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Female Sex Hormones

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Mahmoud Seif

on 1 March 2013

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Transcript of Female Sex Hormones

Main topics are .......... Female Sex Hormones Estrogens Anti-Estrogens Progestins Estrogens Forms Mechanism of action Therapeutic uses Pharmacokinetics Adverse Drug Reactions (ADRs) Natural Synthetic Forms of Estrogens Natural estrogens Estradiol Estrone Estriole The principle estrogen in the premenopausal women. 1/3 activity of estradiol. The primary circulating estrogen after menopause. a metabolite of estradiole . The less active metabolite of estradiole. present in a significant amount during pregnancy. the principal estrogen produced by Placenta. Highly metabolised by first pass metabolism. Synthetic Estrogens Steroidal Estrogen Non Steroidal Estrogens Ehinyl Estradiol Quinsterol Mestranol lesser 1st pass metabolism than naturally occuring ones. More lipophilic >>> stored in the fat tissues >>> slowly released >>> longer duration of action. well absorbed orally, from the skin(trans-dermal patches) and from mucus membranes. Methylation cyclopentyl ether >>> more lipophilic Diethylstelbosterol (DES) DES dipropionate DES dipalmitate DES diphosphate tetrasodium salt
( Fosphosterol) Translation Process Cytoplasm again watch this Nucleus Cytoplasm Mechanism of action Plasma proteins Sex hormones bind with plasma proteins ( as they aren't watersoluble) >>>> dissociate and cross the cell membrane of the cell into ......... They bind with specific proteins forming (hormone -protein complex) and pass into the ........ hormone -protein complex binds with specific site in the genome >>>>> RNA is produced which passes into ........ Contains the Ribosome which performs the ............. producing specific proteins according to the type of tissues ......... ADRs Thromboembolism Myocardial infraction postmenopausal uterine bleeding nausea Hypertension headache peripheral edema breast & uterine carcinoma Pharmacokinetics Finally metabolised and excreted in urine metabolized in the liver >>> undergo enterohepatic circulation >>> Reabsorbed Therapeutic uses Postmenopausal Symptoms Contraception Primary Hypogonadism Osteoporosis Urogenital atrophy Vasomotor instability (Hot Flushes) Decreases the frequency of hip fractures. Treatment must begin within 2-3 years of menopause or earlier if possible. Estrogen decreases the resorption of bones but has no effect on the bone formation. Reestablishes feed-back on hypothalamic control of norepinephrin release >>> decreased the frequency of hot flushes. Estrogen treatment reverses postmenopausal atrophy of vulva, urethra trigonee of the bladder Estrogen therapy mimic the natural cyclic pattern. usually in combination with progestins to stimulate the development of 2ry sex characteristics in young women (11-13) years with hypogonadism. Continued treatment is required after growth is completed. In combination with progestins >>>>>discussed later. They are compounds that interact at estrogen receptors but have different effects on different tissues. They display agonism or antagonism effects according to the type of the tissue. Estrogen Receptor Antagonist Aromatase inhibitors Testosterone Estradiol Estrogen Receptor Aromatase Selective Estrogen Receptor Modulator (SERM) Tamoxifen Clomiphene Raloxifen Cis isomer >>> antiesrogenic activity, so used in treatment of estrogen dependant breast cancer where estrogen stimulates the normal growth of breast. Trans isomer >>> estrogenic activity on the uterus. If a racemic mixture of Tamoxifen is used >>>endometrial hyperplasia and some breast tumers may occure. Ex. * Nolvadex , Tamoxifen 10,20 mg. Used for treatment of postmenopausal osteoporosis. It decreases bone resorption so increase bone density and decrease bone fractures. Decreases cholesterol & LDL, however there is no evidence for efficacy in cardiovascular diseases. Has little or no effect on endometrium >>> no endometrial cancer. 95% of the drug is bound to plasma protein. undergo enterohepatic recycling. Excreted in bile >>>> feaces Hot flushes & leg cramps. Deep vein thrombosis ; pulmonary and retinal. Cholestyramine >>> decreases the absorption of Raloxifen by 60 %. Warfarin >>> 10% decrease in prothrombin time Uses Pharmacokinetics Adverse Drug Reactions Contraindicaton used as ovulation stimulant as a racemic mixture where; 1) Cis isomer >> weak estrogenic agonist.
2) Trans isomer >>> antiestrogen. FSH and LH release from the pitutary is increased leading to ....... stimulates the production of GnRH and .......... Ovulation Stimulation No -ve feed back on the Hypothalamus
so ...... normal estrogen produced by the growing follicle can't bind with its receptor
so that ........ it has a bulky group that block the estrogenic receptors in the hypothalamus so that ........ Mechanism Of Action of clomiphene After ovulation, the follicle is converted into the corpus luteum which secrets the Progesterone. Progesterone promotes the development of a secretory endometrium that can accomodate implantation of newly formed embryo. if conception occur, the corpus luteum will continue secreting the progesterone keeping the endometrium in a favorable state for pregnancy >>> till placental formation >>> continue the process. The high level of progesterone secreted inhibits the production of Gonadotrophins >>> preventing further ovulation. If no conception >>> corpus fades >>> progesterone level is decreased >>> Menstruation. Actions Increases hepatic glycogen Decreases Na reabsorption in the kidney by competetion with aldosterone receptors. increase in body temp. decrease in some plasma amino acids increases excretion of urinary nitrogen Forms Natural Synthetic Progesterone 17-alpha Hydroxy Progesterone 19- nor progesterone Dehydrogesterone t1/2 = 5 min. >>> so used parenterally not orally. * Acetate >>> orally active . *Caproate >>> long acting IM * Parenterally >>> 8 times more active than progesterone * 20 times more active. * No estrogenic or androgenic activity. *for progesterone deficiency (Duphaston) First Generation 2nd Generation 3rd Generation 4th Generation Medroxy progesterone acetate Ethisterone Lynestrenol ( Exluton ) Megesterol acetate Tibolone * 50 times more active than progesterone. * low estrogenic and no androgenic activity. * used parenteral and oral. Has some androgenic activity. Nor Ethisterone 5 times more active than ethisterone. Active orally and parenterally. * more active than medroxy. * No estrogenic or androgenic activity. * used for treatment of uterine & breast cancer. for treatment of Osteoporosis and menopausal symptoms. Levonorgestrel * Active isomer of norgestrel with longer duration of action. * Used as emergency contraceptive in high doses. Micolut 0.03 mg Contraplan 0.75 mg norgestrel derivatives with minimal androgenic activity. Norgestimate Desogestrel Etonogestrel Gestodene Prodrug >>> L-norgestrel+norelgestromine Cilest 0.25 mg Marvelon * active metabolite of Desogestrel. * used as Vaginal contraceptive ring and implantable contraceptive. Nuva ring * lower androgenic activity. * higher progestagenic activity. Gynera *antiandrogenic activity *No acne, hair loss, hirsutism, weight gain Drosperidone * antimineralocorticoid activity (diuretic) >>> no edema or hypertension. * antiandrogegenic activity (No acne, hair loss, hirsutism, weight gain) Yasmin References lippincott in pharmacology 4th eddition Medicinal chemistry Note Book of Mansoura Pharmacy Thank You Pharmacist
Mahmoud Seif
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