Finasteride: the first 5 alpha-reductase inhibitor. 1993

S L Sudduth, and M J Koronkowski
Program on Aging, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360.

Finasteride is a synthetic 4-azasteroid that is a specific competitive inhibitor of 5 alpha-reductase, an intracellular enzyme that converts testosterone to dihydrotestosterone (DHT). It has no binding affinity for androgen receptor sites and itself possesses no androgenic, antiandrogenic, or other steroid hormone-related properties. It is well absorbed after oral administration, with absolute bioavailability in humans of 63% (range 34-108%). The mean time to maximum concentration is 1-2 hours, and it is approximately 90% plasma protein bound. The elimination half-life averages 6-8 hours. The agent is metabolized to a series of five metabolites, of which two are active and possess less than 20% of the 5 alpha-reductase activity of finasteride. Little is known about potential drug interactions, although they appear to be minimal and not clinically relevant. The drug is indicated for the treatment of symptomatic benign prostatic hyperplasia. Its efficacy in regression of prostate gland enlargement is rapid and predictable, although correlation with subsequent improvement in urinary flow and symptoms is highly variable. Dosages of 0.5-100 mg/day regress prostate enlargement; the recommended dosage is 5 mg once/day. Finasteride may hold promise for other DHT-mediated disorders such as acne, facial hirsutism, frontal lobe alopecia, and prostate cancer, but its use in these conditions remains investigational. The frequency of adverse drug events is low, with the most common side effects being impotence, decreased libido, and decreased volume of ejaculate. No reports of intentional overdose have been reported, and dosages of up to 80 mg/day for 3 months have been taken without adverse effect.

UI MeSH Term Description Entries
D008297 Male Males
D011470 Prostatic Hyperplasia Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both. Adenoma, Prostatic,Benign Prostatic Hyperplasia,Prostatic Adenoma,Prostatic Hyperplasia, Benign,Prostatic Hypertrophy,Prostatic Hypertrophy, Benign,Adenomas, Prostatic,Benign Prostatic Hyperplasias,Benign Prostatic Hypertrophy,Hyperplasia, Benign Prostatic,Hyperplasia, Prostatic,Hyperplasias, Benign Prostatic,Hypertrophies, Prostatic,Hypertrophy, Benign Prostatic,Hypertrophy, Prostatic,Prostatic Adenomas,Prostatic Hyperplasias, Benign,Prostatic Hypertrophies
D011471 Prostatic Neoplasms Tumors or cancer of the PROSTATE. Cancer of Prostate,Prostate Cancer,Cancer of the Prostate,Neoplasms, Prostate,Neoplasms, Prostatic,Prostate Neoplasms,Prostatic Cancer,Cancer, Prostate,Cancer, Prostatic,Cancers, Prostate,Cancers, Prostatic,Neoplasm, Prostate,Neoplasm, Prostatic,Prostate Cancers,Prostate Neoplasm,Prostatic Cancers,Prostatic Neoplasm
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000505 Alopecia Absence of hair from areas where it is normally present. Alopecia, Androgenetic,Baldness,Male Pattern Baldness,Pseudopelade,Alopecia Cicatrisata,Alopecia, Male Pattern,Androgenetic Alopecia,Androgenic Alopecia,Baldness, Male Pattern,Female Pattern Baldness,Hair Loss,Pattern Baldness,Alopecia Cicatrisatas,Alopecia, Androgenic,Alopecias, Androgenic,Androgenic Alopecias,Baldness, Female Pattern,Baldness, Pattern,Hair Losses,Loss, Hair,Losses, Hair,Male Pattern Alopecia
D000736 Androstenes Unsaturated derivatives of the steroid androstane containing at least one double bond at any site in any of the rings.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001378 Azasteroids Steroidal compounds in which one or more carbon atoms in the steroid ring system have been substituted with nitrogen atoms. 17- Azasteroids,4- Azasteroids,Azasteroid,17 Azasteroids,4 Azasteroids,Azasteroids, 17-,Azasteroids, 4-
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D058891 5-alpha Reductase Inhibitors Drugs that inhibit 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. They are commonly used to reduce the production of DIHYDROTESTOSTERONE. 3-Oxo-5-alpha-Steroid 4-Dehydrogenase Inhibitor,5-alpha Reductase Inhibitor,Steroid 5-alpha-Reductase Inhibitor,Testosterone 5-alpha-Reductase Inhibitor,3-Oxo-5-alpha-Steroid 4-Dehydrogenase Inhibitors,Steroid 5-alpha-Reductase Inhibitors,Testosterone 5-alpha-Reductase Inhibitors,3 Oxo 5 alpha Steroid 4 Dehydrogenase Inhibitor,3 Oxo 5 alpha Steroid 4 Dehydrogenase Inhibitors,4-Dehydrogenase Inhibitor, 3-Oxo-5-alpha-Steroid,4-Dehydrogenase Inhibitors, 3-Oxo-5-alpha-Steroid,5 alpha Reductase Inhibitor,5 alpha Reductase Inhibitors,5-alpha-Reductase Inhibitor, Steroid,5-alpha-Reductase Inhibitor, Testosterone,5-alpha-Reductase Inhibitors, Steroid,5-alpha-Reductase Inhibitors, Testosterone,Inhibitor, 3-Oxo-5-alpha-Steroid 4-Dehydrogenase,Inhibitor, 5-alpha Reductase,Inhibitor, Steroid 5-alpha-Reductase,Inhibitor, Testosterone 5-alpha-Reductase,Inhibitors, 3-Oxo-5-alpha-Steroid 4-Dehydrogenase,Inhibitors, 5-alpha Reductase,Inhibitors, Steroid 5-alpha-Reductase,Inhibitors, Testosterone 5-alpha-Reductase,Reductase Inhibitor, 5-alpha,Reductase Inhibitors, 5-alpha,Steroid 5 alpha Reductase Inhibitor,Steroid 5 alpha Reductase Inhibitors,Testosterone 5 alpha Reductase Inhibitor,Testosterone 5 alpha Reductase Inhibitors

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