Estrogens and Androgens Flashcards
Estrogen
steroid hormone that diffuses across membrane to bind to nuclear receptor (coronary arteries + HT cells) to stimulate transcription
Tx: contraception, cancer, osteoporosis, premature menopause, infertility, relieve menopausal symptoms, stimulate development in hypogonadism
AE: uterine bleeding, endometrial cancer, MI, HTN, Thromboembolism, HA, Nausea
Estradiol
most potent produced by ovary and main one in premenopausal women
Estrone
produced by ovary and main one in post-menopausal women
Estriol
produced by placenta and main one during pregnancy
GnRH Analogs (3) name them
pulse dose causes increase in FSH/LH
continuous dose causes decrease FSH/LH
Leuprolide, Gonadorelin, and Nafarelin
Raloxifene
Selective Estrogen Receptor Modulators
Antagonist at breast tissue (tx breast cancer) and decreases bone reabsorption and little effect in endometrium
AE: increase thrombus
Tamoxifene
Antagonist at breast tissue ( treat breast cancer)
Agonist in uterus (increases uterine cancer risk)
AE: crystalline retinopathy, macular edema, corneal opacities, cataracts, optic neuritis
Selective Estrogen Receptor Modulators
Clomiphene
Antagonist at all types of receptors and mainly blocks estrogen mediated -FB so it increases LH/FSH to treat infertility and induce ovulation/spermatogenesis
Selective Estrogen Receptor Modulators
Progestogens
Used for?
Names? (7)
AE?
treats hormonal deficiency, contraception, controls dysfunctional uterine bleeding
Drospirenone
Levonorgestrel
Medroxyprogesterone: synthetic are more stable to FPM
Megestrol
Norelgestromin
Norethindrone
Progesterone: produced in response to LH in H/F in adrenal cortex
AE: Weight gain, HA, Depression, Acne
Mifepristone
progesterone antagonist
early in pregnancy can lead to abortion ~ contraceptive
Testosterone
anabolic agent (bone growth and absorption, internal genitalia, and increase muscle mass)
Tx: osteoporosis, chronic wasting, and recovery from sx
Flutamide
androgen receptor antagonist
blocks testosterone at target organs (tx prostatic carcinoma)
Nilutamide and Bicalutamide
androgen receptor antagonist
usually with GnRH to decrease LH/testosterone
Contraceptive
prevent ovulation by impairing gametogenesis and interfering with gestation
combo of progestin and estrogen
AE: Fluid retention, HA, Nausea, Vomit, CV, Cervical Cancer, Abnormal Glucose tolerance, Weight gain
Monophasic
constant dose of both hormones over 21 days
last 7 days is placebo
Triphasic
mimics natural cycle with constant estrogen and elevating progestin in 3 weeks
last week is placebo
Transdermal Patch
contains ethinyl estradiol and norelgestromin
comparable efficacy but less effective if more than 198 lbs (more AE)
Progestin-only Pills
only norethindrone and take daily on continuous schedule
for breastfeeding women, intolerant to estrogen and smokers
Injectable
Medroxyprogesterone acetate
admin every 3 mos and weight gain is common but not for more than 2 years bc infertility and bone loss
Progestin Implant
subdermal implant of etonogestrel (lasts 3 years) and less effective with heavier women
Emergency Contraception
High dose of Progestin (0.75mg levonorgestrel)
High Dose Estrogen + Progestin (100 ng ethinyl estradiol and 0.5mg levonorgestrel)
either must be administered within 72 hours
take 2nd dose 12 hrs after 1st dose
progestin only formulations are usually tolerated better
