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HORMONAL
CONTRACEPTION
DR.P.SARAVANAN
PROF&HOD
DEPT OF PHARMACOLOGY
GMC, NAMAKKAL
FEMALE
CONTRACEPTIVES
CONTRACEPTIONS
Interception in the birth process at
any stage ranging from ovulation to
ovum implantation
HUMAN MENSTRUAL CYCLE
HORMONES, TEMPERATURE & OVULATION
OV
AR
Y
U
T
E
R
U
S
Proliferative phase Secretary phase
Pri Fol Sec Fol Graf Fol
Folicular phase Luteal phase
Cor Luteum Cor Albicans
TYPES OF HORMONAL CONTRACEPTIVES
ORAL
Combined
preparations
(estrogen
&progestin)
Monophasic
Biphasic
Triphasic
Single
preparations
(progestin only
pill)
Minipill
Emergency
TYPES OF HORMONAL CONTRACEPTIVES
PARENTERAL
DMPA
EV + 17OH PC
EC + DMPA
Implants
IU – Devices
TYPES OF HORMONAL CONTRACEPTIVES
ORAL
Combined
preparations
(estrogen
&progestin)
Monophasic
Biphasic
Triphasic
Single
preparations
(progestin only
pill)
Minipill
Emergency
MECHANISM OF ACTION- COMBINED PILLS
Both estrogen & progestin
Act synergistically on HP axis
Inhibit release of FSH & LH(-ve feedback)
Inhibits Ovulation
Estrogen- Inhibits LH surge
Estrogen & Progesteron- impair the nidation of ovum
Progesteron- Increases viscosity of cervical mucus
ESTROGEN
Cause tubal & uterine contractions
Interfere with fertilisation
PROGESTERONE
 Make endometrium- less suitable for the implantation
 Thick, viscid cervical mucous secretion
Prevents sperm penetration
MECHANISM OF ACTION- MINIPILLS
♣.ORAL CONTRACEPTIVES
1.COMBINED PILLS:
 Widely used & is the most effective reverrsible
method
 99-99.5% success rate
ESTROGENS PROGESTIN
Ethinyl estradiol (30µg)
+ Norgestrel (300µg)
Ethinyl estradiol (30µg)
+ Levonorgestrel (150µg)
Ethinyl estradiol (50µg)
+ Norgestrel (500µg)
Mestranol (50µg)
+ Norethindrone (1mg)
Ethinyl estradiol (30µg)
+ Desogestrel (150µg)
SCHEDULE FOR COMBINED PILL- MONOPHASIC
MENSTRUAL CYCLE
1st day 21st 28th
1tab orally daily for 21 consecutive days Pill free period – 7days
1st Pill – 5th day
MENSTRUAL CYCLE
1st day 21st 28th
1tab orally daily for 21 consecutive days Pill free period – 7days
1tab orally daily for 21 consecutive days Pill free period – 7days
1st Pill – 5th day
Day 1-21: Ethinyl estradiol (30µg)
Day 1-10: Norethindrone 0.5mg Day 11-21: Norethindrone 1mg
SCHEDULE FOR COMBINED PILL- BIPHASIC
MENSTRUAL CYCLE
1st day 21st 28th
1tab orally daily for 21 consecutive days Pill free period – 7days
Day 1-6: ES 30µg Day 1-6: ES 30µg
Day 7-11: ES 40µg
Day 1-6: NG0.05mg Day 7-11: NG0.075mg Day 11-21:NG0.125mg
1tab orally daily for 21 consecutive days
1st Pill – 5th day
SCHEDULE FOR COMBINED PILL- TRIPHASIC
MINIPILLS (PROGESTIN-ONLY PILLS)
 Given where estrogen is CI
 Success rate: 98.3%
 Mechanism
 Side effects
 Ex:
 Norethindrone
 Norgestrel
POSTCOITAL PILLS (PROGESTIN-ONLY PILLS)
 High dose of estrogen and/or progestin
 Regimens:
a. 2tab of Levonorgestrel(0.75mg)
 1st tab – within 48hrs of the coitus
 2nd: after 12hrs
b. Ethinyl estradiol + Levonorgestrel
 2tab: within 72hrs
 2tab: after 12hrs
c. Mifepristone600mg
 Single dose within 72hrs
CENTCHROMAN (ORMELOXIFENE)
 Non steroidal estrogen antagonist or SERM
 SAHELI
 MOA:
 Desynchronises the event of ovum transport with
endometrial phase
 Doses:
 1st 3 months: Twice/week
 Then 1/week subsequently
 CI:
 Jaundice, Hepatic dysfunction, PCOD, TB, Cervical
hyperplasia & RD
TYPES OF HORMONAL CONTRACEPTIVES
PARENTERAL
DMPA
EV + 17OH PC
EC + DMPA
Implants
IU – Devices
INJECTABLE CONTRACEPTIVES
a. Depot medroxyprogesterone
acetate(DMPA)
 150mg/3rd month, IM, after parturition
 Indication:
 High compliance, Estrogen is CI & Heavy menstural
bleeding
b. Combined estrogen-progestin injectable
contraceptives:
 Estradiol valerate5mg + 17-OH progesterone
caproate 250mg
 IM every month
 Estradiol cypionate 5mg + DMPA25mg
 IM once in 2 months
IMPLANTS
NORPLANT
6 flexible rods
216mg of
levonorgestrel
Effect 5years
IMPLANON
Single rod
68mg
3years
IUD
a. Intrauterine inserts
 T shaped device
 Releases Levonorgestrel 6mg everyday for 5yrs
b. Transvaginal ring
COMBINATION PILLS - SIDE EFFECTS
 Mild: ( No need to withdraw)
Estrogen: migraine, oedema, bleeding
Progesteron: acne, hirsutism, dec libido, Inc temperature
 Moderate: ( May need to withdraw)
Estrogen: Vertigo, Leg & Uterine cramps, DM
Progesteron: Bleeding, amenorrhoea, Vaginitis
 Serious: ( Must need to withdraw)
Estrogen: Thromboembolism, Jaundice, Hepatic adenoma
Progesteron: MI, cerebrothrombosis
COMBINATION PILLS - CONTRAINDICATION
 Mild: ( No need to withdraw)
Estrogen: migraine, oedema, bleeding
Progesteron: acne, hirsutism, dec libido, Inc temperature
 Moderate: ( May need to withdraw)
Estrogen: Vertigo, Leg & Uterine cramps, DM
Progesteron: Bleeding, amenorrhoea, Vaginitis
 Serious: ( Must need to withdraw)
Estrogen: Thromboembolism, Jaundice, Hepatic adenoma
Progesteron: MI, cerebrothrombosis
NON CONTRACEPTIVE EFFECTS:
Avoids unwanted pregnancy
Relieves dysmenorrhoea
Prevents anemia
Protects against Ovarian & Endometrial CA
MALE
CONTRACEPTIVES
 Inhibit spermatogenesis
No satisfaction is obtained because of following reasons
Complete inhibition of spermatogenesis is difficult
without affecting other tissues.
Takes longer latent period to produce infertility.
Testosterone suppression leads to loss of libido
MALE CONTRACEPTIVES
DRUGS AND APPROACHES
 Antiandrogens – has direct action on testis.
 Estogens and progestins - cause feminization.
 Androgens – poor efficacy ;with progestin efficacious
 Superactive GnRH analogues –inhibits testosterone
 Cytotoxic drugs- cadmium,nitrofurans and indoles
Administration
I.M administration of 100 mg of testostrone
weekly with 500 mg of levenegesterol.
Adverse reactions
 Gynacomastia
 Acne
 Loss of libido
 Impotence
GOSSYPOL
 Non steroidal compound obtained from cotton seed.
 Effective orally
 Inhibits spermatogenesis and sperm motility.
 Serum LH and testosterone levels will not change.
 No hormonal or antihormonal activity.
 Causes hypokalemia- renal loss of k ions
 Muscular weakness
 Edema
 Diarrhea
 Breathlessness
 neuritis
GOSSYPOL -Adverse effects
TYPES OF HORMONAL CONTRACEPTIVES
ORAL
Combined
preparations
(estrogen
&progestin)
Monophasic
Biphasic
Triphasic
Single
preparations
(progestin only
pill)
Minipill
Emergency
TYPES OF HORMONAL CONTRACEPTIVES
PARENTERAL
DMPA
EV + 17OH PC
EC + DMPA
Implants
IU – Devices
THANK U

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Hormonal contraceptions.pptx

  • 3. CONTRACEPTIONS Interception in the birth process at any stage ranging from ovulation to ovum implantation
  • 4. HUMAN MENSTRUAL CYCLE HORMONES, TEMPERATURE & OVULATION
  • 5. OV AR Y U T E R U S Proliferative phase Secretary phase Pri Fol Sec Fol Graf Fol Folicular phase Luteal phase Cor Luteum Cor Albicans
  • 6. TYPES OF HORMONAL CONTRACEPTIVES ORAL Combined preparations (estrogen &progestin) Monophasic Biphasic Triphasic Single preparations (progestin only pill) Minipill Emergency
  • 7. TYPES OF HORMONAL CONTRACEPTIVES PARENTERAL DMPA EV + 17OH PC EC + DMPA Implants IU – Devices
  • 8. TYPES OF HORMONAL CONTRACEPTIVES ORAL Combined preparations (estrogen &progestin) Monophasic Biphasic Triphasic Single preparations (progestin only pill) Minipill Emergency
  • 9. MECHANISM OF ACTION- COMBINED PILLS Both estrogen & progestin Act synergistically on HP axis Inhibit release of FSH & LH(-ve feedback) Inhibits Ovulation Estrogen- Inhibits LH surge Estrogen & Progesteron- impair the nidation of ovum Progesteron- Increases viscosity of cervical mucus
  • 10. ESTROGEN Cause tubal & uterine contractions Interfere with fertilisation PROGESTERONE  Make endometrium- less suitable for the implantation  Thick, viscid cervical mucous secretion Prevents sperm penetration MECHANISM OF ACTION- MINIPILLS
  • 11. ♣.ORAL CONTRACEPTIVES 1.COMBINED PILLS:  Widely used & is the most effective reverrsible method  99-99.5% success rate ESTROGENS PROGESTIN Ethinyl estradiol (30µg) + Norgestrel (300µg) Ethinyl estradiol (30µg) + Levonorgestrel (150µg) Ethinyl estradiol (50µg) + Norgestrel (500µg) Mestranol (50µg) + Norethindrone (1mg) Ethinyl estradiol (30µg) + Desogestrel (150µg)
  • 12. SCHEDULE FOR COMBINED PILL- MONOPHASIC MENSTRUAL CYCLE 1st day 21st 28th 1tab orally daily for 21 consecutive days Pill free period – 7days 1st Pill – 5th day
  • 13. MENSTRUAL CYCLE 1st day 21st 28th 1tab orally daily for 21 consecutive days Pill free period – 7days 1tab orally daily for 21 consecutive days Pill free period – 7days 1st Pill – 5th day Day 1-21: Ethinyl estradiol (30µg) Day 1-10: Norethindrone 0.5mg Day 11-21: Norethindrone 1mg SCHEDULE FOR COMBINED PILL- BIPHASIC
  • 14. MENSTRUAL CYCLE 1st day 21st 28th 1tab orally daily for 21 consecutive days Pill free period – 7days Day 1-6: ES 30µg Day 1-6: ES 30µg Day 7-11: ES 40µg Day 1-6: NG0.05mg Day 7-11: NG0.075mg Day 11-21:NG0.125mg 1tab orally daily for 21 consecutive days 1st Pill – 5th day SCHEDULE FOR COMBINED PILL- TRIPHASIC
  • 15. MINIPILLS (PROGESTIN-ONLY PILLS)  Given where estrogen is CI  Success rate: 98.3%  Mechanism  Side effects  Ex:  Norethindrone  Norgestrel
  • 16. POSTCOITAL PILLS (PROGESTIN-ONLY PILLS)  High dose of estrogen and/or progestin  Regimens: a. 2tab of Levonorgestrel(0.75mg)  1st tab – within 48hrs of the coitus  2nd: after 12hrs b. Ethinyl estradiol + Levonorgestrel  2tab: within 72hrs  2tab: after 12hrs c. Mifepristone600mg  Single dose within 72hrs
  • 17. CENTCHROMAN (ORMELOXIFENE)  Non steroidal estrogen antagonist or SERM  SAHELI  MOA:  Desynchronises the event of ovum transport with endometrial phase  Doses:  1st 3 months: Twice/week  Then 1/week subsequently  CI:  Jaundice, Hepatic dysfunction, PCOD, TB, Cervical hyperplasia & RD
  • 18. TYPES OF HORMONAL CONTRACEPTIVES PARENTERAL DMPA EV + 17OH PC EC + DMPA Implants IU – Devices
  • 19. INJECTABLE CONTRACEPTIVES a. Depot medroxyprogesterone acetate(DMPA)  150mg/3rd month, IM, after parturition  Indication:  High compliance, Estrogen is CI & Heavy menstural bleeding b. Combined estrogen-progestin injectable contraceptives:  Estradiol valerate5mg + 17-OH progesterone caproate 250mg  IM every month  Estradiol cypionate 5mg + DMPA25mg  IM once in 2 months
  • 20. IMPLANTS NORPLANT 6 flexible rods 216mg of levonorgestrel Effect 5years IMPLANON Single rod 68mg 3years
  • 21. IUD a. Intrauterine inserts  T shaped device  Releases Levonorgestrel 6mg everyday for 5yrs b. Transvaginal ring
  • 22. COMBINATION PILLS - SIDE EFFECTS  Mild: ( No need to withdraw) Estrogen: migraine, oedema, bleeding Progesteron: acne, hirsutism, dec libido, Inc temperature  Moderate: ( May need to withdraw) Estrogen: Vertigo, Leg & Uterine cramps, DM Progesteron: Bleeding, amenorrhoea, Vaginitis  Serious: ( Must need to withdraw) Estrogen: Thromboembolism, Jaundice, Hepatic adenoma Progesteron: MI, cerebrothrombosis
  • 23. COMBINATION PILLS - CONTRAINDICATION  Mild: ( No need to withdraw) Estrogen: migraine, oedema, bleeding Progesteron: acne, hirsutism, dec libido, Inc temperature  Moderate: ( May need to withdraw) Estrogen: Vertigo, Leg & Uterine cramps, DM Progesteron: Bleeding, amenorrhoea, Vaginitis  Serious: ( Must need to withdraw) Estrogen: Thromboembolism, Jaundice, Hepatic adenoma Progesteron: MI, cerebrothrombosis
  • 24. NON CONTRACEPTIVE EFFECTS: Avoids unwanted pregnancy Relieves dysmenorrhoea Prevents anemia Protects against Ovarian & Endometrial CA
  • 26.  Inhibit spermatogenesis No satisfaction is obtained because of following reasons Complete inhibition of spermatogenesis is difficult without affecting other tissues. Takes longer latent period to produce infertility. Testosterone suppression leads to loss of libido MALE CONTRACEPTIVES
  • 27. DRUGS AND APPROACHES  Antiandrogens – has direct action on testis.  Estogens and progestins - cause feminization.  Androgens – poor efficacy ;with progestin efficacious  Superactive GnRH analogues –inhibits testosterone  Cytotoxic drugs- cadmium,nitrofurans and indoles
  • 28. Administration I.M administration of 100 mg of testostrone weekly with 500 mg of levenegesterol.
  • 29. Adverse reactions  Gynacomastia  Acne  Loss of libido  Impotence
  • 30. GOSSYPOL  Non steroidal compound obtained from cotton seed.  Effective orally  Inhibits spermatogenesis and sperm motility.  Serum LH and testosterone levels will not change.  No hormonal or antihormonal activity.
  • 31.  Causes hypokalemia- renal loss of k ions  Muscular weakness  Edema  Diarrhea  Breathlessness  neuritis GOSSYPOL -Adverse effects
  • 32. TYPES OF HORMONAL CONTRACEPTIVES ORAL Combined preparations (estrogen &progestin) Monophasic Biphasic Triphasic Single preparations (progestin only pill) Minipill Emergency
  • 33. TYPES OF HORMONAL CONTRACEPTIVES PARENTERAL DMPA EV + 17OH PC EC + DMPA Implants IU – Devices