Drugs Test 2 Flashcards
Clomiphene citrate
SERMs
Orally effective
MOA: Estrogen antagonist (esp. in hypothalmus) which induces FSH secretion. Agonist at other tissues (endometrium)
Used to treat lack of ovulation in patients with intact hypo-pit-ovarian axis. Also PCOS and Amenorrhea.
Side effects: Multiple fetuses; Ovarian hyperstimulation syndrome (shift of vascular fluids to abdominal and thoracic cavities). N/V. Skin rashes. Hot flashes. Thromboembolic events. Endometrial cancer.
FSH and LH injections
Administered for women with hypothalamic anovulatory function
Used for superovulation in normal ovulatory women (FSH/LH) on day 2-3 of menstrual cycle
Given with hCG sequence (stimulates LH surge for ovulation) for ovulaiton in anovulatory syndrome.
Side effects: Multiple fetuses; Ovarian hyperstimulation syndrome (shift of vascular fluids to abdominal and thoracic cavities)
Menotropins
Injected FSH and LH
Given with hCG sequence (stimulates LH surge for ovulation) for ovulation in anovulatory women
Side effects: Multiple fetuses; Ovarian hyperstimulation syndrome (shift of vascular fluids to abdominal and thoracic cavities)
Urofolitropin
Injected FSH
Given with hCG sequence (stimulates LH surge for ovulation) for ovulation in anovulatory women
Side effects: Multiple fetuses; Ovarian hyperstimulation syndrome (shift of vascular fluids to abdominal and thoracic cavities)
Follitropin
MOA: FSH
Given with hCG sequence (stimulates LH surge for ovulation) for ovulation in anovulatory women
Side effects: Multiple fetuses; Ovarian hyperstimulation syndrome (shift of vascular fluids to abdominal and thoracic cavities)
hCG
MOA: Binds to LH/CGR so that has LH-like induction of ovulation. Also stimulates estrogen primed follicle to induce meiotic resumption of oocytes.
Used following follicle stimulation by clomphene or gonadotropins
Leuprolide
MOA: GnRH agonist. If given nonpulsatile it suppresses FSH and LH (after intial transient rise)
Used to shut down HPO & to stimulate follicle production when paired with a FSH/LH or clomiphene.
Also for reducing sx (bleeding) of uterine diseases i.e. fibroids
Ganirelix
MOA: GnRH antagonist.
Used in fertility to prevent endogenous LH surge while promoting folliculogenesis with exogenous gonadotropins.
Used in prostate and breast cancer to inhibit steroid production.
Also for reducing sx (bleeding) of uterine diseases i.e. fibroids
**Do not see transient increase in FSH and LH as with Leuprolide
Certrolix
MOA: GnRH antagonist.
Used in fertility to prevent endogenous LH surge while promoting folliculogenesis with exogenous gonadotropins.
Used in prostate and breast cancer to inhibit steroid production.
Also for reducing sx (bleeding) of uterine diseases i.e. fibroids
**Do not see transient increase in FSH and LH as with Leuprolide
Ethinyle estradiol
Synthetic estrogen with decreased first pass metabolism and is orally available
Classic OCP
Estradiol 17beta
Principle natural form of estrogen.
Not orally available w/ extensive first pass metabolism
Tamoxifen
SERM
MOA: Estrogen antagonist (partial agonist) at Breast and Vasculature. Estrogen agonist at uterus, bone, and lipoproteins.
Oral
Can be used premenopausal.
Treatment and prevention of breast cancer
Side effects: N/V, Rash, Hot flashes, Thromboembolic events, Endometrial cancer
Best response if breast cancer is Estrogen and Progersterone positive.
Raloxifene
SERM
MOA: Agonist of bone, lipoproteins. Antagonist of breast, uterus.
Side effects: DVT
Oral
Toremifen
SERM
MOA: Antagonist in breast. No effect in bone. Agonist in uterus.
Side effects: Hot flashes, lowers LDL and raises HDL
Oral
Fluvestrant
MOA: PURE estrogen antagonist
IM injection once a month.
Side effects: GI, hot flashes, thromboembolism (pure?)
