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