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Hormonal contraception
Dr. Pramod P Bhalerao
Menstrual cycle
Contraception
• Contraception means interception in the birth
process at any stage ranging from ovulation to
ovum implantation.
Contraceptives in current use
• Combination oral contraceptive pills: containing a
combination of estrogen+progestins in varying
amounts or in phased regimens (monophasic,
biphasic, triphasic)
• Minipills (progestin only pills)
Containing progesterone preparation alone
• Postcoital (morning after)pills or emergency
contraceptive pills.
• Centchroman: nonhormonal estrogen receptor
antagonist.
Contraceptives in current use
• Injectable contraceptives
• Depot medroxyprogesterone acetate(DMPA)
• Estradiol valarate+17-hydroxyprogesterone caproate.
• Estradiol cypionate+medroxyprogesterone acetate.
• Recent contraceptive methods
• Levonorgestrel subcutaneous implant
• Levonorgestrel intrauterine inserts
• Hormonal contraception in males
• Testosterone undecanoate
• Testesterone undecanoate+depot medroxyprogesterone
acetate
• gossypol
Oral contraceptives
• Most popular and effective method with 99-
99.5 % success rate.
Estrogen Progestin Name
Ethinyl estradiol(30 µg) Norgestrel(300 µg) MALA D
Ethinyl estradiol(30 µg) Levonorgestrel(150 µg) OVRAL L
Ethinyl estradiol(30 µg) Desogestrel(150 µg) Desogen®
Monophasic combination pills
• No phasic increase or decrease in the
estrogen/progestin content during 21 days of pill
administration.
• The first pill is taken on the 5th day after the start
of menses.
• Thereafter, one pill is to be taken each day
consecutively for 21 days.
• Then , next 7 days are pill free period and the
next course starts again after the 5th day of
menses.
Biphasic pills
• Fixed dose of estrogen for 21 days but with
increasing doses of progesterone during two
successive phases, i.e., from the day 1-10 and
11-21.
Estrogen Progesterone
Ethinyl estradiol (35 µg) Norethindrone (500 µg) From day 1-10
Ethinyl estradiol (35 µg) Norethindrone (1000 µg) From day 11-21.
Triphasic pills
• Higher dose of estrogen near midcycle but
increasing doses of progesterone for three
successive phases i.e., for days 1-6, 7-11, 12-
21 days.
Ethinyl estradiol (30 µg) Norgestrel (50 µg) From day 1-6
Ethinyl estradiol (40 µg) Norgestrel (70 µg) From day 7-11
Ethinyl estradiol (30 µg) Norgestrel (125µg) From day 12-21
OC pills
• Most branded preparations provide packet of
21 tablets only.
• Others provide a packet of 21+7 extra pills,
which contain either lactose or some iron
preparation.
• If the woman misses one pill some day, she
should take 2 pills next day and continue one
pill a day as usual.
• If the pills have been missed for 2-3 days, then
the course should be stopped, mechanical
barriers like condoms, diaphragm or jelly
should be used and the next course should
start from 5th day of menses as usual.
Mechanism of action of OC pills
• Suppression of ovulation by inhibiting the
release of FSH and LH (mainly estrogenic
effect)
• Disruption of proliferative and secretory
phases of endometrium, reducing the chances
of implantation of ovum.
• Progestogenic effects increase the viscocity of
cervical mucus.
Side effects of OC pills
• Mild (no need to withdraw OC)
Estrogenic effects Progestogenic effects
Nausea Increase in apetite
Migraine Weight gain
Breast tenderness Acne
Mild oedema Hirsutism (mild)
Withdrawal bleeding which
at times fail to occur
Decrease in libido
Increase in body
temperature
Side effects of OC pills
• Moderate (may warrant discontinuation of
OC)
Estrogenic Progestogenic
Vertigo Breakthrough
bleeding(spotting)
Leg cramps Monilial vaginitis(urethral
dilatation and bacteriuria)
Uterine cramps Amenorrhoea (even after
stopping OC)
Precipitation of diabetes
Side effects of OC pills
• Severe(needs stoppage of OC)
Estrogenic Progestogenic
Thromboembolism Myocardial infarction
Cholestatic jaundice Cerebrothrombosis
Gall stones
Hepatic adenoma
Contraindications of OC pills(absolute)
• Thromboembolic, coronary and cerebrovascular
disease or a history of it.
• Moderate to severe hypertension;
hyperlipidemia.
• Active liver disease, hepatoma or h/o jaundice
during past pregnancy.
• Suspected/overt malignancy of genitals/breast.
• Porphyria
• Impending major surgery- to avoid postoperative
thromboembolism.
Contraindications of OC pills(relative)
• Diabetes
• Obesity
• Smoking
• Undiagnosed vaginal bleeding
• Age above 35 years
• Migraine
• Gall bladder disease
Side effects
• Estrogens-  risk of endometrial ca.
• Progesterone-  LDL cholesterol
• Progesterone -  bone mineral density.
Preparations available of OC pills
• MALA-D (ethinylestradiol 30µg + norgestrel
300 µg; 21 tabs + 7 tabs of Ferrous sulfate 60
mg each)
• OVRAL-L, (ethinylestradiol 30µg +
Levonorgestrel 150 µg )
If pregnancy occurs during the use of
OC pills
• It should be terminated by suction-
evacuation,because there is risk of
• Malformations,
• Genital carcinoma of female offspring
• Undescended testes in male offspring
Minipills (progestin only pills)
• Given to those cases where estrogens are
contraindicated.
• Success rate is lower as compared to
combination pills (98.3%).
• Pills are prescribed soon after delivery and
continued without interruption.
Mechanism of action of progestin only
pills
• Progestins place the endometrium
prematurely to the secretory phase.
• Increase the viscosity of cervical mucus.
Side effects of progestin only pills
• Acne
• Hirsutism
• Amenorrhoea
Post coital contraception
• High dose estrogen and/or high dose
progestin.
• Two tablets of progestin levonorgestrel (750
µg each)[NORLEVO]. The first tablet must be
taken as soon as possible (within 48 hrs of the
coitus) and the second tablet taken after 12
hrs.
Post coital contraception
• Ethinyl estradiol (50 µg each tablet) +
Levonorgestrel (250 µg each tablet)[OVRAL].
Two such tablets are to be taken within 72 hrs
of unprotected coitus and next 2 tablets after
12 hrs.
Post coital contraception
• Mifepristone (antiprogestine) 600 mg single
dose taken within 72 hrs of unprotected
intercourse.
Postcoital pills
• iPILL (Levonorgestrel 1.5 mg ;single tab)
• To be taken within 72 hrs.
Centchroman (ormeloxifene)
• Nonsteroidal estrogen antagonist
• Developed at CDRI India.
• Oral contraceptive under the brand name
SAHELI.
• Dose 30 mg
• Taken twice in a week for first 3 months and
then once a week subsequently.
Centchromin
• Suppressed proliferative stage of
endometrium.
• If the menstrual cycle is prolonged for more
than 15 days, pregnancy should be ruled out.
Injectable contraceptives
• Depot medroxyprogesterone acetate (DMPA; Depo
Provera)
• Mode of action: same as minipills
• Longer acting progesterone derivative
• Injected i.m.
• Dose 150 mg every 3 months
• Useful in those
• where compliance is a problem,
• patients having heavy menstrual
bleeding
• in those for whom estrogens are
contraindicated
Injectable contraceptives
• Side effects: irregular bleeding ending up in
amenorrhoea and anovulation.
• Osteoporosis may occur on prolonged use as
Gn suppression may cause low estrogen
levels.
• Wight gain
• Increased risk of breast cancer.
• If pregnancy occurs it should be terminated to
avoid risk of congenital deformities.
Recent contraceptive methods
• Norplant
• Intrauterine inserts
Norplants
• A set of 6 capsules each filled with 36 mg of
levonorgestrol (total 216 mg)for subcutaneous
implantationon the inside of upper arm.
• If kept implanted, 1 set of 6 tubes remain
effective for 5 years.
• The contraceptive effects are readily reversible
with removal of implants.
• Mechanism of action: same as minipills.
Intrauterine inserts
• Levonorgestrol
• Released at the rate of 20µg/day.
• For a period of 5 years.
• It acts locally hence systemic side effects are
less.
• Return of fertility is immediate after removal
of these progestaserts.
Contraceptive failure
• Enzyme inducers- phenytoin, phenobarbitone.
• Suppression of intestinal microflora-
tetracycline, ampicillin, etc.,- no deconjugation
of estrogens excreted in bile- enterohepatic
circulation does not occur- blood levels fall.
Non contraceptive health benefits of
oral contraceptives
• The estrogen-progesterone pill is associated
with reduced risk of functional ovarian cysts,
ovarian cancer, endometrial cancer, fibrocystic
breast disease, bleeding uterine fibroids.
• The menses become more regular, with
reduced blood loss, less premenstrual tension
and dysmennorhoea.
Non contraceptive health benefits of
oral contraceptives
• Lower incidence of ectopic pregnancy,
endometriosis, and pelvic inflammatory
disease.
• Combined pills with newer progestins
e.g.,desogestrel are more safe for women who
suffer from weight gain, acne, hirsutism or
raised LDL-c because desogestrel lacks
androgenic side effects.
Non contraceptive health benefits of
oral contraceptives
• A combination pill of estrogen with an anti
androgen (cyproterone acetate) is useful for
treating acne and hirsutism.
Hormonal contraception for Men
• Major issues
• Spermatogenesis takes 64 days. The drugs which
even completely inhibits spermatogenesis will
take a long latent period to produce infertility.
Similarly, return of fertility will be slow.
• Gonadotropin suppression inhibits testesterone
secretion as well, resulting in loss of libido and
impotence (which is unacceptable).
Drugs tried for male contraception
• Antiandrogens
• Estrogens and progestins
• Androgens
• Superactive Gn RH analogues
• Cytotoxic drugs
• gossypol
Hormonal contraception for Men
• Gossypol
• Nonsteroidal drug obtained from cotton seed.
• 20 mg/day for initial 2-3 months followed by
50-60 mg/week as a maintainance dose.
• It should not be used for more than 2 years
otherwise return of fertility may be difficult.
Thank you

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Hormonal contraception

  • 3. Contraception • Contraception means interception in the birth process at any stage ranging from ovulation to ovum implantation.
  • 4. Contraceptives in current use • Combination oral contraceptive pills: containing a combination of estrogen+progestins in varying amounts or in phased regimens (monophasic, biphasic, triphasic) • Minipills (progestin only pills) Containing progesterone preparation alone • Postcoital (morning after)pills or emergency contraceptive pills. • Centchroman: nonhormonal estrogen receptor antagonist.
  • 5. Contraceptives in current use • Injectable contraceptives • Depot medroxyprogesterone acetate(DMPA) • Estradiol valarate+17-hydroxyprogesterone caproate. • Estradiol cypionate+medroxyprogesterone acetate. • Recent contraceptive methods • Levonorgestrel subcutaneous implant • Levonorgestrel intrauterine inserts • Hormonal contraception in males • Testosterone undecanoate • Testesterone undecanoate+depot medroxyprogesterone acetate • gossypol
  • 6. Oral contraceptives • Most popular and effective method with 99- 99.5 % success rate. Estrogen Progestin Name Ethinyl estradiol(30 µg) Norgestrel(300 µg) MALA D Ethinyl estradiol(30 µg) Levonorgestrel(150 µg) OVRAL L Ethinyl estradiol(30 µg) Desogestrel(150 µg) Desogen®
  • 7. Monophasic combination pills • No phasic increase or decrease in the estrogen/progestin content during 21 days of pill administration. • The first pill is taken on the 5th day after the start of menses. • Thereafter, one pill is to be taken each day consecutively for 21 days. • Then , next 7 days are pill free period and the next course starts again after the 5th day of menses.
  • 8. Biphasic pills • Fixed dose of estrogen for 21 days but with increasing doses of progesterone during two successive phases, i.e., from the day 1-10 and 11-21. Estrogen Progesterone Ethinyl estradiol (35 µg) Norethindrone (500 µg) From day 1-10 Ethinyl estradiol (35 µg) Norethindrone (1000 µg) From day 11-21.
  • 9. Triphasic pills • Higher dose of estrogen near midcycle but increasing doses of progesterone for three successive phases i.e., for days 1-6, 7-11, 12- 21 days. Ethinyl estradiol (30 µg) Norgestrel (50 µg) From day 1-6 Ethinyl estradiol (40 µg) Norgestrel (70 µg) From day 7-11 Ethinyl estradiol (30 µg) Norgestrel (125µg) From day 12-21
  • 10. OC pills • Most branded preparations provide packet of 21 tablets only. • Others provide a packet of 21+7 extra pills, which contain either lactose or some iron preparation.
  • 11. • If the woman misses one pill some day, she should take 2 pills next day and continue one pill a day as usual. • If the pills have been missed for 2-3 days, then the course should be stopped, mechanical barriers like condoms, diaphragm or jelly should be used and the next course should start from 5th day of menses as usual.
  • 12. Mechanism of action of OC pills • Suppression of ovulation by inhibiting the release of FSH and LH (mainly estrogenic effect) • Disruption of proliferative and secretory phases of endometrium, reducing the chances of implantation of ovum. • Progestogenic effects increase the viscocity of cervical mucus.
  • 13. Side effects of OC pills • Mild (no need to withdraw OC) Estrogenic effects Progestogenic effects Nausea Increase in apetite Migraine Weight gain Breast tenderness Acne Mild oedema Hirsutism (mild) Withdrawal bleeding which at times fail to occur Decrease in libido Increase in body temperature
  • 14. Side effects of OC pills • Moderate (may warrant discontinuation of OC) Estrogenic Progestogenic Vertigo Breakthrough bleeding(spotting) Leg cramps Monilial vaginitis(urethral dilatation and bacteriuria) Uterine cramps Amenorrhoea (even after stopping OC) Precipitation of diabetes
  • 15. Side effects of OC pills • Severe(needs stoppage of OC) Estrogenic Progestogenic Thromboembolism Myocardial infarction Cholestatic jaundice Cerebrothrombosis Gall stones Hepatic adenoma
  • 16. Contraindications of OC pills(absolute) • Thromboembolic, coronary and cerebrovascular disease or a history of it. • Moderate to severe hypertension; hyperlipidemia. • Active liver disease, hepatoma or h/o jaundice during past pregnancy. • Suspected/overt malignancy of genitals/breast. • Porphyria • Impending major surgery- to avoid postoperative thromboembolism.
  • 17. Contraindications of OC pills(relative) • Diabetes • Obesity • Smoking • Undiagnosed vaginal bleeding • Age above 35 years • Migraine • Gall bladder disease
  • 18. Side effects • Estrogens-  risk of endometrial ca. • Progesterone-  LDL cholesterol • Progesterone -  bone mineral density.
  • 19. Preparations available of OC pills • MALA-D (ethinylestradiol 30µg + norgestrel 300 µg; 21 tabs + 7 tabs of Ferrous sulfate 60 mg each) • OVRAL-L, (ethinylestradiol 30µg + Levonorgestrel 150 µg )
  • 20. If pregnancy occurs during the use of OC pills • It should be terminated by suction- evacuation,because there is risk of • Malformations, • Genital carcinoma of female offspring • Undescended testes in male offspring
  • 21. Minipills (progestin only pills) • Given to those cases where estrogens are contraindicated. • Success rate is lower as compared to combination pills (98.3%). • Pills are prescribed soon after delivery and continued without interruption.
  • 22. Mechanism of action of progestin only pills • Progestins place the endometrium prematurely to the secretory phase. • Increase the viscosity of cervical mucus.
  • 23. Side effects of progestin only pills • Acne • Hirsutism • Amenorrhoea
  • 24. Post coital contraception • High dose estrogen and/or high dose progestin. • Two tablets of progestin levonorgestrel (750 µg each)[NORLEVO]. The first tablet must be taken as soon as possible (within 48 hrs of the coitus) and the second tablet taken after 12 hrs.
  • 25. Post coital contraception • Ethinyl estradiol (50 µg each tablet) + Levonorgestrel (250 µg each tablet)[OVRAL]. Two such tablets are to be taken within 72 hrs of unprotected coitus and next 2 tablets after 12 hrs.
  • 26. Post coital contraception • Mifepristone (antiprogestine) 600 mg single dose taken within 72 hrs of unprotected intercourse.
  • 27. Postcoital pills • iPILL (Levonorgestrel 1.5 mg ;single tab) • To be taken within 72 hrs.
  • 28. Centchroman (ormeloxifene) • Nonsteroidal estrogen antagonist • Developed at CDRI India. • Oral contraceptive under the brand name SAHELI. • Dose 30 mg • Taken twice in a week for first 3 months and then once a week subsequently.
  • 29. Centchromin • Suppressed proliferative stage of endometrium. • If the menstrual cycle is prolonged for more than 15 days, pregnancy should be ruled out.
  • 30. Injectable contraceptives • Depot medroxyprogesterone acetate (DMPA; Depo Provera) • Mode of action: same as minipills • Longer acting progesterone derivative • Injected i.m. • Dose 150 mg every 3 months • Useful in those • where compliance is a problem, • patients having heavy menstrual bleeding • in those for whom estrogens are contraindicated
  • 31. Injectable contraceptives • Side effects: irregular bleeding ending up in amenorrhoea and anovulation. • Osteoporosis may occur on prolonged use as Gn suppression may cause low estrogen levels. • Wight gain • Increased risk of breast cancer. • If pregnancy occurs it should be terminated to avoid risk of congenital deformities.
  • 32. Recent contraceptive methods • Norplant • Intrauterine inserts
  • 33. Norplants • A set of 6 capsules each filled with 36 mg of levonorgestrol (total 216 mg)for subcutaneous implantationon the inside of upper arm. • If kept implanted, 1 set of 6 tubes remain effective for 5 years. • The contraceptive effects are readily reversible with removal of implants. • Mechanism of action: same as minipills.
  • 34. Intrauterine inserts • Levonorgestrol • Released at the rate of 20µg/day. • For a period of 5 years. • It acts locally hence systemic side effects are less. • Return of fertility is immediate after removal of these progestaserts.
  • 35. Contraceptive failure • Enzyme inducers- phenytoin, phenobarbitone. • Suppression of intestinal microflora- tetracycline, ampicillin, etc.,- no deconjugation of estrogens excreted in bile- enterohepatic circulation does not occur- blood levels fall.
  • 36. Non contraceptive health benefits of oral contraceptives • The estrogen-progesterone pill is associated with reduced risk of functional ovarian cysts, ovarian cancer, endometrial cancer, fibrocystic breast disease, bleeding uterine fibroids. • The menses become more regular, with reduced blood loss, less premenstrual tension and dysmennorhoea.
  • 37. Non contraceptive health benefits of oral contraceptives • Lower incidence of ectopic pregnancy, endometriosis, and pelvic inflammatory disease. • Combined pills with newer progestins e.g.,desogestrel are more safe for women who suffer from weight gain, acne, hirsutism or raised LDL-c because desogestrel lacks androgenic side effects.
  • 38. Non contraceptive health benefits of oral contraceptives • A combination pill of estrogen with an anti androgen (cyproterone acetate) is useful for treating acne and hirsutism.
  • 39. Hormonal contraception for Men • Major issues • Spermatogenesis takes 64 days. The drugs which even completely inhibits spermatogenesis will take a long latent period to produce infertility. Similarly, return of fertility will be slow. • Gonadotropin suppression inhibits testesterone secretion as well, resulting in loss of libido and impotence (which is unacceptable).
  • 40. Drugs tried for male contraception • Antiandrogens • Estrogens and progestins • Androgens • Superactive Gn RH analogues • Cytotoxic drugs • gossypol
  • 41. Hormonal contraception for Men • Gossypol • Nonsteroidal drug obtained from cotton seed. • 20 mg/day for initial 2-3 months followed by 50-60 mg/week as a maintainance dose. • It should not be used for more than 2 years otherwise return of fertility may be difficult.