Female Sex Hormones And Hormonal Contraception Oestrogens

These drugs can be classified into three groups.

1. Natural – estradiol, esterone, estriol
2. Semisynthetic – Ethnylestradiol
3. Synthetic: Diethylstibosterol

Natural

Estradiol: Estradiol is most potent, major secretory product of ovary.It is oxidized into esterone by liver; estrone is hydrated to estriol and synthesized by ovarian follicle, adrenal cortex, fetoplacental unit, and testis. Androgen and testestrone are precursor for estrogen. Certain tissue can make estrone from androgen.

Semisynthetic

Ethylestadiol: Highly potent, effective orally

Absorption and Fate: It is absorbed from GI and skin and rapidly metabolized in the liver

Physiologic actions:

Genital system

Ovary: estrogen affects the ovary through indirectly influencing the secretion of gonadotrophin

Uterus: it affects the ‘proliferative phase’ of the endometrium and also increases the growth and sensitivity of myometrium for oxytocin.

Cervix: it makes cervical mucus thin and alkaline

Vagina: Stratification, cornification and glycogen deposit is affected by estrogen.

Breast

Estrogen causes the growth of gland and duct system

Anterior pitutary

Estrogen inhibit release of gonadotrophins (FSH, LH)

Metabolic action:

1. Retention of salt and water
2. Plasma lipid level: it increases the level of high density lipoprotein and triglycerides while decreases the level of low density lipoprotein and cholesterol.
3. Increases Ca^tt bone deposition
4. It has a mild anabolic action

Blood coagulation

Enhance level of factor II, VII, IX, X so, increase the coagulability of blood and may predispose to thromboembolic condition

Therapeutic use: contraceptive in combination with progestogens, Functional uterine bleeding, Dysmenorrhea, Alleviation of menopausal disorder, Osteoporosis, Replacement therapy in ovarian failure, Prevents senile and atrophic vaginitis

Side effects: Thromboembolism, Sodium and water retention, Withdrawal bleeding, nausea, endometrial carcinoma

Contraindication: History of thromboembolism condition, Undiagnosed uterine bleeding, endometrial Carcinoma, liver disease

PROGESTOGENS

Progestrone is natural occuring progestational hormone.it is synthesized by corpus luteum, placenta, adrenal cortex, testis. It is less effective orally due to complete metabolism by liver so it’s given through intramuscular route.

Actions on genital organs:

Ovary – Inhibition of ovulation

Uterus – converts the endometrum for secretory phase and makes the myometrium less sensitive to oxytocin. It also causes relaxation of the uterus in late pregnancy.

Metabolic actions:

• Thermogenic action
• Competes with aldosterone at renal tubule so inhibits sodium reabsorption.

Synthetic /Senisynthetic progestogens:

Derivative of progestrone: Hydroxyprogesterone capriot/medroxyprogestrone Derivative of testestrone:  Dimethisterone

Nortestrone:    Norethisterone

Therapeutic use: Hormonal contraception, functional uterine bleeding, dymennorrhea Ammenorrhea, Endometrial Carcinoma, Premenustral tension.