Testosterone, the principal circulating androgen, acts directlyin many tissues. To be active in the prostate and skin, testosteronemust be converted to dihydrotestosterone by the enzyme 5-reductase(Figure 1). Most dihydrotestosterone in the prostate arisesfrom testicular precursors, although some arises from adrenalprecursors1. In women, although the relative ovarian and adrenalcontributions to intracellular dihydrotestosterone are unknown,the two organs contribute equally to testosterone production2.Finasteride is one of several inhibitors of 5-reductase thathave recently been developed. These drugs selectively blockdihydrotestosterone production and androgen action in the prostateand skin. . . . [Full Text of this Article]
Congenital 5-Reductase Deficiency
5-Reductase
Development of 5-Reductase Inhibitors
Pharmacologic and Physiologic Characteristics of Finasteride
Effects of Finasteride on Serum and Prostatic Androgen Concentrations
Castration as Compared with 5-Reductase Inhibition
Effects of 5-Reductase Inhibition on Reproductive Organs
Treatment of Prostate Disease with 5-Reductase Inhibitors
Benign Prostatic Hyperplasia
Androgen Suppression in Benign Prostatic Hyperplasia
Treatment of Benign Prostatic Hyperplasia with Finasteride
Side Effects
Finasteride and Prostate Cancer
Dermatologic Uses of 5-Reductase Inhibitors
Hirsutism and Male-Pattern Baldness
Acne
Conclusions
Source Information
From the Department of Medicine, Dalhousie University, Rm. 809, Gerard Hall, 5303 Morris St., Halifax, NS B3J 1B6, Canada, where reprint requests should be addressed to Dr. Rittmaster.
References
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Negri, C., Tosi, F., Dorizzi, R., Fortunato, A., Spiazzi, G. G., Muggeo, M., Castello, R., Moghetti, P.
(2000). Antiandrogen Drugs Lower Serum Prostate-Specific Antigen (PSA) Levels in Hirsute Subjects: Evidence That Serum PSA Is a Marker of Androgen Action in Women. J. Clin. Endocrinol. Metab.
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[Abstract][Full Text]
Moghetti, P., Tosi, F., Tosti, A., Negri, C., Misciali, C., Perrone, F., Caputo, M., Muggeo, M., Castello, R.
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[Abstract][Full Text]
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[Abstract][Full Text]
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341: 964-973
[Full Text]
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338: 612-613
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25: 1051-1058
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Bramson, H. N., Hermann, D., Batchelor, K. W., Lee, F. W., James, M. K., Frye, S. V.
(1997). Unique Preclinical Characteristics of GG745, A Potent Dual Inhibitor of 5AR. J. Pharmacol. Exp. Ther.
282: 1496-1502
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332: 75-79
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Oesterling, J. E.
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332: 99-110
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