2. HORMONAL CONTRACEPTIVES
“HORMONAL PREPARATIONS ARE RESPONSIBLE FOR
REVERSIBLE SUPPRESSION OF FERTILITY”
Anti fertility agents are the need of the day
In 20th century condoms, diaphragms, spermicidal
creams, foam tablets etc
Those are intimately related to sexual intercourse,
high failure rate it was despised by most couples.
Rook & Pincus (1995) invented oral progestin for
contraception, when administered it prevent the
fertility from coitus
Recently number of new drugs was identified with
better activities,
Eg. COMBINED PILLS
3. FEMALE CONTRACEPTION
Over 100 million women worldwide currently
using hormonal contraceptives
By this drug the fertility can be suppressed
whenever we need
100% liable fertility regains on discontinuing
therapy
Because of Good efficacy, convenience, low
cost, overall safety, the oral contraceptives are
widely used now.
5. ORAL CONTACEPTIVES:
COMBINED PILL:
It contain both estrogen and progestin – FIRST
GENERATION PILL, but the drugs get accumulated in
the body
Amount of estrogen & progestin is reduced without
affecting efficacy – SECOND GENERATION PILLS
Newly identified progestins – THIRD GENERATION
PILL, Eg: DESOGESTREL.
They are mostly used in combination with progestin
Progestin is having anatiovulatory action
6. COMPOSITION OF COMBINED PILL
PROGESTIN ESTROGGEN
NORGESTREL 0.3mg + ETHINYL ESTRADIOL - 30 g
NORGESTREL 0.5mg +ETHINYL ESTRADIOL - 50 g
LEVONORGESTREL 0.25mg +ETHINYL ESTRADIOL - 50 g
LEVONORGESTREL0.15mg +ETHINYL ESTRADIOL - 30 g
DESOGESTREL 0.15mg +ETHINYL STRADIOL - 30 g
DESOGESTREL 0.15mg +ETHINYL ESTRADIOL - 20 g
7. Both progestin and estrogen synergize to
inhibit ovulation.
1 tablet daily for 21 days starting on the 5th
day of menstruation
The next dose started after a gap of 7 days in
which bleeding occurs, thus a cycle of 28 days
maintained.
Calendar packs of pills are available now
It is the popular and most efficacious method.
8. PHASED REGIMEN
Recommended for women’s more than 35
years
Introduced to permit reduction in total steroid
dose without compromising efficacy
They are biphasic or triphasic
Dose of estrogen kept constant in between 30-
40 g
FIRST PHASE: Amount of progestin is low
SECOND PHASE: Progressively high dose of
progestin
THIRD PHASE: Higher dose of progestin
9. COMPOSITION OF COMBINED PILL
PROGESTIN + ESTROGGEN
LEVONORGESTREL - 50 – 75 – 125 g +
ETHINYLESTRADIOL 30 – 40 - 35 g
NORETHINDRONE - 0.5 – 0.75 – 1mg +
ETHINYL ESTRADIOL 35 – 35 - 35 g
10. MINI PILL:
Also known as Progestin only pill
It designed to eliminate estrogen because long
term use may lead to severe risks.
Low dose progestin only, one pill taken daily,
Produce contraception in women.
Low efficacy 96 - 98%
Eg:
• NORETHINDRONE – 0.35MG
• NORGESTREL - 75 g
11. POSTCOITAL CONTRACEPTION:
It is an emergency contraception
Used in women not taking any contraceptive who had sexual
intercourse risking unwanted pregnancy
LEVONORGESTEREL 0.5mg+ ETHNYLESTRADIOL 0.1mg
This method is known as YUZPE METHOD.
Taken as early as possible
72 hours of unprotected intercourse, repeated after 12
hours.
It is the most popular method
50% women experience nausea
20 women experience vomiting
12. Commonly used and standard regimen is
LEVONORGESTEREL 0.25mg
+ ETHNYLESTRADIOL 50 mic gm
LEVONORGESTEREL 0.75mg
Taken twice within 12 hour gap with 72 hours of intercourse.
Less side effect than others, 6% women feel vomiting
Next period may be somewhat changed
2001 released essential drug list this method replaced the YUZPE
METHOD
LEVONORGESTEREL 1.5mg
single dose with in 72 hours
This regimens having 2-3 times more effective and better tolerated
than YUZPE METHOD
13. ULIPRISTAL
In 2010 ULIPRISTAL, a new drug approved for
emergency contraception
Single dose of ULIPRISTAL 30mg as soon as
possible with 120 hours of intercourse
Have failure rate of 1-3%
14. MEFEPRISTONE 600mg
Single dose daily
Taken within 72 hours of intercourse
This is used in china, Europe, few other
countries
Has lesser side effect than YUZPE method
All this should be preferred only for
unexpected / accidental exposure (Eg: Rape,
Condom rupture). Because all regimens have
higher failure rate & side effect than regular
low dose combined pill
15. MALE CONTRACEPTIVE:
Only way to suppress male fertility by drugs is
to inhibit spermatogenesis.
Complete suppression of spermatogenesis is
difficult.
Risk of adverse effects.
Gonadotropin suppression inhibits
testosterone secretion.