Estrogen

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

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