Diuretics are therapeutic agents used to increase the rate of urine flow, sodium and electrolyte excretion to regulate the amount and composition of body fluids or to remove excess fluid from tissues, and are used in clinical therapy for the treatment of various diseases and syndromes, including hypertension, heart failure, cirrhosis of the liver, kidney failure, kidney and lung disease. [1]

Diuretics are banned in sports because they can be used by athletes for two main reasons.

-First, due to their powerful ability to remove water from the body, diuretics can cause the rapid weight loss required to make weight in sports such as wrestling, Olympic weightlifting, and boxing.

-Second, they can be used to conceal the administration of other doping drugs by reducing their concentration in the urine due to increased urine output. [2]

Furosemide is a potent diuretic and is available in both injectable and oral forms.

Oral furosemide can be administered as a tablet or oral solution.

Intravenous furosemide is twice as potent as oral furosemide, and furosemide is immediate-acting, flushing out the urine within 20 minutes of oral ingestion.

The drug's final half-life is approximately 2 hours, with a total therapeutic effect time of 6 to 8 hours.

Furosemide acts on the renal loop of Henle, inhibiting the sodium-potassium-chloride pump and inducing diuresis and natriuresis (increased sodium loss).

The drug also induces renal synthesis of prostaglandins, which contribute to renal action. [3]

The adverse effects are all related to fluid and electrolyte imbalances and hypovolemia.

These include hyponatremia and/or extracellular fluid volume depletion (associated with hypotension, circulatory collapse, and thromboembolism), hypokalemia (causing cardiac arrhythmias), hypomagnesemia, which can lead to convulsions and metabolic alkalosis, hyperuricemia (sometimes causing gout), and hyperglycemia.

It also increases plasma levels of low-density lipoprotein cholesterol and triglycerides and decreases plasma levels of high-density lipoprotein cholesterol. [4]

Conversely, spironolactone is a potassium-sparing diuretic.

Spironolactone belongs to the class of aldosterone inhibitors, a type of diuretic that antagonizes the action of aldosterone in the distal portion of the distal tubule.

Aldosterone is a hormone belonging to the mineralocorticoid class and is secreted by the adrenal cortex.

It affects the reabsorption of sodium and the excretion of potassium by the kidneys, resulting in increased water retention, blood pressure, and blood volume.

[5] Since potassium is a major intracellular ion, the retention of potassium by the action of spironolactone contributes to better cell volume, which has a positive effect on cell size maintenance.

Aldosterone plays an important role in the last week before a bodybuilding competition.

To suppress aldosterone and eliminate water retention, the body is tricked by deliberately increasing the intake of sodium chloride (table salt).

This seems to suppress sodium retention the next day.

Typically, we stop sodium intake on the last day of glycogen depletion, just before the carbohydrate loading phase.

Abuse of spironolactone can have life-threatening side effects due to a rapid rise in potassium (hyperkalemia) and metabolic acidosis.

The myocardium is very sensitive to this metabolic imbalance and can easily develop severe arrhythmias (ventricular tachycardia, fibrillation) or even cardiac arrest (Mohamad Benaziza 1993).

Electrocardiographic changes in hyperkalemic patients are an ominous sign of potentially fatal arrhythmias.

The fact that the adrenal cortex produces significant amounts of dihydroepiandrosterone (DHEA) makes it understandable that abuse of spironolactone can lead to dose-dependent gynecomastia. [4]

The antiandrogenic properties of spironolactone (breast tenderness and enlargement) are even more pronounced in women who lack gonads (testes) and actually produce testosterone from the ovaries and adrenal glands.

Women use spironolactone to reduce the aesthetic androgenic side effects of androgenic anabolic steroids (AAS), particularly hirsutism.

Spironolactone acts transiently on steroid hormone synthesis, causing hypogonadism, a decrease in sperm count and motility (FSH).

Spironolactone does not act immediately and reaches stable concentrations within almost 3 days of starting treatment.

Doses should be divided into morning and afternoon doses for better metabolism.

The right time to use spironolactone is the first day of the carbohydrate depletion phase.

Potassium-rich foods (bananas or potatoes) are strictly prohibited.

Spironolactone should be tapered off gradually to avoid rebound effects.

The most efficient way to achieve the best results of diuretics should be a combination of a potassium-sparing diuretic and a non-potassium-sparing diuretic, that is, spironolactone and furosemide.

However, the dosage should be reduced by half.

Diuretics are very dangerous substances that are the cause of hypovolemia and dehydration, striated muscle spasms (cramps),loss of coordination and balance, hypotension (drop in systemic blood pressure)All diuretics, except for potassium-sparing ones, increase potassiumosis, which accelerates the depletion of intracellular potassium.

The resulting hypokalemia can lead to serious cardiac arrhythmias secondary to electrolyte shifts/losses.

On the other hand, excessive use of potassium-sparing diuretics such as spironolactone can cause hyperkalemia, which in turn exposes athletes to malignant arrhythmias. [6]

A classic example of cardiovascular collapse due to diuretic abuse is the tragic death of the 'giant killer' Arab Mohammed Benaziza (Momo) at the 1993 Dutch Grand Prix, where, according to his close friend Samir Bannut, he not only abused spironolactone, but also stopped drinking fluids and consumed clenbuterol in powder form.

In addition, diuretics are considered to be one of the most relevant classes with regard to sexual dysfunction, particularly erectile function, ejaculation, and libido (primarily thiazide diuretics and spironolactone).

Spironolactone tends to cause undesirable sexual side effects, and at standard doses can cause breast tenderness, gynecomastia, and erectile dysfunction in men, and menstrual abnormalities in premenopausal women. [8]

Diuretics are preferably used before nighttime sleep to avoid fainting due to low blood pressure.

Potatoes and bananas, which are rich in potassium, can be helpful in cases of hypokalemia,while caffeine and alcohol are strictly prohibited (diuretic effect).

In bodybuilding, diuretics are strictly prohibited during the glycogen depletion phase or the period of preparation before a competition, with the exception of the carbohydrate loading phase, in order to avoid the risk of possible retention of moisture under the skin.

During the week prior to a competition, bodybuilders follow a tapering strategy to increase "muscle fullness" by maximizing muscle glycogen content to achieve a dry, hard appearance by minimizing subcutaneous water retention under the skin,[9] which in turn increases "muscle fullness."[10] Those who use furosemide may find that it is a diuretic that can cause water retention.

Those who plan to use furosemide should also take calcium and magnesium from supplements, along with potassium-rich carbohydrates such as baked potatoes and bananas.

Muscles can't flex or pump without proper electrolyte balance.

Spironolactone, unlike furosemide, is responsible for maintaining anemia in myomas.

This is reflected in the outward appearance of bodybuilders, whose muscles are firm and able to contract.

Furosemide, on the other hand, flushes all electrolytes and especially potassium from the cytoplasm of the muscle, leading to the characteristic flat, drained, empty appearance of the muscle.

Potassium is the main electrolyte in cells and plays an important role in maintaining cell volume.

The tricky part about using spironolactone is that you need to switch to furosemide the day before a performance when serum potassium levels are high.

With furosemide, you flush out the extra potassium so that it doesn't dangerously rise into the bloodstream.

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On the morning of the competition, if you are still retaining water, a moderate dose of furosemide (10 mg) combined with spironolactone (12.5 mg) will safely remove the excess water.

Dehydrated muscles cannot contract properly, so calcium tablets and liquid magnesium are recommended in this case.

The sport of bodybuilding involves risk, craze, and vanity, all of which can pose long-term risks, so exaggeration and the idea that more is better is not a panacea and does not necessarily guarantee success.

The side effects of a particular substance depend on various parameters such as age, time of abuse, dosage, combination of performance enhancing drugs (PEDs), lifestyle, proper nutrition and supplements, medical precautionary rules, and family history.

The abuse of multiple drug combinations is widespread, especially among bodybuilders, to build muscle hypertrophy, burn fat, speed up recovery, prevent the effects of overtraining, increase training intensity and aggression, and control fat, body water, and appetite.

Anabolic androgenic steroids (AAS) combined with diuretics, anti-estrogens, stimulants, alcohol, tobacco, narcotics, and other drugs can increase the risk of serious cardiovascular events, and one of the most dangerous drugs in bodybuilding is diuretics, which can cause fatal hypovolemic shock and severe cardiac arrhythmias, respectively.

In fact, diuretics have been anecdotally linked to the death of some bodybuilders, and the misuse and abuse of diuretics also poses a serious risk to a bodybuilder's health.

Personally, I have used three types of diuretics (Lasix, Aldactone, and Moduretic).

I have experienced the side effects of hypovolemia (low blood pressure, fainting) and muscle cramps (rectus abdominis).

Diuretics can make a difference between two athletes with the same subcutaneous body fat, but the price of their use can jeopardize the whole effect and quit the show, but they are useless if the body fat level is not below 5-6%.

reference

[1].In: Brunton L, Rajo J, Parker K, editors. Goodman and Gilman's Pharmacological Basis of Therapeutics. 11th ed. New York: McGraw-Hill; 2006.

[2].Sports Drug Testing – An Analyst’s Perspective. Trout GJ, Kazlauskas R. Chem Soc Rev. 2004; 33:1-13.

[3].StatPearls Tahir M. Khan; Abdul H. Siddiqui. Last update: May 10, 2019.

[4].Abuse of diuretics as performance-enhancing drugs and masking agents in sports doping: pharmacology, toxicology and analysis. Amy B Cadwallader, Xavier de la Torre, Alessandra Tieri, and Francesco BotrèBr J Pharmacol. Sep 2010; 161(1): 1-16

[5].The role of spironolactone in the treatment of patients with refractory hypertension. Ouzan J, Perault C, Lincoff AM, Carre E, Mertes M. Am J Hypertens. 2002; 15: 333-339.

[6].Myocardial infarction, hyperkalemia and ventricular tachycardia in a young male bodybuilder. Appleby M, Fisher M, Martin M. Int J Cardiol. 1994;44:171-174

[7].Nutrition, pharmacology and training strategies adopted by six bodybuilders: case report and critical reviewPolo Gentile et al. Eur J Transl Myol. 2017 Feb 24; 27(1): 6247.

[8].A review of the positive and negative effects of cardiovascular medications on sexual function: a suggested table for use in clinical practice. P. J. Nikolai et al. Neth Heart J. 2014 Jan; 22(1): 11-19.

[9].Peak Week and Competition Day Strategies of Competitive Natural Bodybuilders Andrew J Chappell and Trevor N. Simper Sports 2018, 6(4), 126