Spironolactone is an aldosterone antagonist that has been widely used for treating patients with hypertension. The drug interferes with the aldosterone receptor which results in lower blood pressure. Aldosterone is a steroid hormone that plays a role in regulating blood pressure. It has also been shown in research that spironolactone blocks dihydrotestosterone (DHT) receptors making it an antiandrogen. Since DHT stimulates sebum production, it has been a target for reducing acne in patients with hormonal acne. Commercially available spironolactone is made in tablet form however a spironolactone acne gel can be made by a compounding pharmacy with a prescription.
What is Spironolactone?
Spironolactone was first approved by the FDA in the 1960s and has mostly been used for treating hypertension. The drug was first investigated as an acne treatment in 1984 and many subsequent studies demonstrated its effectiveness for this indication. While it is not FDA approved for treating acne, it is frequently prescribed off-label for this purpose – especially for women suffering from polycystic ovarian syndrome (PCOS). Spironolactone is an antagonist of the androgen receptor, which means it inhibits the action of testosterone and dihydrotestosterone in the body. The commercially available version of the drug is made in 25mg, 50mg, and 100mg tablets.
Because of spironolactone’s feminizing effects in men like gynecomastia, among other side effects, it is recommended only for use in women. A topical version of spironolactone is not likely to have a significant systemic effect (if any) to produce these side effects. In fact, studies in men with topical spironolactone have shown that there is only local affect in the skin and no affect on hormones. However in general dermatologists avoid prescribing this medication for men.
How Does Spironolactone Work for Treating Acne?
Multiple skin conditions are related to the production of androgens like DHT. These include acne, oily skin, and hirsutism (excessive facial and body hair in women). Spironolactone inhibits androgens at multiple physiological levels to reduce the development of acne. Acne is often associated with puberty in both men and women because of the surges of androgens that occur. These types of hormonal fluctuations also often present in women with changes during the menstrual cycle or during pregnancy.
Sebum production is one of the main contributing factors to the development of acne. Women with high androgenic states will also have increased sebum production due to an increase in circulating androgens. The development or worsening of acne is often associated with androgen excess. Inhibiting sebaceous gland function by inhibiting androgens can lead to a clearance of acne. The consistent use of a medication like spironolactone can help achieve this. It should also be noted that even in women without excess androgens, this medication may be effective as it works through multiple mechanisms.
This is a list that was published in an article in the Journal of Clinical and Aesthetic Dermatology. This list was made specifically for oral spironolactone, however each of these cases could also apply to topical use for treating acne in women.
Cases where spironolactone may be effective:
- Women with acne flares that cycle with menstruation
- Women on oral contraceptives or wanting to be on oral contraceptives who exhibit moderate-to-severe acne vulgaris (AV), especially with a “hormonal pattern” clinically (see text)
- Women not responding to conventional therapy and not wanting to use oral isotretinoin or who are not candidates for oral isotretinoin
- Women with late-onset AV, or persistent-recurrent AV past the teenage years, even in the absence of clinical signs of hyperandrogenism and with normal results of hormonal level testing
- Women with late-onset AV (acne tarda) or sudden onset of AV
- Clinical signs of hyperandrogenism, such as hirsutism, androgenic alopecia, and/or increased sebum production with AV
Note that acne vulgaris is just a medical term for acne designating that it is the common form of acne that involves the formation of comedones, papules, pustules, nodules, and/or cysts as a result of obstruction and inflammation of pilosebaceous units. This differentiates it from less common types of acne that may be caused by an underlying condition or be more severe.
For treating acne, spironolactone generally takes a few months to be effective. Treatment should not be discontinued before then just because there are no results yet. The topical form of the drug might take longer to work than the oral form.
Spironolactone Gel
In studies of young adults, spironolactone gel has been shown to reduce sebum secretion rates. In one study that examined sebum secretion rates, it was shown that the effects of the gel at reducing sebum were localized to the application area. The control side of the face where the gel was not applied did not show any effects from the drug. This may provide further evidence that the gel’s effects are localized and that minimal systemic effects are expected. It is possible that while spironolactone gel blocks DHT receptors, it does not decrease circulating androgens like oral spironolactone. This may mean that the gel will take longer to start working than the oral version, but could also have fewer side effects.
Because the effects of the topical version are localized to the sebaceous glands, researchers have speculated that it may be more effective for patients with high sebum secretion rates. The rates of success are generally high:
- “Treatment proved remarkably effective in that it brought about complete regression of acne in 30%, improvement in 65% of the patients.” (La Clinica Terapeutica)
- “These findings showed the effectiveness of topical spironolactone in decreasing the TLC [total acne lesions].” (The Journal of Dermatological Treatment)
Side Effects of Spironolactone for Acne
Most of the side effects that result from taking oral spironolactone are expected to be less or non-existent with topical use. Usually side effects with topical use will include only erythema (redness) and stinging in the application area, although many patients will not have any side effects.
Women who are able to have children must be on birth control while using spironolactone because of potential feminization of the male fetus. There are numerous benefits to taking birth control while using spironolactone besides this, however. Birth control can help reduce menstrual-related side effects associated with oral use of the drug and reduce the necessary oral dose. These side effects may not exist at all with topical use or may at least be significantly reduced.
In an 8-year follow-up study of patients who were prescribed oral spironolactone for acne, no cases of serious illness were attributed to use of the medication although many women did experience some side effects. The article states: “The long-term use of spironolactone in the treatment of acne in women appears to be safe. Side effects, however, are common, although not usually a cause for stopping the drug.”
As already mentioned, spironolactone topical gel has been shown to only affect the area in which it is applied. Even in studies where the gel was applied to half the face, the side that did not receive medication had no changes. Significant hormonal changes throughout the body also have not been associated with topical use. The drug is therefore expected to migrate only minimally from the application site.
Spironolactone – Treatment Options for Acne
Currently spironolactone gel is not commercially available in the U.S. However a spironolactone 5% gel can be made by a compounding pharmacy with a prescription. A compounding pharmacy is able to make drug products that are not commercially available using bulk pharmaceutical ingredients. Each prescription is made for the individual patient and can be customized to their needs. While acne is often associated only with teenagers, it can affect people of all ages and frequently affects adult women. While there are numerous treatments available for acne many either do not work or have unwanted effects on the skin or body. Spironolactone topical gel is one option healthcare providers have to treat their acne patients – especially for adult women with persistent acne issues.