Spironolactone

• Aldactone

Spironolactone is known as a potassium-sparing diuretic. It acts by competitively inhibiting aldosterone binding to receptor sites, especially in the renal tubes where aldosterone is involved in sodium-potassium exchange. The drug causes increased amounts of sodium and water to be excreted and potassium to be retained. This is different from some other agents of this class, such as a loop diuretic like furosemide, which can significantly increase the excretion of sodium, water, and potassium. In this light, spironolactone is commonly referred to as a "potassium sparing" diuretic. It is used medically for a number of conditions including the treatment of high blood pressure, edema related to congestive heart failure, hyeraldosteronism (the over production of aldosterone), and hypokalemia (drop of potassium, often associated with other medical interventions). Spironolactone is often used (off-label) by competitive athletes and bodybuilders to make short-term adjustments in water weight. The primary focus is to bring about increased muscle definition by shedding subcutaneous water (bodybuilders), or to make category adjustments during the weigh-in procedure in sports with restricted weight classes (athletes). Information on overdose is limited. Patients are unlikely to develop serious features. The misuse of diuretic drugs for physique-or performanceenhancing purposes is characterized as a high-risk practice. Diuretics may produce a life-threatening level of dehydration and electrolyte imbalance when administered without proper medical supervision. Many deaths have been associated with the misuse of these drugs. It is also important to note that the supplementation of potassium, either through pharmaceuticals or a diet rich in potassium, is generally not advised while taking a potassium-sparing diuretic like spironolactone. Excessive potassium intake may cause hyperkalemia, which may lead to cardiac irregularities and possibly death.

Adverse reactions associated with spironolactone administration may include gynecomastia, cramping, diarrhea, drowsiness, lethargy, headache, skin irritation, rash, mental confusion, fever, impotence, loss of muscle coordination, menstrual irregularities, virilization, and deepening of the voice. Spironolactone has also been shown to cause tumors in rats. Breast cancer has been reported in some patients receiving spironolactone, but no causal relationship has yet been established. Additionally, this compound may exhibit anti-androgenic properties, as both a weak inhibitor of androgen/receptor binding and testosterone biosynthesis.