GW’s CREOG Video Project: Learn about some of the side effects of Aromatase Inhibitors, Tamoxifen and Raloxifene by Dr. Catherine Hoeppnner
This powerplant will be reviewing the side effects of aromatase inhibitors tamoxifen and roloxafin as part of the creog video project the objectives will be to review and describe the indication for using aromatase inhibitors tamoxifen and raloxifen as well as understanding the side effects of these drugs before delving into the side effects of aromatase
Inhibitors tamoxifen and riloxafin we will describe briefly the indications for use mainly being chemoprevention and adjuvant endocrine therapy chemoprevention is the primary prevention of cancer specifically breast cancer for tamoxifen and riloxavin these drugs are fda approved for use in prevention of breast cancer there are various criteria that must be met a
Few which are listed here these include age greater than or equal to 35 and either a greater than 1.7 percent five-year risk of breast cancer or thoracic radiation prior to age 30 or atypical hyperplasia or history of globular carcinoma in situ adjuvant endocrine therapy is recommended in those with hormone receptor positive breast cancer for at least five years
Tamoxifen or aromatase inhibitors are used for adjuvant endocrine therapy improvements are seen in risk of recurrence of breast cancer development of secondary breast cancers and overall survival the approach for treatment depends on menopausal status the average age of menopause is 51 years old this is defined as no menstrual periods for greater than 12 months
Or more in the context of this powerpoint this is also defined as no menstrual periods for greater than 12 months in the absence of tamoxifen chemotherapy or other ovarian suppression with a serum estradiol in the postmenopausal range in the context of a patient taking tamoxifen a patient may be amenorrhea and also be defined as being menopausal if their fsh
And serum estradiol are in the postmenopausal range additionally a patient may be iatrogenically postmenopausal if they’ve had a history of a bilateral oophorectomy aromatase inhibitors include medications such as anastrozole letrozole and eczema stain aromatase inhibitors work by inhibiting the enzyme aromatase thereby blocking the conversion of androgens to
Estrogens and decreasing serum levels of estrogen aromatase inhibitors are the preferred adjuvant endocrine therapy in postmenopausal women with breast cancer it is important to know that these are contraindicated in those with preserved ovarian function there are many side effects but some are more commonly seen than others loss of bone density is one important
Side effect additionally joint pain and stiffness is also seen this can be treated either with exercise and nsaids a temporary discontinuation of the medication or initiating diloxatine additional side effects include sexual dysfunction and vasomotor symptoms tamoxifen is in the class of medications called selective estrogen receptor modulators or serms these
Work by competitive antagonism of estrogen receptors in the breast thereby inhibiting growth of breast cancer cells it produces an estrogen effect in the uterus bone liver and coagulation system it is used for both chemo prevention of breast cancer and those with a high risk of breast cancer as well as adjuvant endocrine therapy in those with a history of breast
Cancer one of the biggest side effects is dvt or vte there is also an increased incidence of endometrial hyperplasia and cancer these risks of dvt and vte or thromboembolism as well as endometrial hyperplasia and cancer are age related however the overall risk of these remains low for example the risk of endometrial cancer in those with tamoxifen is four percent
Versus one percent other side effects include cataracts and vasomotor symptoms maloxane is also a serum like tamoxifen however it is important to note specifically which tissues it acts as an antagonist or protagonist on estrogen receptors raloxophen is competitive antagonist of estrogen receptors in the breast thereby inhibiting growth of breast cancer cells
It is also an antagonist of estrogen receptors in the uterus similar to tamoxifen it has estrogen effects in the bones as well as lipids it is used for chemo prevention for breast cancer and is also fda approved for the treatment of osteoporosis while it may have a side effect of thromboembolism it is not as high of a risk as tamoxifen other side effects include
Cataracts and vasomotor symptoms similar to tamoxifen now how do you choose what medication to use it is important to distinguish between chemo prevention or preventing primary breast cancer versus adjuvant endocrine therapy if a patient is going to be prescribed chemo prevention first ask is the patient menopausal or not if the patient is not menopausal you
Can use tamoxifen if the patient is menopausal consider whether or not this patient has a uterus and if so consider using riloxavin for adjuvant endocrine therapy similarly ask yourself is the patient menopausal or not if the patient is premenopausal again default would be to use tamoxifen if the patient is menopausal do they have a normal bone mineral density
Written here as bmd if not use tamoxifen because remember aromatase inhibitors are associated with a loss of bone mineral density if they have a normal bone mineral density you may use either a serum or an aromatase inhibitor lastly consider what their overall vte risk would be if they are not at an increased risk of thermal embolism you could use tamoxifen
Or aromatase inhibitor if they are at an increased risk of vte consider just using aromatase inhibitor now this is a very oversimplified algorithm for prescribing either serms or aromatase inhibitors it is important to take into account the patient’s history and their overall risk of osteoporosis side effect profile as well as thromboembolism risk this summary
Table is courtesy of dr lindsey flugner one of our wonderful graduates it nicely outlines the pros and cons of the serms tamoxifen and riloxavin as well as aromatase inhibitors going line by line you can see the indications as well as the risks here tamoxifen and aromatase inhibitors such as the nastrazole are used as adjuvant therapy for er positive cancers
Tamoxifen and riloxavin are used as chemoprevention of breast cancer whereas aromatase inhibitors are not you may see improved bone mineral density with tamoxifen and roloxavin tamoxifen has an improved fracture risk specifically for non-vertebral fractures and riloxavin has improved vertebral fracture risk riloxavin is also fda approved for osteoporosis aromatase
Inhibitors do not improve bone mineral density conversely they actually increase the risk of osteoporosis across all categories you can see that vasomotor symptoms or hot flushes are seen in all categories there is an increased risk of vte or thromboembolism however the risk is highest with tamoxifen tamoxifen also has the highest risk of endometrial cancer and
Cataracts one of the main side effects seen with aromatase inhibitors is joint and muscle pain lastly the main distinction based on age is that tamoxifen is the only fda approved medication to be used pre-menopausal
Transcribed from video
Side Effects of Aromatase Inhibitors, Tamoxifen and Raloxifene By EDU Chief GW
