TOPICAL SPIRONOLACTONE IN THE TREATMENT OF ALOPECIA
AND INSTRUCTIONS FOR USE

ODORLESS 5% SPIRONOLACTONE LOTION NOW AVAILABLE

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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 [1.2.3.4.]. 

Genetically, only the follicles on the top of the scalp are encoded with the receptor sites [5.6.24.], which explains why hair follicles along the side of the head and in the back of the head do not atrophy. The attached DHT on the receptor sites 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 microscopic vellus hair remains. The good news is that these follicles have the inherent capacity to mature to their former size and thickness.

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.

 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:

(1) It must have potent anti-androgen activity; (2) It should selectively prevent or successfully compete with DHT without changing testosterone levels; (3) It should be effective topically, so it can be conveniently applied with minoxidil solutions or lotions and (4), It should be easily absorbed into the skin, but should have no systemic effects where it is not applied.

 That’s a tall order. Surprisingly, there is such a medication: spironolactone. And it’s not a new medication [7.8.]. For over thirty years spironolactone has been used for its 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 which can include painful gynecomastia [16.17.].

 Applied topically, however, spironolactone does not have systemic side effects [12.18.19.20.]. Clinical evaluators of topical applications of spironolactone concluded, "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 fifteen years and there have not been any reports of systemic side effects. In my own research, the use of topical 5% spironolactone along with Xandrox 5% solution yielded improved results as compared to the use of Xandrox 5% alone.  Likewise, the combination of 5% spironolactone with Regrowth's 5% minoxidil yielded improved results as compared to the use of 5% minoxidil used with daily 1 mg doses of finasteride (with the added 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 many 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]. When both topical 5% spironolactone and topical 5% minoxidil are used daily in the treatment of MPB, the effects of the medications are synergistic.  Whereas neither medication alone is particularly 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 75-80%.

Our extensive R&D have finally produced a spironolactone lotion which almost totally eliminates the inherent disagreeable   smell of spironolactone.  In addition to the 5% concentration of spironolactone in the lotion, there are small (1 to 3 mm) vesicular pockets of pure, unsuspended micronized spironolactone powder.  This should be spread onto the scalp with one's fingertips to optimize the effects of the application. 

 Do not combine medications containing spironolactone and minoxidil in the same container.  The medications slowly react with each other, resulting in a compromise of their pharmacological activities.  However, since it requires many hours for spironolactone and minoxidil to chemically react with each other, they can be consecutively applied to the scalp without compromising each other.

Regrowth's 5% Spironolactone Lotion has a shelf life of more than 18 months when kept at normal room temperatures.

Bibliography

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

 3. Rook A, Dawber R: Diseases of the Hair and Scalp. Oxford, Blackwell Scientific Publications, 1982

 4. Baden HP: Diseases of the Hair and Nails. Chicago, Year Book Medical Publishers, 1987

 5. Lattanand A, Johnson WC: Male pattern alopecia: A histopathologic and histochemical study. J Cutan Pathol 2:58-70, 1975

 6. 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

 7. Menard RH, Stripp B, Gillette JR: Spironolactone and testicular 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 of spironolactones: 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. anminerva 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

INSTRUCTIONS FOR USE:

     Using your fingertips, apply a small amount of the 5% Spironolactone Lotion to those areas of the scalp in which the hair is thinning/receding.

      For optimal results, the 5% Spironolactone Lotion should be applied two times/day at least eight hours apart. 

     If you are going to apply the 5% Spironolactone only once/day, make the application at night.

     Use only the amount necessary to create a thin film of 5% Spironolactone Lotion in the affected area(s).

      If there are any unsuspended, concentrated vesicles of micronized spironolactone in the lotion, rub these into the scalp with gentle pressure.

      When 5% Spironolactone Lotion is used with Regrowth 5% topical minoxidil or Xandrox 5% (5% minoxidil / 5% azelaic acid), apply the minoxidil solution first.  Allow several minutes for it to partially dry.  Then apply the 5% Spironolactone Lotion on top of the minoxidil solution.  The lotion will act as an occlusive dressing and enhance the absorption of both medications.

.      If a rash appears ( the incidence is slightly less than 1% ), discontinue the use of topical spironolactone.

NOTE: Until a more complete list of Q & A's can be completed by Dr. Lee, please click on the following URL: http://www.hairlosshelp.com/html/drleespiroreview.cfm

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