Estrogen Drugs

Question 0

Aromatase Inhibitors

Answer 0

Aromatase inhibitors: Block the synthesis of estrogen in post-menopausal women and are used in the treatment of breast cancer as well as ovarian cancer in post-menopausal women.

Question 1

Fulvestrant

Answer 1

Fulvestrant: Estrogen receptor antagonist. Typically used in aggressive breast cancers.Used to treat metastatic estrogen-dependent breast cancer, also increases the proteosomal degradation of estrogen receptors so it downregulates the levels of estrogen receptors.

Question 2

Clomiphene

Answer 2

Clomiphene: SERM. Used in the treatment of infertility. Blocks estrogen binding in the anterior pituitary, leading to increased release of GnRH and stimulation of ovulation. This serves to inhibit the negative feedback estrogen would normally have on the anterior pituitary, allowing more GnRH to be produced. Antagonist in the anterior pituitary, but not in the ovaries.

Question 3

Raloxifene

Answer 3

Raloxifene: SERM. Second generation drug of tamoxifen. Used to treat estrogen-dependent breast cancer as well as uterine cancer. Also used to treat osteoporosis for post-menopausal women. Used after surgery of tumor removal and after radiation therapy.

Question 4

Tamoxifen

Answer 4

Tamoxifen: SERM. Antagonist of estrogen receptors in the breast. Useful in decreasing the resurgence of breast cancer after surgery for tumor removal or radiation therapy. Used as a preventative measure to prevent new breast cancers from arising. Good Effects: lowers LDL cholesterol, decreases risk of breast cancer, strengthens bones. Bad Effects: increases risk of uterine cancer and increases risk of blood clots.