Simple and short presentation for the mechanism of action, pharmacological actions, indications and adverse effects of selective estrogen receptor modulators (SERMs).
Hi today we will talk about selective estrogen receptor modulators or firms by the term sir it means that these are drugs with tissue selective actions that is they have east hygienic action in some tissues and anti estrogen ik action in some other tissues so the main objective of using these drugs is first to produce beneficiary sturgeon ik effects in some tissues
Such as the bone and the liver and to prevent harmful is gigantic effects in some other tissues such as the breast now we have a look at some commonly used somes so we have clomiphene tamoxifen raloxifene thor emma theme and or minoxidil in the subsequent slides we will focus our discussion on the first three somes that is clomiphene tamoxifen and raloxifene so
First we will talk about the pharmacological action of serbs in this slide we will talk about tamoxifen and raloxifene and in the next slide we will talk about clomiphene so if we look at them oxygen and a toxic mean both of them produces easter edenic effects on bone leading to decreased bone desorption and decreased fracture risk they act on the liver leading to
Decreased ldl and total cholesterol they act on the blood leading to an increased incidence of dvt that is deep venous thrombosis and pulmonary embolism they also act on the uterus but here there is a contrast the moxa pain causes an increased endometrial proliferation hence leading to an increased risk of endometrial cancer while raloxifene does not cause increased
Endometrial proliferation and so there is no increased risk of endometrial cancer now coming to the anti estrogen effects of tamoxifen and raloxifene so they have anti estrogen effects on the breast leading to decreased breast cancer cell proliferation they also have inherently straightening effects on the periphery issues leading to heart pressures and vomiting so
The takeaway from this slide is that both tamoxifen and raloxifene decreased bone resorption decreased fracture risk decreased breast cancer cell proliferation but tamoxifen causes an increased the endometrial product creation but raloxifene does not cause an increased endometrial proliferation so coming to the next drug claw machine claw machine mainly inhibits
The east region receptors in the hypothalamus since chromatin blocks these receptor estrogen then cannot act on these receptors this blocks the negative feedback effect of estrogen on the hypothalamus so the hypothalamus starts sensing that there is a deficiency of easter egg on in the body it therefore starts releasing more of gonadotropin-releasing hormone that
Is g and rh this gnrh goes and acts on the pituitary to increase the secretion of gonadotropic that is a facet and lh follicular stimulating hormone and luteinizing hormone the increased fsh and lh acts on the ovary to cause ovarian stimulation this is allison ovulation now moving to the adverse effects of psalms clomiphene as we discussed causes ovarian stimulation
And therefore has a potential to cause ovarian hyperstimulation syndrome polycystic ovaries multiple pregnancies it may also cause nausea vomiting and hot flashes tamoxifen as we discussed increases endometrial proliferation all therefore there is an increased risk of endometrial cancer there is also an increased risk of bep venous thrombosis and pulmonary embolism
It may also cause nausea vomiting and hot flashes raloxifene does not cause increased endometrial proliferation therefore it does not have an increased endometrial cancer risk however there is an increased risk of deep venous thrombosis and pulmonary embolism it may also cause hot flashes and leg cramps lastly we talked about the indication or uses of clomiphene
Tamoxifen and raloxifene so clomiphene because it stimulates the ovaries it is used in female infertility which is due to an ovulation it is also used in male infertility and in vitro fertilization tamoxifen is used in the treatment and prevention of breast cancer both pre and post menopausal while raloxifene is used in the treatment and prevention of osteoporosis
In postmenopausal woman so to remember as it is highlighted in red clomiphene for infertility tamoxifen for breast cancer and raloxifene for osteoporosis thanks for watching if you liked this video and found it beneficial please do hear but do not forget to press the subscribe button thank you
Transcribed from video
SERM – Selective Estrogen Receptor Modulators By Pharmacology Made Simple By Dr. Yogesh Gulati
