Article

An overview on 5alpha-reductase inhibitors.

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.
Steroids (impact factor: 2.83). 10/2009; 75(2):109-53. DOI:10.1016/j.steroids.2009.10.005 pp.109-53
Source: PubMed

ABSTRACT Benign prostatic hyperplasia (BPH) is the noncancerous proliferation of the prostate gland associated with benign prostatic obstruction and lower urinary tract symptoms (LUTS) such as frequency, hesitancy, urgency, etc. Its prevalence increases with age affecting around 70% by the age of 70 years. High activity of 5alpha-reductase enzyme in humans results in excessive dihydrotestosterone levels in peripheral tissues and hence suppression of androgen action by 5alpha-reductase inhibitors is a logical treatment for BPH as they inhibit the conversion of testosterone to dihydrotestosterone. Finasteride (13) was the first steroidal 5alpha-reductase inhibitor approved by U.S. Food and Drug Administration (USFDA). In human it decreases the prostatic DHT level by 70-90% and reduces the prostatic size. Dutasteride (27) another related analogue has been approved in 2002. Unlike Finasteride, Dutasteride is a competitive inhibitor of both 5alpha-reductase type I and type II isozymes, reduced DHT levels >90% following 1 year of oral administration. A number of classes of non-steroidal inhibitors of 5alpha-reductase have also been synthesized generally by removing one or more rings from the azasteroidal structure or by an early non-steroidal lead (ONO-3805) (261). In this review all categories of inhibitors of 5alpha-reductase have been covered.

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Keywords

1 year
 
5alpha-reductase enzyme
 
5alpha-reductase type
 
androgen action
 
azasteroidal structure
 
Benign prostatic hyperplasia
 
benign prostatic obstruction
 
Drug Administration
 
excessive dihydrotestosterone levels
 
first steroidal 5alpha-reductase inhibitor
 
humans results
 
lower urinary tract symptoms
 
non-steroidal inhibitors
 
non-steroidal lead
 
noncancerous proliferation
 
oral administration
 
peripheral tissues
 
prostatic DHT level
 
prostatic size
 
type II isozymes