Summary
Dihydrotestosterone (DHT) is a potent androgen that plays a significant role in various physiological processes. It is critical for fetal development, particularly in male genital formation and prostate differentiation. DHT influences systemic and local effects through binding to androgen receptors, exhibiting higher affinity than testosterone. This hormone is intricately involved in multiple conditions, such as benign prostatic hyperplasia (BPH), androgenetic alopecia, and prostate cancer. The 5α-reductase enzyme catalyzes the conversion of testosterone to DHT. There are two main types of this enzyme, type-1 and type-2, which affect DHT levels differently. Type-2 is particularly active in the prostate, and its inhibition is the therapeutic target for drugs like finasteride and dutasteride. These drugs are effective in managing BPH by reducing prostate size and alleviating urinary symptoms, also serving as chemopreventive agents for prostate cancer. Another notable role of DHT is in hair follicle miniaturization, which contributes to male pattern baldness. Inhibiting DHT production can mitigate hair loss but may come with side effects such as sexual dysfunction. Despite these benefits, the psychiatric effects of 5α-reductase inhibitors, including heightened risks of depression and self-harm, urge cautious use. Recognizing DHT's involvement in androgen-dependent processes underscores the importance of targeting its synthesis and activity in related therapeutic interventions.
DHT, crucial in male development, binds more effectively to androgen receptors than testosterone. Finasteride inhibits 5α-reductase, impacting prostate size, cancer progression, and erectile function.
Published By:
WD Steers - Urology, 2001 - Elsevier
New steroid derivatives inhibit 5α-reductase, outperforming finasteride in prostate size reduction. Compounds 5, 7, 9, and 10 show significant promise as treatments for androgen-related disorders.
Published By:
V Pérez-Ornelas, M Cabeza, E Bratoeff, I Heuze… - Steroids, 2005 - Elsevier
Finasteride, a 5α-reductase inhibitor, treats BPH and hair loss by reducing DHT. It affects behavior by altering GABAergic neurotransmission.
Published By:
DA Finn, AS Beadles‐Bohling, EH Beckley… - CNS drug …, 2006 - Wiley Online Library
5α-reductase inhibitors may increase self-harm and depression risks within 18 months of use. However, they do not significantly raise suicide risk.
Published By:
B Welk, E McArthur, M Ordon, KK Anderson… - JAMA internal …, 2017 - jamanetwork.com
The study synthesized new steroidal compounds inhibiting 5α-reductase, showing high activity. Trienones exhibited greater inhibitory power than dienones through irreversible Michael addition.
Published By:
E Flores, E Bratoeff, M Cabeza… - Mini reviews in …, 2003 - ingentaconnect.com
5AR inhibitors revolutionized BPH treatment by reducing DHT, shrinking the prostate safely. Dutasteride is more potent than finasteride, inhibiting both enzyme types, enhancing clinical outcomes.
Published By:
LS Marks - Reviews in urology, 2004 - ncbi.nlm.nih.gov
Herbs like GL, UD, BH, SI, and CR show promising 5α-reductase inhibitory activity. This method effectively screens herbal antiandrogenic potential.
Published By:
A Nahata, VK Dixit - Andrologia, 2014 - Wiley Online Library
Studies explore 5α-reductase's role in prostate health, cancer, and hair loss. Finasteride is examined for its inhibitory effects.
Published By:
A Cilotti, G Danza, M Serio - Journal of endocrinological investigation, 2001 - Springer
Dutasteride significantly reduced DHT in BPH patients more effectively than finasteride. It was well tolerated with an adverse event profile similar to placebo.
Published By:
RV Clark, DJ Hermann, GR Cunningham… - The journal of …, 2004 - academic.oup.com
DHT plays a key role in BPH, treatable with 5α-reductase inhibitors. These drugs improve symptoms but may affect libido.
Published By:
G Andriole, N Bruchovsky, LWK Chung… - The Journal of …, 2004 - auajournals.org