ESTROGEN
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.
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
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.
Mechanism Of Action:-
Fig:- Mechanism Of Action Of Estrogen(2)
ERE:- estrogen response element; ER:- estrogen receptor
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.
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,
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.
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
Thank You

estrogen pharma.pptx.....................

  • 1.
  • 2.
    Introduction:-  Definition:- Estrogensare 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 Duringpuberty 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) :- NaturalEstrogen 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) :-  Moatcommon 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) :- Competitiveestrogen 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.