• Seminar created by:kumar samudra gupta
• Roll no.-20
• Developemnt of female reproductive tract
• Developemnt of female secondary sex characters
• Stimulation of proliferative phase of
• Maintain integrity of skeleton in reproductive age
Natural estrogens: secreted by the ovary.
synthesized in the graafian follicle, corpus
luteum and placenta from cholesterol.
Synthetic estrogen: long duration of action
slow metabolic rate.
Structure Activity Relation Ships:
– Aromatic ring with C-3-OH is essential
– Steroidal structures is not essential for
– Alkylation of the aromatic ring decrease
– The 17b-hydroxyl with constant distance
from 3-OH is essential for activity.
– The group between the two hydroxyl
must be hydrophobic.
– Unsaturation of ring B decreases the
– 17a- and 16 position when modified
enhance the activity.
1. Estradiol – known also as 17β – estradiol
– Principle estrogen in premenopausal women
2. Estrone – 1/3 the estrogenic potency of Estradiol
– Primary circulating estrogen after menopause
3. Estriol – significantly less potent than estradiol
– Present in significant amounts during pregnancy,
because its principal estrogen produced by
Synthesis of Estrogen
• The steroid receptor complex undergoes changes and binds with
estrogen responsive element located on target gene where it brings
about changes in transcription..
• 2 estrogen – receptor subtypes mediate the effects of the hormone
1. α receptor – the classic Estrogen Receptor. Found in
breasts,hypothalamus,endothelial cells and vascular smooth
2. β receptor – highly homologous to the α receptor.found in
bone, brain, ovaries
– α receptor
N - terminal portion of receptor contains a region that Promotes
– β receptor
contains a Repressor Domain
ON SEX ORGANS:
Estrogens bring about pubertal changes in the female
including growth of uterus, fallopian tubes and vagina.
It suppress the activity of FSH, and stimulate the secretion of
LH by direct action on pituitary as well as through
It enhances the rhythmic contraction of the fallopian tubes
and uterus and induce a watery alkaline secretion from the
Estrogen is important in maintaining bone mass primarialy by retarding
bone resorption. Osteoclast pit formation is inhibited bone matrix
proteins increase such as osteonectin,osteocalcin,collagen etc.
It controls the action of parathormone , hormone which intake calcium
ions from bones and teeth, thus maintaing a positive calcium balance.
Cause salt and water retention edema
Estrogens decrease plasma LDL cholesterol while HDL and triglycerides
levels are raised atherosclerosis in premenopausal women.
Blood coagulation is increased due to the formation of various clotting
It promotes vasodilation by induce secretion of nitric oxide synthase(NO)
2. HORMONE REPLACEMENT THERAPY: In women after
menopause due to the cessation of ovarian function as
estrogen- progestin HRT therapy suppression of
4. Senile vaginitis: can change vaginal cytology and effective in
preventing atrophic vaginitis in elderly women.
• Most common estrogen therapy
2. Breast tenderness
• Post menopausal uterine bleeding may occur
• There is increased risk of :
1. Myocardial infarction
2. Breast cancer
3. Endometrial cancer
• Other effects
2. Peripheral edema
• Razdan Balkishen, Medicinal Chemistry,First Edition:2010,CBS
publishers & Distributors Pvt. Ltd., Page No.-497-500.
• Tripathi KD, Essentials of Medical Pharmacology,Seventh
Edition:2013, Jaypee Brothers medical Publishers (P) Ltd, Page
• Pharmacology and pharmacotherapeutics by r.s satoskar,21st