HUMAN BIOCHEMISTRY - L. V. Kapilevich - 2016

PART 2. FUNDAMENTALS OF SPORTS PHARMACOLOGY

PHARMACOLOGICAL AGENTS AT VARIOUS STAGES OF ATHLETIC TRAINING

It is well established that the body's adaptation during athletic activities (both training and competition) unfolds in a series of stages. Sports pedagogy has established METABOLISM/2.html">THE CONCEPT OF periodicity (cyclicity) in The Development of adaptation to loads in order to achieve peak athletic performance. The annual training cycle is broken down into shorter stages, or mesocycles, each with specific objectives regarding the development or consolidation of adaptation levels (typically, a mesocycle corresponds to a single training cAMP). Accordingly, each mesocycle comprises recurring intervals with more immediate objectives, known as microcycles (usually 7-10 days in duration). The final day of a microcycle is dedicated to rest and recovery. The adaptive changes during each microcycle can be reinforced or accelerated through targeted, metered pharmacological interventions. The core principle here is that pharmacological support should not be administered continuously; rather, it should coincide with the moment when the training load has already induced specific adaptive Changes in the body (for instance, via metabolic shifts resulting in the accumulation of certain byproducts). This phase presumably corresponds to the first half of the microcycle. Continued loading and the accumulation of toxic metabolites beyond this point no longer promote adaptation, but instead lead to the depletion of the body's energy and plastic resources. From this point onward, a comprehensive recovery regimen—including pharmacological support—must be initiated. The action of medications should aim, firstly, at supporting energy and plastic reserves, and secondly, at the partial elimination or detoxification of Metabolic waste products. Thus, starting from the second half of the microcycle, the pharmacological management of training adaptation should peak by the rest day.

This principle can also be scaled up to the mesocycle as a whole. The volume and intensity of pharmacological interventions should increase toward the end of the training camp. Overall, the annual training cycle is divided into preparatory, base, pre-competitive, competitive, and recovery stages, depending on the specific objectives at hand.

The primary objective of pharmacological support during the recovery stage is the Elimination of Metabolic waste products generated by heavy physical exertion, alongside the medical Treatment of overstrain in various Organ Systems. During periods of intense physical exertion (developmental training), the priority shifts to enhancing Protein Synthesis within the body and ensuring a dietary intake rich in high-quality Proteins and CARBOHYDRATES. During the pre-competitive and competitive periods, the most critical tasks involve building up the body's energy depots, preventing infectious and cold-related illnesses, and maintaining immunological status.

Thus, the MAIN OBJECTIVES OF pharmacological support during any given period of athletic training are dictated by the focus and volume of training and competitive loads, as well as the degree of strain placed on various physiological systems.

The continuous use of any pharmacological agents without regard for the periodicity of athletic training is entirely unacceptable, as this can lead to adverse effects and the development of drug tolerance. Just as administering pharmacological agents that stimulate Muscle mass growth in the absence of intense physical exertion leads to weight gain without increasing strength or endurance, the converse is also true: an insufficient Dietary intake of proteins, carbohydrates, Essential Amino Acids, Trace Elements, and Vitamins during developmental loads inhibits gains in muscle mass and strength. Energy depots are primarily built up through carbohydrate and lipid saturation using high biological value products (HBVP), such as honey, bee bread, nuts, dried apricots, feijoa, and protein/amino acid supplements. The Use of energy-dense Pharmaceuticals (ATP, phosphaden, neoton, creatine phosphate, etc.) is also advisable. The maintenance of athletes' immunological status is achieved through universal agents commonly referred to as adaptogens (of both PLANT AND ANIMAL origin). These include dry and liquid extracts, tinctures, and other dosage forms of ginseng, Rhodiola rosea, Schisandra chinensis, Rhaponticum carthamoides, Cimicifuga dahurica, Acanthopanax senticosus, Eleutherococcus, Zizania, and pantocrin. The combined use of various adaptogens significantly enhances their tonic and adaptogenic effects. In sports pharmacology, adaptogens are typically used to accelerate adaptation and recovery during preparation for major competitions and during intense developmental loads, when There is a high risk of colds and infections due to a temporarily weakened immune system. In this publication, the authors aim to provide a detailed Overview of the scientifically grounded use of approved (non-doping) pharmacological agents designed to regulate recovery processes, prevent overstrain, shorten adaptation timelines (to both physical exertion and changing environmental conditions), and enhance athletes' mental resilience and performance. Below are the schematics for pharmacological support across various stages of training.

Recovery Period

As noted earlier, the primary objectives of pharmacological support for athletes during the recovery phase of the annual training cycle are:

1) the elimination of metabolic waste products from the body;

2) the treatment of overstrain in various organ systems;

3) preparation for subsequent intense physical and psycho-emotional loads.

Pharmacological agents are employed to achieve these objectives. Vitamins A and E—administered either separately or in combination—help stimulate certain oxidation-reduction processes and the Synthesis of specific Hormones. Vitamin C is used to accelerate adaptation to physical exertion and prevent vitamin deficiency. For female athletes, Ferroplex (Hungary), a preparation containing ascorbic acid (vitamin C) alongside iron ions, can be recommended. It is most beneficial to take Ferroplex During the first half of the Menstrual cycle.

Certain vitamin complexes help normalize biochemical reactions within the body and prevent vitamin deficiencies. Others are specialized sports supplements that combine a vitamin complex with a balanced blend of trace elements, making their use in the preparatory period particularly preferable.

The intake of adaptogens such as Safinor, ginseng, eleutherococcus, zizania, pantocrin, and others helps accelerate adaptation to heavy physical exertion and normalizes the functional state of organ systems. Typically, they are taken as tinctures 2–3 times a day—in the morning and before lunch on an empty Stomach. Safinor and Pantocrin are taken as 1 tablet 3 times a day for 10 days. Adaptogen supplementation should begin 3–4 days before THE START OF training, with a standard course lasting 10–12 days. Sedatives and Sleep AIDS are used during this period primarily to manage (suppress) and treat Central Nervous system overstrain following significant psycho-emotional stress. Valerian ROOT (in both tablet and tincture form), motherwort infusion, oxybutycar, and certain other sedatives may be used.

To normalize metabolism during the recovery period, regulate the functional state of organ systems, and accelerate athletic rehabilitation, the following medications are generally prescribed: riboxin (inosine), cocarboxylase, essentiale, and hepatoprotectors (allohol, legalon, etc.).

During this period, a diet rich in carbohydrates and fats is recommended, with proteins playing a slightly lesser role. The inclusion of fresh fruits and vegetables, juices, and high biological value products in the diet is an absolute necessity. Special attention should be paid to the athlete's weight, which during this period should not exceed their normal baseline ("fighting weight") by more than 2–3 kg.

In the second half of the recovery period, the intake of immunomodulators is recommended—preferably non-specific ones such as mummy (shilajit), honey with bee bread, flower pollen supplements, Politabs, and Cernilton (Sweden). Prescription immunomodulatory drugs (such as levamisole and T-activin) should only be administered under strict medical indications.

Preparatory Period (Base Training Phase)

Vitamin supplementation continues during this period, although it is advisable to take an 8–10 day break in the course of multivitamin complexes. It is beneficial if the athlete can start a new formulation. Key vitamin recommendations include cobamamide and B-complex vitamins, which help enhance the synthesis and prevent The breakdown of Muscle Proteins.

During the preparatory period, certain medications with antioxidant properties are recommended—such as encephabol, ubion, alpha-tocopherol acetate, gammalon, Lipoic Acid, and sodium succinate. These agents promote ATP Synthesis in the Brain, stimulate cellular Respiration, exert an antihypoxic effect (which is especially valuable when training in mid-altitude conditions), and enhance athletes' emotional stability and physical performance. During intensive physical loading, supplements that regulate plastic metabolism—meaning those that stimulate Protein synthesis in muscle Cells and support muscle mass growth—are highly beneficial. This group of anabolic agents includes ecdysterone, mildronate, carnitine chloride, and several others.

The preparatory phase of the training cycle is characterized by substantial volumes and intensities of training loads. Consequently, taking immunomodulators during this period is essential to prevent immune system burnout. The most accessible and widespread non-specific immunomodulators in our country include mummy (shilajit), honey (comb honey, preferably in old, dark combs), and flower pollen. The most critical condition for their effectiveness is that they be taken on an empty stomach (preferably in the morning).

At the preparatory stage, the administration of hematoprotectors is recommended, and where medically indicated, riboxin (inosine) and solcoseryl (actovegin)—agents used for the Prevention and treatment of Liver and myocardial overstrain syndromes, respectively—are appropriate. The dietary focus during this period is high-protein and high-carbohydrate. The diet must contain an adequate amount of complete proteins (meat, fish, cottage cheese, cheese, legumes), vitamins, and trace elements. Any protein supplements taken In addition to dietary intake should not exceed 40–50 g (calculated as pure protein).

Pre-competitive Training Period

This period is characterized by a significant reduction in the range of pharmacological agents used. It is recommended to decrease multivitamin intake to 1–2 tablets or dragees per day (changing the current preparation is advised if possible). Among vitamins and Coenzymes, the administration of cobamamide (to prevent muscle mass loss) and cocarboxylase (to regulate carbohydrate and Lipid Metabolism), as well as vitamin C, is advisable. At the beginning of the pre-competition period, preparations such as ecdysteren, mildronate, carnitine chloride, sodium succinate, and others can be recommended, although the dosage should not exceed 1/2 of the preparatory period dose. These medications must be discontinued 5–7 days before the competition.

In the second half of the pre-competition period (8–10 days before the start), the intake of adaptogens and energy-rich supplements (ATP, phosphobion, creatine phosphate, phosphaden, neoton, etc.) is recommended. While adaptogens help accelerate adaptation to changing environmental conditions (since competitions usually take place away from home—abroad, in another region, city, etc.) and speed up recovery processes, energy-dense products and supplements help build an energy depot, promote ATP synthesis, and improve muscle contractility. During the pre-competition period, the administration of immunomodulatory drugs is a prerequisite. The diet during this phase of preparation should be predominantly carbohydrate-based, with fructose being the most appropriate choice. American physicians recommend the following carbohydrate-loading regimen for athletes specializing in endurance sports: 10–12 days before the start, dietary carbohydrate intake is gradually reduced, reaching a minimum by the 5th day. Afterward, carbohydrate intake (preferably fructose) is smoothly increased to a maximum on the day of the competition. Regarding female athletes, ferroplex, conferon, or other iron-containing supplements are recommended throughout the entire menstrual cycle. Quite often, the day of the main competition coincides with menstruation. Its onset can be slightly delayed (by 2–3 days) by taking ascorutin (1 tablet 3 times a day) starting 10–14 days prior to the competition.

Competitive Period

During this period, the number of pharmacological agents used is further reduced. Of all the aforementioned groups, only adaptogens, energy products, intermediates (ATP, phosphaden, phosphobion, inosine, neoton, creatine phosphate, energix), and minimal doses of vitamins (vitamins C, E, and B1 must be included) are retained in the pharmacological support of the competitive period. The combined use of these pharmacological agents helps accelerate recovery between starts, ensures a high contractile capacity of muscle fibers, and stimulates cellular respiration processes.

Actoprotectors belong strictly to competitive pharmacological agents—substances that have only recently entered the arsenal of sports pharmacology but have already gained recognition. Domestic preparations in this category include sodium succinate, limontar (a derivative of citric and succinic acids), and bromantane. Actoprotectors prevent Metabolic Disorders in the body during physical exertion, stimulate cellular respiration, and promote the enhanced synthesis of energy-rich compounds (ATP, creatine phosphate).

Thus, speaking of the pharmacological support of an athlete's training process and competitive activity within the annual training cycle, it should be noted that the largest share of pharmacological support falls on the recovery and, especially, preparatory periods, gradually decreasing as one transitions to the pre-competition and competitive periods.

Correction of Athletes' Condition During Travel

When athletes travel significant distances (typically accompanied by abrupt changes in climate and geography, altitude above sea level, and substantial time zone shifts), special pharmacological correction of their functional state is frequently required.

It is known that a sudden change in time zones is accompanied by acute desynchronosis syndrome, which is based on the disruption of the body's circadian rhythms that synchronize major life processes. Acute desynchronosis manifests as pronounced sleep-wake cycle disturbances, mental status alterations, and vegetative-vascular shifts. Furthermore, in 90% of cases, athletes who do not undergo special correction experience an acute breakdown in adaptation capabilities up to 7–10 days after relocating to a new time zone. Ultimately, this leads to a significant decrease in the athletes' functional readiness and the inability to train properly for upcoming starts. Travel from west to east generally results in a more acute and prolonged form of desynchronosis.

It must be emphasized that the pharmacological correction of these disorders should be an integral part of currently established biomedical and pedagogical Methods for resolving the issue of temporary adaptation. At the same time, pharmacological measures must be rationally combined with early arrival at the competition venue to allow gradual adaptation to the time change (while taking into account the potential negative psychological impact on athletes from prolonged waiting on-site), psychological preparation for the trip (avoiding undue focus on the upcoming time shift), and appropriate adjustment of the training process.

Measures to correct desynchronosis should begin directly during the flight. In this regard, choosing the most convenient departure time is crucial. For travel from east to west, a morning departure is optimal. The main objective under these conditions is to prevent athletes from falling asleep during the flight. For this purpose, the administration of tonic preparations 1–1.5 hours after takeoff is recommended. The best results are usually achieved after fractional doses of the psychostimulant Sydnocarb (10–15 mg every 4 hours of flight). Further sleep prevention should be maintained until local evening. Forty to sixty minutes before bedtime, it is advisable to administer 5% sodium oxybutyrate syrup (30–35 ml) with The addition of 30–40 drops of liquid passionflower extract. This ensures quick and high-quality sleep onset without subsequent morning relaxation. The course of sodium oxybutyrate syrup (taken at night) is continued for the next 3–4 days. In approximately one-quarter of cases, Affective Disorders associated with long-haul flights—such as lowered mood, increased irritability, and inadequate reactions—may become more or less persistent 3–5 days after arrival, requiring the prescription of daytime tranquilizers such as phenibut or mebicar for several days.

For flights from west to east, an evening departure is optimal. The primary objective here is to normalize nighttime sleep during the flight (using mild sleeping pills such as radedorm in doses up to 10 mg). Particular attention should be paid to avoiding overeating on the airplane. During the first two to three days after arrival, mild tonics such as ginseng tincture, liquid eleutherococcus extract, etc., are prescribed during the day, while in the evening, 1 hour before sleep, 5% sodium oxybutyrate syrup with liquid passionflower extract is administered. Beyond the direct manifestations of acute desynchronosis (mainly sleep-wake rhythm disorders), the condition apparently triggers deeper disruptions in the body's regulatory processes. For instance, an Analysis of the dynamics of athlete maladaptation following a time zone change reveals Blood pressure destabilization, muscle tone changes, isolated cardiac function irregularities (rhythm and conduction changes), and other disorders in more than 50% of cases. Therefore, normalizing the sleep-wake cycle and alleviating affective reactions does not yet mean the functional state of athletes who have undergone long-distance travel across significant time zones has been optimized. To achieve this, the use of sodium succinate is recommended (0.3 g for 10 days, taken 1.5 hours before training) against the Background of a combined intake of ginseng tincture (25 drops), liquid eleutherococcus extract (20 drops), and rhodiola rosea extract (20 drops) 2–3 times a day before meals. Other adaptogens of plant, animal, or synthetic origin (ginseng, aralia, dibavol) may also be used.

Currently, the complex of maladaptive phenomena observed in the body during the first few days after relocating athletes to mid-altitude conditions (altitudes up to 700 m above sea level) is well documented. Since mid-altitude training is an essential stage of the annual training cycle in several sports, and due to the frequent holding of major competitions in such environments, pharmacological methods for accelerating the body's adaptation processes in mid-altitudes often acquire exceptional importance. Upon relocating to mid-altitudes, starting from the 2nd–3rd day and lasting up to the 10th day or even longer after arrival, a significant decrease in the functional parameters of the circulatory and respiratory systems, as well as the central nervous system (CNS), is observed. This causes a heightened sense of difficulty in performing physical exertion. Objectively, this is expressed in disturbed nighttime sleep, unmotivated hyper-excitation or, conversely, depression, electrocardiographic symptoms of myocardial strain, breathing difficulties, decreased appetite, and increased fatigue. This entire symptom complex of acute adaptation breakdown in mid-altitudes frequently jeopardizes the goals of training camps as well as The ability to mobilize all resources during major competitions.

The pharmacological tactic for correcting these disorders involves a comprehensive approach to the treatment and prevention of two main syndromes: CNS strain and Cardiovascular system strain. Since relocating to mid-altitude is typically accompanied by a drastic time zone shift, it is advisable to employ the pharmacological strategy for acute desynchronosis correction described above.

To facilitate comprehensive adaptation of the athlete's body to mid-altitude conditions, the combined herbal adaptogenic preparation Safinor is usually prescribed (3 times a day half an hour before meals, with a course duration of 10–12 days). The composition of Safinor (riboxin, saparal, floverine, potassium orotate) simultaneously provides a normalizing effect on CNS Functions (via the psycho-tonic action of saparal) and optimizes cardiovascular functions (due to riboxin and floverine). Administration of the drug should begin 3–4 days prior to moving to mid-altitudes, which ensures the accumulation of Safinor's cumulative effect over

3–5 days post-arrival, generally eliminating the symptoms of acute adaptation breakdown almost entirely. Subsequently, the optimal level of the athletes' functional state in mid-altitudes should be maintained by using a complex of herbal adaptogens including 2 ml of liquid eleutherococcus extract, 30 drops of pantocrine, and 15 drops of liquid rhodiola rosea extract (2 times a day, half an hour before breakfast and lunch). Other adaptogenic preparations of plant, animal, and synthetic origin (ginseng, aralia, dibavol) may also be used.

Self-Assessment Questions

1. At what point in the training period is the Introduction of pharmacological agents necessary?

2. What is the purpose of medicinal products during the recovery phase, periods of intense physical exertion, and the pre-competition and competitive periods?

3. What can lead to negative side effects from the medications used?

4. What substances are classified as products of enhanced biological value?

5. Which preparations are recommended for use during the recovery period?

6. Which medications must be taken during the preparatory period to prevent immune system failure?

7. Which preparations are recommended during the pre-competition and competitive periods?

8. Why is medical correction of athletes' conditions necessary when they travel significant distances?

9. What medications are recommended for correcting desynchronosis?