Selectivity of finasteride as an in vivo inhibitor of 5 alpha-reductase isozyme enzymatic activity in the human prostate

Autor: Jack A. Schalken, Mark Feneley, Paul N. Span, Anthony G.H. Smals, Roger Kirby, M. Voller, Fred Sweep
Rok vydání: 1999
Předmět:
Zdroj: Journal of Urology, 161, pp. 332-337
Journal of Urology, 161, 332-337
ISSN: 0022-5347
Popis: The type II 5 alpha-reductase inhibitor finasteride is used in the treatment of benign prostatic hyperplasia (BPH), reducing local production of the growth promoting androgen dihydrotestosterone (DHT). The effect of prolonged treatment with this time-dependent irreversible inhibitor on the recently described prostatic type I 5 alpha-reductase, however, is not clear. Therefore, we assessed the effects of 5 mg. finasteride per day for 6 months on prostatic 5 alpha-reductase isozymes, and prostatic tissue composition and androgen content of patients suffering from BPH. In prostatic tissue from these patients, the type II enzymatic activity is inhibited 100-fold compared with tissues obtained from placebo treated patients. The type II immunoreactivity is up regulated 2-fold. The type I isozyme is inhibited 3-fold and potentially still contributes to DHT production. In conclusion, finasteride is a selective type II inhibitor in vivo. Further research is warranted to assess the possibly distinct roles o...
Databáze: OpenAIRE