1. MHT, SERM, TSEC Drugs

Question 1

Menopausal Hormone therapy MHT are used for symptoms of menopause, which include night sweats, vaginal dryness, sleep disturbances, mood issues urinary incontinence and?

Answer 1

Hot flahses

Question 2

Bone effects such as fracture and osteoporosis as well as what effects increase during menopause?

Answer 2

Cardiovascular effects (ACS/MI)

Question 3

Tx for menopausal symptoms is estrogen, with or without progestin, with progestin in what situation?

Answer 3

In women with uteruses becuase there is an inc risk of endometrial hyperplasia/carcinoma from unopposed tissue proliferation

Question 4

What therapy provides hormone regulation and pregnancy protection?

Answer 4

CHC (Combined hormone contraceptives)

Question 5

The follow are the availble estrogenic forms of MHT… Estradiol, conjugated estrogens (CE), esterified estrogens (EE), and estropipate, which two are the most common?

Answer 5

Estradiol
Conjugated Estrogens (CE)

Question 6

The following are the availible progestrinic compoments of MHT: medroxyprogesterone (MPA-w CE), methyltestosterone (w EE), and what which is usually given alone?

Answer 6

Progesterone

all oppose estrogen’s effects on the uterus

Question 7

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?

Answer 7

physiological responses

Question 8

Estrogen causes endometrial proliferation in the uterus, which is why it must be given with what to oppose the endometrial hyperplasia/carcinoma risk?

Answer 8

Progestin

Question 9

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?

Answer 9

Aggregation (bad)

Question 10

Women’s health initiative (WHI) study examines MHTs beneficial or preventive effects on heart disease, osteoporosis related fractures and risk of various cancers

Answer 10

MEOW

Question 11

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?

Answer 11

Fractures

Question 12

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?

Answer 12

Breast Cancer (invasive)

Question 13

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?

Answer 13

Vasomotor symptoms and vaginal changes

Question 14

Points of agreement:

1. for younger women, MHT acceptable for mod-sev menopausal sxs up to 59 or within 10 years of menopause
2. vaginal symptoms only- patients should be treated with?

Answer 14

low doses of vaginal topical estrogen

Question 15

Points of agreement:

3. women w a uterus need to take progestin to prevent uterine cancer
4. women with blood clots/strokes: both estrogen alone and combined increase risk, but risk is least in what age group?

Answer 15

50-59 y/o

Question 16

Points of agreement:

5. 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?

Answer 16

MHT is stopped

MHT given lowest dose and shortest duration possible

Question 17

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?

Answer 17

bone

Question 18

TSECs: tissue selective estrogen COMPLEXES has a goal that combines the unique elements of a SERM with an estrogen compound- making a?

Answer 18

Complex (2 in 1)

Question 19

Organize the following drugs into TSECs and SERMs…
Ospemifene
Clomiphene
Bazedoxifene

Answer 19

SERMs: Ospemifene, Clomiphene
TSECs: Bazedoxifene (w/ CE)

Question 20

What drug is used for tx of mod-severe dyspareunia (painful SEX), which is a symptom of vulvar and vaginal atrophy (VVA) of menopause?

Answer 20

Ospemifene

topical is first line however

Question 21

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?

Answer 21

endometrium cancer - no progestin needed in women w uterus

Question 22

Ospemifene has the same SE as estrogen including: hot flashes, effects on coagulation (stroke/VTE), endometrial thickening and hyperplasia but no?

Answer 22

progression to endometrial cancer has been reported thus far

Question 23

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 ?

Answer 23

breast

Question 24

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?

Answer 24

osteoporosis in women with a uterus

Question 25

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?

Answer 25

HER2 maligant cells

see less vaginal bleeding

Question 26

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?

Answer 26

estrogens are contraindicated

Question 27

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?

Answer 27

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

Question 28

Clomiphene has most significant effect on induction of ovulation in women with amenorrhea, PCOS, and dysfunctional bleeding with?

Answer 28

Anovulartory cycles

Question 29

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 ?

Answer 29

hot flashes