This document discusses female and male sex hormones as well as oral contraceptives. It describes the natural and synthetic forms of estrogen, progesterone, and testosterone, their functions, therapeutic uses, and preparations. It then explains how oral contraceptives work by inhibiting ovulation and changes in the reproductive system. Different types of oral contraceptives are classified and their administration, uses, side effects, contraindications, and drug interactions are outlined.

1. Sex hormone and oral
contraceptives
Mr. Sujit Trimbak Karpe
Head of Department,
Sojar college of Pharmacy, Khandvi

2. Female sex hormone
› Oestrogen
› Progesterone

3. Female sex hormone - Oestrogen
A] Natural oestrogen:
› Major oestrogen produced by women are estradiol,
estrone, estriol.
› During first part of menstrual cycle oestrogens are
produced in ovarian follicle by thea cells

4. Female sex hormone - Oestrogen
A] Natural oestrogen:
› Major oestrogen produced by women are estradiol, estrone, estriol.
› During first part of menstrual cycle oestrogens are produced in ovarian
follicle by thea cells.
› Essential to stimulate secondary sex characters in females.
› Essential for growth and activity of mammary gland and endo metrium.
› Essential to pepare endometrium for progesterone action.
› It is known to prepare the uterus for spermatozoal transport.

5. Female sex hormone - Oestrogen
B] Synthetic oestrogen:
› When synthetic oestrogenis administered, released
in circulation, strongly bind to proteins and reaches
to their site of actions that is uterus, vagina, breast,
anterior pituitary, hypothalamus.

6. Female sex hormone - Oestrogen
› Therapeutic application:
› Menopausal syndrome
› Ovarian dysgenesis
› Primary amenorrhoea
› Carcinoma of prostate in male
› To treat breast cancers in postmenopausal women.
› To treat functional uterine bleeding and endometriosis.
› To treat dysmenorrhea.
› As an oral contraceptive with progeasterone.

7. Female sex hormone - Oestrogen
› Contraindications:
› Pre menopausal carcinoma of breast and uterus.
› Hypertension and thromboembolic diseases.
› Undiagnosed genital bleeding.
› Renal and hepatic diseases.
› Side effects:
› Nausea and vomiting
› Breast tenderness
› Salt and water retention caused weight gain, oedema and cardiac failure

8. Female sex hormone - Oestrogen
› Preparations:
› Naturally occurring oestrogen – oestradiol 17 – beta – 0.22 to 1.5 mg I/M
› Semi synthetic steroidal oestrogen
1. Ethynyl estradiole – 0.05 to 0.1 mg orally
2. Mestranol – 0.1 to 0.2 mg orally
3. Quinesterol – 0.05 to 0.1mg orally
› Synthetic non steroidal oestrogen
1. Benzoesterol 0.2 mg to 1 mg orally
2. Hexoestrol 3 to 6 mg orally.

9. Female sex hormone – Progesterone
1] Natural Progesterone
› Steriod derivative.
› Pregnane is the natural progesterone.
› Synthesized in ovary, testis, placenta and adrenals.
› Very short plasma half life 5 min
› Rapidly metabolized by liver and is excreted through
urine as sulphate and glucouronide conjugates.

10. Female sex hormone – Progesterone
1] Natural Progesterone
› Pharmacological action:
› Induces secretary phase in endometrium.
› If ovum is not fertilized secretion of progesterone is inhibited, which is
responsible for onset of menstruation.
› If ovum is fetilised progesterone prepares endometrium for implantation.
› Develops breast for lactation.
› Makes uterus less sensitive to oxytocin.

11. Female sex hormone – Progesterone
2] Synthetic Progesterone
› Are classified in to three groups
1. Progesterone derivatives
2. Testosterone derivatives
3. 19-non-testosterone derivatives

12. Female sex hormone – Progesterone
› Therapeutic uses:
› Mainly as oral contraceptive
› As a diagnostic to test oestrogen secretion.
› Contraindication :
› May increase blood pressure in female
› May cause atherosclerosis.
› Preparation:
› Nor-ethindrone 0.5mg
› Nor-gestrel 0.05mg

13. Male sex hormone – Testosterone
1] Natural Testosterone
› Synthesis:
› Testes, ovary, adrenal cortes and placenta secret enzymes, which play an
important role in synthesis of testosterone.
› It occurs in interstitial cells of leydig and also in subtenticular sertoli cells.
› In systemic circulation it attaches to sex hormone binding protein and reaches the
target cells.
› Metabolism and excretion:
› Inactivated in liver and as conjugate with sulphate and glucouronide, is excreted
in urine.

14. Male sex hormone – Testosterone
1] Natural Testosterone
› Properties:
› Induces secondary sex characters in male like body hair, deep voice and penile growth.
› Support spermatogenesis.
› Induces protein anabolism.
› Therapeutic uses:
› Used to treat cryptochildism
› As replacement therapy in hypogonadism
› In females, it is used to treat breast cancer.
› As it is capable of stimulating haemopoeiasis, it may be used in aplastic anemia and leukaemias.

15. Male sex hormone – Testosterone
1] Natural Testosterone
› Contraindication:
› Carcinoma of prostate.
› Hypertension
› Liver disease
› Preparations:
› Testosterone injection – 50mg I/V three times weekly
› Testosterone propionate – 5 to 25 mg oil I/M four times weekly
› Methyltestosterone – 25 mg to 50 mg sublingually/ orally

16. Oral contraceptive
› These agents when administered internally prevent conception (pregnancy).
› Mechanism of action:
1. Combination selectively inhibit pitutory function. The hypothalamic GRH is
inhibited which leads to inhibition of FSH and LH release from pitutory. This
results in inhibition of ovulation.
2. Combination produces change in cervical mucus, in uterine endometrium,
change in motility and secretion of fallopian tube. All these changes decreases
possibility of conception and implantation.
3. It is postulated that oestrogen produces all above effect while progesterone
only causes endometrium shredding.

17. Oral contraceptive
› Classification:
› Into three groups
1. Oestrogen, progesterone- Combination pill
2. Sequential oestrogen, progesterone- Sequential pill
3. Countinuous low dose progesterone – mini pill.

18. Oral contraceptive

19. Oral contraceptive
› Mode of administration:
Combination pill Administered as a single daily dose from 5th day to
25th day of menstrual cycle, counting 1st day of cycle
as day one
Sequential pill Administered from 5th day to 25th day of menstrual
cycle
First 5 to 20 days of cycle alone oestrogen single daily
dose. Remaining 5 days only oestrogen and
progesterone combination
Minipills Daily in continuation

20. Oral contraceptive
› Therapeutic uses:
› As an oral contraceptive
› Used in endometriosis, characterized by severse days menorrhea.
› Used to treat premenopausal tension and menstrual irregularities.
› Side effect:
› Nausea, vomiting, headache, lethargy, breast discomfort, breakthrough bleeding, oedema, mild
depression are mild side effect.
› Serious side effect includes, amenorrhea, weight gain, increased skin pigmentation, vaginal
infection.
› Moderate side effects includes, thromboembolism, myocardial infraction, GI disorder.

21. Oral contraceptive
› Contraindications:
› Thromboembolic diseases
› Breast and uterine carcinoma
› Vaginal bleeding
› Migraine
› Hypertension
› Epilepsy
› Precaution:
› It is better to follow advice of gynecologist before therapy.
› Great care must be taken in cases with previous history of asthma, diabetes and endocrine disorder.
› Therapy should be discontinued if person reports headache and acute visual disturbance.

22. Oral contraceptive
› Drug interaction:
› Antibiotics like Rifampicin, anti tubercular drug, increases
the incidence of break through bleeding in women .
› Antibiotics like Ampicillin and tetracycline, have been known
for failure of oral contraception.
› Drugs like Phenytoin, Phenobarbiton are potent inducer of
hepatic microsomal enzymes and hence are expected to
increase rate of metabolism of contraceptive.