Aldactone — spironolactone

Spironolactone is an antagonist of aldosterone and is pharmaceutically classified as a 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 likefurosemide, 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).

Brand name

Aldactone, Spironolactone

Spironolactone History

Spironolactone was developed during the late 1950s, and first saw widespread use in clinical medicine during the early 1960s. The drug filled an important need for a diuretic that does not deplete potassium, and therefore has a less dramatic impact on electrolyte balance in the body. In many regards it is looked at as a “safer” and “milder” diuretic compared to other agents in this general category, such as loop diuretics or thiazides, allowing this agent room for market stability and success. Today, spironolactone is widely distributed throughout most for market stability and success. Today, spironolactone is widely distributed throughout most of the developed world. It is available in dozens of brand names, the most commonly identified is probably Aldactone from Searle. It is also widely sold in mixed-ingredient preparations alongside other diuretics. This includes furosemide, as seen in the product Lasilacton, or hydrochlorothiazide, in Searle’s (also widely distributed) mixed diuretic product Aldactazide.

How is Spironolactone Supplied

Spironolactone is most commonly supplied in tablets of 25 mg.

Structural Characteristics of Spironolactone

Spironolactone is an aldosterone antagonist and diuretic. It has the chemical designation 17- hydroxy-7alpha- mercapto-3-oxo-17alpha-pregn-4-ene-21-carboxylic acid y-lactone acetate.

Spironolactone Warnings (Dehydration, Elevated Potassium, Death)

The misuse of diuretic drugs for physique- or performance-enhancing 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.

Spironolactone Side Effects

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 antiandrogenic properties, as both a weak inhibitor of androgen/receptor binding and testosterone biosynthesis.

Spironolactone Administration

When used medically to treat hypertension, the initial recommended dosage in adults is 50 mg to 100 mg per day in divided doses. It may take two weeks for a maximum response to be achieved. The dosage may be adjusted later depending on the individual needs of the patient.

When used (off-label) by male bodybuilders to increase muscle definition or athletes to reduce weight before a weigh-in, a dosage of 100 mg per day in a single morning application, is most common. This may be continued for 3 to 5 days prior to the event, and will often result in a harder and more defined appearance to the muscles (or substantial reduction in body weight prior to rehydration).

Women are occasionally attracted to spironolactone for its effect as an anti-androgen. It is sometimes used as a safety net at a point when androgen levels have become problematic during a cycle, and is used in an effort to reduce the risk of permanent virilization symptoms. A dosage of 25-75 mg daily for 1 to 2 weeks is often used for this purpose, and may be enough to ward off side effects while androgen levels decline (the steroid regimen terminated). Since spironolactone is more effective at lowering endogenous androgen levels than inhibiting androgen action, it is certainly not to be considered a cure-all remedy for adventurous steroid-using female athletes.

Since this compound is one of the mildest (prescription) diuretic options, it is a common starting point for an early competitor. Once familiar with its effects, many attempt to achieve a stronger level of water loss by mixing spironolactone with a thiazide or furosemide (Lasix). The goal is to provide strong water excretion with less calcium/potassium loss than using the stronger diuretics alone. When mixed with hydrochlorothiazide, for example, the 100 mg spironolactone dosage is often cut in half, and an equal amount of the thiazide is taken. The 50 mg/50 mg combination is reported to noticeably increase water excretion without dramatic side effects. The potassium re-absorption seen with spironolactone should be balanced out with the thiazide so potassium levels will not be as greatly affected. On the other hand, Lasix (furosemide) should make an even stronger addition to spironolactone. In this case, dropping the spironolactone dosage to 50 mg and adding 20 mg oral Lasix is a popular choice, and is often said to provide the water-shedding effect that is roughly equivalent to a 40 mg Lasix tablet. Again, the potassium depleting effect of Lasix may be offset to some degree by the potassium sparing effect of spironolactone, so additional potassium supplements are not likely necessary. Many such combination diuretics are widely available, and appear to be well regarded in clinical circles.

It is important to note that while Lasix and Hydrodiuril appear to be more effective at inducing short-term water loss, they also have increased risks as compared to potassiumsparing diuretics, and should be approached with caution.

Spironolactone Availability

Spironolactone is widely manufactured in both single ingredient and multi-ingredient drug preparations. Low cost and wide scale availability make this a poor financial target for counterfeiting.

Bodybuilders reference

Spironothiazid is a diureteic and an ALDOSTERONE antagonist. This means that it suppresses the water retaining actions of the hormone ALDOSTERONE while lowering water retention by lowering electrolytes (potassium, sodium, and calcium). The advantage of the combination is that the potassium absorption effect by the spironolactone can be mediated by the hydrochlorthiazide. Because of this, some of the potassium loss side effects can be avoided. This is probably a safer choice than LASIX though any diuretic use should be medically monitored. Thiazides also lead to a lower loss of calcium.

Side effects are commonly due to imbalances in electrolytes and fluids. They can include irregular pulse rate, cramps, and light headiness. Since the drug has ANTIANDROGENIC quality (spironolactone), men can experience possible gyno, and impotence due to higher dosage and/or prolonged use. These were noted to not occur due to the brief administration period normally employed. According to available literature, it is best to avoid higher potassium intake during use. Dosages were usually 50-150 mg a day for no more than 3 days. Dosages were divided into 2-3 daily dosages.

Anabolic Steroid Guide reference

Aldactone is a diuretic and belongs to the subgroup of potassium-sparing diuretics. Aldactone is an aldosterone antagonist. It influences the body’s own hormone, aldosterone, which accelerates the excretion of potassium and reduces the excretion of sodium and water. Simplified, aldosterone regulates the endogenous water household. The higher the aldosterone level, the more water is stored in the body. The use of Aldactone results in a significant reduction in the aldosterone level so that an increased excretion of sodium and water occurs while, at the same time, potassium is reabsorbed. This also explains why Aldactone is called a potassium-sparing diuretic since it does not cause a loss of potassium like thiazides and furosemides (lasix) do. Athletes must strictly observe that during the use of Aldactone no additional potassium is taken since this would cause a life-threatening increase in the serum potassium level. Potassium-sparing diuretics have relatively low diuretic effects so that Aldactone can be called a mild diuretic. It is interesting to note that Aldactone is also an antiandrogen since it reduces the androgen level. Female athletes take advantage of this characteristic by using it to minimize the virilization symptoms during steroid treatment or the symptoms after treatment. For this purpose Aldactone is normally taken daily for 10 to 14 days, usually in a dose of 50 mg/day. In men this could cause problems since the relationship of the androgen level to the estrogen level changes in favor of the latter. Thus, common side effects in men include pain in the nipples and breast swelling (gynecomastia).

Bodybuilders use Aldactone almost exclusively during the last week before a competition. Since this causes neither a dramatic nor an immediately noticeable draining effect, it is usually taken over 5-6 days in a dosage of 2 tablets of 50 mg daily. Both male and female athletes take it. The main problems in men consist of gynecomastia and possible impotence. Other side effects can be low blood pressure, muscle spasms, dizziness, gastrointestinal pain, vomiting, irregular pulse rate, and fatigue.

Aldactone by Boehringer Mannheim of Germany is often found on the black market. A package contains 50 dragees of 50 mg each and costs approx. $30 on the black market. There are currently no Aldactone fakes available.

Newbies Research Guide reference

Aldactone is a diuretic and belongs to the subgroup of potassium-sparing diuretics. Aldactone is an aldosterone antagonist. It influences the body’s own hor- mone, aldosterone, which accelerates the excretion of potassium and reduces the excretion of sodium and water Simplified; aldosterone regulates the endoge- nous water household. The higher the aldosterone level, the more water is stored in the body. The use of Aldactone results in a significant reduction in the aldosterone level so that an increased excretion of sodium and water occurs while, at the same time, potassium is reabsorbed. This also explains why Aldactone is called a potassium-sparing diuretic since it does not cause a loss of potassium like thiazides and furosemides.

Athletes must strictly observe that during the use of Aldactone no additional potassium is taken since this would cause a life-threatening increase in the serum potassium level. Potassium sparing diuretics have relatively low diuretic effects so that Aldactone can be called a mild diuretic. It is interesting to note that Aldactone is also an antiandrogen since it reduces the androgen level. Female athletes take advantage of this characteristic by using it to minimize the viriliza- tion symptoms during steroid treatment or the symptoms after treatment. For this purpose Aldactone is normally taken daily for 10 to 14 days, usually in a dose of 50 mg/day. In men this could cause problems since the relationship of the androgen level to the estrogen level changes in favor of the latter Thus, common side effects in men include pain in the nipples and breast swelling (gynecomastia).

Bodybuilders use Aldactone almost exclusively during the last week before a competition. Since this causes neither a dramatic nor an immediately noticeable draining effect, it is usually taken over 5-6 days in a dosage of 2 tablets of 50 mg daily. Aldactone should not be used to expediently drain water at the last minute. Both male and female athletes take it. The side effects of potassium-saving diuretics are relatively low compared to thiazides and furosemides. The main problems in men consist of gynecomastia and possible impotence. Other side effects can be low blood pressure, muscle spasms, dizziness, gastrointestinal pain, vomiting, irregular pulse rate, and fatigue. It is important to note that there is Ii’, significant increase in the serum potassium level (see above).

Aldactone is a prescription drug available in American pharmacies. Aldactone by Hoehringer Mannheim of Germany is often found on be black market. A package contains 50 degrees of 50 mg each and costs approx. $30. On the black market. The Mexican Aldactone by Searle can also frequently be found on the black market. The 25-mg tablets are of light-brown color; indented, and have a SEARLE imprint. The original package contains three strips, each with 10 tab-lets. There are currently no Aldactone fakes available. To order online Aldactone, click here.

This drug is a mild diuretic, which works by inhibiting the effects of aldosterone in the body. As with aldactazide, it is often used for the treatment of high blood pressure. Some pre -contest bodybuilders find it helpful in reducing excess water from abnormally high estrogen in the system. Recently woman have been using the drug as an anti – androgen. This drug has the ability to reverse the effects of androgens in woman. This is often a very useful drug when a woman is taking steroids and begins to suffer masculinisation. In this case woman usually stop using this parades and take Aldactone for one to three weeks; until the androgens turn to an acceptable range. This drug like all diuretics can cause some serious side effects; muscle cramping, heart problems and dizziness to mention a few. Aldactone is usually obtained from a doctor who helps the individual with the proper use. Due to the anti-androgenic effects of this drug, male bodybuilders use it for only a few days at a time. It will lower androgens so significantly in some cases that gynecomastia becomes a problem. A dose of one tablet taken to times daily was most Common.

References

Wlliam Llewellyn (2011) – Anabolics
L. Rea (2002) – Chemical Muscle Enhancement Bodybuilders Desk Reference
Anabolic Steroid Guide
Newbies Research Guide

Your experience with Aldactone — spironolactone