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Estrogen and Antiestrogen
By
Dr. Faraza Javaid
Introduction
Estradiol – most potent, secreted by ovary
Esterone – formed by extra glandular conversion of
androstenedione in peripheral tissues
Estriol – conjugated metabolites of estrone and estradiol
Hypothalamus secretes GnRH
Stimulates pituitary to secrete FSH and LH
Act on ovary and cause immature ovarian follicles to begin
developing to dominant follicles ◦
Pituitary hormones
Rising and falling levels create two interrelated cycles: ovarian
and uterine
Sex hormones produced by the gonads are necessary for:
Conception
Embryonic maturation
Development of primary and secondary sexual characteristics at
puberty
Activity in target cells is modulated by receptors.
Therapeutic Uses of Gonadal Hormones
Replacement therapy
Contraception
Management of menopausal symptoms
Several antagonists are effective in cancer chemotherapy
Estrogen
Estradiol
The most potent estrogen produced and secreted by the ovary.
The principal estrogen in the premenopausal woman.
Estrone
A metabolite of estradiol that has approximately one third potency of
estradiol.
Primary circulating estrogen after menopause.
Generated from conversion of androstenedione in peripheral tissues.
Estriol
A metabolite of estradiol
Significantly less potent than estradiol
Present in significant amounts during pregnancy
Produced by the placenta
Plant-derived conjugated estrogen products are also available.
Ethinyl estradiol
Synthetic estrogen
Undergo less first-pass metabolism than naturally occurring
steroids
Effective when administered orally at lower doses.
Selective Estrogen-Receptor Modulators (SERMs)
Nonsteroidal compounds that bind to estrogen receptors and
exert either estrogenic or antiestrogenic effects on target tissues
 Include tamoxifen and raloxifene
Estrogen Mechanism of Action
Steroid hormones diffuse across the cell membrane and bind to
specific nuclear-receptors
Two estrogen-receptor subtypes, α and β, mediate the effects of
the hormone
The α-receptor contains a region that promotes transcription
activation
The β-receptor contains a repressor domain
The transcriptional properties of the α and β estrogen receptors
are different
Affinity for the receptor type varies with the particular estrogen
The receptor isoforms vary in structure, chromosomal location,
and tissue distribution.
Activated steroid-receptor interacts with nuclear chromatin to initiate RNA
synthesis and specific proteins that mediate physiologic functions
The steroid hormones are both receptor and tissue specific and result in
different RNA species in diverse target tissues
Activation of estrogen receptor in the membranes of hypothalamic cells
has been shown to couple to a G protein initiating a second-messenger
cascade
Estrogen-mediated dilation of coronary arteries occurs by the increased
formation and release of nitric oxide and prostacyclin in endothelial cells
Estrogen Therapeutic Uses
Estrogens are used for contraception and postmenopausal hormone
therapy (HT)
Due to concerns over HT risks, National American Menopause
Society recommends that HT be prescribed at lowest effective dose
for the shortest possible time to relieve menopausal symptoms
Extended use of HT may be appropriate for some women in whom
the relief of symptoms outweighs the risk of continuation of HT
Estrogens were previously widely used for prevention of
osteoporosis, but current guidelines recommend use of other
therapies such as alendronate
Estrogen may be used for prevention of osteoporosis if other
therapies are inappropriate or not tolerated
Estrogens are used extensively for replacement therapy in
premenopausal patients who are deficient in this hormone
Estrogen deficiency can be due to inadequate functioning of the
ovaries (hypogonadism), premature menopause, or surgical
menopause
Postmenopausal HT
The primary indication for estrogen therapy in postmenopausal
women is menopausal symptoms, such as vasomotor instability and
vaginal atrophy
For women who have an intact uterus, progestogen is always included
with the estrogen therapy, to reduce endometrial carcinoma risk
 For women who have undergone a hysterectomy, unopposed estrogen
therapy is recommended because progestins may alter the beneficial
effects of estrogen on lipid parameters
Contraception
The combination of an estrogen and progestogen provides effective
contraception via the oral or transdermal route
Estrogen therapy mimicking the natural cyclic pattern, and in combination
with a progestogen, is used to stimulate development of secondary sex
characteristics in young women with primary hypogonadism. Continued
treatment is required after growth is completed
 Estrogen and progestogen replacement therapy is used for women who
have premature menopause or premature ovarian failure ◦ Replacement
therapy is usually continued until about age 50
Pharmacokinetics
Estrogens are transported in the blood bound to serum albumin or
sex hormone–binding globulin
Bioavailability of estrogen taken orally is low due to first-pass
metabolism in the liver
To reduce first-pass metabolism, estrogens may be administered via
the transdermal route (patch, topical gel, topical emulsion, or spray),
intravaginally (tablet, cream, or ring), or by injection
In individuals with liver damage, serum estrogen levels may increase
due to reduced metabolism
Adverse Effects
Nausea
Breast tenderness
Postmenopausal uterine bleeding can occur
Risk of thromboembolic events
Myocardial infarction, and breast and endometrial cancer is increased with
estrogen therapy
The increased risk of endometrial cancer can be reduced by including a
progestogen along with the estrogen therapy
Antiestrogen
Tamoxifen
Raloxifene
Clomiphene
Tamoxifen
MOA:
Competes with estrogen for binding to the estrogen receptor in
breast tissue
Normal breast growth is stimulated by estrogens
Some breast tumors regress following treatment with tamoxifen
Therapeutic Uses
Palliative treatment of metastatic breast cancer in
postmenopausal women
Adjuvant therapy following mastectomy or radiation in breast
cancer
Prophylactic therapy to reduce the risk of breast cancer in high
risk patients
Pharmacokinetics
Administered orally
Tamoxifen is extensively metabolized by CYP450
Raloxifene is rapidly converted to glucuronide conjugates
through first-pass metabolism
Raloxifene is >95% bound to plasma proteins
All three agents undergo enterohepatic cycling
Primary route of excretion is through the bile into feces
Adverse Effects
Hot flashes, Nausea
Menstrual irregularities and vaginal bleeding
Due to its estrogenic activity in the endometrium, hyperplasia and
malignancies have been reported in women maintained on tamoxifen
This has led to recommendations for limiting the length of time on the drug
Tamoxifen is subject to many drug interactions
Some CYP450 inhibitors may prevent formation of active metabolites of
tamoxifen and possibly reduce the efficacy (e.g. amiodarone, haloperidol,
risperidone)
Raloxifene
Second-generation SERM
Antagonist estrogen receptors in the breast tissue
Decreases bone resorption and overall bone turnover
Bone density is increased, and vertebral fractures are decreased
Has little to no effect on the endometrium and, may not predispose to
uterine cancer
Raloxifene lowers total cholesterol LDL in the serum
It has no effect on HDL or triglyceride levels
Therapeutic Uses
Prophylaxis of breast cancer in high-risk women
Prevention and treatment of osteoporosis in postmenopausal
women
Adverse effects
Hot flashes
Leg cramps
Increased risk of DVT, PE, retinal-vein thrombosis
Women who have a past or active history of venous thromboembolic
events should not take the drug
Should be avoided in women who are or may become pregnant
(Category X)
Coadministration with cholestyramine can reduce the absorption of
raloxifene by 60% (Should not be used together)
Clomiphene
Acts as a partial estrogen agonist and interferes with the negative feedback of
estrogens on the hypothalamus
This effect increases the secretion of gonadotropin- releasing hormone and
gonadotropins leading to stimulating ovulation
Uses:
Used to treat infertility associated with anovulatory cycles
Not effective in women with ovulatory dysfunction due to pituitary or ovarian
failure
Adverse Effects
Headache, Nausea
Vasomotor flushes
Visual disturbances
Ovarian enlargement
Question?
A 50 year old women at a very high risk of breast cancer is given
tamoxifen for prophylaxis. What is the main mechanism or effect of
this drug?
a) Blocks estrogen receptor in breast tissues
b) Blocks estrogen receptor in endometrium
c) Increase the risk of osteoporosis
d) Raise plasma LDL and lower HDL
e) Reduces the risk of thromboembolic diseases
Thank You

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Estrogen and Antiestrogen.pptx

  • 2. Introduction Estradiol – most potent, secreted by ovary Esterone – formed by extra glandular conversion of androstenedione in peripheral tissues Estriol – conjugated metabolites of estrone and estradiol
  • 3. Hypothalamus secretes GnRH Stimulates pituitary to secrete FSH and LH Act on ovary and cause immature ovarian follicles to begin developing to dominant follicles ◦ Pituitary hormones Rising and falling levels create two interrelated cycles: ovarian and uterine
  • 4. Sex hormones produced by the gonads are necessary for: Conception Embryonic maturation Development of primary and secondary sexual characteristics at puberty Activity in target cells is modulated by receptors.
  • 5. Therapeutic Uses of Gonadal Hormones Replacement therapy Contraception Management of menopausal symptoms Several antagonists are effective in cancer chemotherapy
  • 6.
  • 7. Estrogen Estradiol The most potent estrogen produced and secreted by the ovary. The principal estrogen in the premenopausal woman. Estrone A metabolite of estradiol that has approximately one third potency of estradiol. Primary circulating estrogen after menopause. Generated from conversion of androstenedione in peripheral tissues.
  • 8. Estriol A metabolite of estradiol Significantly less potent than estradiol Present in significant amounts during pregnancy Produced by the placenta Plant-derived conjugated estrogen products are also available.
  • 9. Ethinyl estradiol Synthetic estrogen Undergo less first-pass metabolism than naturally occurring steroids Effective when administered orally at lower doses.
  • 10. Selective Estrogen-Receptor Modulators (SERMs) Nonsteroidal compounds that bind to estrogen receptors and exert either estrogenic or antiestrogenic effects on target tissues  Include tamoxifen and raloxifene
  • 11. Estrogen Mechanism of Action Steroid hormones diffuse across the cell membrane and bind to specific nuclear-receptors Two estrogen-receptor subtypes, α and β, mediate the effects of the hormone The α-receptor contains a region that promotes transcription activation The β-receptor contains a repressor domain
  • 12. The transcriptional properties of the α and β estrogen receptors are different Affinity for the receptor type varies with the particular estrogen The receptor isoforms vary in structure, chromosomal location, and tissue distribution.
  • 13. Activated steroid-receptor interacts with nuclear chromatin to initiate RNA synthesis and specific proteins that mediate physiologic functions The steroid hormones are both receptor and tissue specific and result in different RNA species in diverse target tissues Activation of estrogen receptor in the membranes of hypothalamic cells has been shown to couple to a G protein initiating a second-messenger cascade Estrogen-mediated dilation of coronary arteries occurs by the increased formation and release of nitric oxide and prostacyclin in endothelial cells
  • 14. Estrogen Therapeutic Uses Estrogens are used for contraception and postmenopausal hormone therapy (HT) Due to concerns over HT risks, National American Menopause Society recommends that HT be prescribed at lowest effective dose for the shortest possible time to relieve menopausal symptoms Extended use of HT may be appropriate for some women in whom the relief of symptoms outweighs the risk of continuation of HT
  • 15. Estrogens were previously widely used for prevention of osteoporosis, but current guidelines recommend use of other therapies such as alendronate Estrogen may be used for prevention of osteoporosis if other therapies are inappropriate or not tolerated Estrogens are used extensively for replacement therapy in premenopausal patients who are deficient in this hormone Estrogen deficiency can be due to inadequate functioning of the ovaries (hypogonadism), premature menopause, or surgical menopause
  • 16. Postmenopausal HT The primary indication for estrogen therapy in postmenopausal women is menopausal symptoms, such as vasomotor instability and vaginal atrophy For women who have an intact uterus, progestogen is always included with the estrogen therapy, to reduce endometrial carcinoma risk  For women who have undergone a hysterectomy, unopposed estrogen therapy is recommended because progestins may alter the beneficial effects of estrogen on lipid parameters
  • 17. Contraception The combination of an estrogen and progestogen provides effective contraception via the oral or transdermal route Estrogen therapy mimicking the natural cyclic pattern, and in combination with a progestogen, is used to stimulate development of secondary sex characteristics in young women with primary hypogonadism. Continued treatment is required after growth is completed  Estrogen and progestogen replacement therapy is used for women who have premature menopause or premature ovarian failure ◦ Replacement therapy is usually continued until about age 50
  • 18. Pharmacokinetics Estrogens are transported in the blood bound to serum albumin or sex hormone–binding globulin Bioavailability of estrogen taken orally is low due to first-pass metabolism in the liver To reduce first-pass metabolism, estrogens may be administered via the transdermal route (patch, topical gel, topical emulsion, or spray), intravaginally (tablet, cream, or ring), or by injection In individuals with liver damage, serum estrogen levels may increase due to reduced metabolism
  • 19. Adverse Effects Nausea Breast tenderness Postmenopausal uterine bleeding can occur Risk of thromboembolic events Myocardial infarction, and breast and endometrial cancer is increased with estrogen therapy The increased risk of endometrial cancer can be reduced by including a progestogen along with the estrogen therapy
  • 21. Tamoxifen MOA: Competes with estrogen for binding to the estrogen receptor in breast tissue Normal breast growth is stimulated by estrogens Some breast tumors regress following treatment with tamoxifen
  • 22. Therapeutic Uses Palliative treatment of metastatic breast cancer in postmenopausal women Adjuvant therapy following mastectomy or radiation in breast cancer Prophylactic therapy to reduce the risk of breast cancer in high risk patients
  • 23. Pharmacokinetics Administered orally Tamoxifen is extensively metabolized by CYP450 Raloxifene is rapidly converted to glucuronide conjugates through first-pass metabolism Raloxifene is >95% bound to plasma proteins All three agents undergo enterohepatic cycling Primary route of excretion is through the bile into feces
  • 24. Adverse Effects Hot flashes, Nausea Menstrual irregularities and vaginal bleeding Due to its estrogenic activity in the endometrium, hyperplasia and malignancies have been reported in women maintained on tamoxifen This has led to recommendations for limiting the length of time on the drug Tamoxifen is subject to many drug interactions Some CYP450 inhibitors may prevent formation of active metabolites of tamoxifen and possibly reduce the efficacy (e.g. amiodarone, haloperidol, risperidone)
  • 25. Raloxifene Second-generation SERM Antagonist estrogen receptors in the breast tissue Decreases bone resorption and overall bone turnover Bone density is increased, and vertebral fractures are decreased Has little to no effect on the endometrium and, may not predispose to uterine cancer Raloxifene lowers total cholesterol LDL in the serum It has no effect on HDL or triglyceride levels
  • 26. Therapeutic Uses Prophylaxis of breast cancer in high-risk women Prevention and treatment of osteoporosis in postmenopausal women
  • 27. Adverse effects Hot flashes Leg cramps Increased risk of DVT, PE, retinal-vein thrombosis Women who have a past or active history of venous thromboembolic events should not take the drug Should be avoided in women who are or may become pregnant (Category X) Coadministration with cholestyramine can reduce the absorption of raloxifene by 60% (Should not be used together)
  • 28. Clomiphene Acts as a partial estrogen agonist and interferes with the negative feedback of estrogens on the hypothalamus This effect increases the secretion of gonadotropin- releasing hormone and gonadotropins leading to stimulating ovulation Uses: Used to treat infertility associated with anovulatory cycles Not effective in women with ovulatory dysfunction due to pituitary or ovarian failure
  • 29. Adverse Effects Headache, Nausea Vasomotor flushes Visual disturbances Ovarian enlargement
  • 30. Question? A 50 year old women at a very high risk of breast cancer is given tamoxifen for prophylaxis. What is the main mechanism or effect of this drug? a) Blocks estrogen receptor in breast tissues b) Blocks estrogen receptor in endometrium c) Increase the risk of osteoporosis d) Raise plasma LDL and lower HDL e) Reduces the risk of thromboembolic diseases