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flutamide for hirsutism

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Flutamide for hirsutism

Flutamide is a potent antiandrogen that strongly binds to androgen receptors on cells in hair follicles and anywhere else in the body. Even though it binds to the cell receptors it does not stimulate the cells into any response. When naturally produced androgens bind to the same receptors on hair follicle cells, the cells may respond with increased activity and terminal hair production. The binding of Flutamide to cell androgen receptors blocks the receptors from binding to naturally produced androgens and so stops natural androgens from stimulating hair growth.

Studies that compare flutamide to spironolactone or cyproterone acetate suggest that overall the beneficial effects on reducing hirsutism are similar. Some suggest flutamide is slightly superior and others say it is slightly less superior. Initially flutamide was given to patients at high dose rates of up to 250mg three times a day. However more recent studies indicate that a similar improvement in hirsutism can be obtained with flutamide doses as low as 62.5mg a day. The reduction in dose significantly reduces the risk of side effects.

For a small subgroup of women flutamide and other oral antiandrogens are highly toxic. Between February 1989 and December 1994 the Food and Drug Administration (FDA) received reports of 20 patients who died and 26 who were hospitalized for hepatotoxicity due to flutamide, a rate around 3 per 10,000 flutamide users. Early symptoms of hepatotoxicity include nausea, vomiting, fatigue and jaundice and if such symptoms occur they must be immediately reported to a doctor. Dermatologists generally recommend that serial blood aminotransferase levels should be monitored during the first few months of flutamide treatment. Any adverse aminotransferase level changes suggest that hepatotoxicity is a significant risk and flutamide use should be stopped. For this and other reasons, some dermatologists do not use flutamide to treat hirsutism however, the side effect risk of flutamide is no better or worse than other oral antiandrogens


Flutamide for hirsutism references

  • Ibanez L, Potau N, Marcos MV, de Zegher F. Treatment of hirsutism, hyperandrogenism, oligomenorrhea, dyslipidemia, and hyperinsulinism in nonobese, adolescent girls: effect of flutamide. J Clin Endocrinol Metab. 2000 Sep;85(9):3251-5.
  • Muderris II, Bayram F, Guven M. Treatment of hirsutism with lowest-dose flutamide (62.5 mg/day). Gynecol Endocrinol. 2000 Feb;14(1):38-41.
  • Muderris II, Bayram F, Guven M. A prospective, randomized trial comparing flutamide (250 mg/d) and finasteride (5 mg/d) in the treatment of hirsutism. Fertil Steril. 2000 May;73(5):984-7.
  • Moghetti P, Tosi F, Tosti A, Negri C, Misciali C, Perrone F, Caputo M, Muggeo M, Castello R. Comparison of spironolactone, flutamide, and finasteride efficacy in the treatment of hirsutism: a randomized, double blind, placebo-controlled trial. J Clin Endocrinol Metab. 2000 Jan;85(1):89-94.
  • Paoletti AM, Cagnacci A, Orru M, Ajossa S, Guerriero S, Melis GB. Treatment with flutamide improves hyperinsulinemia in women with idiopathic hirsutism. Fertil Steril. 1999 Sep;72(3):448-53.
  • Yucelten D, Erenus M, Gurbuz O, Durmusoglu F. Recurrence rate of hirsutism after 3 different antiandrogen therapies. J Am Acad Dermatol. 1999 Jul;41(1):64-8.
  • Muderris II, Bayram F. Clinical efficacy of lower dose flutamide 125 mg/day in the treatment of hirsutism. J Endocrinol Invest. 1999 Mar;22(3):165-8.
  • Venturoli S, Marescalchi O, Colombo FM, Macrelli S, Ravaioli B, Bagnoli A, Paradisi R, Flamigni C. A prospective randomized trial comparing low dose flutamide, finasteride, ketoconazole, and cyproterone acetate-estrogen regimens in the treatment of hirsutism. J Clin Endocrinol Metab. 1999 Apr;84(4):1304-10.
  • Moghetti P, Castello R, Zamberlan N, Rossini M, Gatti D, Negri C, Tosi F, Muggeo M, Adami S. Spironolactone, but not flutamide, administration prevents bone loss in hyperandrogenic women treated with gonadotropin-releasing hormone agonist. J Clin Endocrinol Metab. 1999 Apr;84(4):1250-4.
  • De Leo V, Lanzetta D, D'Antona D, la Marca A, Morgante G. Hormonal effects of flutamide in young women with polycystic ovary syndrome. J Clin Endocrinol Metab. 1998 Jan;83(1):99-102.
  • Muderris II, Bayram F, Sahin Y, Kelestimur F. A comparison between two doses of flutamide (250 mg/d and 500 mg/d) in the treatment of hirsutism. Fertil Steril. 1997 Oct;68(4):644-7.
  • Grigoriou O, Papadias C, Konidaris S, Antoniou G, Karakitsos P, Giannikos L. Comparison of flutamide and cyproterone acetate in the treatment of hirsutism: a randomized controlled trial. Gynecol Endocrinol. 1996 Apr;10(2):119-23.
  • Andrade RJ, Lucena MI, Fernandez MC, Suarez F, Montero JL, Fraga E, Hidalgo F. Fulminant liver failure associated with flutamide therapy for hirsutism. Lancet. 1999 Mar 20;353(9157):983.
  • Falsetti L, De Fusco D, Eleftheriou G, Rosina B. Treatment of hirsutism by finasteride and flutamide in women with polycystic ovary syndrome. Gynecol Endocrinol. 1997 Aug;11(4):251-7.
  • Muderris II, Bayram F, Sahin Y, Kelestimur F, Tutus A, Ayata D. The efficacy of 250 mg/day flutamide in the treatment of patients with hirsutism. Fertil Steril. 1996 Aug;66(2):220-2.
  • Wysowski DK, Fourcroy JL. Flutamide hepatotoxicity. J Urol. 1996 Jan;155(1):209-12.
  • Dodin S, Faure N, Cedrin I, Mechain C, Turcot-Lemay L, Guy J, Lemay A. Clinical efficacy and safety of low-dose flutamide alone and combined with an oral contraceptive for the treatment of idiopathic hirsutism. Clin Endocrinol (Oxf). 1995 Nov;43(5):575-82.
  • Pucci E, Genazzani AD, Monzani F, Lippi F, Angelini F, Gargani M, Barletta D, Luisi M, Genazzani AR. Prolonged treatment of hirsutism with flutamide alone in patients affected by polycystic ovary syndrome. Gynecol Endocrinol. 1995 Sep;9(3):221-8.
  • Erenus M. Efficacy of flutamide versus spironolactone. Fertil Steril. 1995 Mar;63(3):680.
  • Ciotta L, Cianci A, Marletta E, Pisana L, Agliano A, Palumbo G. Treatment of hirsutism with flutamide and a low-dosage oral contraceptive in polycystic ovarian disease patients. Fertil Steril. 1994 Dec;62(6):1129-35.
  • Wysowski DK, Fourcroy JL. Safety of flutamide? Fertil Steril. 1994 Nov;62(5):1089-90.
  • Cesur V, Kamel N, Uysal AR, Erdogan G, Baskal N. The use of antiandrogen flutamide in the treatment of hirsutism. Endocr J. 1994 Oct;41(5):573-7.
  • Howe RS, Chow RP, Stevens CL. Use of flutamide for self-induced androgen excess. A case report. J Reprod Med. 1994 Oct;39(10):838-40.
  • Marugo M, Bernasconi D, Meozzi M, Del Monte P, Zino V, Primarolo P, Badaracco B. The use of flutamide in the management of hirsutism. J Endocrinol Invest. 1994 Mar;17(3):195-9.
  • Cusan L, Dupont A, Gomez JL, Tremblay RR, Labrie F. Comparison of flutamide and spironolactone in the treatment of hirsutism: a randomized controlled trial. Fertil Steril. 1994 Feb;61(2):281-7.
  • Wallace C, Lalor EA, Chik CL. Hepatotoxicity complicating flutamide treatment of hirsutism. Ann Intern Med. 1993 Dec 1;119(11):1150.
  • Grimaldi F, Proto G, Bertolissi F. Flutamide--effects and side effects. Fertil Steril. 1993 Apr;59(4):937.

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