3. ďCan induce estrous cycle in spayed animals.
ďPrimary female sex hormone.
ďAdolf Butenandt & Edward Adeltbert Doisy isolated &
determined the structure of estrogen.
ďEstrogen-mimetic compounds(flavanoids) found in
many plants including saw palmetto, soybeans, etcâŚ
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. ďAvailable in 5,10 and 20 cm sq. delivering 0.025 mg,
0.05 mg and 0.1 mg respt in 24hr for 3-4 daysâŚ.
ďAn oral progestin is added for the last 10-12 daysâŚ
ďAvoids high hepatic deliveryâŚ.
9.
10. I) Female maturation:
ď For normal sexual maturation & growth of females.
ď Stimulate development of vagina,uterus,fallopian
tubes & secondary sexual characters.
ď Stimulate stromal & ductal development in breasts.
ď Axillary & pubic hairâŚ.& for typical female body
contoursâŚ
II) Endometrial effects:
ď For development of endometrial lining.
ď But continuous exposure leads to hyperplasia of
endometrium.
11. III) Metabolic effects:
ďAnabolic natureâŚ.
ďDecreases resorption rate of bone apoptosis of
osteoclasts
ďIncreases levels of hepatic proteins such as transcortin,
TBG, SHBG, transferrin, renin substrate & fibrinogen.
ďIncreases HDL & slight decrease in LDL( plasma
cholesterol).
IV) Effects on blood coagulation:
ďEnhance coagulability of bloodâŚ..
12. V) Other effects:
ďInduces synthesis of progesterone receptors.
ďStimulates central components of stress system &
promotes a sense of well beingâŚ
ďAlso cause loss of intravascular fluid into extracellular
space, producing edemaâŚ
13. I) Primary hypogonadism:
ď In estrogen deficient patients..
ď Treatment usually begins at 11-13 yrs of ageâŚ.
ď To mimic the physiology of pubertyâŚ
ď Start with small doses of estrogen on days 1-21 each
month & increase to adult doses until menopauseâŚ
ď Progestin therapy simultaneouslyâŚ.
14. II) HORMONE REPLACEMENT THERAPY
ďHighly efficacious in suppressing the peri -
menopausal syndromesâŚ.
ďDose of estrogen used is lessâŚ..
conjugated estrogens-0.625mg/day
ďProgestin should be added for 10-12 days each month.
ďRecent findings emphasize a number of risks &
limitationsâŚ.
USE HRT
OR
NOT???
15.
16.
17. ďDeveloped specifically to be used for HRTâŚ
ďSuppresses menopausal syndromes & lowers raised
Gn levels with a dose of 2.5mg dailyâŚ
ďDecreased breast cancer risks..
ďSide effects: weight gain, increased facial hairâŚ
19. ďCompounds that act on estrogen receptorâŚ
ďCan be agonists as well as antagonistsâŚ.
ďSpectrum of activity:
ďźPure agonists (eg.natural estrogen)
ďźMixed agonists/antagonists(eg.Tamoxifen)
ďźPure 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
21.
22. ďAntagonist in breast tissue & agonist in uterus, bone,
liver & pituitaryâŚ.
ď1st
SERM to be introducedâŚ
ďUsed extensively in the treatment of breast cancer in
post-menopausal womenâŚ
ďDose:10-20mg twice dailyâŚ.
ďSide effects: hot flushes, vomiting, dermatitis, vaginal
bleedingâŚ.
23. ďIncrease production of gonadotropins by inhibiting
negative feedback on hypothalamusâŚ.
ďBinds to both ERÎą & ERβ & is a pure estrogen
antagonist
ďChief use is in sterility:
50mg once daily Ă 5 days from 5th
day of cycle
ďAdv effects: polycystic ovaries
hot flushes
vertigo
allergic dermatitis
25. LETROZOLE:
ďInhibits aromatization
resulting in total
estrogen deprivation
ďAdjuvant therapy after
mastectomy in early
breast cancer
ANASTROZOLE:
ďMore potent than
letrozole
ďAdjuvant therapy for
early ER+ve breast
cancer
26. LIFE IS SHORTâŚ..
SMILE ALWAYS........
HELP OTHERSâŚâŚâŚ.
FORGET YOUR EGOâSâŚâŚ
GAIN KNOWLEDGEâŚâŚ
FORGIVE EVERYONEâŚ..
& REMEMBERâŚ..
YOUR HAPPINESS IS DEFINED BY NONE BUT
YOUâŚâŚ
-an anonymous
philosopher