How to take furosemide in bodybuilding. Loop diuretics in bodybuilding. Hypertension drugs
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Athletes who pay a lot of attention to their muscles use diuretics in bodybuilding to remove fluid from tissues as quickly as possible. This allows you to perform high-quality muscle drying and get a beautiful body with a clear and sculpted muscle frame. Herbal diuretic tablets do not affect athletic performance and do not reduce the physical endurance required in sports. With moderate use of diuretics, you can achieve good cutting results without using doping. Abuse of diuretics can have the opposite effect and lead to health problems.
Athletes resort to using diuretics to quickly lose weight, which poses some health risks.
Why do athletes who are cutting need a diuretic?
Taking diuretics in sports is due to the need to quickly remove excess weight caused by excess fluid in the subcutaneous tissue. Taking diuretic pills is easier than buying expensive sports nutrition, using doping and sweating in the gym. Many athletes achieve rapid muscle drying by administering diuretics intravenously before a competition, but a safer method is to take them in tablet form 2 days before the competition. The use of this method allows you to tighten the body, make it visually elastic and prominent, beautifully highlight the muscles and protruding veins. In combination with intense muscle loads in sports, artificially induced fluid loss does not have a negative impact on the level of physical endurance.
Bodybuilders and diuretics
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Among professional bodybuilding athletes, the most popular are “soft” and “hard” diuretics. Soft ones do not cause any significant harm to health and give little effect, so bodybuilders who need quick and noticeable drying use doping and hard diuretics. In a short period of time, they outline the relief muscles, but lead to metabolic disorders, dehydration, disruption of the central nervous system and dizziness.
When taking diuretics in sports, it is necessary to replenish potassium, calcium and electrolytes in the body, since they are washed out in the urine.
Diuretics
are synthetic and herbal diuretics that are used in medicine, for example, for high blood pressure, and in sports, in preparation for championships. Diuretics belong to the group of prohibited drugs, therefore, if doping control finds them in the blood, then the athlete will be dis-qualified -ro-van. At the same time, diuretics help to hide the fact of the use of other prohibited drugs, which are also used There are sports-changes, but, basically, these drugs are used in preparation for something as a way to Che-gon means. However, drugs of this group also increase muscle mass, which may be a pre-condition pa-ra-tov with a high pro-ges-ta-gen-activity. But keep in mind that steroids have side effects, so you should not use them without a doctor’s advice!
If we talk about taking diuretics on a “regular basis,” then such a regimen for taking pre-pa-ra-tov is possible only when using herbal diuretics. For example, such a problem may arise if an athlete takes some medications that significantly increase blood pressure. At the same time, it is worth noting that di-u-re-ti-ki are able to reduce blood plasma by 8-10%, which is significant in your opinion. There is no risk of thrombus. Do not think that “herbs” are absolutely harmless, this is not so! The decision to take diuretics to prevent the consequences of high blood pressure and liver enlargement or swelling should be discussed with a sports physician. Absolutely the same applies to taking syn-te-ti-ches-kih di-u-re-ti-kovs for in-tox-si-ka-tion or heart problems. Any questions related to health should be discussed with specialists in the given area!
It’s clear that if you had the opportunity to hire a coach, a sports doctor, an en-do-kri-no-lo-ga, a massage therapist and other specialists, then you would consult with them, and not looking for information on the “network”, but if you have any violations, then they may and need to be discussed give with doctors, even if not of the highest class, but still with doctors. You can, of course, proceed from the logic of “someone will blow me away,” but this is not rational! Be sure to get tested and make sure that all indicators, except those that you deliberately overestimate, are within normal limits. If something goes beyond the norms, then we need to delve into the study of this issue and understand what needs to be corrected in order to be normal. Call out their meanings, and not wait until “it hurts.” The topic of mo-che-gony means is still a topic, at least, of the co-rev-well-y-s-at-le-tov, that’s why we count-you -I’m on your conscience, and I don’t understand that the re-co-men-da-tions are common, and the nu-ans are on -to decide for yourself!
Diuretics: drugs
Diuretics
are represented not only by a wide range of specific preparations, but also by their types. Synthetic diuretics are subdivided into: thiazides, pet-le-vye and os-mo-ti-ches di-u-re-ti-ki, as well as aldosterone antagonists. The second large group of diuretics are herbs, from which they make vodkas, us-toys and other nasty things. The latter are used as prophylaxis, and synthetic drugs are used as a means to achieve a specific goal. For example, during the masses, if you are “flooded with water”, re-ko-men-du-et-sya with-n-mother pre-pa-ra-ti -tel-no-go pro-khozh-de-niya, or products-you sport-tiv-no-go pi-ta-niya, which contain them. Go-to-get-to-something, or not-to-have any consequences of health problems, not-about-ho-di-mo with with the help of synthetic drugs.
There are a lot of schemes for using synthetic diuretics, since the drugs have different effects on the body, which makes it possible to achieve a synergistic effect. But this topic is not even a separate article, but a whole book, so we will consider the method of using only the most effective methods. racing funds. These include: fu-ro-se-mid, spi-ro-no-lak-ton and three-am-te-ren. When are these pre-pa-ra-ty data applied? As a rule, 2-3 days before the competition, but their reception should be subject to the “drying” system. In general, when we talk about “drying,” we usually mean fat-compressing, although “drying” is not just fat burning, it’s eyeliner to co-rev-no-va-ni-yam. But liquefaction, in fact, is the main stage of “drying”.
Start preparing for the championship follows from the moment the training plan is drawn up, when the athlete plans his performance. For example, he planned that he would compete at such and such a championship in a year, and from this point he calculates all the stages of training. Immediately, “drying” begins 2-3 months before anything, which depends on the in-di-vi-du-al- special characteristics of the athlete. The main “drying” diet is, as a rule, this protein-carbohydrate mixture . The first month athletes start using “short” steroids, as a rule, this pri-mo-bo-lan , also some drug with a pronounced androgenic active is added to the course, for example, masteron . Androgen is needed in order to provide “stiffness” on stage. The total dosage during this period should not exceed 400-500 mg daily.
After 3-4 weeks, Masteron or another selected testosterone is replaced by injectable vin-strol, but the general dosages remain the same, or are slightly increased in size. tu-a-tion. If you are not on schedule, then you have to force it, but within reasonable limits. After another 3-4 weeks, the prima is canceled and replaced ok-san-dro-lo-nom 50 mg per day, and the dosage of Winstrol will increase. If everything goes according to plan, then the total amount of dosage remains the same, if not, then the dosage needs to be increased. “Ok-sa-well” everyone from-me-et in-di-vi-du-al-but, and Winstrol can be installed almost before the day than-pi-o-na- ta. It is also possible and advisable to run in the background during preparation a growth hormone 10 units per day. Is it more effective? Yes, it’s effective, but only if this entire opus is a “children’s book” for you.
What do diuretics have to do with it? Diuretics are used 2-3 days before anything, but this is not the only means of removing fluid. In addition, the athlete must attend training, devote time to cardio and other procedures, that is, di-u-re-ti-ki is only the final touch. Moreover, in order for the effect to be truly obvious, before consuming diuretics, consume a higher quantity of water for several days. yes. But not 4 or 5 liters, but 8-12 liters. Boxers drink this much water for 8-12 days, after which they drain the water for 1-2 days and go to the weigh-in. It’s clear that specific numbers are a purely indi-vidual matter, which can be calculated either in practice, through trial and error, or from a specialist. And still, " how much to weigh in grams»?!
This means that the most popular diuretic is furosemide, which is usually taken in oral form at 20-40 mg per day. There is also an injection form, which acts much faster, but if you have 2-4 days left, then, most likely, it is not for you. bit. If furosemide alone is not enough, you can also add spi-ro-no-lac-tone to the “compote” at about 50-200 mg per day. As a rule, the dose is divided into 4 equal portions and taken every 3-4 hours. It is important to note that the spi-ro-no-lak-ton kal-li-sbe-re-ga-yu-shchy di-u-re-tik and an-ti-an-dro-gene, which can lead to the loss of we -neck mass. At the same time, most likely, before the fight, I will still have to give injections of glucose or I don't care about potassium chloride tablets, but you have to be careful with this, since all these procedures are associated with the risk of cardiac arrest.
That is why some athletes prefer to use triamterene, the action of which is not related to the supply of potassium ions. If triamterene is the only di-u-re-tic during preparation, then its dosages fluctuate in the range of 50-200 mg per day, if it is combined with others diuretics, then, as a rule, triamterene is given at a dose of 25-50 mg per day. It goes without saying that the choice of drugs, dosage, duration of their use and everything else is selected by the athlete individually. . Don’t forget about the side effects of these non-steroidal drugs, which, unlike steroids, lead to death quite a few athletes. Think sensibly and be ok!
Herbal diuretics
Bearberry leaves:
Place half or a whole leaf on a cup, take 3-4 times a day. In medicine, it is used for diseases of the bladder and urinary tract. Pro-ti-in-ka-za-ni-em for use are kidney diseases, since when ras-pas-de-ar-bu-ti-na, which is contained in bearberry leaves, hydro-hi-non is formed, and it irritates pa-ren-hi-mu.
Leaves of Orthosiphon staminate: they are used 2-3 a day 30 minutes before meals, as a rule, tea is brewed from 2g of herb, and, unlike the previous diuretic, this herb does not irritate the parenchyma, due to than, it is not only possible, but also desirable to be used for kidney problems, in general, this plant is even called “We eat tea the Chech-like way,” so let’s re-ko-men-du-eat!
Lespenefril: is a ready-made diuretic, which is also useful for problems with the kidneys and bladder; It is recommended to take Lespenefril 2-6 spoons per day, and in some cases Lespenefril extracts are even given in the form of droppers. This drug promotes the excretion of sodium, potassium and nitrogen compounds, reducing the level of azotemia in renal failure.
Sources:
Y. Bombela "Anabolic Review"
X. Lulman. "Visual pharmacology".
Dr. Luber “Culturalism our way or the secrets of the rocking chair”
A. Pasko “The simplest connection of nutrition to training. Online training"
Andrey Popov “404 not found various articles and publications”
S. Kulinenkov “Pharmacology of sports”
Diuretics in sports are often used for rapid weight loss. Due to the fact that these products remove excess fluid during exercise, endurance does not decrease. Typically, thiazide diuretics are used for this purpose, the abuse of which can lead to interruptions in cardiac activity, decreased strength and deterioration of muscle relief. For this reason, it is sometimes better to use natural remedies instead.
Types of diuretics
Modern diuretic supplements work primarily by increasing the kidneys' excretion of water and sodium. This provokes a decrease in the amount of fluid in the body.
Diuretics in sports are often used for rapid weight loss
The main classification divides diuretics into the following groups of diuretics:
- Saluretics, which also include thiazide and thiazide-like diuretics,
- Potassium-sparing diuretics,
- Herbal diuretics,
- Osmotic diuretics.
There are three more classifications:
- Classification by mechanism of action
- Classification by localization of action.
- Classification by impact strength
Modern saluretics stimulate the release of sodium and potassium from the body
Modern saluretics stimulate the release of sodium and potassium from the body. These include furosemide, ethacrynic acid, the list goes on.
Potassium-sparing diuretics are distinguished by the fact that, along with increasing the excretion of sodium, they retain potassium in the body.
Osmotic diuretics are quite popular, in particular mannitol and urea are used.
Natural diuretics are vegetables, fruits and herbs that can be used more freely, unlike synthetic supplements.
The table shows the characteristics of supplements belonging to the groups of loop diuretics and thiazide diuretics, by which they can be easily compared:
Natural diuretics are vegetables, fruits
Another table will tell you in more detail about all groups of diuretics.
A drug | Bioavailability % | Localization | Daily dose, mg | Duration of action, hours | Number of receptions |
---|---|---|---|---|---|
Thiazide and thiazide-like diuretics | |||||
Hydrochlorothiazide | 60-80 | kidneys | Up to 200 | 12-18 | 1 |
Indapamide | up to 100 | Kidneys and liver | Up to 2.5 | 12-24 | 1-2 |
Chlorthalidone | 60-65 | Kidneys and liver | Up to 100 | 24-72 | 1 |
Metolazone | 50-60 | Kidneys and liver | To 10 | 12-36 | 1 |
Loop diuretics | |||||
Furosemide | 10-90 | Kidneys and liver | Up to 200 | 6-8 | 1-2 |
Bumetanide | 60-90 | Kidneys and liver | To 10 | 4-6 | 1 |
Torasemide | 80-90 | Kidneys and liver | Up to 100 | 24 | 1 |
Potassium-sparing diuretics | |||||
Spironolactone | Up to 90 | Kidneys and liver | Up to 200 | 8-12 | 2 |
Triamterene | 50 | Kidneys and liver | Up to 300 | 12 | 2 |
Amiloride | 50 | Kidneys and liver | Up to 20 | 24 | 1 |
Osmotic diuretics | |||||
Mannitol | 52 | kidneys | Before 1800 | 24 | 1 |
Urea | 50-60 | Kidneys and liver | Up to 1500 | 5-14 | 1 |
Diuretic Indapamide
Why do athletes need diuretics?
Loop diuretics are popular among bodybuilding athletes because they have an immediate effect. These include the popular furosemide. But when using them, care should be taken, as they cause severe dehydration due to increased temperature and physical activity. The body loses a lot of potassium along with fluid.
Athletes use diuretics before competitions to remove excess fluid from the subcutaneous tissue. Then on stage the body will look more prominent. If the drug is administered intravenously, the effect will occur faster. A side effect of this may be. More experienced athletes use diuretic supplements in tablets a couple of days before competitions.
To avoid some serious side effects, loop diuretics and a potassium-sparing diuretic are sometimes taken together. You can avoid intoxication due to accelerated metabolism by taking natural diuretics based on plant extracts.
Spirolon potassium-sparing diuretic
Of course, they are weaker and act more slowly, but unlike synthetic products, they do not upset the balance of electrolytes.
Many athletes take special sports nutrition, which already includes natural diuretics. They remove excess fluid without affecting muscle tissue, without causing potassium deficiency and a number of other side effects inherent in synthetic products. Special purpose sports diuretics should not be used for long periods of time.
Properties of thiazide-like drugs
Thiazide diuretics are very quickly absorbed from the gastrointestinal tract and are therefore quite popular. The mechanism of their action is based on the removal of water and salts from the body. This preserves potassium. Thiazide diuretics are superior to loop diuretics. They are not addictive and their effects do not weaken over time. On the other hand, if thiazide diuretics are taken for a long time, hypoglycemia may occur due to the loss of chloride ions.
Thiazide diuretics are very quickly absorbed from the gastrointestinal tract and are therefore quite popular
Among the domestic drugs belonging to the group of thiazide diuretics, only Diacarb can be distinguished. It has a mild effect and is also low-toxic.
Despite the fact that thiazide diuretics have a weak diuretic effect, they are quite popular because they are easy to use and have a hypotensive effect.
Thiazide and thiazide-like diuretics have the following side effects:
- Remove potassium and magnesium.
- Increases the concentration of calcium in the blood serum.
- Reduces the excretion of uric acid.
- They disrupt carbohydrate metabolism, cause hyperglycemia, aggravate the condition of patients with diabetes, and aggravate renal failure.
- Sometimes they lead to the development of pancreatitis and allergic reactions.
Among the domestic drugs belonging to the group of thiazide diuretics, only Diacarb can be distinguished
The most popular diuretics for athletes
Canephron is a combined natural drug. The following list of components is included in this drug:
- Rosemary,
- Centaury,
- Rose hip,
- Lovage.
The natural composition allows the drug Canephron to act more gently. Essential oils increase blood circulation in the renal pelvis. They prevent excess water and sodium salts from being absorbed. Canephron bases its mechanism of action on this.
The natural composition allows the drug Canephron to act more gently
Canephron has anti-inflammatory and antimicrobial properties due to rosmarinic acid. It allows you to remove bacteria naturally. Thanks to these properties, canephron is successfully used in the treatment of inflammatory diseases of the genitourinary system. Centaury and rosemary relax smooth muscles, relieve spasms and reduce pain during inflammation.
Canephron is available in tablets and drops for oral administration. Canephron has an exceptionally mild effect, it is safe, and can be used for children. The course lasts up to six weeks.
Canephron is usually used for the following diseases:
- Urolithiasis, in order to prevent the reappearance of kidney stones, after their crushing and removal,
- Inflammations of the genitourinary system, such as cystitis and pyelonephritis,
- Edema.
Canephron is often chosen because it protects the kidneys while producing the desired effect.
Furosemide is the most popular diuretic drug used by athletes
Furosemide is the most popular diuretic drug used by athletes. Its mechanism of action is based on the removal of water and salts, sodium, potassium, chlorides and calcium from the body. Athletes chose this drug for a reason, since furosemide quickly and effectively removes excess fluid.
It is often used in the treatment of edema and high blood pressure.
Furosemide is usually used before the performance itself, trying to achieve a better appearance and relief. But it is best to use furosemide a little earlier, a few days before the crucial moment.
Furosemide begins to act almost immediately. The action lasts 3-4 hours. Weight loss is achieved very quickly. The drug is used for oral and intravenous administration. The second option helps to achieve faster results.
But rapid loss of water can cause muscles to lose their shape, because muscle mass is partially composed of water. Therefore, it is better to use safe diuretics of plant origin. Natural remedies are preferable, as they have virtually no contraindications or side effects.
Where to buy diuretics
You can buy diuretics on the American website, where there are always promotions, and using our link you are guaranteed to receive an additional 5% discount. It also works. Therefore, if you have already decided which diuretic is best for you, then it can be found on.
Description
Furosemide is one of the most powerful diuretics, if not the most powerful. In medical practice, it is used in cases of severe poisoning, when the toxic substance has not yet entered the bloodstream and can be removed from the body with water. It is also used in cases of a sharp increase in blood pressure resulting from excessive water retention by the body. Furosemide signals the body about the need for immediate excretion of both intra- and intercellular fluid, which can in some cases lead to irreparable consequences (see Side effects).
Application and dosage
Even for a bodybuilder with low levels of subcutaneous fat, muscle definition may not be visible due to a layer of water under the skin. Diuretics help remove this water from the body and, as a result, increase muscle definition. Remember Olympia 2001? The sharp improvement in Ronnie Coleman's form in the evening part of the competition program was precisely caused by the use of furosemide and the removal of excess water from under the skin. So over the past 20-25 years, diuretics have been and remain an integral part of competitive bodybuilding. It is also possible to use diuretics when, as a result of the use of anabolic steroid drugs that aromatize or exhibit estrogenic or progestogenic activity, an abnormally large amount of water accumulates in the body. But in this case, it is customary to make do with milder drugs.
Another area of use of diuretics in general and furosemide in particular is to mask the use of illicit drugs.
Furosemide is available in two forms: in the form of tablets containing 20 or 40 mg of the active substance, or in the form of a solution for intravenous administration. In the form of a solution, the drug exhibits its properties much more clearly and, most importantly, faster, drying out the body almost in the blink of an eye.
The usual daily dose of the oral form of furosemide does not exceed 40 mg; athletes begin taking the drug 4-5 days before the competition. Injectable furosemide is used only on the day of the competition or one day before the show. If it is necessary to enhance the effect of oral furosemide, about 50 mg of aldactone or hydrochlorothiazide can be taken simultaneously with it.
Side effects
Normal muscle functioning - contraction and relaxation - is based on intracellular electrolytic balance. Disruption of this balance due to a decrease in electrolyte levels due to loss of intracellular fluid can lead, for example, to spontaneous cramps (the muscle contracts but does not relax). If this concerns the abdominal or calf muscles, then everything is not so bad. But if it touches the heart... The death of Momo Benaziza in October 1992 occurred precisely as a result of a spasm that constrained the heart muscle.
In addition to seizures, massive intake of furosemide is accompanied by diarrhea, nausea, and dry mouth. After finishing taking the drug, it is very common for athletes to “swim” with water, sometimes to such an extent that even ordinary movements are difficult.
The use of diuretics in sports
The use of diuretics does not improve physical performance and, thus, cannot have a significant effect on the results of sports competitions. The ban on these drugs is obviously due to the fact that their use can help eliminate other prohibited drugs. In addition, athletes specializing in sports such as boxing, wrestling and judo sometimes use diuretics to quickly reduce body weight in order to meet a specific weight class in competition. Gymnasts, jockeys, high jumpers and representatives of other sports for which excess body weight can serve as an obstacle to successful performance also use these drugs. Using diuretics, you can cause a decrease in body weight of 3% or more in a relatively short period of time. So, for an athlete with a body weight of 72 kg, this reduction will be approximately 2 kg.
Thus, the use of diuretics in sports can lead to significant loss of water from the body and, at the same time, not cause any deterioration in the manifestation of strength, power or local endurance when performing anaerobic physical activity. In sports characterized by fast pace and intense muscle tension, physical performance will apparently not be affected by the use of diuretics, and may even be increased (probably due to weight loss). For example, in one of the studies it was shown that the use of a diuretic in sports or a combination of diet with a diuretic, which led to a decrease in body weight, contributed to an improvement in the result of jumping up from a place.
However, the use of diuretics can lead to a significant decrease in the athlete’s aerobic endurance. Research has shown that when dehydration is caused by diuretics, plasma levels in the blood can decrease by 8-10%, while total body weight decreases by only 3%. This decrease in plasma levels leads to a deterioration in the functions of the cardiovascular system during exercise, as there is a decrease in systolic blood volume. Despite the fact that the results of the studies generally did not reveal a decrease in V02max under the influence of diuretics, endurance indicators did worsen. In one of the studies, to determine the effects of diuretic dehydration, indicators of sports performance were examined in three races at distances of 1500, 5000 and 10,000 m. It turned out that in those conditions when placebo was used instead of a diuretic, the result in running 1500 m worsened by 8 s, in the 5000 m run - by 78 s and in the 10,000 m run - by 157 s. In addition, diuretic dehydration is superimposed on dehydration caused by physical activity or high ambient temperature, which further affects the manifestation of aerobic endurance.
As for the negative impact of diuretics on the human body in general and the athlete in particular, it can occur when the recommended doses are exceeded, the duration of the courses used, and also against the background of the presence of contraindications. The negative effects of diuretics, as mentioned above, include dehydration, hypokalemia (saluretics), hyperkalemia (potassium-sparing diuretics), hypochloremic alkalosis (thiazide diuretics), metabolic acidosis (carbonic anhydrase inhibitors), hyperglycemia, hyperuricemia (thiazide diuretics), hypervolemia (osmotic diuretics), ototoxicity (loop diuretics), hyponatremia, hypomagnesemia (saluretics), hypocalcemia (thiazide diuretics), gynecomastia, impotence, menstrual irregularities (spironolactone), formation of calcium oxalate or phosphate in the kidneys (carbonic anhydrase inhibitors, triamterene).
Diuretics in bodybuilding
As already mentioned, the diuretic furosemide, which belongs to the group of saluretics, is popular among athletes (especially in bodybuilding). Its effect is expressed in a distinctly increased release of water and salts from the body, and the excretion of sodium, chlorides, potassium, calcium and water. Another important quality of this type of drug, which sports specialists should pay attention to, is that the reverse resorption of potassium, sodium and chloride ions slows down. This leads to a significant imbalance in the electrolyte balance. Due to its ability to intensively dehydrate the body, furosemide is used in the treatment of edema and arterial hypertension. Athletes involved in bodybuilding take furosemide shortly before competitions to remove “excess” subcutaneous water and in order to look elastic and lean on stage at the time of competition. The tablets begin to act within 1 hour, and their effect lasts 3-4 hours. Depending on the amount of excess water in the body, more or less frequent urges to urinate appear. In this case, a significant loss of body weight can occur in the shortest possible time. On this basis, furosemide is taken by athletes to stabilize body weight. Athletes, as a rule, prefer the oral form of the drug. Sometimes athletes use the injection or intravenous version on the morning of the competition, as these methods of administration are immediate and are good when the athlete is panicking due to fluid remaining under the skin. However, this use of furosemide may have the opposite effect. The muscles decrease in size, lose their convexity, become flat, and the athlete loses “masculinity.” It may happen that one or another athlete - professional or amateur, who has achieved the best success, right before the start of the competition will be forced to use all kinds of countermeasures, representing intravenous administration of glucose in order to increase blood volume and smooth out the loss of potassium; Many athletes take potassium chloride tablets. But this is unsafe, since an overdose of potassium can lead to cardiac arrest. Based on experience, furosemide is used in the last 2 days before competition.
Athletes specializing in bodybuilding usually use the diuretic furosemide as follows: take half or a whole 40-milligram tablet and wait for the effect. Some athletes repeat this procedure a few hours later 1-2 more times. It should be remembered that furosemide is the most powerful diuretic and one of the most dangerous drugs in the medical arsenal of bodybuilders. Side effects include: hemodynamic disorders, dizziness, dehydration, muscle spasms, vomiting, vascular collapse, diarrhea, feeling of malaise. In extreme conditions, cardiac arrest may occur. It is quite possible that this was the cause of the death of two athletes specializing in bodybuilding: the Austrian bodybuilder Heinz Salmeier, who died in the 1980s, and Mohammed Benaziza, who died in October 1992.
By following the principles of rational combined use of diuretics, their side effects can be minimized. For example, active diuretics that act at the level of the basement membrane (diacarb, hydrochlorothiazide, cyclomethiazide, oxodoline, ethacrynic acid, furosemide, bufenox, clopamide, torsemide) are often combined with triamterene or spironolactone, drugs that act at the level of the apical membrane; this reduces the likelihood of hypokalemia. Can diuretics benefit an athlete's body? In some cases - undoubted, and not at all in relation to concealing other prohibited substances, since one of the main indications for the use of diuretics are various intoxications of the body, both exogenous and endogenous. As for endogenous intoxications, an athlete is more susceptible to them than a non-athlete. This is due to the catabolic processes intensified under the influence of high physical activity, as a result of which various toxic catabolic products accumulate in the athlete’s body - ketone bodies, ammonia, urea, uric acid, etc. Therefore, the use of diuretics could help detoxify the athlete’s body. Thus, we can say that the ban on the use of diuretics is not completely justified from the point of view of protecting the athlete’s health, but, on the contrary, limits the ability of the sports doctor to provide the necessary assistance to the patient.
As for diuretics of plant origin, their use in sports is not prohibited, obviously due to the impossibility today of developing the necessary test systems. In addition to low toxicity, the advantages of plant-based diuretics are their ability to accelerate the elimination of toxic metabolites and under-oxidized products of carbohydrate metabolism from the body, and the absence of electrolyte imbalances, which is extremely important for athletes. This allows herbal preparations to be used for long periods of time without serious side effects. At the same time, we must not forget that the activity of diuretics of plant origin is lower than that of synthetic drugs. Thus, diuretics of plant origin provide a gradual increase in diuresis only on the 3-7th day of use. In addition, manifestations of hypersensitivity to all herbal preparations have been observed in some individuals.
Is it possible from a medical point of view to recommend the use of diuretics to athletes? Although most medical authorities condemn the practice of using various methods of weight loss practiced by representatives of some sports, wrestlers, boxers and other athletes continue to use them. Most athletes can achieve their desired body weight through appropriate dietary programs and harmless and non-prohibited methods of dehydration such as exercise.
It was previously noted that the use of diuretics is not recommended in sports that require aerobic endurance, since athletic performance in this case deteriorates.
Diuretic-induced dehydration may also cause some serious health problems in athletes by making them more susceptible to heat exhaustion and more susceptible to heat stroke during prolonged exercise in high-temperature environments. By increasing the excretion of water from the body, diuretics simultaneously increase the excretion of electrolytes, in particular sodium. Therefore, chronic use of saluretics can lead to a significant decrease in sodium content in the body and disruption of the nervous system with symptoms ranging from muscle weakness to disruption of the normal functioning of the heart, even cardiac arrest.
Obviously, even mild diuretics of plant origin should be used by athletes only as prescribed by a doctor and under medical supervision. As for potent synthetic drugs, there is no doubt that a blanket ban on their use is unjustified. There is no doubt that in some cases, as mentioned above, they can benefit the athlete’s health. Another thing is that these drugs should be used exclusively as prescribed by a doctor and under strict medical supervision, but this is no longer the competence of WADA, but of the services responsible in a given country for organizing medical care for athletes.
Other ways to hide the use of anabolic steroids
As mentioned above, this class includes not only diuretics, but also “other masking substances”: epitestosterone, probenecid, 5-a-reductase inhibitors, plasma replacers and other substances with similar biological effects.
Epitestosterone is a metabolite of testosterone that does not exhibit anabolic properties, but prevents the establishment of the fact of taking anabolic steroids, primarily testosterone, and is also prohibited as a masking agent.
Probenecid is a drug that promotes the elimination of uric acid. The mechanism of its action is to inhibit the reabsorption of uric acid, which enhances its excretion from the body. Probenecid prevents the formation of uric acid salts and promotes their resorption, reducing the risk of joint damage. Therefore, in clinical practice the drug is used to treat chronic gout. In addition, probenecid inhibits the tubular secretion of penicillin and thereby increases its level in the blood.
Probenecid became widely known in sports back in 1988. At the Tour de France, it was discovered in the Spaniard Pedro Delgado. At that time, the drug had not yet been banned, and Delgado calmly reached the finish line and even won, but two weeks later probenecid was included in the list of prohibited drugs. This drug facilitates the excretion of anabolic steroids in the urine and thereby gives (at least in theory) a chance for the athlete using them not to be caught using illegal drugs.
5a-reductase inhibitors include finasteride and dutasteride. In clinical practice, these drugs are used in the treatment of prostate adenoma. The history of the use of 5a-reductase inhibitors dates back to June 19, 1992, when the US FDA approved the use of finasteride to treat men with symptoms of benign prostatic hypertrophy. In October 2002, a new drug appeared on the pharmaceutical market - Avodart® (dutasteride), which inhibits both types of 5a-reductase. The use of these drugs in sports as masking agents is due to the fact that their use makes it difficult to identify anabolic steroids.
Finasteride's chemical structure is N-tert-butyl-3-oxo-4-aza-5a-androst-1-ene-17beta-carboxamide. It is a synthetic 4-azasteroid, a specific inhibitor of the type 2 5-a-reductase enzyme responsible for the conversion of testosterone to dihydrotestosterone (DHT).
Pharmacokinetics. Finasteride, when taken orally, is quickly and completely absorbed into the gastrointestinal tract. Bioavailability is approximately 63-80%. The drug reaches its maximum concentration in the blood plasma 1-2 hours after administration, the half-life is 6-8 hours. About 90% of finasteride binds to blood plasma proteins. The drug penetrates the blood-brain barrier. Approximately 40% of the drug is excreted in the urine as metabolites and about 60% in the feces. A metabolite with a monocarboxyl group is predominantly detected in urine. With repeated doses, slow accumulation in the body is observed: after 17 days of use at a dose of 5 mg day-1, the concentration in the blood plasma is approximately 50% higher than after a single dose.
Pharmacodynamics. The development of the prostate gland, the proliferation of its tissue and the development of hyperplasia depend on the level of DHT (benign prostatic hyperplasia does not occur in men with a hereditary defect of 5a-reductase). By inhibiting the conversion of testosterone to DHT, finasteride effectively reduces the level of DHT, which leads to a decrease in the size of the prostate gland and the severity of dysuric symptoms caused by hypertrophy. Finasteride does not bind to androgen receptors and does not affect the hypothalamic-pituitary axis. After oral administration, finasteride effectively reduces the level of DHT in both blood plasma and prostate tissue within the first 24 hours. However, to achieve a clinical effect, the duration of therapy should be several months. Finasteride reduces the concentration of DHT in the blood serum by approximately 70%, and in the prostate by 85-90%. In addition to inhibiting 5a-reductase, it activates apoptosis in the epithelium and stroma of the prostate through certain proteases, which justifies the reduction in its size.
Indications for use: therapy for benign prostatic hyperplasia in order to reduce its size and the severity of dysuric symptoms. Finasteride is only used in men. The usual dose is 5 mg daily, the duration of treatment is at least 6 months.
Contraindications: hypersensitivity to the components of the drug. Prescribing the drug to women and children is not allowed.
Side effects: rare, usually mild and reversible. Possible decrease in potency and libido, decrease in ejaculate volume, engorgement and enlargement of the mammary glands, rarely - hypersensitivity reactions (swelling of the lips, skin rash).
Since finasteride is a selective inhibitor of type 2 5a-reductase, almost immediately after its invention, work began to search for a drug that could inhibit both isoenzymes, which theoretically would lead to an enhanced therapeutic effect. In the early 1990s, MSD brought a molecule with a similar effect (MK-434) to phase II clinical trials, but the studies were quickly curtailed due to the high toxicity of the drug.
It took GlaxoSmithKline 10 years to invent both types of 5a-reductase inhibitor. The drug received a working name from the name of the manufacturer - G1198745, and then - Avodart® (dutasteride). In 1998, the results of the first phases of clinical trials were published. The results of a phase III study published in 2002 showed that dutasteride led to improvement in symptoms after only 3 months of therapy and a reduction in prostate volume by more than 25% compared with placebo. The time to achieve the treatment effect during dutasteride therapy was shorter, and the effectiveness was greater than that of finasteride.
The use of finasteride and dutasteride is prohibited as substances that mask the use of anabolic steroids by athletes.
Finally, “other masking substances” also include plasma-substituting solutions - a group of drugs used to replace plasma in acute blood loss, shock of various origins, microcirculation disorders, intoxication and other processes associated with changes in hemodynamics. Sometimes they are also called blood substitutes, which is incorrect: they do not perform the function of blood, since they do not contain its formed elements (unless the latter are specially introduced into them) and are also not sources of energy reserves (they do not contain energy substances - glucose, amino acids, etc. ). These drugs include, in particular, albumin, dextratan, hemodez, polyglucin, hydroxyethyl starch, etc. For example, hydroxyethyl starch (HES), a synthetic blood substitute, is a solution for intravenous infusion. He and similar drugs - hemodez, polyglucin - are widely used in medicine as detoxification agents. The drug is a colloidal solution of polysaccharides, does not carry oxygen, does not accelerate metabolism, and does not affect the nervous system or muscle tone. Its effectiveness as a masking agent is also highly questionable. The maximum masking effect achievable with its help is hemodilution, which reduces the hematocrit and hemoglobin level (the use of EPO drugs that increase these blood parameters is not masked by HES in any case). What has been said about hydroxyethyl starch as a masking agent equally applies to other representatives of the group of plasma substitutes.