MHT and SERMS Flashcards
(40 cards)
What are some symptoms of menopause?
- Hot flashes
- Night sweats
- Vaginal dryness/painful intercourse/sexual dysfunction
- Sleep disturbances
- Mood/cognitive issues
- Urinary incontinence
What is the primary therapy for menopausal symptoms?
- Estrogen
- With/without the addition of progestin
- Women with an intact uterus must also be on a progestin
Why must a women with a uterus be on a progestin as well as estrogen?
- To reduce the risk of endometrial hyperplasia/carcinoma from unopposed tissue proliferation with prolonged duration
What are the four estrogenic forms for menopausal hormone therapy?
- Estradiol: in acetate form (tablet/vaginal ring) and cypionate form (injection
- Conjugated estrogens (CE): blend of 6 known estrogen derivatives
- Esterified estrogens (EE): combination of Na+ estrone sulfate and Na+ equilin sulfate
- Estropipate: crystalline estrone solubilized with sulfate and stabilized with piperazine
What are some available progestinic components used for menopausal hormone therapy?
- Medroxyprogesterone
- Methyltestosterone
- Progesterone
What is the MOA of estrogen?
- Bind to estrogen receptors in various tissues, transferred into nucleus resulting in increased gene and ultimately protein, expression resulting in physiological responses
What are the effects of estrogen?
- It has a proliferative effect which causes there to be a requirement that if a woman still has their uterus, need to give a progestin as well to counteract the estrogen
What does estrogen decrease in the body?
- Cholesterol
- Anti-thrombin III
- Osteoclastic activity (bone turnover)
What does estrogen increase in the body?
- Triglycerides and HDL-C
- Clotting factor
- Platelet aggregation
- Sodium/fluid retention
- Thyroid binding globulin (TBG)
What was the objective of the women’s health initiative study?
- Examine MHT’s purported beneficial or preventative effects on heart disease, osteoporosis-related fractures, and risk of various cancers
What are some of the harms that were found in dual menopausal hormone therapy?
- Breast cancer (invasive)
- Coronary heart disease
- Dementia
- Gallbladder disease
- Stroke
- Venous thromboembolism
- Urinary incontinence
What are some benefits that were found in dual menopausal hormone therapy?
- Diabetes
- All fractures
- Colorectal cancer
What are some harms found in estrogen only MHT?
- Dementia
- Gallbladder disease
- Stroke
- Venous thromboembolism
- Urinary incontinence
What are some benefits found in estrogen only MTH?
- Breast cancer
- All fractures
- Diabetes
What is MHT very effective at treating?
- Vasomotor symptoms and vaginal changes (and associated complications)
What is MHT not effective at treating?
- Prevent CVD or dementia
- Benefit on bone and colon cancer are outweighed by the overall risks
What is the MHT treatment for younger women?
- Acceptable option for treating severe menopausal symptoms in relatively young and healthy women
- Individulaization with risk-stratification is key
- Some organizations recommending patch over oral therapy
What is the MHT treatment for women with vaginal symptoms only?
- Low doses of vaginal estrogen (topical)
What is the MHT treatment for women with a uterus?
- Need to take a progestin along with estrogen to prevent uterine cancer
- Women who have had uterus surgically removed able to take estrogen alone
What is the MHT treatment for women with risk of blood clots/stroke?
- Both estrogen alone therapy and estrogen with progestin therapy increase risk of blood clots
- Although risks of blood clots and strokes increase with either type of MHT, risk is less in 50-59 year olds
What is the MTH treatment for women at risk of breast cancer?
- An increased risk of breast cancer is seen within 3-5 years of continuous estrogen with progestin therapy
What is the take home message for MHT?
- Use lowest dose possible to control symptoms
- Treat for the shortest duration possible and reevaluate at least yearly for ongoing need of therapy
What is the goal of SERMs?
- Beneficial pro-estrogenic actions in select tissues with beneficial anti-estrogenic actions in other tissues (brain, bone, breast, endometrium)
What is the goal of TSECs?
- Combines the unique elements of a SERM with an estrogen compound
