Female Gonadal Hormones/Drugs Flashcards
(36 cards)
Synthetic Estrogens
- used in mixed contraceptives (along w/ progesterone)
1. ethinyl estradiol
2. estradiol valerate
naturally occurring estrogens
- Estrogen
- Estrone
- Estriol
Conjugated estrogens
- used to treat menopause if severe Sxs
1. Equilin
Synthetic progestins
- used in contraceptives (?)
- 17-hydroxyprogesterone
- 19-nortestosterone
- drospirenone (anti-mineralcorticoid)
progestins
17-hydroxyprogesterone or 19-nortestosterone derivatives w/ androgenic activity, used for contraception:
=> suppress LH & ovulation,
=> endometrium -> non-receptive to implantation
list of progestins (7 names)
(contraceptives, suppress LH) 1st 5 = 19-nortestosterone derivs.
- norethindrone
- norgestrel
- levonorgestrel
- ethynodiol acetate
- dienogest
* 6. 17-hydroxyprogesteron & medroxyprogesterone “MPA”
Selective Estrogen Receptor Modulators (“SERMs”)
non-steroidal drugs w/ tissue selectivity (agonist/antag. depending on use)
uses = osteoporosis Tx, breast cancer Tx, fertility Tx…
Raloxifene
SERM,
used for osteoporosis (estrogen agonist in bone)
*does NOT increase risk of breast/uterine cancer
Tamoxifen & Toremifene
SERM
used for breast cancer (anti-estrogen @ breast)
* partial agonist => increased risk endometrial hyperplasia & uterine cancer
Clomiphene
SERM used for fertility,
blocks estrogen inhibition of pituitary FSH/LH
=> increase ovulation rate & fertility
Bazedoxifene
SERM used in combo w/ estrogen,
for post-menopausal severe vasomotor Sxs & osteoporosis prevention (*if intact uterus)
* esp. good for ppl who can’t tolerante progestins
Ospemifene
SERM used for dispareunia,
= estrogen agonist @ vaginal epithelium & bone;
NO activity @ breast or uterine tissues.
Mifepristone
progesterone antagonist (competitive), Use: induce abortion
Paroxetine mesylate
SSRI,
used for vasomotor Sxs in post-menopausal women.
Ethinyl estradiol
synthetic estrogen, suppresses FSH & follicle emergence
Use: oral contraceptive (daily)
*slow metabolism
Combined oral contraceptives
estrogen + progesterone for 21 days,
mono-, bi- or tri-phasic dosing.
norethindrone, norgestrel
small dose oral contraception,
mech: induces non-receptive endometrium (less by ovulation block)
Norplant capsule
Sub-dermal contraceptive implant, contains levonorgestrel;
lasts 5 years.
Depo-provera
= intramuscular injection of medroxyprogesterone acetate (“MPA”)
parenteral dose lasts 3 months, subcut also available.
Mirena, progestasert
IUD + levonorgestrel (progestin) -> contraceptive.
Mirena - lasts 5 years
Progestasert - lasts 1 year
Nuvaring
vaginal ring w/ Ethinyl estradiol + etonorgestrel;
Use: on 3 wks, out 1, repeat.
Ortho Evra
transdermal patch with ethinyl estradiol & norelgestromin,
1 patch/wk for 3 wks, 4th wk no patch.
* may have higher risk blood clots!
Emergency contraceptives
- Plan B = large dose levonorgestrel (2 or 1 dose, w/ in 72 hrs)
- Yuzpe Regimen = levonorgestrel + ethinyl estradiol,
- take 12 hrs apart, w/in 72 hrs of intercourse, *more nausea & vomiting - Ulipristal acetate = selective progesterone R modulator,
- use w/in 120 hrs of intercourse (as effective as plan B)
Common Drugs contraindicated in pregnancy
& consequences
- Androgens - fetal virilization
- Diethylstilbesterol - fetal vaginal adenocarcinoma
- isotretinoin - teratogenic
- ACE Is/ARBs
- Statins
- NSAIDs *in 3rd trimester only
