Estrogens
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EstrogensEstrogens (female sex (female sex hormones)hormones)
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NATURAL ESTROGENS- Estradiol
Synthesized- Graafian follicle Corpus luteum Placenta
Estradiol estrone estriol
Drawbacks-Inactive orally-Rapid metabolism in liver - have short duration of action
oxidation hydroxylated
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SYNTHETIC ESTROGENS
Steroidal- Ethinylestradiol Mestranol TiboloneNonsteroidal- Diethylstilbestrol Hexestrol Dienestrol
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REGULATION OF SECRETION-
Daily- 10- 100µgDuring pregnancy- 30 mg/dayPostmenopausal- 2-10 µg/day
ACTIONS
Pubertal changesMetabolic effects- Anabolic Retard bone resorption Induce nitric oxide synthase in endothelium
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MAONuclear receptors
ERα- uterus,hypothalamus,blood vesselsERβ- prostate glands in males ovaries in females
Trasdermal estradiol- estradiol-TTS 3 sizes-5, 10& 20cm2
0.025mg,0.05mg& 0.1mg
USESContraceptivesHormone replacement therapy in postmenopausal women
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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
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SELECTIVE ESTROGEN RECEPTOR MODULATOR (SERM)
Tamoxifen citrate- Potent estrogen antagonist- breast carcinoma cells, blood vessels-Partial agonist- uterus, bone, liver & pituitary.
RaloxifeneAntagonist – endometrium & breastPartial agonist- bone & cvs
OrmeloxifeneAntagonist- breast & uterus
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PROGESTINS
Progestin= favouring pregnancyNatural progestin ProgesteroneSynthetic progestins
Progesterone derivativesMedroxyprogesterone acetateMegestrol acetateDydrogesteroneHydroxyprogesterone caproate
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19-Nortestosterone derivatives
Older compounds Newer compounds
Norethindrone Norethynodrel Ethynodiol diacetate LynestrenolAllylstrenolNorgestrelLevonorgestrel
Desogestrel Norgestimate Gestodene
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ACTIONPrepration of uterus for nidation Maintenance of pregnancyCNSPituitaryMetabolismBody temperature
MOASteroid receptorsFemale genital tract, breast,CNS and pituitary
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USES1. Contraceptives2. HRT3. Dysfunctional uterine bleeding4. Habitual abortion
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ANTIPROGESTINS
Mifepristone19-norsteroidPotent antiprogestationalAntiglucocorticoidAntiandrogenic
USES1.Termination of pregnancy-upto 7 weeks2.Cervical ripening3.Induction of labour4.Cushing syndrome
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