An antiandrogen, or androgen antagonist, is any of a group of
hormone receptor antagonistcompounds that are capable of preventing or inhibiting the biologic effects of androgens, malesex hormones, on normally responsive tissues in the body (see androgen insensitivity syndrome). Antiandrogens usually work by blocking the appropriate receptors, competing for binding sites on the cell's surface, obstructing the androgens' pathway.
Antiandrogens are often indicated to treat severe male sexual disorders, such as
hypersexuality(excessive sexual desire) and sexual deviation, specifically paraphilias, as well as use as an antineoplasticagent and palliative, adjuvantor neoadjuvanthormonal 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). They are also occasionally used as a male contraceptiveagent, to purposefully prevent or counteract masculinisation in the case of transwomenundergoing sex reassignment therapy, and to prevent the symptoms associated with reduced testosterone, such as hot flashes, following castration.
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 desireor libido).
Sometimes as a part of a program for registered sex offenders recently released from prisons, the offender is administered anti androgen drugs to reduce the likelihood of repeat offending by reducing sexual drive etc.
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 aldosteroneantagonist 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.
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 imidazolederivative used as a broad-spectrumantifungal agent effective against a variety of fungal infections, side effects include serious liverdamage 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 enzymethat 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 don't counteract the effects or production of other androgens other than DHT.
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