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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 ...
Dutasteride (Avodart) was the second steroidal 5α-reductase approved after finasteride. It is a competitive inhibitor of all three 5α-reductase isoenzymes [4] and it inhibits types 1 and 2 better than finasteride, leading to it causing further reduction in DHT, with >90% reduced DHT levels following 1 year of oral administration. [1]
The mechanism of 5α reductase inhibition is complex, but involves the binding of NADPH to the enzyme followed by the substrate. 5α-Reductase inhibitor drugs are used in benign prostatic hyperplasia, prostate cancer, pattern hair loss (androgenetic alopecia), and hormone replacement therapy for transgender women.
It includes direct antagonists of the androgen receptor (AR), androgen synthesis inhibitors like 5α-reductase inhibitors and CYP17A1 inhibitors, and antigonadotropins like GnRH analogues, estrogens, and progestogens. [3] In addition, it includes both steroidal antiandrogen (SAAs) and nonsteroidal antiandrogen (NSAAs).
Pages in category "5α-Reductase inhibitors" The following 40 pages are in this category, out of 40 total. This list may not reflect recent changes. ...
Other 5α-reductase inhibitors such as finasteride (a type 2 inhibitor) have been used off-label to treat excessive hair growth in women with hirsutism. [ 3 ] [ 23 ] Since dutasteride is an inhibitor of both type 1 and 2 5α-reductases, it could theoretically be a more effective therapy for hirsutism.
This combination can be useful because it may take up to six months for symptomatic relief to be found when using 5α-Reductase inhibitors such as dutasteride compared to alpha-1 receptor blockers, which can provide relief in some cases within 48 hours. [19]