Estrogens and Antiestrogens Flashcards
positive feedback loop.
hypothalamus produces GnRH.
this stimulates the anterior pituitary to produce FSH and LH.
This stimulates the ovary to produce estrogen and progesterone
those work on uterus
estrogen forms in contraceptives
pill, transdermal, vaginal ring
estrogen in oral contraception : Ethinyl estradiol
20-35 mcg.
metabolized by the liver.
start with the lowest dose.
can increase dose if breakthrough bleeding occurs.
monophasic
pill dosing stays the same for 28 days
biphasic
pill dosage changed after 14 days
triphasic
pill dosage changes every 7 days.
caution and contraindications of estrogen as a contraceptive
over 35 y/o and smoker, uncontrolled HTN, venous thromboembolism, breast cancer, hx of stroke, cirrhosis, migrane with aura, ischemic heart disease
advantages of oral contraceptives
highl effective , rapidly reversible, regulate menstrual bleeding, improve dysmenorrhea, decrease blood loss, reduces risk of ovarian and endometrial cancer
drug interactions with oral contraceptives
anticonvulsants (increase in microsomal enzyme activity),
rifampin is the only abx that can reduce serum estrogen and progestin levels.
griseofulvin, antifungal, associated with HF.
estrogen in menopause indications
vasomotor symptoms, genitourinary symptoms, vaginal dryness, burning, UTI.
benefits outweighs the risk in women younger than 60 and those within 10 years of menopause.
estrogen in menopause formulations
oral, transdermal, gels, emulsions, lotions, intravaginal creams
estrogen systemic treatment
oral or transdermal formulations. oral formulation has great effect on liver dueto first pass effect. (will increase tryglicerides, HDL, sex hormone binding globulin.
transdermal form is associated with lower risk of venous thrombosis and stroke. and has less effect on lipids than oral dosing.
Conjugated Equine Estrogens CEE (premorin)
derived from pregnant mares urine. comprised of estrone. synthetic version is plant based (Soy and Yams)
0.625 mg
micronized 17 beta estradiol
structurally identical to the main product of premenopausal ovary
1mg
esterified estrogens
comparable serum estrone/ estradiol levels to conjugated estrogen.
ethinyl estradol (estrase)
more potent than others for Menopausal Hormone Therapy, used in low doses.. 5 mcg.
vaginal dosing of estrogen
use lowest doses for vaginal atrophy. vasomotor symptoms can be treated in higher doses.
adverse effects of estrogen in menopause hormone therapy.
breast soreness, headaches, HTN, exacerbation of diabetes, cholestasis, thromboembolic events, endometrial hyperplasia
contraindications of estrogen in Meopause Hormone Therapy
hx of breast cancer, CAD, venous thromboembolic event, stroke/TIA, active liver disease, vaginal bleeding, high risk of endometrial cancer
estogen in bone health
transdermal is effective.
1. raloxifine (Evista): selective estrogen receptor modulator.
- Bazedoxifene (Duavee): combination estrogen derivative with selective estrogen receptor modulator.
spironolactone
selective estrogen receptor modulator.
estrogen agonist in bone prevents bone loss, improves bone mineral density, decreases rx for fracture.
increase in thromboembolism and hot flashes.
no effect on heart disease or endometrium.
Ospemifene (Osphena)
Selective estrogen receptor modulator.
increases thickness and moisture of vaginal mucosa..
Indication: dysparenunia in postmenopausal females. vaginal dryness in postmenopausal females.
estrogen agonist effect in endometrium.
potential risk for endometrial cancer if uterus is intact. increased risk for DVT and stroke.
60 mg daily is typical dose.
Which adverse reaction is common with menopausal estrogens?
elevation of systemic blood pressure
Patients treated with androgen therapy should be instructed to seek emergent evaluation if which adverse reaction occurs?
priapism (sustained erection)
Which is an effect of estrogen?
maintenance of bone density by decreasing the rate of bone reabsorption
