EstrogensEstrogens (female sex (female sex hormones)hormones)
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
SYNTHETIC ESTROGENS
Steroidal- Ethinylestradiol Mestranol TiboloneNonsteroidal- Diethylstilbestrol Hexestrol Dienestrol
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
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
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
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
PROGESTINS
Progestin= favouring pregnancyNatural progestin ProgesteroneSynthetic progestins
Progesterone derivativesMedroxyprogesterone acetateMegestrol acetateDydrogesteroneHydroxyprogesterone caproate
19-Nortestosterone derivatives
Older compounds Newer compounds
Norethindrone Norethynodrel Ethynodiol diacetate LynestrenolAllylstrenolNorgestrelLevonorgestrel
Desogestrel Norgestimate Gestodene
ACTIONPrepration of uterus for nidation Maintenance of pregnancyCNSPituitaryMetabolismBody temperature
MOASteroid receptorsFemale genital tract, breast,CNS and pituitary
USES1. Contraceptives2. HRT3. Dysfunctional uterine bleeding4. Habitual abortion
ANTIPROGESTINS
Mifepristone19-norsteroidPotent antiprogestationalAntiglucocorticoidAntiandrogenic
USES1.Termination of pregnancy-upto 7 weeks2.Cervical ripening3.Induction of labour4.Cushing syndrome
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