reproductive pharm Flashcards
GnRH analog with agonist props if pulsatile & antagon props if continuous (down regulates GnRH receptor in pituitary - decr FSH & LH)
use: infertility (pulsatile), prostate CA (continuous), uterine fibroids (contin), precocious puberty (contin)
leuprolide
bind estrogen receptors
use: hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in post menopause, men with androgen dependent prostate CA
estrogens: ethinyl estradiol, DES, mestranol
selective estrogen receptor modulator- antagon at estrogen receptors in hypothal - prevents normal feedback inhib - incr release of LH & FSH from pituitary - ovulation
use: infertility d/t anovulation (PCOS)
clomiphene
selective estrogen receptor modulator: antagon at breast, agon at bone & uterus
use: treat & prevent recurrence of ER/PR pos breast CA
tamoxifen
selective estrogen receptor modulator: antagon at breast, & uterus, agonist at bone
use: tx osteoporosis
raloxifene
aromatase inhibitors used in post menopause with ER pos breast cancer
Anastrozole/exemestane
bind progesterone receptors, decr growth, incr vascularization of endometrium
use: in OCP’s & to tx endometrial cancer, abnormal uterine bleeding
progestins
competitive inhib of progestins at progesterone receptors
use: terminate pregnancy, given with misoprostol PGE1
mifepristone
estrogen & progestins inhib LH/FSH which prevents estrogen surge - no LH surge - no ovulation
progestins: thicken cervical mucus - limit access of sperm to uterus; inhib endometrial prolif - less suitable for implanting embryo
OCP’s: synthetic progestins, estrogen
beta2 agonists that relax uterus, used to decr contraction frequency during labor
terbutaline, ritodrine
synthetic androgen that acts as partial agonist at androgen receptors
use: endometriosis, hereditary angioedema
danazol
agonists at androgen receptors
use: tx hypogonadism, promote 2’ develop of sex characteristics, stimul anabolism to promote recovery after burn/injury
testosterone, methyltestosterone
anti androgen 5 alpha reductase inhibitor that decr conversion of testosterone to DHT
use: BPH, male pattern baldness
Finasteride
anti androgen non steroid competitive inhib of androgen receptors
use: prostate carcinoma
flutamide
anti androgen that inhib steroid synth via inhib 17,20 desmolase
use: PCOS, other
SE: gynecomastia, amenorrhea
ketoconazole
anti androgen that inhib steroid binding, 17 alpha hydroxylase, and 17,20 desmolase
use: PCOS, other
SE: gynecomastia, amenorrhea
spironolactone
alpha1 antagonist that inhib smooth m. contraction
selective for alpha 1A,D receptors on prostate
use: BPH
tamsulosin
inhib PDE5 - incr cGMP & smooth m. relaxation in corpus cavernosum, incr blood flow, penile erection
use: ED
sildenafil, vardenafil, tadalafil
direct arteriolar vasodilator
use: androgenetic alopecia, severe refractory HTN
minoxidil