Everything about Androgen Antagonist totally explained
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,
male sex
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.
Indications
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
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). They are also occasionally used as a
male contraceptive agent, to purposefully prevent or counteract masculinisation in the case of
transwomen undergoing
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 desire or
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.
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.
- 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 don't counteract the effects or production of other androgens other than DHT.
Antiandrogen withdrawal response
The term
antiandrogen withdrawal response (AAWR) describes the medical course taken when cancer cells adapt to feed on the antiandrogens rather than androgen, so that treatment must be halted in order to starve those cells thriving on the antiandrogens.
Further Information
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