ESTROGEN & ANDROGEN

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 Estrogens

Estradiol known as 17-β-Estradiol most imp Estrogen produced in Ovary…

principle Estrogen in Postmenopausal women…

Estrone have 1/3rd potency of Estradiol…

primary circulating Estrogen after Menopause.

Estriol, metabolite of Estradiol produced by Placenta...

Estrone & Equilin prep used in HRT (Hormone replacement therapy)

PAST PAPER SERIES 

Tamoxifene & Raloxifene; Selective Estrogen Receptor Modulator…nonsteroidal..exert estrogenic or Antiestrogenic effects…

MOA=bind to sex hormone in plasma...diffuse across cell memb...bind to nuclear

protein.. Two estrogen receptor α & β…α-receptor is CLASSIC receptor…α-receptor

promote Transcription while β- contain REPRESSER domain….result in synthesis of

different protein…

T.E= used for Contraception& Postmeopausal hormone therapy..prevention of

Osteoporosis…

S.E= nausea, breast tenderness….

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Selective Estrogen Receptor Modulator

Toremifene is an orphan drug…

MOA=bind to estrogen receptor...show different effects…Raloxifene exhibit of

anatagonism of Estrogen...decrease bone resorption & bone turnover...lower cholesterol

and LDL

Clomiphene partial agonist…interfere with negative feedback of Estrogen

T.E= Tamoxifene used in Metastatic breast cancer...Raloxifene for prophylaxis of

breast cancer….Clomiphene used to treat Infertility…

S.E= Tamoxifene cause hot flushes, nausea, Vaginal bleeding, menstrual irregularities

Raloxifene cause leg cramps, hot flush, pulmonary embolism, deep-vein thrombosis..

Clomiphene risk of twins or triplets

Progestogens

Progestrone=produced in response to LH…Both inmale & female…develop sec

endometrium for new Embryo….high level produced in Menses…continue the

pregnancy…

MOA

1)increase Glycogen thrpugh insulin-mediated mechanism…

2) decrease Na+ reabsorption in kidney due to competition with Aldosterone at Mineralocorticoid receptor.

3) Increase in body temp…

4) decreases in plasma Amino acid

5) increase excretion of urinary nitrogen

T.E= for contraception, dysmenorrheal, infertility, Dysfunctional uterine bleeding

S.E= weight gain, depression, change in libido, acne, hirsutism…Medroxyprogestrone

cause risk of Osteoporosis…

Antiprogestin Mifepristone = Progestrone antagonist…potent Glucocorticoid

activity…cause Abortion.

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CONTRACEPTIVES


Contraceptives

Drugs decrease fertility by preventing ovulation, impairing Gametogenesis, interfering

with Gestation

1) Combination Oral Contraceptive= combination of Progestine &Estrogen 

Monophasic combination; Estrogen + Progestin over 21 days

Triphasic combination; contant dose of Estrogen + increasing dose of Progestin over 21days

2) Transdermal patch=Ethinyl Estradiol + Norelgestromin for 3 week...4 week bleeding

occurs…

3) Vaginal ring= Ethinyl Estradiol + Etonogestrel for 3 week

4) Progestin-only pills= Norethindrone5) Injectable Progestin= Medroxyprogestrone acetate inj..every 3month…

6) Progestin implants= tonogesterl 4cm cap for 3year….

7) Progestin Intrauterine Device= Levonorgestrel-releasing intrauterine sys...upto 5yr.. 

8) Postcoital Contraception=called emergencycontraceptive…high dose of progestin 

(0.75mg) or high dose of Estrogen (100ug) within 72hr of intercourse… 

MOA=Estrogen negative feedback on LH & FSH , inhibit ovulation….Progestin inhibit LH 

release & thickness...inhbit transport of sperm…..

S.E= depression, fluid retention, thromboembolism, hyprtension, M.I, OVARIAN CANCER, Cervical cancer due to Human Papilloma virus…abnormal glucose intolerance contraindicated in pregnancy, liver disease, cerebrovascular.. 

Androgens 

Group of steroid have anabolizng & masculinizing effects in both male & female… 

Testosterone produced by Leyding cells…

MOA= bind to specific receptor...diffuse into prostate,skin, seminal vesicle...convert into 

5α-DIHYDROTESTOSTERONE(DHT)……

In brain, liver adipose tissue converted into Aromatose…bind to DNA ...specific protein 

T.E= increase androgen secretions in Hypogonadism….treat Senile Osteoporosis…

Donazol used in Endometriosis & breast disease….DihydroEpiAndrosterone (DHEA)

antiaging

P.K= I.M inj…alkylation at 17α position

S.E= growth of facial hair, acne, impotence, gynecomastia, abuse by athletes 

Antiandrogens 

Interfere with synthesis of Androgens or blocking their receptor….Finnastride & 

Dutasteroid……used in Prostatic cancer



 

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