5-alpha-reductase inhibitor
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5α-reductase inhibitors (or 5-alpha-reductase inhibitors) are a group of drugs with antiandrogenic activity, used in the treatment of benign prostatic hyperplasia and androgenic (or androgenetic) alopecia. These drugs decrease the levels of available 5α-reductase prior to testosterone binding with the enzyme, thus reducing levels of dihydrotestosterone that derives from such a bond.
Clinical use
Indications
5α-reductase inhibitors are clinically used in the treatment of conditions which are exacerbated by dihydrotestosterone. Specifically, these indications may include: (Rossi, 2004)
- mild-to-moderate benign prostatic hyperplasia
- androgenic (or androgenetic) alopecia
Adverse drug reactions
Adverse drug reactions (ADRs) experienced with 5α-reductase inhibitors are generally dose-dependent. Common ADRs include impotence, decreased libido, decreased ejaculate volume. Rare ADRs include: breast tenderness and enlargement, and allergic reaction. (Rossi, 2004)
Pharmacology
The enzyme 5α-reductase is involved in the conversion of testosterone to the active form dihydrotestosterone by reducing the Δ4,5 double-bond. In benign prostatic hyperplasia, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth - inhibiting the enzyme reduces the excessive prostate growth. In alopecia, pattern-baldness is one of the effects of androgenic receptor activation. Reducing the levels of dihydrotestosterone thus reduces alopecia.
Examples
- finasteride (Proscar, Propecia)
- dutasteride (Avodart)
- FCE 28260, an experimental compound
References
- Rossi S (Ed.) (2004). Australian Medicines Handbook 2004. Adelaide: Australian Medicines Handbook. ISBN 0-9578521-4-2
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
