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1.11
Estrogen
| Term | Definition |
|---|---|
| Estradiol (E2) | main hormone during reproductive years |
| Estriol (E3) | pregnancy (placenta) |
| Estrone (E1) | post menopause (fat/adipose tissue) |
| Estrogen MOA: 2 estrogen receptors | 1. ERalpha (uterus, vagina, breast, blood vessels) 2. ERbeta (prostate and ovaries) |
| Estrogen MOA: estrogen upon binding to receptor undergoes: | dimerization |
| Estrogen MOA: Dimerized complex enters ______ and binds to: | nucleus, Estrogen Response Elements (EREs) |
| Estrogen MOA: Gene transcription occurs resulting in : | protein and cofactor synthesis |
| Secondary female sexual characteristics: | estrogen promotes and maintains |
| uterine lining (endometrium) | estrogen builds up |
| bone growth during puberty | estrogen promotes; closure of epiphysis |
| bone density | estrogen bone density and maintain |
| cholesterol | estrogen increases HDL and decreases LDL |
| body fat | estrogen increases |
| blood clotting | estrogen increases coagulability, increases synthesis clotting factors (2,7,9, 10) and decreases antithrombin 3 |
| cancer | estrogen increases risk of endometrial and breast cancer |
| enterohepatic circulation of estrogen: | estrogen enters hepatic circulation |
| enterohepatic circulation of estrogen (liver): | sulfate and glucuronide conjugation biliary secretion of conjugates into the intestine |
| enterohepatic circulation of estrogen (glut microbial flora (microbial enzyme)): | hydrolysis of sulfate and glucuronide conjugates in the gut allows them to be reabsorbed |
| Estrogen excess side effects | nausea, edema, migraine headache, hypertension, breast fullness/tenderness, melasma |
| Estrogen deficiency side effects | increased spotting, early or midcycle, breakthrough bleeding |
| Therapeutic uses of estrogen (3) | 1. primary hypogonadism (body produces little to no hormones) 2. postmenopausal hormonal therapy/hormone replacement therapy (HRT) 3. Suppress Ovulation |
| Adverse effects of estrogen | 1. uterine bleeding 2. cancer 3. nausea 4. breast tenderness |
| Estrogen Preparations: Estradiol tablets drugs | (ESTRACE) |
| Estrogen Preparations: Estradiol IM injections drugs | estradiol valerate (DELESTROGEN) estradiol cypionate (DEPO-ESTRAIOL) |
| Estrogen Preparations: Estradiol transdermal patch drugs | ESTRADERM VIVELLE ALORA (twice weekly) |
| Estrogen Preparations: Estradiol vaginal preps (all avoid 1st pass effects) | Vaginal cream (ESTRACE) Vaginal table (VAGIFEM) |
| Estrogen Preparations: Estradiol conjugated estrogens | PREMARIN |
Created by:
megangodfrey97
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