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Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production .
Bicalutamide is used primarily in the treatment of early and advanced prostate cancer. [1] It is approved at a dosage of 50 mg/day as a combination therapy with a gonadotropin-releasing hormone analogue (GnRH analogue) or orchiectomy (that is, surgical or medical castration) in the treatment of stage D2 metastatic prostate cancer (mPC), [2] [3] and as a monotherapy at a dosage of 150 mg/day ...
Estradiol, testosterone, and prolactin levels with 100 mg/month estradiol undecylate in oil by intramuscular injection in 14 to 28 men with prostate cancer. [65] A follow-up of the study with more men and with additional hormones was also subsequently published. [70] Sources were Jacobi & Altwein (1979) and Derra (1981). [65] [70]
Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer.
In accordance, clomifene, a selective estrogen receptor modulator with antiestrogenic activity, has been found to increase testosterone levels to as much as 250% of initial values in men with hypogonadism, [103] and a study of clomifene treatment in normal men observed increases in FSH and LH levels of 70–360% and 200–700%, respectively ...
[19] [20] [21] It also is used for suppressing estrogen production in transgender men. [22] It is considered a possible treatment for paraphilias. [23] Leuprorelin has been tested as a treatment for reducing sexual urges in pedophiles and other cases of paraphilia. [24] [25]
Any circulating estrogen in post-menopausal women as well as men is the result of estrogen escaping local metabolism and entering the circulatory system. [ 12 ] Exemestane is an irreversible, steroidal aromatase inactivator of type I, structurally related to the natural substrate 4-androstenedione .
Triptorelin is used to treat prostate cancer as part of androgen deprivation therapy. [9]Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people (in conjunction with estradiol valerate for trans women or testosterone for trans men).
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