SPIRONOLACTONE - ALDACTONE

Background: Spironolactone does many things to our bodies. First, it is a "potassium sparing" diuretic (water pill) commonly used to remove surplus fluid from the body's bloodstream or tissues. It also acts as an aldosterone inhibitor (prevents salt retention) and can be used to treat high blood pressure, hypertension and in some cases advanced heart failure. As for its indications in hair, Spironolactone is known to be a well tolerated and effective antiandrogen. It is sometimes used to treat female pattern baldness and excessive facial hair (hirsutism) in women and occasionally men use it as an antiandrogen under close supervision by their doctors.  Hirsutism is most often caused by increased production of male sex hormones also known as androgens. It is also affected by increased sensitivity to androgens in the hair follicles, and the secretory glands around the hair follicles, called sebaceous glands. 

Recently there are studies (Berardesca E, Gabba P, Ucci G, Borroni G, Rabbiosi G.) which suggest that topical spironolactone can act as an antiandrogen in human sebaceous glands, competing with DHT receptors and producing a decrease of labeled DHT. This means that topical spironolactone may slow down or stop hairloss by working as a DHT receptors blocker.  Despite the fact that most doctors caution male patients against using Spironolactone orally for hairloss for fear of adverse reactions such as loss in sex drive, impotence, breast development., some have been experimenting with low dose Spironolactone with some success. However, we do not have hard core data or studies to substantiate that.  

Brand Name: Aldactone. Comes in 25mg, 50 mg, 100 mg. Generic is now available on the market.  

Side effects: Some of the possible side effects associated with spironolactone are:

• Nausea
• Headache
• Low blood pressure
• Constipation / diarrhea
• Dizziness
• Shortness of breath
• Rashes
• Vomiting
• Does dependent effects in females
• Breast pain or tenderness, gynecomastia (in men)

Do not use salt substitutes or low-sodium milk products that contain potassium while taking spironolactone. These products could cause high levels of potassium in your blood.

Topical Spironolactone:  A study conducted by Berardesca E. et al concluded that 5% topical spironolactone cream acts as an antiandrogen in human sebaceous glands, competing with DHT receptors and producing a decrease of labelled DHT. The inhibition of DHT receptors by spironolactone was found to be related to the decrease of tritiated DHT granules in the sebaceous glands of the treated site.... more info

Spironolactone is insoluble in water but easily soluble in alcohol. Since topical minoxidil is an alcohol based product, some forum members have simply added crushed Spironolactone tablets directly into topical minoxidil to make their own Spironolactone protocol. However, we cannot vouch if this is the proper way to make topical spironolactone. Click below for more discussions about how to make your own topical spironolactone lotion.
 
Discussion # 1
Discussion # 2

Oral Spironolactone:  Doctors frequently prescribe Spironolactone to treat acne, pattern baldness and hirsutism in women. In a study by Lumachi F, Rondinone R. on the use of cyproterone acetate, finasteride, and spironolactone to treat idiopathic hirsutism in women, it was concluded that the short-term results of treatment with cyproterone acetate, finasteride, and spironolactone are similar, but spironolactone is effective for a longer time...more info. Men who wish to use Spironolactone orally should do so ONLY under close supervision of their doctors. Depending on the individual, the daily dose can vary from 25 mg to 200 mg. It is recommended that Spironolactone be taken together with food. The effect of food on spironolactone absorption (two 100-mg Aldactone tablets) was assessed in a single dose study of 9 healthy, drug-free volunteers. Food increased the bioavailability of unmetabolized spironolactone by almost 100%.

Levels and Metabolism:  Rapidly metabolized to canrenone, an active metabolite with a half-life of 10-35 hours. Highly protein bound. Half-life with chronic use is 13-24 hours. 

Vendor Dr. Klein

Other - earlier coverage or discussion on spironolactone
 

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