It's been firmly established that alopecia androgenetica, more commonly known as male pattern baldness or just pattern baldness, is initiated by dihydrotestosterone (DHT) attaching to the receptor sites on the hair follicles []. Genetically, only the follicles on the top of the head are encoded with the receptor sites[5.6.24.], which explains why hair along the side of the head and in the back of the head is not lost with age. The attached DHT on the receptor site is perceived as a foreign body and the immune system begins to destroy the hair follicle, shortening the growth phase and causing the hair shaft to become progressively finer in texture[6]. In extreme cases, only a vellus hair remains. The good news is that the follicles have the inherent capacity to mature to their former size.

Encouraged with the success of finasteride to reduce the amount of DHT in the scalp of patients with male pattern baldness (MPB), doctors and scientific researchers took another look at existing medications that are known to act as anti-androgens.

However, there have to be stringent criteria for an anti-androgen that can be used to combat or even reverse pattern alopecia. The ideal anti-androgen should have the following properties:



That’s a tall order. Surprisingly enough, there is such a medication:

spironolactone. And it’s not a new medication [7.8.]. For over thirty years spironolactone has been used as an antihypertensive and a diuretic. More recently, it has been used to treat hirsutism in women [9.10.]. Using spironolactone to treat hirsutism may sound contradictory, but body hair (e.g. chest, face, axilla, pubis, etc.) is promoted by testosterone and since spironolactone is a potent anti-androgen, it’s successfully used to eliminate unwanted hair on the body[11].

On the top of the head, where the hair is adversely affected by DHT, spironolactone has just the opposite effect[]. Spironolactone exhibits anti-androgenic effects in both males and females[14.15.]. Taken orally, it is such a potent anti-androgen that, although it is an effective anti-hypertensive drug, it is rarely used to treat men with hypertension because of its feminizing properties, including painful gynecomastia[16.17.].

However, applied topically, spironolactone does not have any systemic side effects[]. Clinical evaluations of topical applications of spironolactone concluded that "as far as the topical use is concerned spironolactone seems to be highly effective with absence of systemic effects"[19]. Physicians have been treating patients for MPB for well over twelve years and there have not been any reports of side effects. In my own experience with a combination topical solution of 5% minoxidil and 2% spironolactone, the results are at least as good as 5% minoxidil topically and finasteride 1 mg orally with the decided advantage of zero side effects.

Among its other properties as an anti-androgen, spironolactone is a potent competitive inhibitor of DHT at its receptor sites[21]. Therefore, spironolactone effectively prevents DHT from attaching to the receptor sites on the hair follicles[22]. As a result, the follicles no longer atrophy and can mature again to their normal size. And it does so without decreasing the circulating levels of DHT in the body. By comparison, finasteride inhibits the formation of DHT, causing troublesome side effects in a small percentage of patients.

Multiple studies in various medical centers document that spironolactone is effective when applied topically[22]. In studying the anti-androgenic effects of topical spironolactone at the Department of Dermatology at New York University School of Medicine, researchers established that spironolactone concentrations of 0.01% to 5% produced a dose responsive decrease[23]. We chose to use the combination of 5% minoxidil and 2% spironolactone in an alcohol-based solution. The effect of the medications is more than synergistic. They’re additive. Whereas neither medication alone is effective for the majority of patients, the success of the combination has been experimentally proven. Our own success rate with this formulation has been approximately 70-75%.

Still, there are some minor drawbacks with the use of topical spironolactone. The spironolactone has an inherent disagreeable odor and spironolactone is not particularly stable in solution form. When spironolactone is mixed in the same solution as minoxidil, the resulting solution becomes extremely malodorous. Once again we engaged the services of a distinguished pharmacologist and an analytical biochemist to produce a formula that will not compromise the bioavailability of the 5% minoxidil nor the 2% spironolactone. At the same time we want to mask the unpleasant odor of the spironolactone and stabilize the compounds in solution. We haven’t solved all the problems yet, but we’re making good progress.






  1. Hamilton JB: Male hormone stimulation is prerequisite and an incitant in common baldness. Am J Anat 71:451-480, 1942
  2. Rattner H: Ordinary baldness. Arch Dermatol Syph 44:201-213, 1941 Rook A, Dawber R: Diseases of the Hair and Scalp. Oxford, Blackwell Scientific Publications, 1982
  3. Baden HP: Diseases of the Hair and Nails. Chicago, Year Book Medical Publishers, 1987
  4. Lattanand A, Johnson WC: Male pattern alopecia: A histopathologic and histochemical study. J Cutan Pathol 2:58-70, 1975
  5. Blauer M, Vaalasti A, Pauli SL, Ylikomi T, Joensuu T, Tuohimaa P: Location of androgen receptor in human skin. J Invest Dermatol 97:264 268, 1991
  6. Menard RH, Stripp B, Gillette JR: Spironolactone and testicular
  7. cytochrome P-450: Decreased testosterone formation in several species and changes in hepatic drug metabolism. Endocrinology 1974;94:1628-1636
  8. Menard RH, Martin HF, Stripp B, et al: Spironolactone and cytochrome P-450: Impairment of steroid hydroxylation in the adrenal cortex. Life Sci 1975;15:1639-1648
  9. Schapiro G and Evron S. A novel use of Spironolactone:treatment of hirsutism. J Clin Endocrinol Metab. 1988;51:429-432
  10. Cumming D, Yang J, Rebar R, Yen S.: Treatment of hirsutism with Spironolactone. JAMA. 1982;247:1295-8.
  11. Boiselle A, Tremblay RR: Clinical usefulness of spironolactone in the treatment of acne and hirsutism, abstracted. Clin Res 1978;26:840A
  12. Yamamoto A, Ito M. Topical spironolactone reduces sebum secretion rates in young adults. J Dermatol, 1996 Apr,23:4,243-6
  13. Berardesca E, Gabba P, Ucci G, Borroni G, Rabbiosi G: Topical spironolactone inhibits dihydrotestosterone receptors in human sebaceous glands: an autoradiographic study in subjects with acne vulgaris. Int J Tissue React 10:115-119, 1988
  14. Burke BM, Cunliffe WJ: Oral spironolactone therapy for female patients with acne, hirsutism or androgenetic alopecia. Br J Dermatol 112:124-125, 1985
  15. Stripp B, Taylor AA, Bartter FC, et al: Effect of spironolactone on sex hormones in man. J Clin Endocrinol Metabol 1975;41:777-781
  16. Mann NM: Gynecomastia during therapy with spironolactone. JAMA 190:160-162,1963
  17. Rose LI, Underwood RH, Newmark SR, Kisch ES, Williams GH: Pathophysiology of spironolactone-induced gynecomastia. Ann Int Med 87:398-403, 1977
  18. Corval P, Michaued A, Menard J, et al: Antiandrogenic effect ofspironolactones: Mechanism of action. Endocrinology 1975;97:52-8
  19. Messina M, Manieri C, Musso MC, Pastorino R.: Oral and topical spironolactone therapies in skin androgenization. Panminerva Med, 1990 Apr-Jun,32:2,49-55
  20. Wendt A, Hasan SH, Heinz I, Tauber U: Systemic effects of local antiandrogen therapy. Arch Dermatol Res 273:171,1982
  21. Price VH: Testosterone metabolism in the skin: A review of its function in androgenetic alopecia, acne vulgaris, and idiopathic hirsutism including recent studies with antiandrogens. Arch Dermatol 1975;111:1496-1502
  22. Stoughton RB: Penetration of drugs through the skin. Dermatologica 152 (suppl): 27-36, 1976
  23. Matias JR, Malloy V, Orentreich N: Synergistic antiandrogenic effects of topical combinations of 5 alpha reductase and androgen receptor inhibitors in the hamster sebaceous glands. J Invest Dermatol 91:429-433, 1988
  24. Takayasu S, Wakimoto H, Itami S, Sano S: Activity of testosterone 5 alpha-reductase in various tissues of human skin. J Invest Dermatol 74:187-191,1980
  25. Sawaya ME, Hoenig LS, Hsia SL: Increased androgen binding capacity in sebaceous glands in scalp of male pattern baldness. J Invest Dermatol 92:91-95, 1988, Martin HF, Stripp B, et al: SpiroH

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