2. BY
NABEEL AHAMED

3. Can induce estrous cycle in spayed animals.
Primary female sex hormone.
Adolf Butenandt & Edward Adeltbert Doisy isolated &
determined the structure of estrogen.
Estrogen-mimetic compounds(flavanoids) found in
many plants including saw palmetto, soybeans, etc…

4. 1.Estradiol
2.Estrone
3.Estratriol
Natural
MESTRANOL
ETHINYL-
ESTRADIOL
TIBOLONE
STILBESTROL
HEXESTROL
DIENESTROL

5. Synthetic substances Xenoestrogens
Plant products Phytoestrogens
Fungal products Mycoestrogens

7. PREPARATIONS AVERAGE REPLACEMENT DOSAGE
Ethinyl estradiol 0.005-0.02mg/d
Micronized estradiol 1-2mg/d
Estradiol cypionate 2-5mg every 3-4 weeks
Estradiol valerate 2-20mg every other week
Estropipate 1.25-2.5mg/d
Conjugated, esterified, or mixed estrogenic substances:
Oral 0.3-1.25mg/d
Injectable 0.2-2mg/d
Transdermal Patch
Chlorotrianisene 12-25mg/d
Methallenestril 3-9mg/d
Quinestrol 0.1-0.2mg/week

8. Available in 5,10 and 20 cm sq. delivering 0.025 mg,
0.05 mg and 0.1 mg respt in 24hr for 3-4 days….
An oral progestin is added for the last 10-12 days…
Avoids high hepatic delivery….

10. I) Female maturation:
 For normal sexual maturation & growth of females.
 Stimulate development of vagina,uterus,fallopian
tubes & secondary sexual characters.
 Stimulate stromal & ductal development in breasts.
 Axillary & pubic hair….& for typical female body
contours…
II) Endometrial effects:
 For development of endometrial lining.
 But continuous exposure leads to hyperplasia of
endometrium.

11. III) Metabolic effects:
Anabolic nature….
Decreases resorption rate of bone apoptosis of
osteoclasts
Increases levels of hepatic proteins such as transcortin,
TBG, SHBG, transferrin, renin substrate & fibrinogen.
Increases HDL & slight decrease in LDL( plasma
cholesterol).
IV) Effects on blood coagulation:
Enhance coagulability of blood…..

12. V) Other effects:
Induces synthesis of progesterone receptors.
Stimulates central components of stress system &
promotes a sense of well being…
Also cause loss of intravascular fluid into extracellular
space, producing edema…

13. I) Primary hypogonadism:
 In estrogen deficient patients..
 Treatment usually begins at 11-13 yrs of age….
 To mimic the physiology of puberty…
 Start with small doses of estrogen on days 1-21 each
month & increase to adult doses until menopause…
 Progestin therapy simultaneously….

14. II) HORMONE REPLACEMENT THERAPY
Highly efficacious in suppressing the peri -
menopausal syndromes….
Dose of estrogen used is less…..
conjugated estrogens-0.625mg/day
Progestin should be added for 10-12 days each month.
Recent findings emphasize a number of risks &
limitations….
USE HRT
OR
NOT???

17. Developed specifically to be used for HRT…
Suppresses menopausal syndromes & lowers raised
Gn levels with a dose of 2.5mg daily…
Decreased breast cancer risks..
Side effects: weight gain, increased facial hair…

18. Senile vaginitis
Acne
Delayed puberty in girls
Dysmenorrhoea
Carcinoma prostate
Dysfunctional uterine bleeding

19. Compounds that act on estrogen receptor…
Can be agonists as well as antagonists….
Spectrum of activity:
Pure agonists (eg.natural estrogen)
Mixed agonists/antagonists(eg.Tamoxifen)
Pure antagonists(eg.fulvestrant)

20. Name Uses Effects/location
clomifene used in anovulation
antagonist at
hypothalamus
femarelle
managing menopause
symptoms, osteoporosis
agonist at brain and
bone
ormeloxifene contraception
agonist at bone;
antagonist at breast and
uterus
raloxifene
osteoporosis, breast
cancer
agonist at bone;
antagonist at breast and
uterus
tamoxifen breast cancer
agonist at bone and
uterus, antagonist at
breast
toremifene breast cancer
lasofoxifene
osteoporosis, breast
cancer, vaginal atrophy
agonist at the bone,
antagonist at breast and
uterus

22. Antagonist in breast tissue & agonist in uterus, bone,
liver & pituitary….
1st
SERM to be introduced…
Used extensively in the treatment of breast cancer in
post-menopausal women…
Dose:10-20mg twice daily….
Side effects: hot flushes, vomiting, dermatitis, vaginal
bleeding….

23. Increase production of gonadotropins by inhibiting
negative feedback on hypothalamus….
Binds to both ERα & ERβ & is a pure estrogen
antagonist
Chief use is in sterility:
50mg once daily × 5 days from 5th
day of cycle
Adv effects: polycystic ovaries
hot flushes
vertigo
allergic dermatitis

24. RALOXIFENE:
Partial
agonist/antagonists
1st
line drug for
osteoporosis in post-
menopausal women
Side effects: hot flushes,
leg cramps
ORMELOXIFENE:
Antagonist in breast &
uterus
For dysfunctional
uterine bleeding
Side effects: nausea,
headache

25. LETROZOLE:
Inhibits aromatization
resulting in total
estrogen deprivation
Adjuvant therapy after
mastectomy in early
breast cancer
ANASTROZOLE:
More potent than
letrozole
Adjuvant therapy for
early ER+ve breast
cancer

26. LIFE IS SHORT…..
SMILE ALWAYS........
HELP OTHERS……….
FORGET YOUR EGO’S……
GAIN KNOWLEDGE……
FORGIVE EVERYONE…..
& REMEMBER…..
YOUR HAPPINESS IS DEFINED BY NONE BUT
YOU……
-an anonymous
philosopher