1. MHT, SERM, TSEC Drugs Flashcards
Menopausal Hormone therapy MHT are used for symptoms of menopause, which include night sweats, vaginal dryness, sleep disturbances, mood issues urinary incontinence and?
Hot flahses
Bone effects such as fracture and osteoporosis as well as what effects increase during menopause?
Cardiovascular effects (ACS/MI)
Tx for menopausal symptoms is estrogen, with or without progestin, with progestin in what situation?
In women with uteruses becuase there is an inc risk of endometrial hyperplasia/carcinoma from unopposed tissue proliferation
What therapy provides hormone regulation and pregnancy protection?
CHC (Combined hormone contraceptives)
The follow are the availble estrogenic forms of MHT… Estradiol, conjugated estrogens (CE), esterified estrogens (EE), and estropipate, which two are the most common?
Estradiol Conjugated Estrogens (CE)
The following are the availible progestrinic compoments of MHT: medroxyprogesterone (MPA-w CE), methyltestosterone (w EE), and what which is usually given alone?
Progesterone
all oppose estrogen’s effects on the uterus
The MOA of estrogen is to bind estrogen receptors (ER) a/b in tissues, transfer it into the nucleus resulting in increased gene and protein expression resulting in?
physiological responses
Estrogen causes endometrial proliferation in the uterus, which is why it must be given with what to oppose the endometrial hyperplasia/carcinoma risk?
Progestin
Along with endometrial proliferation, estrogen also causes decreased production of cholesterol, anti-thrombin and osteoclasts (good for osteoporosis), as well as increased production of TGs/HDL, clotting factors and platelet?
Aggregation (bad)
Women’s health initiative (WHI) study examines MHTs beneficial or preventive effects on heart disease, osteoporosis related fractures and risk of various cancers
MEOW
WHI tested postmenopausal women with estrogen and progestin combination to see harms and benefits. Harms were numerous, including increased breast cancer, CAD, dementia, stroke, venous thromboembolism (VTE), benefits were few, including decrease in DM, colorectal cancer and?
Fractures
WHI also tested postmenopausal women with estrogen alone and the harms included, GB disease, urinary incontinence, VTE, stroke and dementia, benefits included decrease in fractures and DM as well as what cancer?
Breast Cancer (invasive)
WHI study found that benefits outweigh risks in postmenopausal women, and MHT should not be used to prevent CVD or dementia… MHT very effectively minimizes and treats what symptoms and changes, however?
Vasomotor symptoms and vaginal changes
Points of agreement:
- for younger women, MHT acceptable for mod-sev menopausal sxs up to 59 or within 10 years of menopause
- vaginal symptoms only- patients should be treated with?
low doses of vaginal topical estrogen
Points of agreement:
- women w a uterus need to take progestin to prevent uterine cancer
- women with blood clots/strokes: both estrogen alone and combined increase risk, but risk is least in what age group?
50-59 y/o
Points of agreement:
- for women at inc risk breast cancer: inc risk seen in 3-5 years of continous estrogen w progestin therapy…
* **ALL risks and benefits are attenuated/eliminated several years after?
MHT is stopped
MHT given lowest dose and shortest duration possible
SERMs: selective estrogen receptor modulators goal is to have beneficial proestrogenic agonist actions in select tissues and anti estrogenic in other tissues such as brain breast endometrium and?
bone
TSECs: tissue selective estrogen COMPLEXES has a goal that combines the unique elements of a SERM with an estrogen compound- making a?
Complex (2 in 1)
Organize the following drugs into TSECs and SERMs…
Ospemifene
Clomiphene
Bazedoxifene
SERMs: Ospemifene, Clomiphene
TSECs: Bazedoxifene (w/ CE)
What drug is used for tx of mod-severe dyspareunia (painful SEX), which is a symptom of vulvar and vaginal atrophy (VVA) of menopause?
Ospemifene
topical is first line however
Ospemifene is an estrogen agonist in the vagina, and anti-estrogenic on the breast. It increases superficial cell growth, inc vaginal excretions, decreases vag pH, and reduces pain, there is NO known increased risk of?
endometrium cancer - no progestin needed in women w uterus
Ospemifene has the same SE as estrogen including: hot flashes, effects on coagulation (stroke/VTE), endometrial thickening and hyperplasia but no?
progression to endometrial cancer has been reported thus far
Ospemifene contraindications are the same as estrogens, including abnomal vaginal bleeding, thromboembolic diseases (CVA/MI/VTE/PE), and estrogen related neoplasia such as uterine, ovarian and ?
breast
Bazedoxifene w CE is indicated for women with INTACT uterus, for tx of moderate to severe vasomotor symptoms due to menopause in women w uterus, also used for prevention of post-menopausal?
osteoporosis in women with a uterus
Bazedoxifene has antagonisitic activity in endometrium (replaces the progestin concept in women w uterus) and in breast tissue, but also as agonist effects in BONE (CE). It does NOT stimulate endometrial proliferation and destroys what malignant cells?
HER2 maligant cells
see less vaginal bleeding
Bazedoxifene SE have all estrogen related SE because of the CE, and Bazedoxifene specific SE including worsening hot flashes/sweating. Contraindicated in all situations in which?
estrogens are contraindicated
Clomiphene (SERM) is purely anti-estrogenic in actions, and is indicated for infertility in anovulatory women, with a MOA that primarily blocks inhibitory actions of?
estrogen on hypothalamus GnRH and pituitary gonadotropin release
(inc gonadtropin secretion= stimulate ovaries to develop oocyte follicles) dosed oral at days 5 and 9 of cycle
Clomiphene has most significant effect on induction of ovulation in women with amenorrhea, PCOS, and dysfunctional bleeding with?
Anovulartory cycles
Clomiphene used in infertility has SE that include, multiple births (3-5% inc risk twins), ovarian cysts leading to ovarian cancer, luteal phase dysfunction and ?
hot flashes
