This ppt is on the pharmacology of hormonal contraceptives...

2. Dr. V.SATHYA NARAYANAN M.D,
PROFESSOR OF PHARMACOLOGY
SRM MCH & RC, CHENNAI, INDIA

3. HORMONAL CONTRACEPTIVES
 Hormonal preparations used for reversible
suppression of fertility
 Need of the day
 Mortality rate has declined and birth rate has
increased
 High failure rate with other contraceptive
methods

6. HORMONAL CONTRACEPTIVES
 100 million women use
 Fertility suppressed at will as long as desired
 Fertility returns on discontinuation
 Safe
 Convenient
 Low cost

9. MECHANISM OF ACTION
 Inhibit Gonadotropin release
 Estrogen reduces FSH, progestin reduces LH
 Both synergize to inhibit midcycle LH surge 
no ovulation
 Thick cervical mucus secretion  hostile to
sperm
 Cause uterine, tubal contractions
 Make endometrium unsuitable for
implantation

12. ORAL CONTRACEPTIVES
 Combined pill
 Phased pill
 Mini pill
 Postcoital pill

14. COMBINED PILL
 Most popular & most effective
 Contains an estrogen + a progestin
 Ethinyl estradiol + a progestin ( norgestrel or
levonorgestrel or desogestrel) ( OVRAL)
 Both synergize to inhibit ovulation
 Progestin blocks the risk of endometrial cancer,
ensures prompt bleeding
 Start on 5th
day of menses, 1 tab/day for 21 days
 After 7 days gap next course is started

16. PHASED PILL
 Biphasic or triphasic ( ethinyl estradiol with
levonorgetrel)
 Reduce total progestin dose
 Recommended for women over 35 years of
age, with other risk factors

18. MINIPILL
 Progestin only pill ( norethindrone or
norgestrel)
 Estrogen is eliminated because of risks
 Low dose progestin is taken daily without gap
 Efficacy is lower
 Less popular

20. POSTCOITAL PILL
 YUZPE method – 2 OVRAL tablets as early
as possible after coitus , repeated after 12
hours
 S/E – nausea, vomiting
 Or levonorgestrel 0.75 mg as early as possible
,then 1 tab after 12 hours
 Taken within 72 hours of coitus
 Or mifepristone 600mg single dose

22. INJECTABLE CONTRACEPTIVES
 Use only under close suprvision
 Given I.M
 Long acting progestin alone injected once in
2-3 months – depot medroxyprogesterone
acetate 150 mg or norethindrone enanthate
 S/E – amenorrhoea, menstrual irregularities,
carcinogenesis, weight gain, dec bone
mineral index
 Return of fertility takes 6- 3o months

23. INJECTABLE CONTRACEPTIVES
 Long acting progestin + estrogen once a
month
 Reasonable menstrual bleeding pattern
 Estrogen is harmful

24. IMPLANTS
 Drug delivery systems implanted under the
skin  slowly release progestin over 1-5
years
 Norplant – subcut implantation of
levonorgestrel, works upto 5 years
 Progestasert – progesterone impregnated
intrauterine insert acting on endometrium
replaced yearly

27. HEALTH BENEFITS
 Lower risk of endometrial, ovarian, colorectal
cancer
 Cycles become regular
 Less blood loss
 No premenstrual tension, pain
 Low incidence of fibrocystic breast disease
 Improvement in endometriosis, pelvic
inflammatory disease

29. NONSERIOUS ADVERSE EFFECTS
 Nausea, vomiting similar to morning sickness
 Mild headache
 Breast discomfort
 Breakthrough bleeding
 Weight gain, acne
 Pigmentation of cheeks, nose, forehead
 Carbohydrate intolerance, diabetes in few
taking high dose pills
 Mood swings with minipills

37. SERIOUS COMPLICATIONS
 Leg vein thrombosis, Pulmonary thrombosis
with older pills
 Coronary, cerebral thrombosis resulting in
MI, Stroke  not seen with low dose pills
 Rise in BP
 Minor increase in breast cancer
 Benign hepatomas
 Gall stones

41. ABSOLUTE CONTRAINDICATIONS
 Thromboembolic disorders
 Coronary artery disease
 Cerebrovascular disease
 Hypertension, hyperlipidemias
 Active liver disease, hepatoma, H/O jaundice
 Suspected genital / breast carcinoma
 Porphyria
 Impending major surgery

45. RELATIVE CONTRAINDICATIONS
 Diabetes
 Smoking
 Mild hypertension
 Obesity
 Migraine
 Age above 35 years
 Gall bladder disease
 Undiagnosed vaginal bleeding
 Uterine leiomyoma
 Mentally ill

50. DRUG INTERACTIONS
 Contraception failure with enzyme inducers
like rifampin, phenytoin, carbamazepine
 Also with tetracycline, ampicillin
 Wise to increase the dose or use alternative
methods

52. PRACTICAL POINTS
 Misses a pill  2 tab next day and continue as
usual
 Missed more than 2 tab  use alternate
methods , start pills on 5th day of menses
 If pregnancy occurs  terminate it
 If breakthrough bleeding occur  switch to high
estrogen pill
 Use Progestin only pill if estrogen is
contraindicated
 Use desogestrel if androgenic side effects occur
due to older progestins

54. CENTCHROMAN
 Nonsteroidal SERM
 Oral contraceptive Developed in india
 Act as an antiimplantation agent
 Failure rate 1-3%
 No usual side effects of hormonal
contraceptives
 Does not affect blood sugar, lipid profile
 Not teratogenic, carcinogenic or mutagenic
 More experience has to be gained

56. MALE CONTRACEPTIVE
 No satisfactory solution yet
 Anti androgens  loss of libido
 Estrogens & progestins  feminization
 Androgens  not reliable
 Cytotoxic drugs like cadmium are toxic

58. GOSSYPOL
 Obtained from cotton seed
 Nonsteroidal compound
 Effective orally
 Suppress spermatogenesis
 Infertility develops after few months
 Does not affect libido, potency
 S/E – Hypokalemia, edema, diarrhoea

60. THANK YOU…