Reproductive Drugs Flashcards
What is Leuprolide
MOA
Use
SE
GnRH analog with agonist properties when used pulsatile; antagonist when used in continuous fashion–>decr FSH, LH
Use: Infertility (pulsatile)
Continuous-prostate CA with flutamide; uterine fibroids, precocious puberty
SE: Antiandrogen, N/V
Estrogens (ethinyl estradiol, DES, mestranol)
MOA
Use
SE
Bind estrogen receptors
Use: Hypogonadism or ovarian failure, menstrual abnormalities, HRT in postmenopausal women,
Can use in men with androgen dependent prostate CA
SE: Incr risk of endometrial CA, bleeding in postmenopausal women
Clear cell adenoCA of vagina in females exposed to DES in utero
Incr risk of thrombi
Do not give to pts with ER+ breast CA or history of DVT
What is Clomiphene?
SERM
Used to treat infertility due to anovulation
Antagonist at estrogen receptors in hypothalamus
Prevent normal feedback inhibition–> increase release of LH & FSH from pit–> OVULATION
May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances
What is Tamoxifen?
SERM
Estrogen antagonist on breast tissue, but agonist in uterus and bone
Prevent and treat ER+ breast CA
Associated with endometrial CA and thrombolytic events
What is Tamoxifen?
SERM
Estrogen antagonist on breast tissue, but agonist in uterus and bone
Prevent and treat ER+ breast CA
Associated with endometrial CA and thromboembolic events
What is Raloxifene
SERM
Estrogen agonist on bone (decrease resorption of bone so can be used for osteoporosis), antagonist on uterus
Increased risk of thromboembolic events
Describe hormone replacement therapy (HRT)
For relief or prevention of menopause symptoms and osteoporosis (incr estrogen, decr osteoclast)
Unopposed Estrogen Replacement Therapy (ERT) increase the risk for endometrial CA SO PROGESTERONE IS ADDED
Possible incr cardiovascular risk
What are Anastrozole and Exemestane?
Aromatase Inhibitors used in postmenopausal women with Br CA
What are the progestins used for?
Bind progesterone receptors
Decrease growth and vascularization of endometrium
OCPs, treat endometrial CA and abnormal uterine bleeding
What is Mifepristone (RU-486)
Competitive inhibitor of progestins at progesterone receptors
Use: Pregnancy Termination. Given with Misoprostol (PGE1)
SE: Heavy bleeding, GI distress (N/V, anorexia)
Oral Contraception (synthetic progestins, estrogen)
Estrogen and Progestins inhibit Lh/FSH–>prevent estrogen surge
Progestins–> thickens cervical mucus which cock blocks sperm from uterus
–>Inhibit endometrial proliferation so not as suitable for embryo
Contraindicated in smokers >35 y/o (incr risk of cardiovasc events); pts with history of thromboembolic events and stroke, or estrogen dependent tumor
Terbutaline
B2 agonist that relaxes the uterus, used to decrease contraction frequency in woman in labor
Danazol
MOA
USE
SE
Synthetic androgen that is a partial agonist at androgen receptors
Use: Endometriosis and hereditary angioedema
SE: Weight gain, edema, acne, hirsutism, masculinization, decrease HDL, hepatotox
Testosterone, Methyltestosterone
Agonist at Androgen receptors
USE
Treats hypogonadism, promotes secondary sex characteristics
Stimulation anabolism to promote recovery after burn or injury
SE: Masculinization of females, decrease testicular release of testosterone bc no LH released–> gonadal atrophy
Premature closure of epiphyseal plates
Incr LDL, Decr HDL
What is FInasteride
Antiandrogen
Blocks 5a-reductase
Useful in BPH
Also promotes hair growth in male pattern baldness
To prevent male pattern baldness give a drug that promotes female breast growth
