What drug is an estrogen antagonist?

What drug is an estrogen antagonist?

Tamoxifen is a nonsteroidal estrogen receptor antagonist that is mainly used for the treatment of estrogen receptor-positive breast cancer.

What is estrogen receptor antagonists used for?

Estrogen receptor antagonists bind to estrogen receptors and inhibit the action of estrogen. Estrogen controls the growth of certain types of breast cancers called estrogen receptor positive cancers. So estrogen receptor antagonists are useful in treating patients with estrogen sensitive breast cancers.

Is Tamoxifen estrogen antagonist?

Tamoxifen is both an antagonist and an agonist of the estrogen receptor. However, a molecular explanation exists for this apparent paradox. The dual action is a function of the estrogen receptor complex present in a particular cell or tissue.

Is estrogen an agonist or antagonist?

Droloxifene is growth inhibitory in MCF-7 human breast cancer cells and therefore acts as an antagonist, whereas estrogen is mitogenic to these cells and acts as an agonist.

What are the side effects of estrogen blockers?

More common side effects

• Hot flashes. A hot flash is also called a hot flush.
• Vaginal dryness and other vaginal issues. Vaginal dryness and vaginal discharge can be bothersome.
• Fatigue.
• Nausea and vomiting.
• Diarrhea.
• Constipation.
• Weight gain.
• Mood swings.

Why are aromatase inhibitors better than tamoxifen?

Aromatase inhibitors are, for postmenopausal women, an even more effective endocrine treatment than tamoxifen, with further proportional reductions in recurrence rates of about 30%. Aromatase inhibitors versus tamoxifen in early breast cancer: patient-level meta-analysis of the randomised trials.

Why is tamoxifen an antagonist?

In breast tissue, tamoxifen acts as an ER antagonist so that transcription of estrogen-responsive genes is inhibited. A beneficial side effect of tamoxifen is that it prevents bone loss by acting as an ER agonist (i.e., mimicking the effects of estrogen) in this cell type.

What are estrogen agonists?

Estrogen agonist/antagonists are used for fertility, breast cancer, PCOS, and osteoporosis. They work by changing hormone levels in the body.

Why is tamoxifen a SERM?

Tamoxifen and raloxifene are both selective estrogen receptor modulators (SERMs). The medicines can block estrogen mediated breast cancer growth and development but will also maintain bone density in postmenopausal women and lower circulating cholesterol.

What happens to your body when taking an estrogen blocker?

Because these drugs affect hormones, side effects often include symptoms associated with menopause: Hot flashes, mood swings, night sweats, osteoporosis, vaginal discharge and vaginal dryness are among the most common.

Do I really need an aromatase inhibitor?

Aromatase inhibitors are not useful for pre-menopausal women, so they should only be used if you have gone through menopause. These drugs can cause bone thinning (osteoporosis), so they’re not likely to be a good option in women who already have thin or weakened bones.

Which is an adverse effect of estrogen receptor antagonists?

Side effects of antiestrogens include hot flashes, osteoporosis, breast atrophy, vaginal dryness, and vaginal atrophy. In addition, they may cause depression and reduced libido.

What is a SERM drug?

Selective estrogen receptor modulators (SERMs) are now being used as a treatment for breast cancer, osteoporosis and postmenopausal symptoms, as these drugs have features that can act as an estrogen agonist and an antagonist, depending on the target tissue.