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 inmany plants including saw palmetto, soybeans, etc…
PREPARATIONS AVERAGE REPLACEMENT DOSAGEEthinyl estradiol 0.005-0.02mg/dMicronized estradiol 1-2mg/dEstradiol cypionate 2-5mg every 3-4 weeksEstradiol valerate 2-20mg every other weekEstropipate 1.25-2.5mg/dConjugated, esterified, or mixed estrogenic substances:Oral 0.3-1.25mg/dInjectable 0.2-2mg/dTransdermal PatchChlorotrianisene 12-25mg/dMethallenestril 3-9mg/dQuinestrol 0.1-0.2mg/week
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….
I) Female maturation: For normal sexual maturation & growth of females. Stimulate development of vagina,uterus,fallopiantubes & secondary sexual characters. Stimulate stromal & ductal development in breasts. Axillary & pubic hair….& for typical female bodycontours…II) Endometrial effects: For development of endometrial lining. But continuous exposure leads to hyperplasia ofendometrium.
III) Metabolic effects:Anabolic nature….Decreases resorption rate of bone apoptosis ofosteoclastsIncreases levels of hepatic proteins such as transcortin,TBG, SHBG, transferrin, renin substrate & fibrinogen.Increases HDL & slight decrease in LDL( plasmacholesterol).IV) Effects on blood coagulation:Enhance coagulability of blood…..
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 extracellularspace, producing edema…
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 eachmonth & increase to adult doses until menopause… Progestin therapy simultaneously….
II) HORMONE REPLACEMENT THERAPYHighly efficacious in suppressing the peri -menopausal syndromes….Dose of estrogen used is less…..conjugated estrogens-0.625mg/dayProgestin should be added for 10-12 days each month.Recent findings emphasize a number of risks &limitations….USE HRTORNOT???
Developed specifically to be used for HRT…Suppresses menopausal syndromes & lowers raisedGn levels with a dose of 2.5mg daily…Decreased breast cancer risks..Side effects: weight gain, increased facial hair…
Senile vaginitisAcneDelayed puberty in girlsDysmenorrhoeaCarcinoma prostateDysfunctional uterine bleeding
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)
Name Uses Effects/locationclomifene used in anovulationantagonist athypothalamusfemarellemanaging menopausesymptoms, osteoporosisagonist at brain andboneormeloxifene contraceptionagonist at bone;antagonist at breast anduterusraloxifeneosteoporosis, breastcanceragonist at bone;antagonist at breast anduterustamoxifen breast canceragonist at bone anduterus, antagonist atbreasttoremifene breast cancerlasofoxifeneosteoporosis, breastcancer, vaginal atrophyagonist at the bone,antagonist at breast anduterus
Antagonist in breast tissue & agonist in uterus, bone,liver & pituitary….1stSERM to be introduced…Used extensively in the treatment of breast cancer inpost-menopausal women…Dose:10-20mg twice daily….Side effects: hot flushes, vomiting, dermatitis, vaginalbleeding….
Increase production of gonadotropins by inhibitingnegative feedback on hypothalamus….Binds to both ERα & ERβ & is a pure estrogenantagonistChief use is in sterility:50mg once daily × 5 days from 5thday of cycleAdv effects: polycystic ovarieshot flushesvertigoallergic dermatitis
RALOXIFENE:Partialagonist/antagonists1stline drug forosteoporosis in post-menopausal womenSide effects: hot flushes,leg crampsORMELOXIFENE:Antagonist in breast &uterusFor dysfunctionaluterine bleedingSide effects: nausea,headache
LETROZOLE:Inhibits aromatizationresulting in totalestrogen deprivationAdjuvant therapy aftermastectomy in earlybreast cancerANASTROZOLE:More potent thanletrozoleAdjuvant therapy forearly ER+ve breastcancer
LIFE IS SHORT…..SMILE ALWAYS........HELP OTHERS……….FORGET YOUR EGO’S……GAIN KNOWLEDGE……FORGIVE EVERYONE…..& REMEMBER…..YOUR HAPPINESS IS DEFINED BY NONE BUTYOU……-an anonymousphilosopher