This document discusses hormonal contraceptives, including their mechanisms of action and types. It begins by listing the possible methods of contraception and then focuses on hormonal methods. It explains that hormonal contraceptives work by suppressing GnRH and the subsequent release of LH and FSH from the pituitary gland, preventing follicle maturation and ovulation. The main types discussed are combined oral contraceptive pills containing estrogen and progestin, progestin-only pills, and emergency contraception. Combined pills can be monophasic, biphasic, or triphasic depending on hormone levels. Potential side effects and regimens for emergency contraception are also summarized.

1. HORMONAL
CONTRACEPTIVES
Dr. Pravin Prasad
M.B.B.S., MD Clinical Pharmacology
Lecturer, Lumbini Medical College
15 July 2018 (31 Ashadh 2075), Sunday

2. BY THE END OF THE CLASS, MBBS
SEM IV STUDENTS WILL BE ABLE
TO:
List the possible methods of contraception
Understand the mechanism of action of
hormonal contraceptives
Appreciate the differences between different
oral contraceptive pills
Enumerate the regimens used for the
emergency contraception

3. Natural Methods
Physical Methods
Hormonal Methods
Sterilization
WHAT ARE THE POSSIBLE
METHODS OF CONTRACEPTION?
Oral
Injectable
Implants
Intrauterine

4. HORMONAL CONTRACEPTIVES
Route Formulation
Oral
• Combined Pills
• Monophasic
• Phased
• Progestin-only pills
• Emergency pills

5. NORMAL PHYSIOLOGY
GnRH
(pulse)
Leutinizing
Hormone
(LH)
Follicle
Stimulating
Hormone
(FSH)
Estrogen
Progesterone

6. HORMONAL CONTRACEPTIVES:
CENTRAL ACTION
Sustained level of Progestin:
Suppression of GnRH pulse
Decreased release of LH and FSH from
pituitary
Sustained level of Estrogen:
Decreased FSH from pituitary
Decreased FSH and LH surge
Failure of maturation of follicle and hence
ovulation

7. HORMONAL CONTRACEPTION:
MECHANISM OF ACTION
Thick cervical
mucous
Hostile
Endometrium
• Hyperproliferati
ve
• Hypoproliferati
ve
• Atrophic
Uterine and
Tubal
Contractions

8. COMBINED ORAL CONTRACEPTIVE
PILLS
Among the most effective non-surgical modality
 Failure rate on perfect use: 0.3%
Contains:
 Estrogen (E) as Ethinylestradiol
 Progestin (P) as Norgestrel, Levonorgestrel, Desogestrel
May contain:
 Same amount of E and P: Monophasic
 Different amount of E and P: Biphasic, Triphasic
(17α- alkyl-19-
nortestosterone)

9. COMBINED OCP: MONOPHASIC
Ethinylestradiol 0.03mg
Levonorgestrel 0.15mg

10. COMBINED OCP: BIPHASIC
E 0.01mg
E 0.02mg, P 0.15mg
Dummy

11. COMBINED OCP: TRIPHASIC
0.18mg
&
0.035
mg0.215mg &
0.035 mg
0.25 mg &
0.035 mg
Dummy

12. COMBINED OCP: SIDE EFFECTS
Low-dose preparations:
Minimal health risks in women with no
predisposing risk factors
Provides many beneficial health effects
Predisposing risk factors:
Smoking
Hypertension
Diabetes

13. COMBINED OCP: SIDE EFFECTS
Cardiovascular Side effects:
Thrombosis, thromboembolism
☞ More with transdermal preparation
Hypertension
☞ More with high dose formulation
Alteration in lipid profile
☞ Rise in Triglyceride levels

14. COMBINED OCP: SIDE EFFECTS
Cancer
Breast Cancer (small increase)
Increased risk of Cervical cancer: 2-fold
☞ Long term use (>5 years)
☞ Persistent human papilloma virus infection
Hepatic adenoma and Hepatocellular
carcinoma
☞ Long term use (4-8 years)
Decreased
incidence:
Endometrial Ca.
Ovarian Ca.
Colorectal Ca.

15. COMBINED OCP: SIDE EFFECTS
Metabolic and endocrine effects
Impaired glucose intolerance, dyslipidemia
☞ Seen with older high dose steroids
preparations
Raised protein synthesis from liver (Estrogen)
☞ May increase total hormone levels
Increased coagulation factors (Estrogen)
☞ Compensated by progestin induced increase
in fibrinolytic proteins

16. COMBINED OCP: SIDE EFFECTS
Miscellaneous
Breakthrough bleeding
Withdrawal bleeding may fail
☞ Rule out pregnancy
Acne and hirsituism
☞ Androgenic activity of 19-norprogestins
Aggravation of migraine intensity
Nausea, edema, mild headache

17. PROGESTIN ONLY PILLS
Contains only 17α- alkyl-19-nortestosterone
Also known as Minipills
Acts primarily by producing uterine changes
Additional mechanism: suppression of
ovulation
Useful when estrogen related side effects are to
avoided
Less efficacious than combined OCP
Failure rate on perfect use: 0.5%

18. PROGESTIN ONLY PILLS:
MECHANISM OF ACTION
Thick cervical
mucous
Hostile
Endometrium:
• Hyperproliferat
ive
• Hypoproliferati
ve
• Atrophic

19. PROGESTIN ONLY PILL: EXAMPLE
Norethindrone 0.35 mg
No Dummy tablets
To be taken on the same
time everyday
If dose missed for more
than 3 hrs, take dose
immediately
Extra precaution for next
two days

20. PROGESTIN ONLY PILL: SIDE
EFFECTS
Irregular, unpredictable spotting
Breakthrough bleeding
Acne
Do not decrease lactation: preferred in nursing
mothers

21. EMERGENCY CONTRACEPTION
Indicated for emergency condition only
Higher dose of steroids
Less effective than standard regimens
Probably acts by:
Effects on gametes function and survival
Effects on implantation
May dislodge a just
implanted blastocyst or
may interfere with
fertilization/implantation

22. EMERGENCY CONTRACEPTION:
REGIMENS USED
Two one pill regimen:
Levonorgestrel 0.75 mg (within 72 hours of
exposure)
After 12 hours
Levonorgestrel 0.75 mg
One pill regimen:
Levonorgestrel 1.5 mg (within 72 hours of
exposure), single oral dose (SOD)
Ulipristal 30 mg (within 120 hours of
exposure), SOD

23. CONCLUSION
Hormonal contraceptives are one of the
measures of contraception
All combined oral contraceptive pills differ in
terms of steroid as well as their strength present
in them
Side effects of combined OCP were due to high
dose formulations
Progestin only pills can be used to avoid the
estrogenic side effects of combined OCP
Emergency contraception is for emergency only

24. QUESTIONS?
Thank you…