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 competitive 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 oral 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 be 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 this or that 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 1-2 more times after a few hours. 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, it is 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 both in blood plasma and in 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 to placebo. The time to achieve the treatment effect during therapy with dutasteride 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.
Preparation Furosemide belongs to the class of pharmaceutical diuretics (diuretics) that help remove fluid from the body. Furosemide is widely popular in sports as a means of rapid weight loss before competitions and to hide the use of illegal drugs. In bodybuilding, Furosemide is most often used to remove water from the body and give muscles a more prominent shape.
Furosemide in medicine
This drug is used to treat edema, intoxication and poisoning, as well as to lower blood pressure. By activating kidney function (increasing renal blood flow) and reducing the activity of certain enzymes, the body begins to remove fluid from the body much faster.
Furosemide for weight loss
There is an opinion that Furosemide can be used in weight loss and fat burning, but this is a misconception. The only justification for taking this drug is the purposes indicated at the very beginning of the article. That is, for sporting purposes before competitions.
Taking Furosemide by ordinary people, although it leads to significant weight loss (up to 3%), but this loss is carried out solely due to severe dehydration of the body, and with it the increased release of potassium, calcium, bicarbonates and phosphates, which is very harmful to health and contributes to the development of various pathologies - for example, the formation of kidney stones.
Side effects
Taking Furosemide may be accompanied by the following side effects:
Expert conclusions
The use of Furosemide as a fat burner and weight loss aid is unfounded and potentially hazardous to health. Taking this drug does not help reduce the amount of subcutaneous fat and does not affect metabolism. The effect of weight loss is achieved due to severe dehydration of the body.
Taking Furosemide is justified only by competitive athletes who need a quick weight loss before competitions to get into the desired weight category, to hide the use of prohibited drugs and in bodybuilding - to remove water from the body and improve the quality of muscles.
Important! Taking any pharmacological drugs for sports purposes and weight loss can cause irreversible harm to health. Consult your doctor!
Contents of the article:
Loop diuretics are used quite often in bodybuilding. These are powerful diuretics that are superior to thiazide drugs in terms of ridding the body of fluid and salts, but at the same time reduce blood pressure to a lesser extent. We also note that drugs in this group do not increase cholesterol levels and do not upset its balance.
Loop diuretics in bodybuilding are used shortly before the start of competitions to quickly remove excess fluid from the body, which makes it possible to give the muscles additional relief. Oral medications begin to work on average an hour after administration and act on the body for 4–4 hours.
Also, when taking diuretics, weight loss is observed. This fact is the main reason for using diuretics to stabilize your weight. The most popular are oral medications. In case of emergency, injectable diuretics are also used to quickly remove fluid from the body.
The most popular diuretic is Furosemide. Most often, to achieve goals, athletes only need to consume from 20 to 40 milligrams of the drug (0.5–1 tablet). If it is necessary to remove a large amount of liquid, the procedure can be repeated after a few hours.
It should be noted that Furosemide is a powerful diuretic and caution must be exercised when using it. Improper use may lead to side effects. To avoid such a situation, you should carefully read the instructions for diuretics, and also use complex use.
The most popular among athletes is the combination of diuretics, for example, Furosemide or entacrynic acid, with Triamterene or Spirolactone. These drugs act on the apical membrane, which significantly reduces the risk of hypoglycemia.
I would also like to say a few words about the ban on the use of diuretics by athletes. One of the indications for the use of drugs of this class are various types of intoxication of the body. It should be noted that athletes are much more susceptible to endocrine intoxication compared to ordinary people. This is due to the strong catabolic processes occurring in the body during training. Thus, it can be argued that the ban on the use of diuretics in sports somewhat limits doctors’ ability to provide assistance to an athlete.
Now we will look at the most popular drugs among athletes.
The drug is well absorbed by the intestines and almost immediately after administration it comes into contact with blood proteins. The therapeutic effect is observed within half an hour after the drug enters the body. The maximum concentration of the active substance is created in one or two hours, and Uregit works from 4 to 8 hours. If the injection form of the product is used, the product begins to work within 10 minutes.
Uregit has high diuretic activity and works at the level of the basal cells of the tubular epithelium, or more precisely, in the ascending part of the loop of Henele. The drug blocks the activity of enzymes involved in energy production, which affects the operation of the pumps. With long-term use of the drug, it helps reduce blood pressure.
Since the drug helps accelerate the excretion of potassium and magnesium from the body, with its long-term use it is possible to develop hypomagnesemia and hypokalemia. Pain may occur in the esophagus and large intestine. This is the result of the irritating effect of the active substances of the drug. To prevent the above problems, before using Uregit, the product should be diluted in an isotonic sodium chloride solution.
When used intravenously, the therapeutic effect will be achieved much faster, in about 10 minutes. The drug will work in this case from 2 to 4 hours. The half-life of Furosemide is 0.5 to 1 hour.
The drug has a variety of effects on renal tubular cells. Since the drug suppresses the activity of energy-producing substances, for example, hexokinase, there is not enough energy for the sodium pump to operate and its activity is suppressed.
The drug has a depressing effect on the process of resorption of chlorine and sodium, which leads to an increase in the flow of passive sodium from the intercellular space and leads to an increase in the intracellular pool of sodium-plus. The drug also has a stimulating effect on blood flow in the kidneys and accelerates the excretion of phosphates, potassium, calcium, magnesium and bicarbonates from the body.
The drug also increases the content of kinins and prostaglandins, which results in an increase in the overall dynamics of the kidneys and accelerates the excretion of sodium from the body. Furosemide also helps reduce blood pressure.
If the permissible dosages are exceeded, the volume of pulsating blood may be reduced. With prolonged use of the drug, the development of hypokalemia, hypochloremia, and metabolic alkolosis is possible. Exacerbation of gout may occur with high uric acid excretion, and hyperglycemia has also been observed in rare cases.
Learn more about the effects of loop and thiazide diuretics on the body from this video:
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.
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.
Among professional bodybuilding athletes, the most popular are “soft” and “hard” diuretics. Soft ones do not cause 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.
Special sports diuretics
Modern bodybuilders prefer to drink loop diuretics, which have a “harsh” effect. These include Lasix, Furosemide, Chlorthalidone, Torsemide, Triamterene and Acetazolamide. Many manufacturers offer athletes special sports nutrition, which includes herbs with diuretic properties. They effectively eliminate excess fluid in tissues, improve muscle definition without reducing the physical endurance of muscles and do not lead to hypokalemia.
Risks of using diuretics in sports
Drying with the use of diuretics in sports is today prohibited by many sports federations - up to the use of herbal teas with a diuretic effect. This is due to their harmful effects on health with constant use and the use of diuretics as a “screen” when taking prohibited stimulants (doping).
