sex hormones Flashcards
compare forms of estrogen
estradiol (E2) = primary
estrone (E1) = less active
ethinyl estradiol = MORE potent
what estrogen HRT is indicated for patients with intact uterus, no uterus, and at moderate CVD risk?
intact = estrogen + progestin
absent = estrogen
moderate CVD risk = avoid PO
what conditions is estrogen HRT contraindicated?
breast cancer
liver disease
stroke, CVD, high CVD risk
DVT
what drugs are progestins?
DPM2N3
Drospirenone Progesterone Megestrol Medroxyprogesterone Norethindrone Norgestrel Norgestimate
what is the MOA of progestins?
act on receptor of others (estrogen, androgen, mineralocorticoids)
suppresses ovulation by (-) feedback
How does progestin provide contraception?
suppress ovulation by dec. GnRH
Matures endometrial lining
Dec. transit of sperm (thickens mucus)
compare deficiency and excess of estrogen on endometrium
def: early cycle breakthrough bleeding; hypomenorrhea/amenorrhea
excess: other effects…
compare deficiency and excess of progestin on endometrium
def: late cycle bleed; hypermenorrhea
excess: hypOmenorrhea/amenorrhea
What women are CI for estrogen + progestin?
CVD, DVT/PE, Afib, stroke
smokers >35 YO
compare dosage forms of contraceptives
monophase = traditional
multiphasic = mimic natural hormone changes, may have less side effects
extended interval = placebo pills q3mos, less frequent menses, may improve endometriosis, PMDD
continuous = no placebo pills; PREVENTS menstruation; may improve endometriosis, PMDD
which progestins are most androgenic?
2nd generation
norgestrel
leveonorgestrel
which progestins are less androgenic?
norgestimate
what drug is anti-androgenic?
drospirenone
name androgens
testosterone
oxandrolone
methyltestosterone
danazol
describe dermatological effects of androgens
male pattern baldness, inc. sweat and sebum (acne!), hair growth (hirsutism in females)
how is testosterone administered/
parenterally
what are uses of modified androgens?
methyltestosterone
oxandrolone
danazol
methyltestosterone = hypogonadism oxandrolone = weight gain danazol = endometriosis
what classes of agents are “down regulators”?
GnRH antagonists = degarelix, cetrorelix, ganirelix
GnRH agonists = leuprolide, goserelin, nafarelin
what is the MOA and use of GnRH antagonists?
dec. LH and FSH to dec. sex hormones
use: hormone dependent cancers
what agents are “synthesis inhibitors”?
17-hydroxylase inhibitors: abiraterone, spironolactone 5-alpha reductase inhibitors: finasteride, dutasteride aromatase inhibitors: anastrozole, letrozole, exemestrane
differentiate between abiraterone and spironolactone uses
abiraterone = POTENT- used for castration, resistant metastatic prostate cancer spironolactone = weak - used for hirsutism in females or transgender
what are 5 alpha reductase inhibitors used for? What AEs are associated with them?
treat BPH and male pattern baldness
AEs: impotence, dec. libido
what are aromatase inhibitors used for? what AEs are associated with them?
estrogen-dependent cancers (breast)
AEs: similar to menopause
What agents are “receptor modulators”
SERMs = tamoxifen, raloxifene, clomiphene SPRMs = Ullipristal
