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Additional information about the drug Finasteride


Finasteride, sold under the brand names Proscar and Propecia among others, is a medication used mainly to treat an enlarged prostate or scalp hair loss in men.
Side effects are generally mild.
Finasteride was introduced for the treatment of prostate enlargement in 1992 and was approved for the treatment of scalp hair loss in 1997.
Contents
1 Medical uses
1.1 Enlarged prostate
1.2 Prostate cancer
1.3 Scalp hair loss
1.4 Excessive hair growth
1.5 Transgender hormone therapy
2 Contraindications
3 Adverse effects
3.1 Sexual dysfunction
4 Overdose
5 Interactions
6 Pharmacology
6.1 Pharmacodynamics
6.2 Pharmacokinetics
7 Chemistry
8 History
9 Society and culture
9.1 Generic names
9.2 Brand names
9.3 Controversy
9.4 Athletics
9.5 Miscellaneous
10 References
Medical uses
Enlarged prostate
Physicians sometimes prescribe finasteride for the treatment of benign prostatic hyperplasia (BPH), informally known as an enlarged prostate. Finasteride may improve the symptoms associated with BPH such as difficulty urinating, getting up during the night to urinate, hesitation at the start and end of urination, and decreased urinary flow. It provides less symptomatic relief than alpha-1 blockers such as tamsulosin and symptomatic relief is slower in onset (six months or more of treatment with finasteride may be required to determine the therapeutic results of treatment). Symptomatic benefits are mainly seen in those with prostate volume > 40 cm 3. In long-term studies finasteride but not alpha-1 inhibitors reduce the risk of acute urinary retention (−57% at 4 years) and the need for surgery (−54% at 4 years). If the drug is discontinued, any therapeutic benefits are reversed within about 6–8 months.
Prostate cancer
A 2010 Cochrane review found a 25 or 26% reduction in the risk of developing prostate cancer with 5α-reductase inhibitor chemoprevention.
Scalp hair loss
Finasteride is also used to treat male pattern baldness (androgenetic alopecia) in men, a condition that develops in up to 80% of Caucasian men.
Excessive hair growth
Finasteride has been found to be effective in the treatment of hirsutism (excessive facial and/or body hair growth) in women. In a study of 89 women with hyperandrogenism due to persistent adrenarche syndrome, finasteride produced a 93% reduction in facial hirsutism and a 73% reduction bodily hirsutism after 2 years of treatment. Other studies using finasteride for hirsutism have also found it to be clearly effective.
Transgender hormone therapy
Finasteride is sometimes used in hormone replacement therapy for transgender women due to its antiandrogenic effects, in combination with a form of estrogen. However, little clinical research of finasteride use for this purpose has been conducted and evidence of safety or efficacy is limited.
Contraindications
Finasteride may cause birth defects in a male fetus if a pregnant woman takes finasteride or is exposed to finasteride pill fragments.
Adverse effects
A 2010 Cochrane review concluded that adverse effects from finasteride are rare when used for BPH.
The FDA has added a warning to 5α-reductase inhibitors concerning an increased risk of high-grade prostate cancer, as the treatment of BPH lowers PSA ( prostate-specific antigen ), which could mask the development of prostate cancer.
Sexual dysfunction
Finasteride causes short-term sexual dysfunction in some men.
The 2010 Cochrane review found that compared with placebo, men taking finasteride are at increased risk for impotence, erectile dysfunction, decreased libido, and ejaculation disorder for the first year of treatment; the rates of these effects became indistinguishable from placebo after 2–4 years and these side effects usually got better over time.
Overdose
Finasteride has been studied in humans at single doses of up to 400 mg and at continuous dosages of up to 80 mg/day for three months, without adverse effects observed.
Interactions
No significant drug interactions have been observed between finasteride and a limited selection of medications.
Pharmacology
Pharmacodynamics
Finasteride is a 5α-reductase inhibitor.
Finasteride results in a decrease of circulating DHT levels by about 65 to 70% with an oral dosage of 5 mg/day and of DHT levels in the prostate gland by up to 80 to 90% with an oral dosage of 1 or 5 mg/day.
As of 2012, the tissues in which the different isozymes of 5α-reductase are expressed are not fully clear.
By inhibiting 5α-reductase and thus preventing DHT production, finasteride reduces androgen signaling in tissues like the prostate gland and the scalp. In the prostate, this reduces prostate volume, which improves BPH and reduces risk of prostate cancer. Finasteride reduces prostate volume by 20 to 30% in men with benign prostatic hyperplasia.
Neurosteroids like 3α-androstanediol (derived from DHT) and allopregnanolone (derived from progesterone ) activate the GABA A receptor in the brain ; because finasteride prevents the formation of neurosteroids, it functions as a neurosteroidogenesis inhibitor and may contribute to a reduction of GABA A activity. Reduction of GABA A receptor activation by these neurosteroids has been implicated in depression, anxiety, and sexual dysfunction.
Pharmacokinetics
The mean oral bioavailability of finasteride is approximately 65%.
Finasteride is extensively metabolized in the liver, first by hydroxylation via CYP3A4 and then by aldehyde dehydrogenase.
Chemistry
See also: List of 5α-reductase inhibitors
Finasteride, also known as 17β-( N -tert-butylcarbamoyl)-4-aza-5α-androst-1-en-3-one, is a synthetic androstane steroid and 4-azasteroid.
History
In 1942, James Hamilton observed that prepubertal castration prevents the later development of male pattern baldness in mature men.
In 1975, copies of Imperato-McGinley’s presentation were seen by P. Roy Vagelos, who was then serving as Merck ‘s basic-research chief. He was intrigued by the notion that decreased levels of DHT led to the development of smaller prostates. Dr. Vagelos then sought to create a drug which could mimic the condition found in these children to treat older men who were suffering from benign prostatic hyperplasia.
Finasteride was developed by Merck under the code name MK-906.
Society and culture
Generic names
Finasteride is the generic name of the drug and its INN, USAN, BAN, and JAN, while finastéride is its DCF.
Brand names
Finasteride is marketed primarily under the brand names Propecia, for pattern hair loss, and Proscar, for BPH, both of which are products of Merck & Co.
Controversy
Men in the U.S. and Canada concerned about persistent sexual side effects “coined the phrase ‘post-finasteride syndrome’, which they say is characterized by sexual, neurological, hormonal and psychological side effects that can persist in men who have taken finasteride for hair loss or an enlarged prostate”.
Athletics
From 2005 to 2009, the World Anti-Doping Agency banned finasteride because it was discovered that the drug could be used to mask steroid abuse.
Miscellaneous
The Food and Drug Administration advises that donation of blood or plasma be deferred for at least one month after taking the last dose of finasteride.
Harold Bornstein, the former

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