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- Where are estrogen synthesized in premenopausal nonpreg women?
- Ovaries
- Where are progesterone synthesized
- 1. ovary 2. testes 3. adrenal cortex 4. placenta
- 3 types of estrogen
- 1. estrodial 2. estrone 3. estriol
- How is estradiol made?
- Coversion of testosterone to estradial via aromatase
- Describe how estrogen and progresterone are released starting from hypothalamus
- 1. Hypothal secretes GnRH in a pulsating fashion to stimulate anterior pituitary 2. Anterior Pit produce and secrete FSH and LH 3. FSH/LH act on ovaries to produce and secrete estrogen/progesterone
- What inhibits anterior pituitary and hypothalamus?
- 1. Estrogen/Progesterone inhibits ant-pit and hypothalamus 2. Ovaries also produce Inhibin to inhibit anterior pituitary
- 3 types of estrogen preparations
- 1. human estrogen (17B-estradiol) 2. Non-human estrogens (premarin) 3. Synthetic estrogens
- 2 synthetic estrogens
- 1. ethinyl estradiol (most common) 2. Estrogen esters (estradiol valerate)
- 2 types of transdermal preparations and difference
- 1. estradiol (human) - fewer side effects w/reduced risk of blood clots 2. ethyinyl estradiol - increase risek of blood clots
- There are natural and synthetic preparations of progestin, list the 3 types of synthetic progestin
- 1. 17-hydroxyprogesterone acetate derivatives 2. sprionolactone derivatives 3. 19-nor testosterone derivatives
- What are the progestin preparations estrogenic and/or androgenic acvity
- 1. 17-hydroxyprogesterone acetate derivatives-no androgenic or estrogenic activity 2. sprionolactone derivatives-weak anti-androgenic activity (no estrogenic or androgenic activity) 3. 19-nor testosterone derivatives - varying androgenic activity, there is estrogenic activity
- Name 2 17 hydroxyprogesterone acetate derivatieves
- 1MPA and 17-hydroxy progesterone (caproate)
- Who is indicated for caproate (17-hydroxyprogesterone)
- For preg pts whose had premature births in the past
- Name the spironolactone derivative of progestin
- drosprenone
- Name the 1st generation 19-nor testerone derivative. (1)
- 1. norethindrone
- Name the 2nd generation 19-nor testerone derivative. (3)
- 1. levonorgesterl (highest androgenic activity) 2. norgestrel 3. ethynodiol diacetate
- Name the 3rd generation 19-nor testerone derivative. (2)
- 1. desogestrel 2. norgestimate
- Name the 4th generation 19-nor testerone derivative. (1)
- dienogest
- Which of the generations have highest risk of VTE?
- 3rd generation
- Describe estrogen receptors (2)
- 1. Have alpha/beta receptors with different gene products and non-redundant functions 2. mechanistically similar to glucocorticoid receptors
- Describe progesterone receptor (2)
- 1. Have A and B receptors 2. mechanistically similar to steroid hormone receptors]
- What is the direct genomic effect of estrogen receptors
- ligand induces homo/hetero dimer formation leading to interaction w/ERE
- what is the indirect genomic effect of estrogen receptors
- ER binds to other transcription factors to effect transcription of non-ERE containing genes such as AP1, SP1 and NFkB]
- 3 ways endogenous estrogen effects growth/development
- 1. develop primary and secondary female characteristics 2. growth of myometrium and endometrial lining 3. support female reproductive structures
- How does endogenous estrogen effect menstrual cycle?
- 1. Required for ovarian follicular development 2. required for regulation of cycle
- 3 metabolic effects of estrogen
- 1. decrease bone resortption 2. decrease cholesterol 3. increase coagulability due to upregulation of genes involved in factors 2,7,9,10 and decreases antithrombin
- 4 phsyiologic actions of endogenous progesterone
- 1. increase blood flow of endometrium 2. increase cholesterol 3. raise body temp 4. during pregnancy, it supresses menstration and uterine contractility
- 4 therapeutic uses of estrogen
- 1. contraceptive 2. postmenopausal therapy 3. hypogonadism in femaes 4. dysmenorrhea
- 4 therapeutic uses of anti-estrogen
- 1. infertility 2. hormone sensitive breast cancer 3. osteoporosis 5. endometriosis
- Drug used to tx infertility
- clomiphene
- Drugs used to tx hormone sensitive breast cancer (3)
- 1. tamoxifen (SERM) 2. fulvestrant (ER antagonist) 3. anastrozole (armatase inhibitor)
- Drugs used to tx osteoporisis
- ralxifene (forteo)
- Drug used to tx endometriosis
- danazol-androgen to block estrogen action
- 4 therapeutic uses of progestin
- 1. contraceptived (w or w/o estrogen) 2. HRT in post menopause 3. endometrial cancer 4. dysmenorrhea
- What signals the start of menses?
- When there is no implantation, progesterone levels signaling the start of menses
- For contraceptives, what type of delivery systems avail for combined (estrogen+progestin)
- 1. oral 2. vaginal ring 3. transdermal
- For contraceptives, what type of delivery systems avail for progestin only
- 1. oral 2. IM or SQ injections 3. Subdermal implants 3. IUD
- How does estrogen prevent ovulation (4)
- 1. suppress FSH secretion 2. stabilizes endometrium to prevent irregular breakthrough bleeding 3. increase progesterone receptors 4. increase fallopian tube peristalisis
- How does progestin prevent ovulation (3)
- 1. Suppress LH secretion 2. Creates thick, viscous mucus to inhibit sperm transport 3. produce endometrium that is not receptive to implantation
- Which combination oral contraceptives contain progestin + ethinyl estradiol?
- 1. Spironolactone - drosprenone 2. 1st, 2nd, 3rd generations (norethidrone, levonorgestrel, norgestrel, ethynodiol diacetate, desgestrel, norgestimate)
- Which combination oral contraceptives contain progestin + ethinyl valerate?
- Dienogest (4th gen)
- Which of the combo oral contraceptive have the most androgenic activity (oily skin)
- levonorgestrel
- Types of regimens avail for combo oral contraceptives (4)
- 1. 21/7 2. 84/7 3. 24/4 4. 365/0
- Of the pills in dosage regimen, which is the MOST important one to not miss
- The first pill of the next pack right after the "off" period
- 4 new combo oral drugs for extended cycle control or shortened hormone free interval and their regimen
- 1. seasonale (84/7 2. Seasonique (84/7lower dose w/4withdrawl bleeds) 3. Yaz (24/4) 4. Loestrin 24/4 + iron
- 5 risks of combo oral drugs
- 1. VTE 2. CVD risk in smokers over 35yo 3. MI 4. Strokes 5. Cervical cancer
- 4 common SE of combo oral drugs
- 1. irregular bleeds (goes away by 3rd cycle) 2. HA 3. weight gain 4. bloating/edema
- 7 absolute contraindications for combo oral drugs
- 1. family DVT/PE 2. uncrontrolled HTN 3. Smoker>35yo 4. migraine w/aura 5. DM w/organ damage 6. Hx breast cancer 7. Liver disease
- Name the combo vaginal ring and regimen
- NuvaRing: use for 3wks and remove 1 week
- Name combo patch and regimen
- OrthoEvra; wear 1wk/patch x 3 wks then 4th wk patch free
- What SE often associated with Patches compared to oral?
- breast tenderness
- Who may patches not be effective for?
- women over 198lb