Aldactone

Aldactone (spironolactone) is an aldosterone receptor antagonist that causes the kidneys to remove water and sodium from the body, with reduced losses of potassium. It's in the class of drugs known as 'potassium-sparing' diuretics. Generally, Aldactone is used to reduce edema (swelling) caused by heart, liver or kidney problems, hypertension, and for patients with hyperaldosteronism.

Potassium sparing diuretics are diuretic drugs that do not promote the secretion of potassium into the urine. They are typically used as part of a drug stack or with loop diuretics. For example, in patients with high blood pressure or heart failure. The danger of using this drug incorrectly is raising potassium levels beyond the normal range, which can result in arrhythmias (irregular heartbeat).

Aldactone is listed on the World Health Organization's List of Essential Medicines, which means its considered an important medication needed in a basic health system. Bodybuilders have used this drug as a diuretic several days leading up to competition to help with their goal of a ripped and dry physique.

spironolactone-chemical-structure

Fig 1. Spironolactone Chemical Structure

Table of Contents

History


Spironolactone was introduced clinically in 1959, and it was originally thought it would be phased out; however, it is still widely used. The brand name Aldactone was manufactured by Pfizer and FDA approved in 1985.

Medical uses


Aside from the main uses as a diuretic with heart failure, edema, and hypertension, aldactone is also a progestin and antiandrogen.

Off Label Uses


It is used off label for reducing unwanted androgen levels in the body in the treatment of hyperandrogenism in women (excessive androgen levels), and also as a component of hormone replacement therapy (HRT) for transexual-women. In women, it can help with head hair loss and hirsutism, which is hair on unwanted areas of a females body.

Acne


Another off label use of aldactone is for acne in women, working by inhibiting the activity of sebaceous glands preventing the release of sebum.

How it Works and Availability


Aldactone works by blocking the actions of a hormone in the body called aldosterone. This hormone is produced by glands found above the kidneys called the adrenal glands. Aldosterone acts in the kidneys, where it is involved in controlling the balance of salt and water in the body. This causes the kidney's to eliminate excess water, save potassium, and lower blood pressure.

Aldactone is available in 25, 50 and 100 mg tablets in the United States by prescription only.

aldactone spironolactone pfizer

Fig 2. Aldactone by Pfizer

Half Life


Although the plasma half life of aldactone itself is short (1.3 hours), the half lives of the active metabolites are longer (ranging from 2.8 to 11.2 hours). Aldactone is estimated to be 90% protein bound.

Dosage for medical patients


Depending on the patients medical condition and weight, the dosages will vary and a doctor will decide how best to proceed. With enema and hypertension patients, dosages will typically be 25 to 100mg per day.

Bodybuilding and Dosages


Potassium sparing diuretics are mild and have low diuretic effects; however, the athlete must be careful not to take any potassium while on it because potential life threatening increases in serum potassium levels.

Since it is an antiandrogen as mentioned earlier, aldactone is especially popular among female athletes because of its ability to minimize virilization effects of anabolic steroids. Women will typically take it for up to 2 weeks at 50mgs per day. For men, the opposite desired result can occur, so they may notice sensitive nipples, which are caused by the start of gynecomastia symptoms.

As a mild diuretic, with quite a long activity in the body, both male and female bodybuilders will use aldactone the last week before their competition to lean out and flush water. Typically, 50mg per day split dose will do the job.

Another trick is stacking with a loop diuretic, such as lasix, but this should only be done by those with experience with these compounds. In fact, it is not recommended to use Aldactone unless the bodybuilder is extremely experienced with the ins and outs of manipulating their water. Males can also experience impotence symptoms since it is a progestin and anti-androgen.

Side Effects


If these symptoms begin, medical care may be necessary:

  • Hyperkalemia
  • Altered heart beats
  • Confusion
  • Tremors
  • Decreased or no urine output
  • Shallow breathing
  • Muscle pain or weakness
  • Numbness

Less serious but common side effects include:

  • Skin rash
  • Headache
  • Dizziness
  • GI Symptoms of nausea, vomiting, gas, and stomach pain
  • In males: impotence, and gynecomastia symptoms can occur

Interactions


As stated above, potassium should be avoided during usage. Also, pregnant women should never take Aldactone.

Trade names


  • Aldactone
  • Allopur
  • Deverol
  • Jenaspiron
  • Duraspin
  • Osyrol
  • Spironolactone
  • Spiresis
  • 5pirldon
  • Spirix
  • Spiron
  • Spironolactone
  • Verospiron

Forums


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