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Liver Conjugates steroids to make t hem water soluble. After the liver, it is carried to the kidneys and excreted. Target Cell. Cytoplasm. Nucleus. Carried to liver.
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Liver Conjugates steroids to make them water soluble After the liver, it is carried to the kidneys and excreted Target Cell Cytoplasm Nucleus Carried to liver A simple hormone can have many different actions on target cells because modification can occur going into and out of both cytoplasm and nucleus. Alter E receptor Alter E Ligand Alter Alter C27 Cholesterol C21 Progesterone C19Testosterone Carried to target cells C18Estrogen Ovary Steroidogenesis 97% E & P 3% T Adrenal steroids convert in fat to E1 & E2 99% bound in blood to SHBG and albumin Clinical Gynecologic Endocrinology and Infertility, 8th edition by Fritz and Speroff
Female HormonesTrue or False • Steroidogenesis starts with cholesterol. • Steroidogenesis cleaves carbon atoms from cholesterol to make progesterone, testosterone, and estrogen. • Blood binding of steroids acts to buffer and extend the life of naturally occurring steroids. • Target cells modify steroids as they enter and as they leave both the cytoplasm and the nucleus of cells. • The liver conjugates and makes steroids water soluble. • The kidney excretes steroids once they are water soluble. • 30% of female estrogen is from adrenal steroids converting in fat to estradiol and estrone. • Estradiol is 12 times as potent as Estrone and 80 times as potent as Estriol. • The ethinyl group, a triple bonded carbon pair, allows oral administration of estrogen when attached to estrogen as ethinyl-estradiol by stabilizing it through the harsh stomach environment. • Selective Estrogen Receptor Modulators, SERMs, as not estrogen. • Unopposed estrogen increases the risk of endometrial cancer from 1/1000 to 1/400, RR 2.4. • Postmenopausal estrogen does not increase the risk of breast cancer according to the Women’s Health Initiative. • Postmenopausal progesterone does increase the risk of breast cancer according to the Women’s Health Initiative. • ER and PR positive breast cancers do better, in general, than ER and PR negative breast cancers. • Tamoxifen, a SERM, down-regulates breast estrogen effect but acts as a pure estrogen on the endometrium.
Female HormonesTrue or False • To stop heavy uterine bleeding, consider Premarin 10 mgm IV q 2 hours in the hospital. It works buy increases DVT risk and may cause hemorrhage later. • To stop heavy uterine bleeding, progesterone is preferred if you have a few days to slow the bleeding. • #2 results in more uterine spotting, but does not increase the risk of DVT and is usually a permanent fix to the problem. • #2 - A birth control pill cycle pack of 21 pills can be taken 1 PO QID, then TID, then BID, then QD until finished. Birth control pills contain mostly progesterone but, also, some estrogen. • #2 – Progesterone 10 mgm daily can be used the last 10 days of each cycle. “Take one a day for 10 days starting a week before you think your period will start.” • Premarin is extracted from horse’s urine and does NOT contain estradiol. • Testosterone is not used to decrease endometrial bleeding because it does not down-regulate estrogen receptors.