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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 .
[8] [7] Severe side effects include an increased risk of heart disease and osteoporosis. [8] Use during pregnancy may harm the baby. [8] Anastrozole is in the aromatase-inhibiting family of medications. [8] It works by blocking the production of estrogens in the body, and hence has antiestrogenic effects. [8]
The stilbene core (similar to the nonsteroidal estrogen, diethylstilbestrol) essentially mimics steroidal estrogens such as 17β-estradiol, while the side chain overlays with the 11th position of the steroid nucleus. [9] Triphenylethylene derivatives have an additional phenyl group attached to the ethylene bridge group.
Enclomifene is the (E)-stereoisomer of clomifene, while zuclomifene is the (Z)-stereoisomer. [ 4 ] [ 5 ] Whereas zuclomifene is more estrogenic , enclomifene is more antiestrogenic . [ 3 ] In accordance, unlike enclomifene, zuclomifene is antigonadotropic due to activation of the ER and reduces testosterone levels in men. [ 3 ]
The side effects of cyproterone acetate (CPA), a steroidal antiandrogen and progestin, including its frequent and rare side effects, have been studied and characterized.It is generally well-tolerated and has a mild side-effect profile, regardless of dosage, when it used as a progestin or antiandrogen in combination with an estrogen such as ethinylestradiol or estradiol valerate in women.
Hormone and metabolic modulators modify the effects of hormones or accelerate or slow down enzyme reactions, for example anti-Estrogens are substances that block the effects of estrogen in the body (usually to prevent tumors) and are used by athletes to counter the side effects of steroids. [15]
In particular, estrogen applied topically may have a different spectrum of side effects than when administered orally, [11] and transdermal estrogens do not affect clotting as they are absorbed directly into the systemic circulation, avoiding first-pass metabolism in the liver.
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 ...
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