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The Secret Weapon of Hormone Change: How do 5α-reductase inhibitors regulate your body hair?
In modern medicine, 5α-reductase inhibitors (5-ARIs) have become a topic of great concern. These drugs are widely used for their anti-androgenic properties and are used to treat enlarged prostates and hair loss. The mechanism by which these drugs work involves inhibiting 5alpha-reductase, an enzyme that plays an important role in the metabolic conversion of endogenous steroids.
Inhibition of 5α-reductase reduces the conversion of testosterone to the more potent dihydrotestosterone (DHT), thereby affecting a variety of androgen-related diseases.
Medical purposes
5-ARIs are mainly used to treat a variety of diseases exacerbated by DHT, including:
- Mild to moderate benign prostatic hyperplasia and lower urinary tract symptoms
- Pattern Hair Loss in Men and Women
- Treatment of hirsutism in women
However, the jury is still out on its potential effectiveness as a treatment for acne. In addition, 5-ARIs are also used in hormonal therapy for transgender women to help reduce body hair growth and slow hair loss.
Available forms
5-ARIs currently available on the market include:
- Finasteride (brand name: Proscar, Propecia): Helps inhibit the second and third types of 5α-reductase, reducing DHT levels by about 70%.
- Dutasteride (brand name Avodart): Inhibits all three 5α-reductase enzymes while reducing DHT levels by 95%.
- Epristeride (brand name Aipuliete, Chuanliu): used in China to treat benign prostatic hyperplasia, but its effect on DHT is only about 25% to 54%.
- Alfatradiol (brand name Ell-Cranell Alpha, Pantostin): topical 5-ARIs used in Europe to treat pattern alopecia.
Side effects
Although 5-ARIs are generally well tolerated, several risks may occur in men, including decreased libido, erectile dysfunction, and ejaculatory dysfunction. Studies show that the incidence of these side effects ranges from 3.4% to 15.8%.
In addition, 5-ARIs have been linked to an increased risk of certain rare but highly aggressive forms of prostate cancer, prompting an FDA warning against this class of drugs.
Emotional changes
Some studies have pointed out that the use of 5-ARIs may be associated with an increased risk of depression. Particularly during the first 18 months of treatment, the incidence of depression increased significantly.
Although the risk of depression decreased slightly over time, it still showed some marginal increase.
Pharmacology
The inhibition mechanism of 5α-reductase is quite complex and involves the binding of NADPH to the enzyme, followed by the binding of the substrate. This process ultimately results in lower production of DHT, which also increases testosterone and estrogen levels.
Historical background
Finasteride was the first 5-ARI to be introduced for medical use, officially launched in 1992, and received approval for the treatment of pattern alopecia in 1997. Subsequently, advances in drug development led to the emergence of drugs such as doxasteride and eplerenone.
Future research directions
5-ARIs are also currently being studied in combination with the nonsteroidal antiandrogen drug bicalutamide for the treatment of prostate cancer, suggesting that they may have additional potential for applications in the future.
Whether it is inhibiting DHT to reduce hair loss or treating benign prostatic hyperplasia, 5α-reductase inhibitors are undoubtedly an indispensable part of modern medical treatment. But will such treatment affect the patient's quality of life or even cause other health problems?
