Contraceptives

The gonadal hormones and

antagonists
 Objectives
At the end of this session, you will be able to:
List types of contraceptives
Describe hormonal contraceptives and their
mechanisms
Explain gonadal hormone antagonists
What are the different types of contraception?

The different methods of contraception include:

Barrier methods
Intrauterine devices
Sterilization
Hormonal methods
 Barrier methods
Designed to prevent
sperm from entering
the uterus
Types of barrier
methods include:
Male condoms
Female condoms
Diaphragms
Cervical caps
Contraceptive
sponges
Spermicides
 Intrauterine devices
An IUD is a small, T-shaped device that is inserted
into the uterus to prevent pregnancy.
A health care provider inserts the device
types
A copper IUD
A hormonal IUD
 Sterilization
Sterilization is a permanent form of birth control
that either prevents a woman from getting
pregnant or prevents a man from releasing sperm.
A health care provider must perform the
sterilization procedure, which usually involves
surgery.
These procedures usually are not reversible.
Types
A sterilization implant
Tubal ligation
Vasectomy
 Hormonal methods
Hormonal methods of birth control use hormones
to stop ovulation and prevent pregnancy
Hormones can be introduced into the body
through various methods, including:
Pills, injections, skin patches, transdermal gels, vaginal
rings, and implantable rods.
 Hormonal methods types
Combined oral contraceptives
("the pill").
Progestin-only pills (POPs).
Contraceptive patch.
Injectable birth control.
Vaginal rings.
Implantable rods.
Emergency Contraceptive
Pills (ECPs).
 Hormonal regulation of the female reproductive
system
GnRH stimulates the release of FSH and LH from the anterior
pituitary gland.
FSH initiates follicular growth and the secretion of estrogens by the
growing follicles.
LH triggers ovulation and promotes formation of the corpus luteum.
Stimulated by LH, the corpus luteum produces and secretes
estrogens and progesterone
Neurohormonal control of the female reproductive system

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 Hormonal contraception
Includes
Oral
Parenteral
Implanted contraception
Oral contraceptives
1. The combined pills (estrogen with progestin)
2. Progestin only pills

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 Contraceptives cont
The combined pill
Most commonly used
Combines both estrogen & progestin
Estrogen: ethinyl estradiol, mestranol
Progestin: norethindrone, levonorgestrel or
desogestrel
The combined pill is taken for 21 consecutive days
followed by placebo pills for 7 days

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 Mechanism of action:
Estrogen inhibits the release of FSH from the
anterior pituitary by a negative feedback effect
suppresses development of ovarian follicles.
Progestins inhibit secretion of LH prevents
ovulation.
Progestins also make the cervical mucus less
suitable for the passage of sperm (makes it more
viscous)
progestins and estrogen make the uterus
unfavourable for implantation.
 Adverse Effect
Weight gain due to fluid retention and
anabolic effect of both estrogen and
progesterone
Mild nausea, flushing, dizziness and
depression
Skin changes like acne and increased
pigmentation
Amenorrhea of variable duration
 Drug Interaction
OCPs are metabolized by CYP450 so
coadministration of enzyme inducers like
Rifampicin, Carbamazepine, Phenytoin and
Phenobarbitone may decrease contraceptive
effectiveness.
Broad spectrum antibiotics like amoxycilline,
Ampicilline alter intestinal flora, inhibit intero
hepatic cycling of estrogen leading to failure of
effectiveness.
 Progestine only coantraceptives
Progestine only pills
Usually contain norethisterone and
levonorgestrel
Mechanism of action:
Makes cervical mucus inconvenient for sperm
migration.
It also hinders implantation through its effect on the
endometrium and on the motility and secretion of
the fallopian tube.
It is preferred in lactating women and in whom
estrogen is contraindicated.
 Emergency contraception ( Post coital
contraception)
Is a method of contraception used within 72
hours of unprotected sexual intercourse.
It should not be used in place of the normal
family planning methods.
Its use is recomended when:
A woman has made sex against her will (raped).
A condom has broken
An IUD come out of its place
 The most commonly used emergency
contraceptive is a pill containing levonorgestril
0.75 mg 1 tab. as soon as possible and the
same dose after 12 hrs.
 Long acting contraceptives

A) Medroxy progesterone acetate

For 3 months
Administered intramuscularly.
Menstrual irregularities are common but may
be corrected after repeated uses.
Infertility may persist for some months after
cessation of treatment.
B) Implantation
Six non-biodegradable capsules containing
levonorgestrel are implanted subcutaneously.
The tubes release their progestin content over
5 years.
Unwanted effects: irregular bleeding,
headache.
 Norplant I vs. Norplant II

Six capsules Two capsules

Five years Three years
 Drugs for infertility

Antiestrogens for infertility

o In unovulatory women
Clomifen and tamoxifen
Clomiphene is a medication patients take by mouth (orally).
It causes the body to make more of the hormones that cause
the eggs to mature in the ovaries
They work by inhibiting the feedback inhibition of estrogens
in the hypothalamus and so increase FSH and LH release
Use of clomiphene increases the risk of having a multiple
pregnancy.
There is a 10% chance of twins according to a study done in USA
 Drugs for infertility

o For women who lack appropriate pituitary function:

or
o When a woman does not respond to clomiphene
Gonadotrophins e.g menotrophin (FSH and LH in
equal amount)
Gonadotropins are hormones that are injected in a
woman to directly stimulate eggs to grow in the ovaries,
leading to ovulation
The chance of a multiple birth is higher with
gonadotropins than with clomiphene
30% of women have multiple births.
About two-thirds of multiple births are twins.
Triplets or larger multiple births account for the remaining third.
 Drugs for infertility
Bromocriptine or Cabergoline
Bromocriptine and cabergoline are pills taken orally to
treat abnormally high levels of the hormone prolactin,
which can stop ovulation.
Certain medications, kidney disease, and thyroid disease
can cause high levels of prolactin.
Once prolactin levels become normal, 85% of women
using bromocriptine or cabergoline ovulate.
Surgical Treatments for Female Infertility
If disease of the fallopian tubes is the cause of infertility,
surgery can repair the tubes or remove blockages in the tubes.
Success rates, however, are low.
also increase the risk of ectopic pregnancy (tubal pregnancy)
 Antiprogestins
Mifepristone
PR antagonist & blocks binding of progesterone
to PRs
Used
In combination with Misoprostol for the
termination of early pregnancy