detail about estrogen hormone, its regulation , mechanism of action

1. ESTROGEN
Presented by:- Shouvik Kumar Nandy (1991402006)
Subject:- Advanced Pharmacology II

2. Introduction:-
 Definition:- Estrogens are a group of sex hormones that promote
the development and maintenance of female characteristics in the
human body.
 Female sex hormone.
 Mostly estrogens are produced by women ovary, also formed in
liver.
 They are released by the follicles on the ovaries and secreted by
the corpus luteum.
 It helps the menstrual cycle, It plays a role in development of so-
called female secondary sex characteristics, such as breasts, wider
hips etc.

3. Regulation of estrogen
 During puberty Hypothalamus and Anterior Pituitary release FSH
which stimulate the secretion of estrogen from ovary.
 In ovary theca cells and Granulosa cells release estrogen in to the
blood stream.
 Daily secretion 10-100mcg.
 During pregnancy large quantity release up to 30 mg/day.
 Post menopausal- 2-10 mcg/day.
Fig:- Estrogen secretion

4. Different Types Estrogen(1):-
Natural Estrogen Synthetic Estrogen
Steroid Synthetic Nonsteroidal Synthesis
Estradiol Esthinly Estradiol Diethylstilbestrol
Estrone Mestranol Chlorotrianisene
Estriol Quinestrol Methallenestrill
 The major estrogen produced by women are Estradiol, Estrone and Estriol.
 Estradiol is the major secretory product of the ovary.
 Most estrones and estrios are formed in liver from Estradiol.

5. Mechanism Of Action:-
Fig:- Mechanism Of Action Of Estrogen(2)
ERE:- estrogen response element; ER:- estrogen receptor

6. Therapeutic use(2):-
 Postmenopausal HT:- The primary indication for estrogen therapy in postmenopausal women is
menopausal symtoms, such as vasomotor instability and vaginal atrophy.
 Contraception:- The combination of estrogen and progestogen provides effective contraception
via the oral, transdermal, or vaginal route.
 Other uses:- Estrogen use to development of secondary sex characteristics in young women with
primary hypogonadism.

7. Pharmacokinetics(2):-
 Naturally occurring estrogen:- The agents
absorbed through the gastrointestinal track,
skin, and mucous membranes. Metabolized by
microsomal enzymes of the liver. Although
there is some first-pass metabolism.
 Synthetic estrogen analogs:- these compounds
are well absorbed after oral administration.
They are stored in adipose tissue, from where
they are released slowly.
 Metabolism:- estrogens are transported in the
blood bound to serum albumin or sex
hormone- binding globulin. To reduce first-
pass metabolism, the drugs may be
administered via the transdermal route (patch,
topic gel), intravaginally ( tablet, cream, or
ring), or by injection.
Absorption(3) Well absorbed orally
Distribution(3) Natural estrogens are largely plasma
protein bound.
Metabolism(3)  Converted to estrone and vice
versa in liver.
 It converted to estriol.
 Sulfation & conjugation.
Excretion(3) • Duo to de conjugation is intestine.
• Mainly excreted in urine,

8. Adverse Effect(2):-
 Moat common of estrogen therapy:- Breast tenderness,
Hypertension,
Nausea.
 Postmenopausal uterine bleeding:- To avoid confusion with vaginal bleeding caused by
endometrial cancer, use the smallest amounts of estrogen cyclically.
 Increased risk for breast and endometrial cancer.

9. Anti Estrogen Drugs(2):-
Competitive estrogen
receptor
Aromatase inhibitors
SERMS(selective estrogen receptor
modulators)
• Inhibit negative
feedback of estrogen in
anterior pituitary.
• Use:- treatment of
male, female infertility
• Drug:- Clomiphene
Citrate (given orally)
• Decrease estrogen level
in body.
• Use:- treatment of Breast
cancer
• Drug:- Letrozole
• Work as partial agonist.
• Use:- treatment of
Osteoporosis & Breast
cancer.
• Drug:- Tamoxifen,
Raloxifene

10. REFERENCE:-
1) Bertram G Katzung, Basic and clinical pharmacology; 10 th edition (2007); page no- (654- 656)
2) Lippincott, Pharmacology; 6 th edition; Page no:- (351- 355)
3) https://www.slideshare.net/docpravin/estrogen-and-progestins

11. Thank You