Dr. V.SATHYA NARAYANAN M.D,
PROFESSOR OF PHARMACOLOGY
SRM MCH & RC, CHENNAI, INDIA
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
HORMONAL CONTRACEPTIVES
 100 million women use
 Fertility suppressed at will as long as desired
 Fertility returns on discontinuation
 Safe
 Convenient
 Low cost
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
ORAL CONTRACEPTIVES
 Combined pill
 Phased pill
 Mini pill
 Postcoital pill
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
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
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
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
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
INJECTABLE CONTRACEPTIVES
 Long acting progestin + estrogen once a
month
 Reasonable menstrual bleeding pattern
 Estrogen is harmful
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
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
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
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
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
RELATIVE CONTRAINDICATIONS
 Diabetes
 Smoking
 Mild hypertension
 Obesity
 Migraine
 Age above 35 years
 Gall bladder disease
 Undiagnosed vaginal bleeding
 Uterine leiomyoma
 Mentally ill
DRUG INTERACTIONS
 Contraception failure with enzyme inducers
like rifampin, phenytoin, carbamazepine
 Also with tetracycline, ampicillin
 Wise to increase the dose or use alternative
methods
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
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
MALE CONTRACEPTIVE
 No satisfactory solution yet
 Anti androgens  loss of libido
 Estrogens & progestins  feminization
 Androgens  not reliable
 Cytotoxic drugs like cadmium are toxic
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
THANK YOU…

Hormonal contraceptives satya ppt

  • 2.
    Dr. V.SATHYA NARAYANANM.D, PROFESSOR OF PHARMACOLOGY SRM MCH & RC, CHENNAI, INDIA
  • 3.
    HORMONAL CONTRACEPTIVES  Hormonalpreparations 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  100million 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  Combinedpill  Phased pill  Mini pill  Postcoital pill
  • 14.
    COMBINED PILL  Mostpopular & 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  Biphasicor triphasic ( ethinyl estradiol with levonorgetrel)  Reduce total progestin dose  Recommended for women over 35 years of age, with other risk factors
  • 18.
    MINIPILL  Progestin onlypill ( 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  YUZPEmethod – 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  Useonly 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  Longacting progestin + estrogen once a month  Reasonable menstrual bleeding pattern  Estrogen is harmful
  • 24.
    IMPLANTS  Drug deliverysystems 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  Lowerrisk 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  Legvein 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  Thromboembolicdisorders  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  Contraceptionfailure with enzyme inducers like rifampin, phenytoin, carbamazepine  Also with tetracycline, ampicillin  Wise to increase the dose or use alternative methods
  • 52.
    PRACTICAL POINTS  Missesa 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  Nosatisfactory solution yet  Anti androgens  loss of libido  Estrogens & progestins  feminization  Androgens  not reliable  Cytotoxic drugs like cadmium are toxic
  • 58.
    GOSSYPOL  Obtained fromcotton seed  Nonsteroidal compound  Effective orally  Suppress spermatogenesis  Infertility develops after few months  Does not affect libido, potency  S/E – Hypokalemia, edema, diarrhoea
  • 60.