Selective Estrogen Receptor Modulators (SERMs) – Gynecology | Lecturio


[Music] hi today I’d like to talk to you about the gynecologic care of women with breast cancer but before I do that I just want to review some of the medications that we use to treat women with breast cancer there’s a whole group of medications called selective estrogen receptor modulators or CERN’s for short this is a class of synthetic compounds that actually interact with the estrogen receptor and so depending on what tissue they are interacting with the estrogen receptor they have different effects either agonistic or antagonistic and there’s different ones so first let’s review what the structure of estradiol looks like so 17 beta estradiol looks like this while clomiphene citrate another selective estrogen receptor modulator which is used for infertility ovulation induction looks like this and tamoxifen which you’ve probably heard of is used to treat breast cancer at least Estrin receptor positive breast cancer looks like this so hormones and selective Estrin receptor modulators work this way hormones or the medications the serbs go into the circulation they diffuse into a cell through the cytoplasm and into the nucleus to bind to the estrogen receptors you either Estrin receptor alpha or Estrin receptor beta these receptors then interact with the DNA within the nucleus and change transcription that is the making of messenger RNA or mRNA the mRNA provides the message at the ribosomes to make proteins so let’s now talk about breast cancer in the u.s. breast cancer is the most common non cutaneous malignancy among women representing four in ten female cancer survivors in the US long term survival is common after breast cancer with the five-year survival rate being almost 90 percent which is very good news the most common malignancy that affects women younger than 45 is breast cancer so after surviving breast cancer it’s important to know how to take care of these patients so patients who have estrogen receptor-positive tumors will be given tamoxifen to down-regulate estrogen within their breast tissue so again to review selective estrogen receptor modulators compete with the estrogen compete for the estrogen receptor and blocks the growth of er-positive cancer cells they have mixed agonist and antagonist capability and they are most applicable in premenopausal patients so patients who are still reproductively capable it is currently recommended that the treatment be extended from five now to ten years tamoxifen though does have risks there are increased risk of stroke increased risk of endometrial cancer blood clots osteopenia which is before osteoporosis with decreased bone density there’s an increased risk of fractures hot flushes which is commonly called in layman’s terms hot flashes changes in menstruation mood changes and increased triglycerides which can cause long-term cardiovascular problems there are another group of drugs that we use and those are called aromatase inhibitors and they’re more appropriate for the postmenopausal patient or a woman who has already gone through menopause so let’s review how aromatase inhibitors work so strategy gnosis that is the formation of steroids occurs with cholesterol going down a very long pathway that leads to androgens turning in to estrogens through aromatisse which is also abbreviated sip 19 a one aromatase inhibitors inhibit this enzyme so that there’s less estrogen being made that is ester own or estradiol an aromatase inhibitors do have symptomatic symptoms including vaginal dryness decreased libido decreased libido essentially means decreased sexual drive there’s increased musculoskeletal pain and there’s also increase in cholesterol which can have long-term cardiovascular effects [Music]

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