Gonadal steroid Hormones
Terms
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- Where is estrogen produce in men and post-menopausal women?
- Adipose Tissue
- Where in the ovary is estradiol produces
- In granulosa cells from androgen secreted by thecal cells
- Major ciculating homrmon in postmenopausal women and men is
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Estrone
Estradiol in premenopausal - Difference between estrogen binding to sex steroid binding globulin and albumin
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SSBG is high affinity, low capacity
Albumin is low affinity, high capacity - Estrogen effect on progestin receptors
- Estrogen stimulates progesterone receptors in endometerial tissue, so progesterone can counter act effects of estrogen
- Difference between natural, synthetic and conjugated estrogens
- Conjugate can be taken orally, the rest are transdurmal or IV, IM
- Use of Estrogens
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Birth control
Replacement therapy
Hypogonadotropic females
Uterine bleeding
Also for prostatic carcioma (inhibit GnRH) - Estrogen and Progestin in replacement therapy. When do you use one or both?
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If uterus is present, need progestin to prevent edometerial hyperplasia and cancer.
No uterus, estrogen alone is ok - Negative Side Effects of Estrogen therapy
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26% increase in breat cancer (>5 yrs)
Increase risk of cardiovascular disease
Increase in stroke, clots
Increase cholesterol and gall bladder disease - Postive side effects of Estrogen therapy
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Few hip fractures
Decrease colorectal cancer (37%) - Contraindications to estrogen therapy
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Breast or endometerial cancer
Endometriosis
Vaginal Bleeding
Pregnany
DVTs
Hypertension
Liver disease - Estrogen and hot flashes
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Good more moderate to sever hot flashes
Use behavior modification for mild hot flashes - Two antiestrogen drugs
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Clomiphene Citrate
Tamoxifen - Clomiphene Citrate
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Inhibits estrogen receptor feedback at pituitary
Increase amplitude of LH and FSH to treat fertility - Estrogen receptor blocker for infertility
- Clomiphene Citrate
- Tamoxifen
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Blocks estrogen receptors in breast cancer cells
Acts as agonist for bone density and lipoprotein profiles - Side effects of Tamoxifen
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Like menopause
May increase risk of endometrial cancer - Aromatase inhibitor
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Anastrozole
Letrozole
Exemestane
Blocker conversion of cholesterol to estrogen in adipose tissue - 2nd line drug for breast cancer
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Anastrozole
Letrozole
Exemstane
Not as effective has Tamoxifen - Aromataze inhibitors in pre vs post menopausal women
- Work only on adipose, so more effective in post menopausal women
- Raloxifene
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Full estrogen antagonist on breast and uterus
Agonist at all other sites. - Full anatagonist of estrogen in the breast and uterus, but acts as an agonist elsewhere
- Raloxifene
- Three places where progesterone is produced
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Corpus Luteum
Fetal Placenta
Adrenals - CNS effects of progesterone
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respiratory stimulant
Thermogenenisis
High doses, anesthertic properties - Medroxyprogesterone acetate
- Progesterone commonly used in hormone replacement regimen
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Norethindrone
Norgestrel
Nogestimate
Desogestrel - Progesterones used in OCP
- Use of progesterone
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Birth Control
Replacement therapy
Suprresion of Estrogen (bleeding, endometriosis, estrogen dependent cancers)
Diagnositic Tests - Side Effects of Progesterone
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Weight gain
Hirsutism
Libidi change
Bad for cholesterol - Contraindications for progesterone replacment therapy
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Hepatic Disease
Suspected pregnancy
Undiagnosed vaginal bleeding - Antiprogesterone drug and its use
- Mifepristone for abortions
- Trade off with OCP
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No increase in heart disease, stroke
Some increase in DVTS and HTN
Increase in Hepatic and Gall Bladder disease
Decrease in endometerial cancer, ovarian cancer - Plan B
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High dose estrogen plus levonorgestrel for morning after contraception
Causes N/V - Levonorgestrel
- Progestin in Plan B morning after pill
- Absolute CI's to OCP
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Clotting disorder
MI
Hyperlipidemia
Carcinom of breat or Uterus
Vaginal Bleeding
Pregnancy
History of Liver tumors - What is testosterone bound to in seminiferous tubules
- Androgen binding globulin
- Where testosterone is efficiently converted to 5-HT
- Prostate, scrotal skin, hair follicles and brain
- Danazol
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Testosterone Alkyl for Angioneurotic Edema
Increase inhbitor of edema and restors complement factors
Also for Endometriosis - Testosterone for angioneuortic edema
- Danazol
- Use for androgen replacement therapy
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Induce puberty in hypogonadotrophic hypogonadism
Treat short stature (though may cause epiphyseal plate to fuse earlier) - Most common testosterone ester
- Testosterone enanthate
- Side effects of testosterone
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Virilizing effects (women and children)
Feminizing effects in men (more converted to estrogen)
Liver disease and edema - Flutamide
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Testosterone receptor blocker
used for prostate cacner, but needs to be given with GnRH analog to prevent secondary increase in testosterone (blocks feedback inhibition) - Cyporterone acetate
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Oraly active test receptor antagonist
Not in US, but used for precocious puberty, baldness, and inhibition of libido in dangerous men - Testosterone blocker for prostate cancer. Give with GnRH analog
- Flutamide
- Inhibitors of androgen synthesis
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Ketoconazole
Spironolactone
Inhibit P450, which lowers testosterone, but compensation and short action limit their effectiveness - 5 alpha reductase inhibitor
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Finasteride
For BPH, and baldness (Propecia) - Propecia
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Finasteride
5alpha reductase inhibitor - Finasteride
- 5 alpha reducatse inhibitor for BPH and baldness