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14-September-2008 11:27:24 - Antiandrogen 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. Contents 1 Indications 2 Examples 3 Antiandrogen withdrawal response 4 See also 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. See also GnRH antagonist GnRH agonist Baldness treatments v d e Acne-treating agents D10 Antibacterial agents Azelaic acid Benzoyl peroxide blue light therapy Tea tree oil Kerolytic agents Glycolic acid Salicylic acid Anti-inflammatory agents Aspirin Ibuprofen red light therapy Antibiotics Clindamycin Erythromycin Sulfacetamide Tetracyclines Trimethoprim Hormonal Antiandrogens Contraceptives Retinoids Adapalene Isotretinoin Tazarotene Tretinoin v d e Sex hormones and related agents primarily G03, also L02, H01C - human endogenous in CAPS Progestogens: receptor Agonist PROGESTERONE, Dienogest, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin, Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone SPRM Asoprisnil, CDB-4124 Antiprogestogen Mifepristone Androgens: receptor Agonist TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, see also anabolic steroids Antiandrogen Bicalutamide, Cyproterone, Dienogest, Flutamide, Nilutamide, Spironolactone Estrogens: receptor Agonist ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate SERM Afimoxifene, Arzoxifene, Bazedoxifene, Clomifene, Fulvestrant, Lasofoxifene, Raloxifene, Tamoxifen, Toremifene AI Aminoglutethimide, Anastrozole, Atamestane, Exemestane, Fadrozole, Formestane, Letrozole, Vorozole Antiestrogen Mepitiostane Gonadotropins: FSHR/LHCGR ovulation stim. Clomifene, Urofollitropin Antigonadotropin Danazol, Gestrinone GnRH: receptor Agonist Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin Antagonist Abarelix, Cetrorelix, Ganirelix v d e Receptor antagonists: hormone antagonists Hypothalamic/pituitary axes Adrenal axis: Corticotropin releasing hormone antagonists - Aldosterone antagonists Thyroid axis: Antithyroid agents Gonadal axis: Androgen antagonists - Gonadotropin-releasing hormone antagonists - Selective estrogen receptor modulator Eicosanoid Leukotriene antagonists - Prostaglandin antagonists Other Cholecystokinin antagonists Retrieved from http://en..org/wiki/Antiandrogen Categories: Hormonal agents Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Català Česky Deutsch Español 日本語 Português This page was last modified on 10 May 2008, at 11:1
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