Antiandrogen - Wikipedia, the free encyclopedia http://en.wikipedia.

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Antiandrogen
From Wikipedia, the free encyclopedia

An antiandrogen, or androgen antagonist, is any of a group of hormone receptor antagonist compounds that
are capable of preventing or inhibiting the biologic effects of androgens,[1] male sex hormones, on normally
responsive tissues in the body. Antiandrogens usually work by blocking the appropriate receptors, competing for
binding sites on the cell's surface, obstructing the androgens' pathway.

Contents
1 Indications
2 Examples
3 Antiandrogen herbs
4 See also
5 References

Indications
Antiandrogens are often indicated to treat severe male sexual disorders, such as hypersexuality (excessive
sexual desire) and sexual deviation such as paraphilias, as well as use as an antineoplastic agent and palliative,
adjuvant or neoadjuvant hormonal therapy in prostate cancer.

Antiandrogens can also be used for treatment of benign prostatic hyperplasia (prostate enlargement), acne
vulgaris, androgenetic alopecia (male pattern baldness), and hirsutism (excessive hairiness). On occasion, they
are also used as a male contraceptive agent, to purposefully prevent or counteract masculinisation in the case of
transsexual women undergoing sex reassignment therapy, and to prevent the symptoms associated with reduced
testosterone, such as hot flashes, following castration. They can also be used for the treatment of polycystic
ovarian syndrome (PCOS).

The administration of antiandrogens in males can result in slowed or halted development or reversal of male
secondary sex characteristics, reduced activity or function of the accessory male sex organs, and hyposexuality
(diminished sexual desire or libido).

Sometimes as a part of a program for registered sex offenders recently released from prisons, the offender is
administered antiandrogen drugs to reduce the likelihood of repeat offending by reducing sexual drive, etc.

Examples
Currently available antiandrogen drugs (brand names, which may include other active ingredients, in
parentheses) include:

Spironolactone (Aldactone, Spiritone), a synthetic 17-spirolactone corticosteroid, which is a renal

competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used
primarily to treat low-renin hypertension, hypokalemia, and Conn's syndrome.
Cyproterone acetate (Androcur, Climen, Diane 35, Ginette 35), a synthetic steroid, a potent antiandrogen
that also possesses progestational properties.

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Antiandrogen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Antiandrogen

Flutamide (Eulexin), nilutamide (Anandron, Nilandron) and bicalutamide (Casodex), nonsteroidal, pure
antiandrogens. Flutamide is the oldest and has more unwanted side-effects than the others. Bicalutamide
is the newest and has the least side-effects.
Ketoconazole (Nizoral), an imidazole derivative used as a broad-spectrum antifungal agent effective
against a variety of fungal infections; side-effects include serious liver damage and reduced levels of
androgen from both the testicles and adrenal glands. Ketoconazole is a relatively weak antiandrogen.
Finasteride (Proscar, Propecia) and dutasteride (Avodart), inhibitors of the 5-α-reductase enzyme that
prevent the conversion of testosterone into dihydrotestosterone (DHT). Finasteride blocks only
5-α-reductase type II, dutasteride also blocks type I. They are not general antiandrogens in that they do
not counteract the effects or production of other androgens other than DHT; however, DHT is 3-5 times
more potent than testosterone or other androgens (except in skeletal muscle tissue, where testosterone is
the main androgen).There are a number of in vivo and in vitro plant/herbal inhibitors of the 5-alpha
reductase
DDE The metabolite of DDT is DDE, which acts as a weak antiandrogen.
Bexlosteride
Izonsteride
Epristeride
Turosteride

Antiandrogen herbs
The best known plant-derived anti-androgen is 3,3'-Diindolylmethane(DIM)[2]

Spearmint tea has antiandrogenic properties in females with hirsutism.[3],[4]

Scutellaria baicalensis may also have antiandrogenic properties.[5]

The compound N-butylbenzene-sulfonamide (NBBS) isolated from Pygeum africanum is a specific androgen
antagonist.[6],[7]

Glycyrrhiza glabra has shown antiandrogenic activity in male rats[8]

A herbal formula (termed KMKKT) containing Korean Angelica gigas Nakai (AGN) root and nine other oriental
herbs has shown in vitro anti-androgen activity.[9]

Pygeum africanum contains an antiandrogenic compound atraric acid.[10]

Duke's data base lists several more herbs http://www.ars-grin.gov/cgi-bin/duke/activity.pl

See also
Antiestrogen
Baldness treatments
GnRH antagonist
GnRH agonist
5-alpha-reductase_inhibitor

References

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Antiandrogen - Wikipedia, the free encyclopedia http://en.wikipedia.org/wiki/Antiandrogen

1. ^ antiandrogen (http://www.mercksource.com/pp/us/cns/cns_hl_dorlands_split.jsp?pg=/ppdocs/us/common
/dorlands/dorland/one/000005872.htm) at Dorland's Medical Dictionary
2. ^ Plant-derived 3,3'-Diindolylmethane is a strong androgen antagonist in human prostate cancer cells.
(http://www.ncbi.nlm.nih.gov/pubmed/12665522)
3. ^ Grant P. 'Spearmint herbal tea has significant anti-androgen effects in polycystic ovarian syndrome. A randomized
controlled trial Phytotherapy Research 2010 24:2 (186-188)
4. ^ Akdogan M. Tamer MN. Cure E. Cure MC. Koroglu BK. Delibas N."Effect of spearmint (Mentha spicata
Labiatae) teas on androgen levels in women with hirsutism." Phytotherapy Research. 21(5):444-7, 2007 May.
5. ^ Bonham M., Posakony J., Coleman I., Montgomery B., Simon J., Nelson P.S."Characterization of chemical
constituents in Scutellaria baicalensis with antiandrogenic and growth-inhibitory activities toward prostate
carcinoma" Clinical Cancer Research 2005 11:10 (3905-3914)
6. ^ Papaioannou M. Schleich S. Roell D. Schubert U. Tanner T. Claessens F. Matusch R. Baniahmad A. ,"NBBS
isolated from Pygeum africanum bark exhibits androgen antagonistic activity, inhibits AR nuclear translocation and
prostate cancer cell growth.",Investigational New Drugs. 28(6):729-43, 2010 Dec.
7. ^ Schleich S. Papaioannou M. Baniahmad A. Matusch R.,"Extracts from Pygeum africanum and other
ethnobotanical species with antiandrogenic activity.", Planta Medica. 72(9):807-13, 2006 Jul.
8. ^ Zamansoltani F. Nassiri-Asl M. Sarookhani MR. Jahani-Hashemi H. Zangivand AA. "Antiandrogenic activities of
Glycyrrhiza glabra in male rats.", International Journal of Andrology. 32(4):417-22, 2009 Aug
9. ^ Jiang C., Lee H.-J., Li G.-X., Guo J., Malewicz B., Zhao Y., Lee E.-O., Lee H.-J., Lee J.-H., Kim M.-S., Kim
S.-H., Lu J. "Potent antiandrogen and androgen receptor activities of an Angelica gigas-containing herbal
formulation: Identification of decursin as a novel and active compound with implications for prevention and
treatment of prostate cancer" Cancer Research 2006 66:1 (453-463)
10. ^ Schleich S. Papaioannou M. Baniahmad A. Matusch R.,"Activity-guided isolation of an antiandrogenic compound
of Pygeum africanum." Planta Medica. 72(6):547-51, 2006 May.
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Categories: Hormonal agents

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