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5α-Reductase inhibitors (5-ARIs), also known as dihydrotestosterone (DHT) blockers, are a class of medications with antiandrogenic effects which are used primarily in the treatment of enlarged prostate and scalp hair loss. They are also sometimes used to treat excess hair growth in women and as a component of hormone therapy for transgender ...
This is a list of 5α-reductase inhibitors (5α-RIs), drugs which inhibit one or more isoforms of the enzyme 5α-reductase.This enzyme is responsible for the conversion of the androgen hormone testosterone into the more potent dihydrotestosterone (DHT) and is essential for the production of neurosteroids like allopregnanolone, tetrahydrodeoxycorticosterone (THDOC), and 3α-androstanediol from ...
The first compounds developed were selective 5-alpha reductase type 1 inhibitors, but the most potent one inhibits both type 1 and 2. The fluorine atom is an important part of the structure. [8] Benzo(f)quinolonone are also tricyclic compounds, but derivatives of the 4-azasteroid structure.
5α-Reductase type 1 inactivated male mice have reduced bone mass and forelimb muscle grip strength, which has been proposed to be due to lack of 5α-reductase type 1 expression in bone and muscle. [29] In 5 alpha reductase type 2 deficient males, the type 1 isoenzyme is thought to be responsible for their virilization at puberty. [6]
A small risk of gynecomastia has been associated with 5α-reductase inhibitors (1.2–3.5%). [36] [41] Based on reports of 5α-reductase type 2 deficiency in males and the effectiveness of 5α-reductase inhibitors for hirsutism in women, reduced body and/or facial hair growth is a likely potential side effect of these drugs in men.
However, 5α-reductase inhibitors have been found to increase the risk of developing certain rare but aggressive forms of prostate cancer (27% risk increase), although not all studies have observed this. [35] No impact of 5-α-reductase inhibitor on survival has been found in people with prostate cancer. [35]
PDE also likely improves symptoms when used with 5-alpha reductase inhibitors. Several phosphodiesterase-5 inhibitors are also effective but may require multiple doses daily to maintain adequate urine flow. [91] [92] Tadalafil, a phosphodiesterase-5 inhibitor, was considered then rejected by NICE in the UK for the treatment of symptoms ...
The enzyme is active at acidic pH and is sensitive to the 4-azasteroid inhibitor finasteride. Deficiencies in 5αR2 activity of the can lead to a condition known as 5α-reductase 2 deficiency , which is a cause of 46,XY DSD that presents as atypical male genitalia.