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Introduction 5α-Reductase inhibitors (5α-RIs) therapy with finasteride or dutasteride and α1-adrenergic receptor blockers such as tamsulosin are widely used for treatment of lower urinary tract symptoms (LUTS) due to benign prostatic hyperplasia (BPH) [1, 2]. 5α-RIs therapy with finasteride is also widely used for treatment of male pattern hair loss (MPHL), commonly known as androgenetic alopecia (AGA) [3, 4]. However, one of the main concerns with 5α-RIs therapy is the serious adverse effects on sexual function [1, 5–16]. Considerable controversy exists

Horm Mol Biol Clin Invest 2010;1(2):95–102 2009 by Walter de Gruyter • Berlin • New York. DOI 10.1515/HMBCI.2010.010 2010/16 Article in press - uncorrected proof The influence of low dose finasteride, a type II 5a-reductase inhibitor, on circulating neuroactive steroids Michaela Dušková*, Martin Hill and Luboslav Stárka Institute of Endocrinology, CZ 11694 Prague 1, Czech Republic Abstract Background: Finasteride is a 5a-reductase inhibitor that has received clinical approval for the treatment of human benign prostatic hyperplasia and androgenetic alopecia

: 10.1365/s10337-008-0613-7. M. L. Constanzer, C. M. Chavez and B. K. Matuszewski, Picogram determination of finasteride in human plasma and semen by high-performance liquid chromatography with atmospheric-pressure chemical-ionization tandem mass spectrometry, J. Chromatogr.   658 (1994) 281-287; DOI: 10.1016/0378-4347(94)00250-9. F. Q. Guo, L. F. Huang, K. P. Wong, Y. H. Dai, Y. W. Li, Y. Z. Liang, K. L. Huang, K. J. Zhong and M. J. Wu, A rapid, simple, specific liquid chromatographic-electrospray mass spectrometry method for the determination of finasteride in

Horm Mol Biol Clin Invest 2010;2(3):293–299 2010 by Walter de Gruyter • Berlin • New York. DOI 10.1515/HMBCI.2010.035 2010/009 Article in press - uncorrected proof Human type 3 5a-reductase is expressed in peripheral tissues at higher levels than types 1 and 2 and its activity is potently inhibited by finasteride and dutasteride Kazutoshi Yamana, Fernand Labrie and Van Luu-The* Research Center in Molecular Endocrinology, Oncology and Human Genomics (CREMOGH) and Department of Molecular Medicine, Faculty of Medicine, Laval University and the Laval University

FACILE WATER MEDIATED SYNTHESIS OF FINASTERIDE FORM-I, AN AZAANDROSTANE STEROID Divvela V. N. Srinivasa Rao3, Ganala Naga Trinadhachari3, Racha Lenin3 Koilpillai Joseph Prabahar3, Andra Naidub and Ramesh Dandala*3 a Chemical Research Department, APL Research Center, Hyderabad-500 072, India b Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-500 072, India E-mail: rdandala@aurobindo.com Abstract: A simple and efficient procedure for the selective synthesis of finasteride Form-I from bis-finasteride tetrahydrofuran monohydrate solvate in

by daily subcutaneous injection of testosterone for 10 days. Rats of the test group were administered 100 mg/kg of petroleum ether extract of Citrullus colocynthis fruit along with testosterone. Graded doses i.e, 1, 2.5, and 5 mg/kg dose of isolated steroidal fraction were also tested in three groups of rats. Finasteride was used as positive control. Treatment with C. colocynthis extract reduced prostatic weights of the treated animals considerably. The isolated steroidal fraction also diminished the weight of prostate in dose dependent fashion. Histological

suggests that the new type 3 5a-reductase is responsible for 5a-reductase activity in DU-145 cells. Steroid profile analysis shows that in the absence of inhibitor 5a-androstanedione is first pro- duced, followed by the production of androsterone and dihy- drotestosterone. The concentration of testosterone was not detectable. In the presence of Finasteride, an inhibitor of 5a- reductase, there was no transformation of 4-androstenedione and also there was no production of testosterone. The present data clearly indicate that the biosynthesis of dihydrotestos

in prostate cancer incidence of about 25% among men taking finasteride compared to men taking placebo. However, the effect of finasteride on the natural history of prostate cancer is not well understood. We adapted a convolution model developed by Pinsky (2001) to characterize the natural history of prostate cancer in the presence and absence of finasteride. The model was applied to data from 10,995 men in PCPT who had disease status determined by interim diagnosis of prostate cancer or end-of-study biopsy. Prostate cancer cases were either screen-detected by

involving conjugation and excretion ( Figure 1 ). Figure 1 Role of 5α- and 5β-reductases in the metabolism and clearance of glucocorticoids. Cortisol is metabolized by 11β-hydroxy-steroid dehydrogenase type 2 to cortisone and the latter can be converted by 11β-hydroxy-steroid dehydrogenase type 1 to cortisol. Cortisol metabolism via ring A reduction takes place by 5α- and 5β-reductases. Inhibition of 5α-reductases by finasteride or dutasteride reduces the metabolism and clearance rate of cortisol and results in increased levels of active cortisol. The principal urinary

U, Kośmider A, Piwowarski J. Oenothein B’s contribution to the anti-inflammatory and antioxidant activity of Epilobium sp. Phytomedicine 2011; 18(7):557-60. 30. Hiermann A, Bucar F. Studies of Epilobium angustifolium extracts on growth of accessory sexual organs in rats. J Ethnopharmacol 1997; 55(3):179-83. 31. Azzolina B, Ellsworth K, Andersson S, Geissler W, Bull HG. Inhibition of rat alpha-reductases by finasteride: evidence for isozyme differences in the mechanism of inhibition. J Steroid Biochem Mol Biol1997; 61:55-64. 32. Tindall DJ, Rittmaster RS. The