Hormone Replacement Therapy Flashcards
Human estrogen replacements
- estradiol
- estrone
- estriol
synthetic estrogen replacements
- ethinyl estradiol
- mestranol
- conjugated estrogens
- diethylstilbestrol
phytoestrogen replacements
- soy
- red clover
- flax
- alfalfa
- black cohosh
- dong quai
Oral estrogens:
- conjugated estrogens
- Esterified estrogens
- Estropipate
- Mocronized estradiol
Progestogens:
- Dydrogesterone
- medroxyprogesterone
- micronized progesterone
- Norethindrone
- norgestrel
- levonorgestrel
how is estradiol metabolized
3A4
Estrogen Indic.
-relief of vasomotor symptoms
Estrogen ADRs:
-N, HA, breast tenderness, bleeding
Serious; CHD, CVA, VTE, breast ca, gallbladder disease
-less likely with transdermal
estrogen warning
- increased risk of stroke
- dementia
- CHD
why no unopposed estrogen in pt with uterus?
endometrial cancer
phytoestrogen risks:
- increased proliferation of breast tissue in vitro
- may decrease risk of breast ca. in asians
- women with breast cancer should avoid these
phytoestrogens may help with what part of menopause?
hot flashes
how does red clover interact with warfarin?
may increase bleeding
warning for black cohosh?
liver damage
wild yam ADRs:
vomitting
Flibanserin indications:
premenopausal hypoactive sexual desire disorder (HSDD)
Flibanserin contra:
P450, 3A4 inhibitors, hepatic impairment
flibanserin ADRs:
sedation, hypotension, syncope, cns depression,
REMS program: hypotension, syncope with EtOH use
NAMS guidelines:
- lowest dose, shortest duration
- estrogen most effective
- avoid compounded hormones
compounded estrogen:
biest: estradiol and estriol
Triest: estradiol, estrone, estriol
breast cancer tx:
-Selective estrogen receptormodulator (SERMs)
-steroidal estrogen receptor antagonist
-aromatase inhibitors
all anti estrogens
SERMs:
- tamoxifen
- toremifene
- Raloxifene
steroidal estrogen receptro antagonist
Fulvestrant
Aromatase inhibitors:
- Anastrozole
- Exemestane
- Letrozole
Tamoxifen uses:
- developed as OC
- adjuvant therapy for breast ca
- prevention in high risk women
Tamoxifen warnings:
- hypercalcemia
- uterine malignancies
- endometrial hyperplasia and polyps
- clots
- liver abnormalities
- ocular disorders
how is tamoxifen metabolized?
p450
tamoxifen adrs
vasomotor symptoms, vaginal atrophy, hair loss, n/v, menstrual irregularities, inc risk of VTE, inc risk of endometrial ca, live damage, retinal deposits, cataracts
DI’s from tamoxifen:
- Warfarin, anastrozole, letrozole, rifampin
- paroxetine, fluoxetine, bupropion- causes death
- prego category D
Raloxifene uses:
-breast cancer prevention in high risk post menopausal its
Tamoxifen vs. raloxifine:
Tamoxifene: better in preventing noninvasive breast ca, but higher incidence of clots
raloxifine: fever cases of uterine ca, fewer clots, fewer cataracts
Opemifene (SERM drug) Indic:
dyspareunia from vulvovaginal atrophy due to menopause
Opemifene contra:
Clots, CVA, MI, prego, estrogen-dependent neoplasia, undx genital bleed
Ospemifene ADRs:
Clots, hot flashes, vag discharge, muscle spasms, hyperhidrosis
Toremifene indic.
tx of metastatic breast cancer in postmenopausal women with estrogen-receptor positive or unknown tumors
toremifene ADRs:
- hypercalcemia,prolonged QT, endometrial hyperplasia
- hotflashes, sweating, N, dizziness, edema, cataracts, clots, LFT elevation
Toremifene DIs:
- p450, 3a4
- thiazides
Bazedoxifene/CE Indic:
moderate to severe vasomotor symptoms
-prevention of menopausal osteoporosis
bazedoxifene black box:
- endometrial ca in women with uterus
- CVD or dementia
- CVA and DVT
Aromatase inhibitors:
non-steroidal: anastrozole, letrozole
steroidal: exemestane
aromatase inhibitor Indic.
-first-line adjuvant breast ca tx in postmenopausal
aromatase inhibitors ADRs:
hot flashes, N, thin hair
Fulvestrant indic.
-postmenopausal women with hormone receptor positive metastatic breast ca that has progressed on tamoxifen
is fulvestrant good to use with p450 drugs?
yes
fulvestrant ADRs:
-N, asthenia, hot flashes, HA
