Diuretics are therapeutic agents that increase the rate of urine flow and the excretion of sodium and electrolytes to adjust the volume and composition of body fluids or to eliminate excess fluid from tissues.
They are used to treat hypertension, heart failure, cirrhosis, renal insufficiency, and various kidney and lung diseases.
Diuretics are banned for athletes for two primary reasons.
First, their powerful ability to eliminate water can induce rapid weight loss for making weight in sports like wrestling, weightlifting, and boxing.
Second, by increasing urine volume, they can dilute the concentration of banned substances in the urine, potentially masking the use of doping agents.
Furosemide is a potent diuretic available in both injectable and oral forms.
The oral form is administered as tablets or a solution, while the intravenous injection is twice as potent as the oral route.
Furosemide takes effect within 20 minutes of oral ingestion, has a half-life of about 2 hours, and its effects last for 6 to 8 hours.
Furosemide induces diuresis by inhibiting the sodium-potassium-chloride pump in the loop of Henle in the kidneys and aids renal function by promoting prostaglandin synthesis.
Side effects are related to fluid and electrolyte imbalances and hypovolemia.
Hyponatremia or extracellular fluid depletion is associated with hypotension, circulatory collapse, and thromboembolism, while hypokalemia can cause cardiac arrhythmias.
Hypomagnesemia can lead to cramps and metabolic alkalosis, hyperuricemia can cause gout, and hyperglycemia can result in metabolic issues.
Additionally, it increases low-density lipoprotein (LDL) cholesterol and triglycerides while decreasing high-density lipoprotein (HDL) cholesterol.
Spironolactone is a potassium-sparing diuretic and belongs to the class of aldosterone antagonists, which antagonize the action of aldosterone in the distal convoluted tubules.
Aldosterone is a mineralocorticoid secreted by the adrenal cortex that regulates sodium reabsorption and potassium excretion, thereby increasing water retention, blood pressure, and blood volume.
The potassium-retaining effect of spironolactone positively impacts the maintenance of cell volume.
Aldosterone plays a crucial role before a bodybuilding competition.
To suppress aldosterone and eliminate water retention, the body is tricked by intentionally increasing sodium chloride intake.
This makes it seem as though sodium retention is suppressed the following day.
Sodium intake is discontinued on the last day of glycogen depletion, right before the carbohydrate loading phase.
Abuse of spironolactone can lead to life-threatening side effects due to a rapid rise in potassium (hyperkalemia) and metabolic acidosis.
The myocardium is highly sensitive to these metabolic imbalances, which can easily trigger severe arrhythmias (ventricular tachycardia, fibrillation) or cardiac arrest.
(Mohamad Benaziza 1993) Electrocardiogram (ECG) changes in patients with hyperkalemia are a warning sign of fatal arrhythmias.
Because the adrenal cortex produces a significant amount of DHEA, spironolactone abuse can cause dose-dependent gynecomastia.
The antiandrogenic properties of spironolactone (breast tenderness and enlargement) are more pronounced in women with gonadal dysfunction, and women use it to reduce the androgenic side effects of AAS (especially hirsutism).
Spironolactone acts on steroid synthesis, causing hypogonadism that reduces sperm count and motility (FSH).
Steady-state concentrations are reached within about 3 days of starting treatment, and the dosage should be split between morning and afternoon.
The appropriate time to use spironolactone is on the first day of carbohydrate depletion.
Potassium-rich foods (bananas, potatoes) are strictly forbidden, and the dose should be gradually tapered to prevent a rebound effect.
For best results, a combination of the potassium-sparing diuretic spironolactone and a non-potassium-sparing diuretic like furosemide is effective, and the dosages should be halved.
Diuretics are extremely dangerous substances that can cause hypovolemia, dehydration, and muscle cramps, leading to loss of coordination and balance, and hypotension.
All diuretics, except for potassium-sparing ones, increase potassium excretion, accelerating intracellular potassium depletion. The resulting hypokalemia from electrolyte loss can trigger severe cardiac arrhythmias.
Conversely, overuse of potassium-sparing diuretics like spironolactone causes hyperkalemia, increasing the risk of malignant arrhythmias.
One case of cardiovascular collapse due to diuretic abuse is the tragic death of ‘the Giant Killer’ Mohammed Benaziza at the 1993 Dutch Grand Prix.
According to his friend Samir Bannout, Benaziza abused spironolactone, ceased water intake, and took clenbuterol.
Furthermore, diuretics are strongly linked to sexual dysfunction (impaired erection, ejaculation, and libido), with thiazide diuretics and spironolactone being the main culprits.
In men, spironolactone causes breast tenderness, gynecomastia, and erectile dysfunction, while in premenopausal women, it can lead to menstrual irregularities.
To avoid fainting from hypotension, it is advisable to take diuretics before sleeping at night.
Potassium-rich potatoes and bananas are useful for hypokalemia, but caffeine and alcohol are forbidden.
In bodybuilding, diuretics are strictly prohibited during the glycogen depletion phase (excluding carb-loading) or the pre-contest preparation period to prevent water retention.
During the week before a competition, bodybuilders use a tapering strategy to maximize muscle glycogen for a “full muscle” look and minimize subcutaneous water under the skin to create a dry appearance.
Those taking furosemide should supplement with calcium and magnesium.
Spironolactone helps maintain muscle hardness by preventing anemia in the muscle tissue, whereas furosemide flushes out potassium, leaving muscles drained and flat.
One should switch to furosemide the day before the show to regulate serum potassium levels. If water remains on the morning of the competition, a moderate dose of furosemide and spironolactone can be taken together to eliminate it.
Dehydrated muscles have difficulty contracting, necessitating the intake of calcium tablets and liquid magnesium.
The sport of bodybuilding involves risks, crazes, and vanity, and can pose serious long-term dangers.
The side effects of a particular substance vary depending on numerous factors, including age, duration of abuse, dosage, combination of PEDs, lifestyle, nutrition, supplementation, preventive measures, and family history.
Polypharmacy, the abuse of multiple drugs, is widespread among bodybuilders to achieve muscle hypertrophy, burn fat, enhance recovery speed, prevent the effects of overtraining, increase training intensity and aggression, and control fat and body water.
AAS can be combined with diuretics, anti-estrogens, stimulants, alcohol, tobacco, and narcotics. Diuretics, in particular, elevate the risk of severe cardiovascular events by causing potentially fatal hypovolemic shock and severe cardiac arrhythmias.
In fact, there are documented cases where diuretic abuse has been linked to the deaths of bodybuilders.
The misuse and abuse of diuretics pose a serious threat to the health of bodybuilders.
Over the years, I have seen many athletes who use Lasix, Aldactone, and Moduretic experience hypovolemia (hypotension, fainting) and rectus abdominis cramps.
Diuretics can make a difference between two athletes with the same subcutaneous body fat, but they are not very effective if body fat is not below 5-6%.
Furthermore, the price of using them can jeopardize the overall effect.
