estrogen & progestins

estrogen

MOA: works on sex characteristics for women, metabolic actions (bones & heart); vasomotor symptoms; genitourinary; mental

USE: hormone therapy (with progestin!); female hypogonadism or turner syndrome; acne; cancer palliation (advanced prostate cancer & metastatic breast cancer); gender therapy

AE: endometrial hyperplasia, endometrial cancer, breast cancer, and cardiovascular thromboembolic events (hyperplasia and enodmetrial cancer can be resolved with progrestin); gallbladder disease, jaundice, headache; nausea; chloasma (patchy brown facial discoloration); fluid retention with edema

PK: oral (estradiol); transdermal (spray [Evamist], Gels [EstroGel, Digivigel and Elestrin], patches(can be applied one or twice a week; rotate sites) [Alora climara, estraderm]— spray is applied DAILY (one-three sprays; let it dry for 2 min before dressing and at least 30 minutes before showering) to forearm; gel is DAILY to one arm (shoulder to wrist or to the thigh); patches are applied to the skin of the trunk; intravaginal (inserts, creams(PM) and vaginal rings(leave it for 3 mos then replace; can stay during sex; if fall out wash it and reinsert); Parenteral (IM & IV

DI: CYP1A2, and CYP3A4 inducers may lower estrogen levels; inhibitors increase estrogen levels; decrease effectiveness of some anti diabetic drugs and thyroid preparations; anticoagulants and other meds with clotting

L; blood pressure, serum triglycerides, TSH , endometrial biopsy for unscheduled bleeding that continue for 6 mos

CI: hx of DVT, PE, stroke or MI that occurs due to thromboembolic event. pregnant or vaginal bleeding without a know cause. hx of liver disease. estrogen dependent tumors, or breast cancer ;breast feeing

estrogen black box

increased risk for endometrial cancer

may increase risk of DVT and stroke

not for heart disease or dementia

phytoestrogens

plant based compound

selective estrogen receptor modulators

tamoxifen, raloxifene, ospemifene

use: tamoxifene- blocks ERs; prevents and treats breast cancer, activates ER: protects against osteoporosis and helps with lipids BUT puts risk for endometrial cancer and thromboembolism

raloxifene-does not activate ERs- no uterine risk; protects against breast cancer and osteoporosis; BUT increases risk of thromboembolism and causes hot flashes—approved for prevention and treatment of osteoporosis.

ospemifene- estrogen receptor agonist; approved for genitourinary symptoms of menopause

Duavee (conjugated estrogens/bazedoxifine)- for prevention of vasomotor symptoms and osteoporosis in post menopausal women with uterus.

progesterone

medroxyprogesterone acetate (Provera) (for endometrial hyperplasia) ; norethindronel norethindrone (Micronor)(; norgestimate and dropsirenone

use: menopausal hormone therapy; dysfunctional uterine bleeding; amenorrhea and endometriosis; endometrial hyperplasia (suppresses it) and carcinoma; supports early pregnancy (or pregnancy in general with corpus lutes deficiency); in vitro fertilization to prevent prematurity In patients with high risk for preterm birth

AE: breast tenderness; headache; abdominal discomfort; arthralgia (joint pain) and depression; spotting ; breakthrough bleeding; irregular menses; progestins with estrogen can cause breast cancer for postemonpausal women; fluid retention and weight ; amenorrhea

PK: oral ;IM, SUbq; intravaginal; intrauterine; transdermal

CI: undiagnosed abnormal vaginal bleeding; active thrombophlebitis (inflamed vein); acute liver disease, carcinoma of breast; breast feeding (Causes neonatal jaundice) pregnant women in high doses

true or false: endometrial risk is increased in patients with a uterus who take unopposed estrogen

true!

menopausal hormone therapy consist of what and why; s/s it is trying to alleviate

low dose of estrogen (with or whithout progestin)

to compensate for the loss of estrogen that happens during menopause

typically vasomotor symptoms(hot flashes; drenching sweats) prevention of urogenital atrophy , prevention of osteoporosis and fractures

AE of hormone therapy

increase risk of cardiovascular events; increase thromboembolic events like DVT and stroke; breast cancer (EPT); HT in OA >65 increases risk for dementia

hormonal therapy preparations: oral medication names

conjugated equine estrogens (Premarin)

estradiol (Estrace)

estropipate

hormonal therapy preparations: transdermal therapy

estradiol

hormonal therapy preparations: oral estrogen and progestin

conjugated equine estrogen/medroxyprogesterone acetate (PrempO)

estradiol/norethindrone acetate (Activella)

ethinyl estradiol/norethinderone (Femhrt)

hormonal therapy preparations: combination estrogen/progestin patches

estradiol/norethindone (CombiPATCH)

estradiol/levonorgestrel (Climara PRO0

black box warning: estrogen therapy

endometrial cancer risk is increased in patients with a uterus who take unopposed estrogen

estrogen may incrase the risk for deep vein thrombosis and stroke

estrogen is not indicated for heart disease or dementia and may increase risk of dementia in ages >65

PATIENT EDUCATION: estrogen t

take medication with food and dosing at night

small breast cancer risk and endometrial cancer

avoid smoking exercise regularly