1. FEMALE SEX HORMONES

2. FEMALE SEX HORMONES ESTROGENS NATURAL SYNTHETIC
Estradiol(major estrogen): secreted by ovary
Estrone: oxidation of estradiol in liver
Estriol: hydroxylation of estrone
SYNTHETIC
Ethinyl Estradiol(EE)
Mestranol
Tibolone

3. FEMALE SEX HORMONES PROGESTINS NATURAL SYNTHETIC
Progesterone
SYNTHETIC
1- Progesterone derivatives
Older- MPA
Newer- Nomegestrol acetate
2- 19-Nortestosterone derivatives
Older- Levonorgestrel
Newer- Desogestrel

4. FUNCTIONS OF ESTROGEN 1-Pubertal changes in the female:
Growth of uterus, fallopian tubes and vagina
Proliferation of endometrium
Growth of breasts- proliferation of ducts and stroma & accumulation of fat
Acne: due to small amount of androgens produced simultaneously

5. FUNCTIONS OF ESTROGEN 2. Metabolic effects 3. Bone
Anabolic but weaker than testosterone
3. Bone
Continued action of estrogen promotes fusion of epiphyses
Retarding bone resorption
Osteoclast pit formation is inhibited
Increased expression of bone matrix proteins such
as osteonectin, osteocalcin & collagen

6. FUNCTIONS OF ESTROGEN 4. BP: Mild salt & water retention Edema
BP may rise
5. Blood:
Blood coagulability is increased
Induce the synthesis of clotting factors (factors II, VII, IX and X)

7. FUNCTIONS OF ESTROGEN 6. Lipid profile:
Decrease plasma LDL cholesterol
Increase HDL and triglyceride levels
Atherosclerosis in premenopausal- rare
7. Glucose:
Impair glucose tolerance
Diabetes may precipitate
8. Bile:
Increase lithogenicity of bile by increasing cholesterol secretion and reducing bile salt secretion

8. ORAL CONTRACEPTIVE PILLS

9. INTRODUCTION
ORAL CONTRACEPTION method of contraception in which pills are taken orally to prevent pregnancy.
OCPs are also known as the BIRTH CONTROL PILLS

10. Types Of OCPs Combined Oral Contraceptives
Monophasic Pills
Biphasic Pills
Triphasic Pills
Progesterone Only Contraceptives
Emergency contraceptives

11. COMBINED OCPs Contain Estrogen & Progesterone
Taken for 21 consecutive days followed by 7 pill free days

12. PROGESTRONE ONLY PILLS(POPs)
Also known as the ‘Minipill’
Ingested once daily everyday
No pill free days
Higher failure rate

13. MECHANISM OF ACTION

14. NON-HORMONAL CONTRACEPTIVES
Available under brand name ‘SAHELI’
It contains Centchroman(Ormeloxifene), which is a SERM(Selective Estrogen Receptor Modulator)

15. SIDE EFFECTS OF OCPs A- Nonserious side effects: Nausea and vomiting:
Similar to morning sickness of pregnancy
Chloasma:
Pigmentation of cheeks, nose and forehead
Similar to that occurring in pregnancy

16. SIDE EFFECTS OF OCPs Headache, Migraine may be precipitated
Breakthrough bleeding or spotting
Amenorrhoea:
Especially with injectables and minipill
Breast discomfort
Carbohydrate intolerance and precipitation of diabetes

17. SIDE EFFECTS OF OCPs Lipid profile:
No significant alteration with low dose OCs
E: raise plasma HDL/LDL ratio (beneficial)
P: nullifies this

18. OCP: WEIGHT GAIN OR LOSS
Older progestins(Levonorgestrel)
May be due to androgenic action
Weight gain
Acne
Increased body hair
Newer progestins (desogestrel)
No androgenic action
No weight gain

19. SERIOUS COMPLICATIONS
1- Leg vein and pulmonary thrombosis:

20. SERIOUS COMPLICATIONS
1- Leg vein and pulmonary thrombosis:
Marginal with the newer reduced E content pills
Increased risk in:
Women >35 years of age
Diabetics
Hypertensives
Smokers

21. SERIOUS COMPLICATIONS
2. Coronary and cerebral thrombosis:
Myocardial infarction
Stroke
3. Rise in BP:
Less frequent with the low-dose pills
If the BP rises, best is to stop OCs
Both E & P are responsible
Increase the renin activity
Salt and water retention

22. SERIOUS COMPLICATIONS
4. Genital carcinoma:
Animal data:
An increased incidence of vaginal, cervical, and breast cancers

23. SERIOUS COMPLICATIONS
Extensive epidemiological data over the past 30 years has
shown that:
OCPs do not increase the occurrence of these cancers but risk is increased in predisposed individuals
Growth of already existing hormone dependent tumour may be hastened
Minor increase in breast cancer incidence among current OC users, but not among past users
Since breast cancer is rare in young women, this finding is considered inconsequential
Protective effect against endometrial carcinoma

24. SERIOUS COMPLICATIONS
5. Benign hepatomas:
May rupture or turn malignant
Incidence slightly higher in OC users
6. Gallstones:
Slightly increased incidence in OCs users

25. BREAKTHROUGH BLEEDING(BTB)
Spotting or bleeding from the uterus occurring between menstrual periods
Side effect of some oral contraceptives
Usually occurs during the first one or two cycles and resolves itself spontaneously

26. BREAKTHROUGH BLEEDING(BTB)
CAUSE:
Insufficient estrogens or.
Excess estrogen
Dosage of estrogen in the OCs pills is much lower than the quantity produced naturally by the ovaries
Higher quantities produced by the ovaries induce proliferation
Low levels supplied by the pills:
Produce atrophy(responsible for bleeding)
But sufficient to inhibit the endogenous secretion of the gonadotropins.

27. TREATMENT
Usually occurs during the first one or two cycles and resolves itself spontaneously
Switch to a non-hormonal method  
Pill with a higher estrogen
Stimulate proliferation of the endometrium

28. BENEFICIAL EFFECTS OF OCPs
Reduced menstrual blood loss and associated Anaemia
Cycles become regular
Improvement in:
Premenstrual tension
Dysmenorrhoea
Endometriosis
Pelvic inflammatory disease
Fibrocystic breast disease
Ovarian cysts

29. BENEFICIAL EFFECTS OF OCPs
Lower risk of developing:
Endometrial carcinoma Q
Ovarian carcinoma Q
Colorectal cancer

30. PHARMACOKINETICS OF ESTROGENS
TETRACYCLINE Q/AMPICILLIN WITH OCPs:
Metabolise in liver
Conjugation with glucuronic acid and sulfate
Excreted in urine and bile & reach the small intestine
Deconjugation by hydrolytic enzymes of intestinal bacteria
Release of active estrogenic hormone
Enterohepatic circulation of active hormone
Ultimate disposal occurs mostly in urine

31. ENZYME INDUCERS WITH OCPS
Phenytoin Q
Phenobarbitone Q
Primidone
Carbamazepine Q
Rifampin Q
Metabolism of estrogenic as well as progestational component is increased
SOLUTION:
Switch over to a preparation containing 50 µg of EE
Alternative method of contraception.

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