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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 .
[64] [58] Symptoms that may indicate liver dysfunction include nausea, vomiting, abdominal pain, fatigue, anorexia, "flu-like" symptoms, dark urine, and jaundice. [64] As of 2022, at least 10 case reports of bicalutamide-associated hepatotoxicity or liver failure, two of which were fatal, have been published in the literature.
Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
In transgender women, breast development is a desired effect of antiandrogen or estrogen treatment. [63] [212] Breast development and gynecomastia induced by bicalutamide is thought to be mediated by increased activation of the ER secondary to blockade of the AR (resulting in disinhibition of the ER in breast tissue) and increased levels of ...
An estrogen synthesis inhibitor is a type of drug which inhibits the enzymatic synthesis of estrogens, such as estradiol. They include: They include: Aromatase inhibitors (CYP19A1 inhibitors): inhibit the synthesis of estrogens from androgens
Raloxifene is a selective estrogen receptor modulator (SERM) and hence is a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues. [6] It has estrogenic activity in some tissues, such as bone and the liver , and antiestrogenic activity in other tissues, such as the breasts and uterus . [ 6 ]
Enclomifene (INN Tooltip International Nonproprietary Name), or enclomiphene (USAN Tooltip United States Adopted Name), a nonsteroidal selective estrogen receptor modulator of the triphenylethylene group, acts by antagonizing the estrogen receptor (ER) in the pituitary gland, which reduces negative feedback by estrogen on the hypothalamic-pituitary-gonadal axis, thereby increasing gonadotropin ...
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally ...