Estrogens

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Estrogens

  1. 1. Estrogens (female sex hormones)
  2. 2. <ul><li>NATURAL ESTROGENS- Estradiol </li></ul><ul><li>Synthesized- </li></ul><ul><li>Graafian follicle </li></ul><ul><li>Corpus luteum </li></ul><ul><li>Placenta </li></ul><ul><li>Estradiol estrone estriol </li></ul><ul><li>Drawbacks </li></ul><ul><li>Inactive orally </li></ul><ul><li>Rapid metabolism in liver </li></ul><ul><li>have short duration of action </li></ul>oxidation hydroxylated
  3. 3. SYNTHETIC ESTROGENS Steroidal- Ethinylestradiol Mestranol Tibolone Nonsteroidal - Diethylstilbestrol Hexestrol Dienestrol
  4. 4. REGULATION OF SECRETION - Daily- 10- 100µg During pregnancy- 30 mg/day Postmenopausal- 2-10 µg/day ACTIONS Pubertal changes Metabolic effects- Anabolic Retard bone resorption Induce nitric oxide synthase in endothelium
  5. 5. MAO Nuclear receptors ER α - uterus,hypothalamus,blood vessels ER β - prostate glands in males ovaries in females Trasdermal estradiol- estradiol-TTS 3 sizes-5, 10& 20cm 2 0.025mg,0.05mg& 0.1mg USES Contraceptives Hormone replacement therapy in postmenopausal women
  6. 6. ANTIESTROGENS Clomiphene citrate MAO - induces Gn secretion by blocking estrogenic feedback inhibition of pituitary USE - 1.Sterlity due to failure of ovulation 2.Aid in vitro fertilization 3.Male infertility
  7. 7. <ul><li>SELECTIVE ESTROGEN RECEPTOR MODULATOR (SERM) </li></ul><ul><li>Tamoxifen citrate </li></ul><ul><li>- Potent estrogen antagonist - breast carcinoma cells, blood vessels </li></ul><ul><li>Partial agonis t- uterus, bone, liver & pituitary. </li></ul><ul><li>Raloxifene </li></ul><ul><li>Antagonist – endometrium & breast </li></ul><ul><li>Partial agonist- bone & cvs </li></ul><ul><li>Ormeloxifene </li></ul><ul><li>Antagonist - breast & uterus </li></ul>
  8. 8. PROGESTINS Progestin= favouring pregnancy Natural progestin Progesterone Synthetic progestins Progesterone derivatives Medroxyprogesterone acetate Megestrol acetate Dydrogesterone Hydroxyprogesterone caproate
  9. 9. 19-Nortestosterone derivatives Older compounds Newer compounds Norethindrone Norethynodrel Ethynodiol diacetate Lynestrenol Allylstrenol Norgestrel Levonorgestrel Desogestrel Norgestimate Gestodene
  10. 10. ACTION Prepration of uterus for nidation Maintenance of pregnancy CNS Pituitary Metabolism Body temperature MOA Steroid receptors Female genital tract, breast,CNS and pituitary
  11. 11. <ul><li>USES </li></ul><ul><li>Contraceptives </li></ul><ul><li>HRT </li></ul><ul><li>Dysfunctional uterine bleeding </li></ul><ul><li>Habitual abortion </li></ul>
  12. 12. <ul><li>ANTIPROGESTINS </li></ul><ul><li>Mifepristone </li></ul><ul><li>19-norsteroid </li></ul><ul><li>Potent antiprogestational </li></ul><ul><li>Antiglucocorticoid </li></ul><ul><li>Antiandrogenic </li></ul><ul><li>USES </li></ul><ul><li>Termination of pregnancy-upto 7 weeks </li></ul><ul><li>Cervical ripening </li></ul><ul><li>Induction of labour </li></ul><ul><li>Cushing syndrome </li></ul>

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