How Do Selective Estrogen Receptor Modulators Work?

Reviewed on 1/21/2022

How do selective estrogen receptor modulators work?

Selective estrogen receptor modulators (SERM) are a class of medications used to relieve postmenopausal symptoms and to prevent bone loss (osteoporosis) associated with menopause. SERMs are also used to treat ovulatory dysfunction and to reduce the risk of invasive breast cancer in postmenopausal women at risk or who have osteoporosis.

Selective estrogen receptor modulators work by modulating the activity of estrogen receptors, proteins in cells that are activated by estrogen. Estrogen is a hormone that has many important functions including the development of female secondary sexual characteristics, regulation of reproductive cycle, and maintenance of bone health.

Selective estrogen receptor modulators have both estrogen agonistic and antagonistic properties, depending on the type of tissue. SERMs bind to estrogen receptors and activate estrogen pathways in some tissue while blocking its effects in other types of tissue. SERMs work in the following ways:

Selective estrogen receptor modulators may also be combined with estrogen for postmenopausal women with an intact uterus, who are undergoing estrogen replacement therapy. SERMs reduce the risk of endometrial hyperplasia that can occur with estrogen therapy.

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How are selective estrogen receptor modulators used?

Selective estrogen receptor modulators are oral tablets approved by the FDA for use in the following conditions:

  • Menopausal vasomotor symptoms (hot flashes)
  • Prevention and treatment of postmenopausal osteoporosis
  • Treatment of ovulatory dysfunction in women desiring pregnancy
  • Vaginal dryness due to vulvar and vaginal atrophy in menopause
  • Moderate to severe dyspareunia (painful sexual intercourse due to perimenopausal vaginal dryness)
  • Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis
  • Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer

What are side effects of selective estrogen receptor modulators?

Side effects of selective estrogen receptor modulators may include the following:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with travel medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

What are names of selective estrogen receptor modulator drugs?

Generic and brand names of selective estrogen receptor modulator drugs include:

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References
https://reference.medscape.com/drugs/selective-estrogen-receptor-modulators

https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022247s000lbl.pdf

https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203505s000lbl.pdf

https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf

https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/016131s026lbl.pdf

https://www.uptodate.com/contents/ovulation-induction-with-clomiphene-citrate

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