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  • treatment of androgen-dependent skin
  • Flutamide has been researched and used extensively in the treatment of androgen-dependent skin and hair conditions in women including acne, seborrhea, hirsutism, and scalp hair loss, as well as in hyperandrogenism (e.g., in polycystic ovary syndrome or congenital adrenal hyperplasia), and is effective in improving the symptoms of these conditions. (wikipedia.org)
  • Unlike flutamide and nilutamide, the drug is said to be short-acting and inactive by injection, but it has been found to be active topically in animals, and hence could be useful for the treatment of androgen-dependent skin conditions. (wikipedia.org)
  • estrogens
  • Evidence suggests that a growth factor released by PGCs, bone morphogenic protein 15 (bmp15), promotes female development by increasing expression of cyp19a1a, an aromatase enzyme that converts androgens to estrogens. (deepdyve.com)
  • antiandrogen
  • Spironolactone (Aldactone): An antimineralocorticoid (aldosterone antagonist) with additional/coincidental antiandrogen activity. (wikipedia.org)
  • Cyproterone acetate (abbreviated as CPA), sold alone under the brand name Androcur or with ethinylestradiol (EE) under the brand names Diane or Diane-35 among others, is an antiandrogen and progestogen which is used in the treatment of androgen-dependent conditions like acne, excessive hair growth, early puberty, and prostate cancer, as a component of feminizing hormone therapy for transgender women, and in birth control pills. (wikipedia.org)
  • In the U.S., where CPA is not available, other drugs with antiandrogen properties like the diuretic spironolactone and the progestin medroxyprogesterone acetate are used instead to treat androgen-dependent conditions besides prostate cancer. (wikipedia.org)
  • adrenal androgens
  • Castration, therefore, does not suppress adrenal androgens and achieves a "hormone-reduced" rather than a "hormone-free" state, hence, the recent renaming of this stage of the disease as castration-resistant in preference to hormone-refractory. (aacrjournals.org)
  • This has been determined to be due to uptake of circulating weak adrenal androgens like dehydroepiandrosterone (DHEA) and androstenedione (A4) by the prostate and their de novo transformation into testosterone and DHT. (wikipedia.org)
  • inhibit
  • In addition, it does not inhibit 5α-reductase and is not known to inhibit other enzymes involved in androgen steroidogenesis (e.g. (wikipedia.org)
  • Although GnRH agonists stimulate the same receptors that GnRH does, since they are present continuously and not in a pulsatile manner, they serve to inhibit the pituitary gland and therefore block the whole chain. (wikipedia.org)
  • precocious puberty
  • Also used for androgen-dependent indications in women and transgender women, precocious puberty in boys, and as a means of chemical castration for sexual deviation in men. (wikipedia.org)
  • CPA is used in the treatment of prostate cancer, precocious puberty, androgen-dependent skin and hair conditions such as acne, seborrhea, hirsutism (excessive hair growth), and androgenic alopecia (pattern hair loss), hyperandrogenism (e.g., in PCOS), and to reduce sex drive in sex offenders or men with paraphilias or hypersexuality. (wikipedia.org)
  • indications
  • Used for androgen-dependent indications in women and transgender women, particularly in the United States where cyproterone acetate is unavailable. (wikipedia.org)
  • The high-dose formulations are used to treat prostate cancer and certain other androgen-related indications while the low-dose formulations which also have an estrogen are used as combined birth control pills and are used in menopausal hormone therapy for the treatment of menopausal symptoms. (wikipedia.org)
  • therapeutic
  • Although there have been recent reports of significant responses with the use of cytotoxic agents in the treatment of castration-resistant disease ( 3 ), there remains an urgent need for new therapeutic strategies in both an adjuvant setting and following failure of androgen ablation therapy. (aacrjournals.org)
  • aromatase
  • melanocortin-4 receptor results in obesity in mice.The prolactin inhibition of follicle stimulating hormone-induced aromatase activity in. (tylerweitzman.tk)
  • tumors
  • Although the majority of these patients respond initially to androgen ablation, virtually all tumors eventually progress with castration-resistant disease ( 2 ). (aacrjournals.org)
  • binds
  • Along with the DBD, the LBD contributes to the dimerization interface of the receptor and in addition, binds coactivator and corepressor proteins. (wikipedia.org)
  • mifepristone
  • Some steroid antagonists: Androgen: cyproterone acetate Progestins: mifepristone, gestrinone Steroid hormones are transported through the blood by being bound to carrier proteins-serum proteins that bind them and increase the hormones' solubility in water. (wikipedia.org)
  • affinity
  • Some of these receptors such as FXR, LXR, and PPAR bind a number of metabolic intermediates such as fatty acids, bile acids and/or sterols with relatively low affinity. (wikipedia.org)
  • enzymes
  • In addition, it does not inhibit 5α-reductase and is not known to inhibit other enzymes involved in androgen steroidogenesis (e.g. (wikipedia.org)
  • aromatase
  • The excess cortisol may also affect other endocrine systems and cause, for example, insomnia, inhibited aromatase, reduced libido, impotence in men, and amenorrhoea/oligomenorrhea and infertility in women due to elevations in androgens. (wikipedia.org)
  • selectivity
  • exhibits 100-fold selectivity for OX1 over OX2 receptors. (adooq.com)
  • For these reasons, they have improved efficacy and selectivity as antiandrogens and do not lower androgen levels, instead acting solely by directly blocking the actions of androgens at the level of their biological target, the AR. (wikipedia.org)
  • genes
  • In response, these receptors work with other proteins to regulate the expression of specific genes, thereby controlling the development, homeostasis, and metabolism of the organism. (wikipedia.org)
  • mechanism
  • A direct mechanism of action involves homodimerization of the receptor, translocation via active transport into the nucleus, and binding to specific DNA responsive elements activating gene transcription. (wikipedia.org)
  • metabolism
  • Many types of ERβ receptors exist in order to help regulate gene expression and subsequent health in the body, but binding of 17βE2 (a naturally occurring estrogen) specifically improves cardiac metabolism. (wikipedia.org)
  • gene
  • Because the receptor gene is expressed in several forms, it has many different (pleiotropic) effects in different parts of the body. (wikipedia.org)
  • activity
  • Like all sulfonylureas, glimepiride acts as an insulin secretagogue.It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors. (hisupplier.com)
  • effects
  • However, it has a small (1%) risk of seizures and has central nervous system side effects like anxiety and insomnia due to off-target inhibition of the GABAA receptor that the first-generation NSAAs do not have. (wikipedia.org)