Immunomodulatory and antioxidant effects. Administered in a course of 2-3 tablets 3 times a day for 20-30 days |
Adapton Adaptonum |
Micro-powder of leuzea, Chinese magnolia vine fruits, vitamins E and C, flower pollen, and excipients in a 0.42 g tablet |
Enhances physical performance (endurance) and recovery processes via central and peripheral actions on muscles |
Note. Adaptogens have been used as agents for recovery and performance enhancement in sports, military medicine, gerontology, heavy-industry environments,
and operator performance for many decades.
Summarizing the data on adaptogens, it can be concluded that they function within the organism in the following ways:
1) they tone the central nervous system, improve memory, learning processes, conditioned reflex activity, and synaptic transmission in the sympathetic and parasympathetic fibers of the Peripheral Nervous System;
2) they normalize the function of the body's Endocrine System (both anabolic and catabolic);
3) they control the generation and expenditure of energy in the effector Cells of muscles, liver, Kidneys, brain, and other Organs;
4) they counteract the immunosuppressive effects resulting from training and competition processes by influencing humoral and cellular Immunity;
5) they exert an antioxidant effect, preventing the toxic consequences of free-radical Oxidation of Unsaturated Fatty acids, which is typically heightened during exhaustive physical exertion;
6) they prevent hypoxia, which almost invariably accompanies intense physical exertion;
7) they exhibit anabolic properties that need to be supported during intense physical work (training) to prevent body mass loss and protein degradation in athletes when catabolic processes prevail;
8) they enhance microcirculation in the cerebral vessels and working muscles by improving the rheological properties of blood (due to the presence of vitamins E and C, coumarin derivatives, ecdysten, and other ingredients).
Thus, adaptogens can be regarded as a promising class of biologically active agents that broaden the thresholds of adaptation to physical loads while remaining non-toxic and non-doping compounds.
Agents with Plastic and Energetic Action
High physical loads and a significant intensification of metabolism lead to a functional deficiency of vitamins, electrolytes, microelements, glucose, Glycogen, L-carnitine, ATP, and creatine phosphate. First and foremost, the reserves of carbohydrates decline significantly, followed by fats and proteins. This triggers a catabolic phase wherein body mass begins to drop, necessitating The stimulation of the anabolic phase using anabolic substances, including non-steroidal agents that support or increase Muscle mass (ecdysterone, adenine, guanine, methyluracil, potassium orotate, etc.).
Potassium orotate serves as a precursor for The Biosynthesis of uridine phosphate, a component of nucleic acids. In sports medicine, this group of agents is used during periods of heavy physical loads to treat Protein metabolism disorders, stimulate metabolic processes (especially in endurance-dominant sports), prevent and treat myocardial overstrain, alleviate hepatic pain syndrome, and accelerate recovery processes.
Methyluracil stimulates Protein Synthesis in the body, enhances the absorption and synthesis of glycogen, increases the effectiveness of sports training, and improves overall body tone, performance, and recovery.
Purine derivatives—such as riboxin (inosine, inosine-F)—increase The activity of Krebs cycle enzymes. Phosphaden (adenosine 5'-monophosphate) induces muscle mass growth and enhances the synthesis of proteins and nucleic acids. It improves microcirculation in The Heart muscle and acts as a preventive measure against myocardial overstrain. ATP synthesis is accelerated. Agents with energetic action facilitate the recovery and creation of energy depots, increase glycogen reserves, promote The transport of fatty acids from the Cytoplasm into Cell/35.html">Mitochondria (L-carnitine), activate enzyme systems involved in oxidation, and boost athletes' resistance to hypoxia. Compounds such as ATP, creatine phosphate, and glucose serve as Energy Sources within the anaerobic-aerobic performance zone. During prolonged exertion, they activate lipolysis.
Lecithin and glutamic acid enhance the activity of ATPase. GABA (gamma-aminobutyric acid) improves the adaptive capacity of the central nervous system and accelerates recovery.
The dosages and administration schedules for plastic and energetic agents are presented in Table 11.
Table 11. Main Plastic and Energetic Agents
Agent |
Dosage and Schedule |
Application |
Potassium orotate |
0.5–2.0 g daily for 30–40 days |
To stimulate metabolic processes and enhance protein and nucleic acid synthesis in speed-strength and endurance sports |
Methyluracil |
1.5–2.5 g daily for 20 days |
Increases Protein and RNA synthesis, especially during the catabolic phase; accelerates carbohydrate assimilation, improves performance, and speeds up recovery |
Ecdysten and preparations containing Leuzea (Leveton, Adapton, Leuzea) |
0.005–0.01 g 3 times daily for 15–20 days |
Effective in cases of reduced protein and nucleic acid synthesis during the catabolic phase of training; promotes gains in muscle mass and strength in athletes |
Riboxin (Inosine) |
0.4 g 2 times daily for 1–2 months |
Exerts a protective effect on the myocardium, particularly during overstrain; stimulates depressed PROTEIN SYNTHESIS AND accelerates athletic recovery |
L-carnitine |
4.0 g daily for 3 weeks or as a single dose before competitions |
Acts as a cofactor in the Fatty acid oxidation system, transporting fatty acids across The inner mitochondrial membrane where the Beta-Oxidation system is located. The released energy vastly exceeds Glycolysis and The oxidation of Krebs cycle metabolites. Acts as an antioxidant |
Adenosine monophosphate (AMP) |
0.025 g twice daily for 3 weeks |
Participates in the REGULATION OF ENERGY supply processes and accelerates the restoration of athletic performance |
Nooton |
1 ampoule 40 min before performance |
Restores Energy Metabolism via creatine in endurance sports |
Panangin (magnesium and potassium salts of aspartic acid) |
1 tablet 3 times daily for 1 month |
Normalizes diminished energy potential in endurance-dominant sports |
Mildronate — a structural analog and precursor of carnitine |
1 g 3 hours before competitions |
Stimulates glycolysis reactions within The Tricarboxylic Acid Cycle; acts as a protective agent against physical overload-induced overstrain |
Actovegin-forte (Solcoseryl) |
1–3 dragees 2 times daily for 2–3 weeks |
Improves Oxygen transport to substrates and activates energy-dependent processes under increased energy demand |
Lipoic acid |
2 tablets 3 times daily for 2–3 weeks |
Plays a vital role in cellular energy production. Participates in the Regulation of Lipid and Carbohydrate Metabolism and improves liver function. Recommended with lecithin (0.5 g daily) |
Sodium succinate (succinic acid salt) |
2 tablets 2 times daily for 3 weeks |
Improves microcirculation, activates energy metabolism, increases the balance of energy-rich compounds, enhances cardiovascular and liver function, exhibits anti-acidotic properties, and accelerates recovery |
Plant- and animal-derived adaptogens: Ginseng, Zamaniha, Leuzea, Rhodiola rosea, Schisandra, etc. |
Individual dosages |
Increase nucleic acid and protein synthesis, stabilize muscle mass, boost ATP synthesis, and enhance glycogen utilization |
Note. Other plastic and energetic agents also exist.
Proper nutrition is a critically important factor for shifting the catabolic phase into the anabolic one in athletes.
Carbohydrate loading during recovery or prior to prolonged, intense physical exertion (such as marathons) is considered well-founded and is widely utilized in sports medicine.
Nootropics
Nootropics are agents that are classified as non-doping both in chemical structure and pharmacological action. They represent a relatively new class of pharmacological substances that stimulate learning, improve memory and mental performance, and facilitate information transfer between and within the cerebral hemispheres (derived from the Greek words "noos" — mind, intellect, thought, soul, memory; and "tropos" — direction, inclination, affinity). They are also referred to as neurometabolic stimulators. A stimulating effect on the central nervous system is not strictly universal (as seen with acephene, piracetam, aminalon, and others), since There are also agents with sedative properties (phenibut, picamilon, pantogam, and mexidol). S. B. Seredenin and T. A. Voronina note that nootropics activate the higher integrative activity of the brain, restore impaired memory and cognitive functions, and increase the body's resistance to extreme factors. In our country, the Classification of nootropics proposed by T. A. Voronina is widely used:
1. Pyrrolidone nootropic compounds (piracetam, etiracetam, aniracetam, oxiracetam, etc.).
2. Cholinergic agents (Choline, lecithin, tacrine, amiridine, etc.).
3. Neuropeptides, their analogues and fragments (eberatide, N-acyl-prolyldipeptides, etc.).
4. Brain metabolism activators (L-carnitine, acetyl-L-carnitine, etc.).
5. Cerebral vasodilators (vincamine, etc.).
6. Calcium antagonists (nimodipine, etc.).
7. Antioxidants (mexidol, dibunol, etc.).
8. Substances affecting the systems of excitatory and inhibitory Amino Acids (gammalon, nicotinoyl-GABA, milacemide, nooglutil, etc.). Sports physicians should keep in mind that groups II and III of nootropics (cholinomimetics and neuropeptides) can be classified as doping agents.
Nootropic drugs correct Learning and Memory impairments caused by extreme factors (hypoxia, electroshock, ischemia, chemical agents, Sleep deprivation), increase brain resistance to harmful influences (hypoxia, Temperature increases or decreases), improve specific hemorheological parameters, and normalize cerebral Circulation. This is due to their ability to affect the brain's energy processes—enhancing the synthesis of high-energy phosphates, proteins, and nucleic acids, glucose utilization, ATP synthesis, and mitochondrial Respiration.
Nootropics are the best medications for correcting learning and memory processes under extreme conditions.
Considering that physical exertion is an extreme factor, and that training involves The Development of specific skills and their retention, nootropics represent a promising class of non-doping pharmacological agents capable of affecting the central link of movement execution pathways and preventing "central fatigue".
In cases of pharmacological correction of athletes' conditions in combat sports, particularly for the Prevention of brain injuries, it is advisable to use psychoenergizers (gammalon, nootropil, encephabol, cerebrolysin, etc.), which can be considered as means of restoring altered metabolism and cerebral blood flow.
Antioxidants and antihypoxants
The formation of free radicals in excessive quantities can be a cause of decreased performance in endurance-oriented athletes. Free radicals in the form of unsaturated fatty acid hydroperoxides exert a toxic effect on Introduction/36.html">Biological Membranes, disrupting their functional lability. This leads to impaired energy metabolism and membrane permeability in working muscle cells, as well as a decline in performance, which requires pharmacological correction with antioxidants, resulting in enhanced human motor activity. Among these, alpha-tocopherol, ascorbic acid, polyphenolic plant adaptogens, dibunol, ionol, and others have been studied. It has been shown that the Antioxidant Properties of biologically active preparations (plant-derived adaptogens, combination products containing adaptogens and antioxidants: elton, leveton, adapton, and phytoton) contribute to the improvement of athletic performance.
In vitro and In Vivo Studies have established that combination adaptogens exhibit clear antioxidant action. A spontaneous decrease in ultra-weak luminescence is observed upon exposure to the studied preparations. Adapton proved to be the most active, while Elton had a less pronounced effect.
When studying the chemiluminescence state of athletes' urine, a primary dependency on athletic qualification was discovered. In student volunteers subjected to active physical exertion, the intensity of urine chemiluminescence increases by 60% by the 20th day of the study and by 40% by the 10th day under conditions of daily training and administration of preparations.
Other data were obtained when determining the studied parameters in highly trained athletes. Single bouts of maximal-power physical exertion cause a decrease in the urine chemiluminescence of athletes. In the group of highly qualified athletes, the total light sum of luminescence decreased by the 20th day of training. A correlation was revealed between the level of human physical fitness and the body's response to high-intensity physical exertion, which is confirmed by Changes in the ultra-weak luminescence of urine.
By the 20th day, Adapton reduced chemiluminescence more actively. It also increased the time to exhaustion during pedaling by 27% to a greater extent than the others. There is a clearly defined correlation between its antioxidant effect and its ability to enhance physical performance, specifically athletes' endurance in overcoming fatigue. This may be due to the presence of vitamins E and C in the compositions, which are classic antioxidants that block The process of fatty acid peroxidation and possess anti-radical activity. A similar effect may also be exerted by flower pollen, which contains these same vitamins, has its own phenolic antioxidants, and is found in The structure of adaptogens such as eleutherococcus, leuzea, rhodiola rosea, and schisandra chinensis (Table 12).
A satisfactory correlation is noted between the increase in performance under The Influence of course administration of preparations and their antioxidant effect. However, the degree of expression of these phenomena is much lower than upon the administration of combined adaptogenic preparations that include the studied ingredients individually. Vitamins E and C do not reliably affect physical performance, though there is a directional trend toward a tonic effect. The same can be said about flower pollen and eleutherococcus extract. All other adaptogens affect chemiluminescence and physical performance. This is confirmed by changes in malondialdehyde in the blood serum of athletes who received combination adaptogen preparations.
Table 12. Effect of vitamins E and C, flower pollen, extracts, and adaptogen tinctures on physical performance and ultra-weak urine luminescence on the 20th day of their daily administration (control taken as 100%)
No. |
Preparations |
Physical performance (%) |
Ultra-weak luminescence (%) |
1 |
Vitamin E (0.1 g), 4 drops daily |
100.6 + 9.8 |
81.5 + 11.8* |
2 |
Vitamin C (0.5 g), 2 g daily |
106.8 + 10.3 |
92.7 + 8.8 |
3 |
Flower pollen, 2.4 g daily |
110.9 ± 9.8 |
91.6 + 8.1 |
4 |
Eleutherococcus extract |
109.6 + 10.7 |
89.7 + 14.8 |
5 |
Leuzea extract |
1 12.7 + 8.2* |
85.4 + 10.6* |
6 |
Rhodiola extract |
109.8 + 9.9 |
87.6 + 6.8* |
7 |
Schisandra tincture |
114.9 + 8.6* |
69.7 + 8.1* |
Note. * - data are statistically significant.
It can be considered that the accumulation of hydroperoxides in an athlete's body is a performance-limiting factor, while antioxidants contribute to the normalization of this process and the optimization of endurance during excessive physical exertion.
The performance of almost all types of exercises is associated with hypoxia both in working muscles and the brain, as well as in other organs. The prophylactic use of antihypoxants can be regarded as part of athlete recovery. N. I. Volkov and co-authors believe that four ranges of exercises can be distinguished, differing in The rate of development and severity of developing tissue hypoxia: latent, compensated, pronounced hypoxia with ensuing decompensation, and decompensated tissue hypoxia. This classification is useful for diagnosing hypoxic states in athletes during intense muscular activity, as well as for selecting means and Methods of hypoxic training for athletes. Hypoxic load occurs in those muscle areas that perform heavy work. It is the cause of acute fatigue. In severe hypoxia, disorders of energy metabolism, biological membrane permeability, and other changes are observed. Pharmacological agents recommended for hypoxic syndrome include: coenzyme compositum, sodium oxybate (banned in shooting sports), ubiquinone compositum, and cerebrum compositum (Vidal registry). A number of adaptogens of plant and animal origin (saitarin - an alcoholic extract from saiga horn sheaths), nootropics, antioxidants, and other preparations possess antihypoxant properties.
Immunomodulators
Immunodeficiency states in athletes and their prevention represent a highly relevant task, as athletes constitute a risk group due to relocations across climatic and geographical zones, high injury rates, decreased immunological reactivity, and excessive physical exertion. A decrease in immunological reactivity also leads to reduced athletic performance. Immunomodulating agents not only restore but also enhance performance. Therefore, immunostimulating pharmacological agents can be considered as corrective medications, particularly when performing prolonged and intensive endurance work.
The pharmaceutical industry offers immunomodulating products: Galium-Heel, Galstena, Multisanostol, Oligogal-Se, Sant-e-Gel, Vitabex, Vitrum Atherolitín, Vitrum Life, Vitrum Century, Diactivanad-N, immunoglobulin, intraglobin, Calcevita, Bereш Plus drops, Complivit, Levamisole-Ebewe, Mega Vite, Multitest KI, Orthomol Immun, Orthomol Immun Junior, Pentaglobin, Polivit Geriatric, Retrovir, Ribasan Forte, Stress Formula 600, Stress Formula with Zinc, Sulotrim, T-activin, Celascon Effervescent, Cycloferon, Endobulin, Endur-VM, Estifan, Echinacin Liquidum, and others registered in Russia and listed in the Vidal dictionary. Beekeeping products such as propolis and its preparations, pure flower pollen (Apivit), and combination adaptogenic preparations are immunomodulators. They are registered as dietary supplements by the Ministry of Health of the Russian Federation and hold anti-doping certificates. These include Eleutherococcus, Leuzea, Elton, Leveton, Phytoton, and Adapton, which are recommended for use in sports medicine. The physician is provided with the opportunity to choose the most suitable agents from this arsenal, though preference should be given to low-toxicity herbal remedies.
Vitamins and Vitamin Complexes
Vitamins and Coenzymes represent a critical group of pharmacological agents with metabolic action used in sports medicine. This is because intense physical exertion and a sharp upswing in metabolism can induce a functional vitamin deficiency that limits athletic performance. Vitamins do not inherently enhance performance; rather, they act as factors that facilitate the recovery of athletic capacity. Indications for vitamin supplementation include the prevention of hypovitaminosis during the spring season, adaptation to new climate zones, and The Need for targeted regulation of anabolic and catabolic processes.
Decreased vitamin intake or increased depletion resulting from impaired absorption and accelerated metabolism can lead to deficiency states and reduced physical performance. Conversely, hypervitaminosis resulting from excessive vitamin administration negatively affects athletic performance.
Protein metabolism is regulated by vitamins B12, B6, B5, A, E, and K.
Carbohydrate metabolism is influenced by vitamins B1, B2, C, PP, B5, and lipoic acid.
Lipid Metabolism is positively supported by vitamins B6, B12, PP, B5, choline, L-carnitine, and lipoic acid.
Biocatalytic activity resides not in the vitamins themselves, but in coenzymes—products of their biotransformation that bind with protein molecules to form the enzymes that catalyze biochemical reactions. Coenzymes exhibit low toxicity and a broad spectrum of pharmacological activity (e.g., cocarboxylase, riboflavin, Pyridoxal phosphate, cobamide). Sports medicine also utilizes specialized preparations derived from vitamins (such as pyriditol, pantogam, oxycobalamin, dipromonium, and ubiquinone).
Practice shows that combination vitamin supplements are best used alongside adaptogens of animal and plant origin, nootropics, antioxidants, and agents with plastic and energetic action. For instance, Supradyn (containing 12 vitamins and 8 trace elements) has proven effective during the recovery period when combined with Elton or Leveton, which broaden its spectrum of action as an antioxidant and immunomodulator. The recommended regimen is 1 capsule twice daily after meals for three weeks, taken alongside Elton or Leveton (2 tablets 3 times daily). This combination enhances the body's adaptation to physical stress (in speed-power sports, endurance training, and mental resilience). Marinil-Sport (2 tablets 3 times daily for 3 weeks) is best combined with Adapton (2 tablets twice daily for 3 weeks), which accelerates recovery and boosts athletic performance in swimmers and track-and-field athletes.
Modern multivitamin complexes incorporate essential additives such as electrolytes and trace elements, the concentrations of which can drop significantly during intense physical exertion.
Consequently, preference should be given to vitamin complexes specifically balanced for these vital ingredients. One must also account for fluid loss, as large amounts of sweat (up to 1–2 liters) can be excreted during training and competition, leading to dehydration. Under physiological conditions, water excretion occurs via the following pathways:

Along with water loss, the concentrations of salts and trace elements change significantly.
The total body content of sodium chloride includes 100 g of sodium and 80–100 g of chlorine located in the extracellular fluid. These minerals maintain osmotic pressure, are essential for normal nerve and muscle excitability, and activate various enzymes. The daily requirement for sodium chloride is 10–20 g, which increases to 15–25 g under heavy physical loads involving high sweat loss.
The Human Body contains about 150 g of potassium (90% of which resides in the intracellular fluid). Potassium is required for transmitting electrical signals in Nerve Cells, activating specific enzymes, synthesizing creatine phosphate, and ensuring the contractility of cardiac and Skeletal Muscle. The daily potassium requirement is 2 g.
The human Skeleton stores 1000–1500 g of calcium (90%) and 500–800 g of phosphorus (80%). Calcium is essential for Muscle contraction, while phosphorus is a key component of energy-rich phosphates (ATP, creatine phosphate). Acting through buffer systems (such as the phosphate buffer), phosphorus helps regulate acid-base balance. The daily requirement for each of these minerals is 1.5–2 g.
As an essential mineral, magnesium is present in the body in amounts ranging from 20–30 g and is distributed across all cells. It is required for the synthesis of ATP and creatine phosphate, as well as for muscle contraction. Approximately 50% of total body magnesium is stored in the skeleton. The daily requirement is 0.3–0.4 g. Magnesium intake should be increased in cases of heavy sweat loss, high-protein diets, or elevated Calcium and phosphorus levels.
Trace elements—including iron, zinc, copper, manganese, cobalt, selenium, molybdenum, iodine, silicon, vanadium, chromium, nickel, cadmium, and lead—are present in the body in very low concentrations. They are indispensable for normal metabolism, as they serve as Structural components of enzymes (iron, copper, zinc, molybdenum, selenium), vitamins (cobalt), and hormones (iodine).
In cases of water-electrolyte imbalance, the following preparations are recommended: Dianil, Infesol-40, Levulose, Lymphomyosot, Osteopan, Plasmalyte-148 aqueous solution, glucose solution, 0.9% sodium chloride solution, 5% sodium chloride with glucose, Ringer's solution, Hartmann's solution, compound sodium lactate, and Revitalize-Multi-M ADS (Vidal 1998).
When acidosis is present, alkaline drinks or specific medications such as Kalinor, Hartmann's solution, and Stilamine are recommended.
Iron deficiency in the body can impair the blood's oxygen-transport capacity, which is unacceptable during intense physical exertion as it may lead to tissue hypoxia. For prevention, the following preparations are recommended: Actiferrin, Vitrum Superstress, Vitrum Circus, Sorbifer Durules, Tardyferon, Ferrtab Comp, Ferronal, Ferrum Lek, Heferol, Enfamil-2, Enfamil with Iron, and others.
Dietary Supplements
Combined dietary supplements are complex formulations designed to correct specific physiological functions. Substances such as glucose, vitamins and coenzymes, electrolytes, trace elements, AMP, ATP, creatine phosphate, tissue extracts, L-carnitine, lipid-protein-carbohydrate blends, and many others function simultaneously as foods and medicines. When packaged in ampoules and vials, they are considered medications; when supplied as powders, they are classified as foods. Currently, the Research Institute of Nutrition of the Russian Academy of Medical Sciences has registered over 500 such products for athletes. Mass media advertising often features overly optimistic claims, and sports physicians must remain vigilant because commercial advertising is not always reliable (offering miraculous claims regarding weight regulation, immunity, physical performance, rehabilitation, impotence, malignancies, Hearing, Vision, etc.). According to the anti-doping control service of VNIIFK, amphetamine derivatives were detected in certain batches of Herbalife, which was popular at the time. Amphetamines are sometimes added to combined pharmacological products aimed at rapid weight loss, as they elevate mood and suppress appetite. Anabolic Steroids have likewise been uncovered in geriatric multivitamin preparations. Unaware that manufacturers might include such "surprises," a specialist can easily find themselves in a compromising position, forced to prove their non-involvement in doping administration. Having an anti-doping certificate protects both the athlete and the physician. Reviewing certificates of conformity and hygiene issued to the distributor helps minimize the risk of accidental doping.
Table 13. Sequence of non-doping groups of preparations that enhance physical performance and adaptation to increasing exercise stress (an exemplary pharmacological support scheme for 3 months prior to competition)
Weeks of the training cycle |
Pharmacological groups of preparations |
|||||
Adaptogens |
Vitamins |
Energy-yielding agents |
Plastic preparations |
Nootropics |
Antioxidants |
|
1 |
+ |
+ |
- |
+ |
- |
- |
2 |
+ |
++ |
- |
+ |
- |
- |
3 |
+ |
++ |
- |
+ |
- |
- |
4 |
+ |
+ |
+ |
+ |
+ |
|
5 |
++ |
+ |
+ |
+ |
+ |
+ |
6 |
++ |
+ |
+ |
++ |
+ |
+ |
7 |
+ |
+ |
+ |
++ |
+ |
- |
8 |
+ |
++ |
+ |
+ |
- |
+ |
9 |
+ |
+ |
- |
- |
- |
- |
10 |
+ |
++ |
- |
+ |
- |
+ |
11 |
+ |
+ |
- |
++ |
+ |
- |
12 |
++ |
+ |
+ |
+ |
+ |
+ |
13 |
++ |
+ |
+ |
++ |
+ |
++ |
14 |
+++ |
++ |
+ |
+ |
+ |
+ |
15 |
+++ |
++ |
++ |
++ |
+ |
+ |
Note. Average therapeutic and maintenance doses taking into account age, body weight, and constitution (+); increased dosage (++); short courses or a single high dose administered prior to competition (+++).
Dietary supplements exhibit significantly lower toxicity than synthetic pharmacological agents. In some cases, they consist of medicinal substances such as vitamins, adaptogens derived from exotic plants (e.g., yohimbe) and animals (shark Cartilage), carbohydrate-based energy products, proteins, and others. For instance, the dietary supplements Elton, Leveton, and Phytoton contain adaptogens: Eleutherococcus, Rhaponticum carthamoides (leuzea), Rhodiola rosea, and Schisandra chinensis, respectively. Adapton incorporates all of the aforementioned components. Furthermore, all of these supplements are rich in such valuable energy sources as bee pollen and propolis, as well as antioxidant vitamins E and C. Thanks to this composition, these supplements possess unique pharmacological properties: enhanced performance and accelerated recovery, antioxidant and immunomodulatory effects, and improved blood rheological properties. They are protected by invention patents and hold hygienic certificates (Ministry of Health of the Russian Federation), anti-doping certificates (ADC), and certificates of conformity. These products are approved by the Institute of Nutrition of the Russian Academy of Medical Sciences and the Russian Federation of Sports Medicine for use in sports medicine. They are effective in endurance-dominated sports, speed-strength events, team sports, and combat sports, as they feature a fairly wide spectrum of pharmacological action ranging from effects on the central nervous system to target organs. Preparations such as Leuzea, Eleutherococcus, and Apivit are also suitable for addressing specific challenges in sports pharmacology. Currently, A large number of companies are entering the Russian market, introducing sports nutrition products that have not undergone qualified control for either efficacy or safety. A list of some such products was published by S. Malyutin and S. Samarin in the book Sports Nutrition Academy (Moscow, 1997). Their sheer number is impressive, and their prices are simply exorbitant. Dietary supplements should be used with caution in sports medicine. One must be certain of their efficacy and safety.
It is assumed that competitions take place by week 15. A significant role in choosing the pharmacological correction regimen is played by the focus of the training process. Most researchers distinguish three main groups of sports: predominant endurance training, strength training, and speed training. Based on these three qualities, it is possible to organically align the classification proposed by A. G. Dembo (1980), which identifies nine sports groups, with the modern classification of sports proposed by J. Mitchell (1985). According to the latter, all sports are divided into 4 groups depending on the intensity of static and/or dynamic loads:
✵ High intensity of both static and dynamic loads, for example, boxing, cycling. This group develops speed and strength.
✵ High intensity of dynamic and low intensity of static loads, for example, marathon, tennis, basketball. This group predominantly trains endurance.
✵ High intensity of static and low intensity of dynamic loads, for example, gymnastics, weightlifting, karate, etc. This group predominantly trains strength.
✵ Low intensity of both static and dynamic loads, for example, golf, shooting. This group is close to group 9 in A. G. Dembo's classification.
Universal regimens for The Use of non-doping pharmacological agents depending on the orientation of the training process have not been established. This depends on numerous factors: the continuous updating and expansion of the range of agents; the need to account for the stage of the training process and the conditions in which it is conducted, the athlete's condition, and so forth.
At the same time, general approaches to the use of non-doping pharmacological agents in sports involving the development of various physical qualities can serve as a guideline, irrespective of the athlete's training stages (Table 14).
Given the heightened interest of specialists and athletes themselves in vitamin supplements, it is advisable to provide the dosages of the main vitamins most widely recommended by sports medicine specialists. It should be noted that in the absence of disease and with A balanced diet, the requirement for most Vitamins can be met through prophylactic doses of complexes such as Glutamevit, Complivit, Selmevit, Gerimax, Revivona, and Sanasol.
Table 14. Use of non-doping pharmacological agents in sports with the development of various physical qualities
Pharmacological groups of agents |
||||||||
Adaptogens |
Vitamins |
Energy-yielding substances |
Plastic agents |
Nootropics |
Antioxidants |
Immunomodulators |
Antihypoxants |
|
Endurance |
++ |
+++ |
++ |
++ |
— |
++ |
4- |
+ |
Speed-strength |
+++ |
++ |
+++ |
++ |
— |
— |
— |
— |
Combat sports |
+ |
+ |
+ |
+ |
+++ |
— |
— |
— |
Team sports |
++ |
++ |
++ |
+ |
++ |
— |
— |
— |
Coordinative sports |
++ |
+ |
+ |
— |
++ |
— |
— |
— |
Table 15. Average vitamin dosages (mg) recommended at individual stages of training with various orientations of the training process
Vitamins |
Non-athletes |
Classification of sports |
|||
Speed-strength |
Endurance |
||||
Training period |
Competitive period |
Training period |
Competitive period |
||
A |
1,5 |
2 |
2-3 |
3 |
3-6 |
B1 |
1,5 |
2-4 |
2-4 |
3-5 |
4-8 |
B2 |
2 |
2 |
3 |
3-4 |
4-8 |
PP |
20 |
30 |
30-40 |
30-40 |
40 |
C |
70 |
100-140 |
140-200 |
140-200 |
200-400 |
E |
7-10 |
14-20 |
24-30 |
20-30 |
30-50 |
Gels, ointments, creams, liniments
Various therapeutic ointments and gels, as well as sports massage creams and liniments, are widely used within the complex of physical performance recovery tools. They help improve muscle BLOOD AND Lymph circulation, relax skeletal muscles and increase their elasticity, restore normal metabolism within them, eliminate metabolic products accumulated in the muscles, and relieve pain in the joints, muscles, and ligaments.
Muscle and joint pain and Swelling that sometimes occur after physical exertion are the result of microtraumas to Blood Vessels, muscle fibers, and strains of tendons and ligaments.
The therapeutic and restorative effects of ointments, gels, and creams are due to The properties of their constituent components. Some ointments cause tissue hyperemia (warming), while others, conversely, cool the muscles and ligaments or relieve swelling and inflammation.
The application of these agents is aimed at local pain relief, reduction of swelling and inflammatory processes, resorption of hematomas, restoration of impaired blood flow, and physical performance as a whole.
In cases of acute injuries (at least During the first two days), warming ointments and compresses must not be used. In such instances, agents with analgesic and anti-inflammatory effects are indicated. Typically, fresh injuries are treated with gels (such as Troxevasin, Venoruton, etc.) which, without warming the Tissues, are readily absorbed and cool the application site. Certain ointments and creams are used as compresses on painful areas. At the same time, it must be borne in mind that
each individual may react differently to various ointments. The applied agents produce a pronounced therapeutic effect in some people, a less pronounced effect in others, and may trigger an allergic reaction in a few. Therefore, in all cases of applying topical medications, be sure to consult a physician and carefully read the enclosed instructions for use!
In physical training and sports practice, the following domestic and foreign preparations are most frequently used.
1. Apizartron
An ointment containing bee venom. It possesses anti-inflammatory and mild warming effects. It is indicated for contusions, muscle inflammation (myositis), radiculitis, and neuralgia. The ointment is applied to the affected area of the body and rubbed in with massage. Analogues include Viranin and Viprosal.
2. Vipratox
An ointment containing snake venom. It is used in the same cases as Apizartron.
3. Sanitas Balm
A fat-based ointment containing methyl salicylate, which provides analgesic and anti-inflammatory effects, along with essential oils, turpentine, and camphor. It is used for myositis, neuralgia, and radiculitis. The ointment is applied to the affected area and rubbed in with a light massage.
4. Tiger Balm
It consists of various Essential oils and aromatic substances in a base of fat and paraffin. It is used for the same indications as Sanitas Balm.
5. Gymnastogal
Provides analgesic, warming, and anti-inflammatory effects. It is used for bruises, tendon and ligament strains, myositis, radiculitis, etc. Apply 1–2 g of the ointment to the painful area and massage it in.
6. Heparin Ointment
Features resorption and anti-edematous effects, while also providing anti-inflammatory and vasodilating action. It is used for inflammatory conditions, bruises, and to help resorb hematomas. A 3–5 cm strip of ointment is applied to the injured area and gently rubbed in or covered with a bandage.
7. Heparoid
A heparin-based ointment. Used for the same indications as heparin ointment.
8. Hevcamen
An ointment composed of menthol, camphor, essential oils, paraffin, and petrolatum. It is used as a counter-irritant and analgesic rub for neuralgia, muscle aches, and similar conditions.
9. Efcamon
An ointment with analgesic and warming properties. It is used for myositis, bruises, etc. Apply a 1–3 cm strip of ointment to the affected area and massage it in.
10. Nicoflex
A sports cream with a mild warming effect. It is used for bruises, muscle soreness, muscle strain, spasms, and cramps. Apply a 1–3 cm strip of cream to the painful area and massage it in.
11. Rahtofit-Sport
An herbal cream. It provides anti-inflammatory and resorptive effects, promoting the healing of minor Skin injuries and inflammation. It is used for bruises, sprains, myositis, muscle pain, spasms, and cramps. The cream is applied to the affected area and massaged in.
12. Finalgon
A strongly warming ointment. It is used for strains of muscles, tendons, and ligaments, as well as myositis, radiculitis, etc. Apply a 0.5–1.0 cm strip of ointment to the affected area and gently rub it in using the plastic applicator. Avoid contact with mucous membranes and abrasions.
13. Venoruton
A gel containing active plant ingredients. It provides an analgesic effect, mildly cools the application site, and relieves muscle tension. Do not use heat treatments or warming agents simultaneously when using this product. The gel is applied to the affected area of the body several times a day. An equivalent alternative is Troxevasin.
14. Turpentine Ointment
Used as a counter-irritant and anti-inflammatory agent. It provides local irritant, analgesic, and antiseptic effects. It is used to accelerate muscle recovery following heavy physical exertion.
15. Menovazin
A liniment consisting of menthol, novocaine, anesthesin, and ethyl alcohol. It provides analgesic and cooling effects, and is used for neuralgia, myalgia, and joint pain. The painful areas of the skin are rubbed with the preparation 2-3 times a day. Long-term use is not recommended.
16. Preparations based on capsicum tincture: camphocin, capsitrin, pepper-camphor liniment, and compound pepper liniment.
They exert irritating and counter-irritant effects, causing local hyperemia. They are used for rubbing painful areas in cases of neuralgia, myositis, radiculitis, Lumbago, contusions, and to accelerate recovery.
1. List the groups of permitted, non-doping performance-enhancing agents.
2. Which preparations belong to the adaptogen group?
3. Which preparations belong to the group with plastic and energetic action?
4. What effects do nootropic drugs produce?
5. What mechanisms underlie the action of antioxidants?
6. What is the rationale for athletes to use immunomodulators?
7. Are there any restrictions on the intake of vitamin supplements?
8. What effects do dietary supplements have on the body?
9. What are the Applications of various gels, ointments, creams, and liniments?
Last update: 06/08/2026
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