ORAL
CONTRACEPTIV
E
Contraception
It is an artificial method or
technique that is been used to
prevent pregnancy as a
consequence of sexual
intercourse
These drug control the fertility
they are also called Antifertility
drug
Physiology of
menstrual cycle
Definition
The cyclic event that take place in a
rhythmic fashion during the reproductive
period of women's life is called menstrual
cycle.
Duration of 1 menstrual cycle – 28 days
First occurrence of menstrual cycle is
called menarche
Permanent cessation of menstrual cycle
is called menopause
Hormones involved
If an egg is not fertilized
If an egg is fertilized
Pharmacological action
to prevent pregnancy
By inhibiting ovulation thus it prevent
fertilization
By altering mucus in the cervix which
make it hard for the sperm to travel further
By changing the endometrium lining of the
uterus so that it cannot support a fertilized
egg
By altering the fallopian tubes so that they
cannot effectively move egg towards the
uterus
Oral contraceptive
Oral contraceptive are
prescribed medication taken by
oral route to prevent pregnancy
It is also called as birth control
pills.
Birth control pills prevent
pregnancy 99% of the time
when it is taken every day or
exactly as prescribed.
These are hormonal preparation
used for reversible suppression of
fertility, and it is referred as
Hormonal Contraceptives.
The pill contain hormones that
regulates menstruation and
premenstrual syndrome (PMS)
symptoms.
The main disadvantage of oral
contraceptive is it fails to protect
from Sexually Transmitted
Infections (STIs)
T Combined oral contraceptive
Y
P Progestin only pills
E Postcoital or emergency
S contraceptive
Combined
oral
contracepti
It contain combination of an
Estrogen and a Progestin.
Conventional: It is 28 days pack
containing 21 days of active pill
and 7 days of placebo.
Extended cycle: 3 month pack
containing 84 days active pill
and 7 days of placebo.
Continuous: active pills taken
365 days of the year
Administration starts at the first
day of the menses. On the
completion of the course,
bleeding occur within 3 to 4
days.
The administration is restarted
on the day 5 of the next cycle.
Formulation of
Combined
oral contraceptives
Monophasic oral
contraceptives
It contain same amount of Estrogen
and Progestin in each active pill
21 days of ingestin pills
Followed by 7 days of placebo pills.
Monophasic birth control pills are
mostly used to prevent pregnancy
in women who are sexually active
Example :
Ethinyl estradiol (EE)
Biphasic oral contraceptives
Biphasic birth control pills provide a lower
ratio of estrogen/progestin during the
first half of the pill cycle and a higher
dose during the second half
in order to mimic the pattern of
increasing and decreasing estrogen and
progesterone levels during a woman's
regular menstrual cycle.
Example:
Triphasic oral contraceptives
The amount of estrogens may be
fixed or variable, while the amount
of progestin increase in 3 equal
phases.
Those levels change every seven
days during the first 3 weeks of the
pills.
Example:
Progestin only pills
(Minipills)
These are oral contraceptives containing
progestin hormone only .
These pills do not posses estrogens but
contain lower progestin dose when
compared to combination oral
contraceptives
The minipills are taken daily on a
continuous schedule.
They are less effective than the
combination pill as they produce irregular
menstrual cycle more frequently.
The progestin only pills has limited
patient acceptance because of anxiety
over the increased possibility of
It may be used by patients who are
breast feeding ( unlike estrogen,
progetins do not have an effect on milk
production) or smoker
Example
TYPES DOSE BRAND NAME
Norethisterone 350µg Micronor
Noriday
Levonorgestrel 30µg Microval
Norgeston
Di norgestrel 75µg Neogest
Etynodiol 500µg femulen
diacetate
Disogestrel 75µg Cerazette
Post-coital
( Emergency)
contraceptive
Emergency contraceptive pills
prevent the pregnancy by delaying
the ovulation
Oral administration of progestin either
alone or in combination with estrogen, is
effective if administered within 72 hours
of unprotected intercourse and repeated
after 12 hours.
The intrauterine device is more effective
than hormonal methods as it works for up
to 5 days after the intercourse.
3 Regimens (formulation)
LEVONORGESTRE
L (0.5mg) +
ETHINYLESTRADIO
L (0.1mg) taken
within 72 hours of
unprotected
intercourse and
repeated after 12
hours.
LEVONORGESTR
EL (0.75mg) taken
twice with 12 hours
gap within 72 hours
of intercourse. This
regime is 2-3 times
more effecient and
better tolerated as
demonstrated by
the clinical trials .
MIFEPRISTONE (600mg) taken in a single
dose within 72 hours of intercourse
pharmacokinetics
ETHINYLOESTRADIOL LEVONORGESTREL
Absorption: oral Absorption: oral
Distribution: Distribution :
Bioavailability : 40 to Bioavailability: 70%
45% Metabolism: in liver
Metabolism: in liver by cytochrome p450
by cytochrome p450 enzymes
enzymes Excretion: through
Excretion: mainly urine
through urine, may
be by bile
Mechanism
of action
Inhibition of ovulation
Combination of
Estrogen and progestin
prevent ovulation by
suppressing the
secretion of
Gonadotropins (FSH
and LH) through
negative feedback
inhibition on the
anterior pitutiary.
Prevention of fertilization
Female genital tract become inhospitable
and has the following changes
The progestin is responsible for thickening of
cervical mucus and prevent the passage of
sperm.
Motility and secretion
of fallopian tubes
Inhibition of implantation
Implantation does not occur until the
endometrium is in right state .
A balance between estrogen and
progestin maintain the endometrium this
can be disturbed easily.
Pharmacological
Action
Ovaries
Combined or
progestin only
drugs
depresses
function of
ovaries.
Follicular
development is
decreased
Endometrial changes
Combined drugs may
cause stromal
deciduation towards
end of menstrual
cycle.
Progestational effect
on glandular tissue
during last 5 days of
cycle
Increase in thyroxine
binding globulin
May cause
hyperglycemia,
glycouria,
THERAPEUTI
C
USES
MILD
Moderate adverse effects
WEIGHT GAIN
AMENORRHEA
Severe Adverse Effect
Thromboembolic
disease
