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Additional information about the drug Dutasteride
Dutasteride, sold under the brand name Avodart among others, is a medication used primarily to treat enlarged prostate in men.
Dutasteride is a 5α-reductase inhibitor, and hence is a type of antiandrogen.
Dutasteride was developed by GlaxoSmithKline.
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
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 Availability
10 Research
11 References
12 External links
Medical uses
Enlarged prostate
Dutasteride is used for treating benign prostatic hyperplasia (BPH); colloquially known as an “enlarged prostate”.
Prostate cancer
A 2010 Cochrane review found a 25–26% reduction in the risk of developing prostate cancer with 5α-reductase inhibitor chemoprevention.
Scalp hair loss
Dutasteride is approved for the treatment of male androgenetic alopecia in South Korea and Japan at a dosage of 0.5 mg per day.
Excessive hair growth
Although no reports specific to dutasteride currently exist,
Transgender hormone therapy
Dutasteride is sometimes used as a component of hormone therapy for transgender women in combination with an estrogen and/or another antiandrogen like spironolactone.
Contraindications
Women who are or who may become pregnant should not handle the drug. Dutasteride can cause birth defects, specifically ambiguous genitalia and undermasculinization, in male fetuses.
Children and people with known significant hypersensitivity (e.g., serious skin reactions, angioedema ) to dutasteride should not take dutasteride.
Adverse effects
Dutasteride has overall been found to be well-tolerated in studies of both men and women, producing minimal side effects.
The FDA has added a warning to dutasteride about an increased risk of high-grade prostate cancer.
Sexual dysfunction, such as erectile dysfunction, loss of libido, or reduced semen volume, may occur in 3.4 to 15.8% of men treated with finasteride or dutasteride.
Several small studies have reported an association between 5α-reductase inhibitors and depression.
Overdose
There is no specific antidote for overdose of dutasteride.
Interactions
5α-Reductase inhibitors can also prevent the formation of neurosteroid metabolites like allopregnanolone from progesterone and hence may reduce or block the sedative, anticonvulsant, anxiolytic, and various other effects of progesterone, particularly in the case of oral progesterone (which is disproportionately converted into these metabolites due to first-pass metabolism ).
Pharmacology
Pharmacodynamics
Dutasteride belongs to a class of drugs called 5α-reductase inhibitors, which block the action of the 5α-reductase enzymes that convert testosterone into DHT.
Since 5α-reductase inhibitors degrade testosterone to DHT, the inhibition of them could cause an increase in testosterone. However, a 2018 review found that initiation of 5α-reductase inhibitors did not result in a consistent increase in testosterone levels, with some studies showing increases and others showing no change. There was no statistically significant change in testosterone levels from 5α-reductase inhibitors in the overall meta-analysis, though men with lower baseline testosterone levels may have a higher chance of having experiencing testosterone levels.
In addition to inhibition of DHT production, 5α-reductase inhibitors like dutasteride are also neurosteroidogenesis inhibitors, preventing the 5α-reductase-mediated biosynthesis of various neurosteroids including allopregnanolone (from progesterone ), THDOC (from deoxycorticosterone ), and 3α-androstanediol (from testosterone).
Pharmacokinetics
The oral bioavailability of dutasteride is approximately 60%.
Chemistry
See also: List of 5α-reductase inhibitors
Dutasteride, also known as N -[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide, is a synthetic androstane steroid and a 4-azasteroid.
History
Dutasteride was patented in 1996
Society and culture
Avodart (dutasteride) 500 µg soft capsules.
Generic names
Dutasteride is the generic name of the drug and its INN, USAN, BAN, and JAN.
Brand names
Dutasteride is sold primarily under the brand name Avodart and, in combination with tamsulosin (see dutasteride/tamsulosin ), under the brand names Combodart and Duodart.
Availability
Dutasteride is available widely throughout the world, including in the United States, Canada, the United Kingdom, Ireland, many other European countries, Australia, and South Africa, as well as in Latin America, Asia, and elsewhere.
Research
Dutasteride has been studied in combination with bicalutamide in the treatment of prostate cancer.
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