Female reproductive pharmacology Flashcards
What is the MOA for estrogens and progestins?
suppress FSH and LH to inhibit ovulation and alteration of cervical mucus in endometrium
What are commonly used estrogens?
ethinyl estradiol;
mestranol
Commonly used progestins?
norgestrel;
norethindrone
medroxyprogesterone
How are the estrogens and progestins available?
orally as monophasic, biphasic or triphasic combos;
some progestin only preparations
What are common side effects of estrogen and progestins?
headache, nausea; breast tenderness; weight gain; depression; thromboembolism
What are absolute contraindications of estrogens and progestins?
thrombophlebitis; thromboembolic disorders;
cerebral vascular disease; coronary occlusion;
possible pregnancy;
smoking over 35;
impaired liver function;
possible breast cancer
What are off label uses of estrogens and progestins?
female hypogonadism; HRT; acne; dysmenorrhea; uterine bleeding
Why use postcoital contraceptives?
prevents pregnancy if used w/in 72 hours of unprotected intercourse
What are postcoital contraceptive types?
estrogens alone; progestins alone; combination pills;
mifepristone (RU486)
What are intauterine devices?
create hostile environment in endometrium via low grade intrauterine inflammation and increased PG formation => interfere w/ implantation of fertilized ovum
What are examples of intrauterine devices?
Copper T 380;
Progesterone T
Define menopause
permanent cessation of menstruation secondary to loss of ovarian follicular activity
What is used to treat menopause?
HRT
What effects of menopause is HRT used to treat?
prevent hot flashes; atrophic changes in UG tract; osteoporosis
If estrogen replacement therapy is used alone, what is the risk? What might be use to mitigate the risk?
endometrial growth and cancer;
concomitant progesterone use to prevent
Why is HRT no longer widely used?
associated with increased breast cancer and stroke risk
What are selective estrogen receptor modulators (SERM)?
Tamoxifen;
Raloxifene
What is the MOA of tamoxifen?
estrogen ANTAGONIST in breast;
estrogen agonist in endometrium;
estrogen agonist in bone
When is tamoxifen used?
hormone responsive breast CA;
reduces risk of breast CA in high risk women
What are side effects of tamoxifen?
increases risk for endometrial CA;
hot flashes;
increase risk of venous thrombosis
What is the MOA for Raloxifene?
partial estrogen agonist in bone;
estrogen ANTAGONIST in breast;
estrogen ANTAGONIST in uterus
Why is raloxifene used?
prevents osteoporosis in post menopausal women;
reduces risk of breast CA in high risk women;
NO INCREASED ENDOMETRIAL CA RISK
What are side effects of raloxifene?
causes hot flashes and increases risk of venous thrombosis
MOA of Clomiphene
fertility agent => nonsteroidal agent selectively blocks estrogen receptos in pituitary, reducing neg feedback mech increasing FSH and LH and stimulation of ovulation
Patient comes to your clinic looking to get pregnant. What medication would you give her and what side effects are associated?
Clomiphene = multiple birth pregnancy
MOA for danazol
inhibits ovarian steroid synthesis
Clinical use for danazol
endometriosis;
fibrocystic breast disease
MOA for anastrozole and exemestane
aromatase inhibitors => decrease estrogen synthesis
clinical use for anastrozole and exemestane
breast CA in post-menopausal women
MOA of mifepristone (RU486)
progesterone and glucocorticoid antagonist
clinical use for mifepristone
postcoital contraceptive;
abortifacient
MOA of dinoprostone
PGE2 analog
clinica uses for dinoprostone
induce labor => causes cervical ripening and uterine contractions;
abortifacient
MOA for Ritodrine and Terbutaline
Beta 2 agonists
clinical uses for Ritodrine and Terbutaline
relax uterus => suppress premature labor
