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Anti-Estrogens and Antiprogestins – Reproductive Pharmacology

by Pravin Shukle, MD
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    Let's move on to anti-estrogenic agents. Let's start off with SERMs. What is a SERM? A SERM stands for selective estrogen receptor modulator. Now, the classic and prototypical drug that you really need to know well is tamoxifen. Tamoxifen is used as an ER agonist – pardon me, antagonist in breast tissue. It reduces the risk of breast cancer in those patients that are ER positive. Now, ER agonists in endometrial tissue promote endometrial hyperplasia and increase the risk of endometrial cancer. What are the side effects of tamoxifen? As an agonist, you can get hot flashes and prevent osteoporosis. As an antagonist, you increase the risk of venous thromboembolism. The next of the SERMs that are important to know is raloxifene. Now, raloxifene is used in a slightly different therapeutic area. It is approved for the prevention and treatment of osteoporosis. It has antagonistic effects that include reducing the risk of breast cancer, but its agonistic effects – there is no estrogenic effects on endometrial tissue, which is unlike tamoxifen. Now, the big issue here is, is that because it's working peripherally, but not on endometrial tissue, this is why we find that it's a particularly useful drug for treating diseases like osteoporosis. Other agents are used for menopausal symptoms as well and osteoporosis prevention alongside of estrogens. Clomiphene reduces negative feedback in pituitary tissue, so that increases LH and FSH secretion. This is an ovulation inducer in patients who are anovulatory. Let's move on to the full antagonists. Fulvestrant is a pure estrogen antagonist in all tissues. So, it is unlike the SERMs, in that it has antagonistic actions everywhere. The SERMs have agonistic actions in some tissues and antagonistic in others. It is used in breast cancer with resistance to tamoxifen. And it is used in women...

    About the Lecture

    The lecture Anti-Estrogens and Antiprogestins – Reproductive Pharmacology by Pravin Shukle, MD is from the course Reproductive Pharmacology. It contains the following chapters:

    • Antiestrogens – SERMs
    • Full Antagonists
    • Aromatase Inhibitors
    • Other Antiestrogens
    • Antiprogestins

    Included Quiz Questions

    1. Estrogen receptor antagonist in the breast Estrogen receptor agonist in the uterus
    2. Estrogen receptor antagonist in the breast Estrogen receptor antagonist in the uterus
    3. Estrogen receptor agonist in the breast Estrogen receptor agonist in the uterus
    4. Estrogen receptor agonist in the breast Estrogen receptor antagonist in the uterus
    5. Estrogen receptor antagonist in the breast With no activity in the uterus
    1. Raloxifene
    2. Tamoxifene
    3. Medroxyprogesterone
    4. Estradiol therapy
    5. Premarin, a therapy consisting of horse urine
    1. Increases ovulation rate
    2. Acts on the pituitary
    3. Agonist of GnRH receptors
    4. Works to reduce GnRH receptor function on pituitary
    5. Reduces LH and FSH
    1. Hirsutism
    2. Nausea
    3. Vomiting
    4. Cramping
    5. Bleeding

    Author of lecture Anti-Estrogens and Antiprogestins – Reproductive Pharmacology

     Pravin Shukle, MD

    Pravin Shukle, MD


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