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ORAL
CONTRACEPTIVES
By: Mr. Vinayak M.Gaware
Department of Pharmaceutical
Chemistry
Gynecological Diseases
 Menopause
 Dysmenorrhea
 Hypomenorrhe
a
 Hpyermenorrh
ea
 Oligomenorrhe
a
 Polymenorrhea
 Endometriosis
Introduction
 A woman becomes pregnant when an egg
released from her ovary is fertilized by a man's
sperm. The fertilized egg attaches to the inside
of a woman's uterus, where it receives
nourishment and develops into a baby.
Hormones in the woman's body control the
release of the egg from the ovary -- called
ovulation -- and prepare the body to accept the
fertilized egg.
 Hormonal contraceptives (the pill, the patch,
and the vaginal ring) all contain a small
amount of man-made estrogen and progestin
hormones. These hormones work to inhibit the
body's natural cyclical hormones to prevent
pregnancy. Pregnancy is prevented by a
combination of factors. The hormonal
contraceptive usually stops the body from
ovulating.
 Hormonal contraceptives also change the
cervical mucus to make it difficult for the sperm
to go through the cervix and find an egg.
Hormonal contraceptives can also prevent
pregnancy by changing the lining of the womb
so it's unlikely the fertilized egg will be
implanted.
 Defination: A birth control pill taken by
mouth. Most oral contraceptives include both
estrogen and progesterone. When given in
certain amounts and at certain times in
the menstrual cycle, these hormones prevent
the ovary from releasing an egg
for fertilization
 Birth control pills (oral contraceptives) are
prescription medications that prevent
pregnancy.
 Birth control (contraceptive) medications
contain hormones (estrogen and
progesterone, or progesterone alone).
 Birth control pills may also be prescribed to
reduce menstrual cramps or prevent anemia.
 Some women experience various levels of
side effects of birth control pills
 There are four types of OCP:
 Combined pills: Combination birth control pills are
a daily medication that contains 2 hormones
(estrogen and progestin) to prevent pregnancy.
 Phased pills: Pills with phases provide different
amounts of hormones over three weeks.
 Progestin only pills: Progestin-only birth control
pills are a daily medication that contain only 1
hormone. They may be prescribed if you have
side effects from other types of birth control pills.
 Emergency pills:
 Morning after pills can be used after sex to stop a
pregnancy before it starts
 Emergency Contraceptive Pill: Any method of
contraception which is used after intercourse and
before the potential time of implantation to prevent
pregnancy. Emergency hormone contraceptive
regimens are highly effective and decrease the risk
of pregnancy by 75 percent
Mechanism of Action
 Hormonal birth control medications prevent
pregnancy through the following ways:
 By blocking ovulation (release of an egg from
the ovaries), thus preventing pregnancy
 By altering mucus in the cervix, which makes it
hard for sperm to travel further
 By changing the endometrium (lining of the
uterus) so that it cannot support a fertilized
egg
 Women with the following conditions should not
use estrogen- containing birth control
medications:
 Allergy to any component of the product
 History of blood clot disorders
 History of stroke or heart attack
 Severe hypertension
 Diabetes that causes blood vessel problems
 Poorly controlled diabetes
 Severe headaches (for example, migraines)
 Breast cancer
 Liver cancer (or liver disease)
Available Dosage Forms
 Birth control (contraceptive) medications
contain hormones (estrogen and
progesterone, or progesterone alone).
 The medications are available in various
forms, such as pills, injections (into a muscle),
topical (skin) patches, and slow-release
systems (vaginal rings, skin implants, and
contraceptive-infused intrauterine devices
Pills Topicals
Female Condom
Vaginal Ring IUD Male Condoms
Drugs used as OC
 Mifepristone
 Norgestril
 Levonorgestrol
Mifepristone
 Mifepristone, also known as RU-486, is a
medication typically used in combination
with misoprostol to bring about
an abortion during pregnancy. This
combination is 97% effective during the first 63
days of pregnancy. It is also effective in
the second trimester of pregnancy.
Effectiveness should be verified two weeks
after use. It is taken by mouth.
 Mifepristone acts directly by antagonizing the
effects of progesterone at PRs, as well as
indirectly by causing a decrease in
progesterone secretion from the corpus
luteum. These combined effects lead to an
increase in the level of prostaglandins, which
stimulates uterine contractions.
 Mifepristone also causes a softening of the
cervix, which aids in expulsion of the fertilized
ovum. Mifepristone treatment is followed by
the use of misoprostol, a prostaglandin E2
analog, to ensure a complete abortion.
 Common side effects include abdominal pain,
feeling tired, and vaginal bleeding. Serious
side effects may include heavy vaginal
bleeding, bacterial infection, and birth defects
if the pregnancy does not end.
Norgestril
 Norgestrel (a form of progestin) is a hormone that prevents
pregnancy by making vaginal fluid thicker to help
prevent sperm from reaching an egg (fertilization), and
changing the lining of the uterus (womb) to prevent
attachment of a fertilized egg. If a fertilized egg does not
attach to the uterus, it passes out of the body. This
medication also stops the release of an egg (ovulation) in
about half of a woman's menstrual cycles.
 This medication is used to
prevent pregnancy. It is often
referred to as the "mini-pill"
because it does not contain
any estrogen.
 Side effects
 Nausea, vomiting, stomach cramping/bloating,
dizziness, headache,
tiredness, breast tenderness, decrease in
breast size, acne, oily scalp, hair
loss, weight gain, and vaginal infections may
occur.
Levonorgestrol
 Levonorgestrol is a hormonal
medication which is used in a number of birth
control methods. It is combined with
an estrogen to make combination birth control
pills. As an emergency birth control, sold under
the brand name Plan B among others, it is
useful within 120 hours of
unprotected sex. The more time that has
passed since sex, the less effective the
medication becomes, and it does not work
after pregnancy (implantation) has occurred. It
decreases the chances of pregnancy by 57 to
Side Effects:
 Nausea/vomiting, abdominal pain,
tiredness, dizziness, changes in vaginal
bleeding, breast tenderness, or headache may
occur.
 https://www.youtube.com/watch?v=kMY-
v0F6bX0
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Oral contraceptives

  • 1. ORAL CONTRACEPTIVES By: Mr. Vinayak M.Gaware Department of Pharmaceutical Chemistry
  • 2. Gynecological Diseases  Menopause  Dysmenorrhea  Hypomenorrhe a  Hpyermenorrh ea  Oligomenorrhe a  Polymenorrhea  Endometriosis
  • 3. Introduction  A woman becomes pregnant when an egg released from her ovary is fertilized by a man's sperm. The fertilized egg attaches to the inside of a woman's uterus, where it receives nourishment and develops into a baby. Hormones in the woman's body control the release of the egg from the ovary -- called ovulation -- and prepare the body to accept the fertilized egg.
  • 4.  Hormonal contraceptives (the pill, the patch, and the vaginal ring) all contain a small amount of man-made estrogen and progestin hormones. These hormones work to inhibit the body's natural cyclical hormones to prevent pregnancy. Pregnancy is prevented by a combination of factors. The hormonal contraceptive usually stops the body from ovulating.
  • 5.  Hormonal contraceptives also change the cervical mucus to make it difficult for the sperm to go through the cervix and find an egg. Hormonal contraceptives can also prevent pregnancy by changing the lining of the womb so it's unlikely the fertilized egg will be implanted.
  • 6.  Defination: A birth control pill taken by mouth. Most oral contraceptives include both estrogen and progesterone. When given in certain amounts and at certain times in the menstrual cycle, these hormones prevent the ovary from releasing an egg for fertilization
  • 7.  Birth control pills (oral contraceptives) are prescription medications that prevent pregnancy.  Birth control (contraceptive) medications contain hormones (estrogen and progesterone, or progesterone alone).  Birth control pills may also be prescribed to reduce menstrual cramps or prevent anemia.  Some women experience various levels of side effects of birth control pills
  • 8.  There are four types of OCP:  Combined pills: Combination birth control pills are a daily medication that contains 2 hormones (estrogen and progestin) to prevent pregnancy.  Phased pills: Pills with phases provide different amounts of hormones over three weeks.  Progestin only pills: Progestin-only birth control pills are a daily medication that contain only 1 hormone. They may be prescribed if you have side effects from other types of birth control pills.
  • 9.  Emergency pills:  Morning after pills can be used after sex to stop a pregnancy before it starts  Emergency Contraceptive Pill: Any method of contraception which is used after intercourse and before the potential time of implantation to prevent pregnancy. Emergency hormone contraceptive regimens are highly effective and decrease the risk of pregnancy by 75 percent
  • 11.  Hormonal birth control medications prevent pregnancy through the following ways:  By blocking ovulation (release of an egg from the ovaries), thus preventing pregnancy  By altering mucus in the cervix, which makes it hard for sperm to travel further  By changing the endometrium (lining of the uterus) so that it cannot support a fertilized egg
  • 12.  Women with the following conditions should not use estrogen- containing birth control medications:  Allergy to any component of the product  History of blood clot disorders  History of stroke or heart attack  Severe hypertension  Diabetes that causes blood vessel problems  Poorly controlled diabetes  Severe headaches (for example, migraines)  Breast cancer  Liver cancer (or liver disease)
  • 13. Available Dosage Forms  Birth control (contraceptive) medications contain hormones (estrogen and progesterone, or progesterone alone).  The medications are available in various forms, such as pills, injections (into a muscle), topical (skin) patches, and slow-release systems (vaginal rings, skin implants, and contraceptive-infused intrauterine devices
  • 14. Pills Topicals Female Condom Vaginal Ring IUD Male Condoms
  • 15. Drugs used as OC  Mifepristone  Norgestril  Levonorgestrol
  • 16. Mifepristone  Mifepristone, also known as RU-486, is a medication typically used in combination with misoprostol to bring about an abortion during pregnancy. This combination is 97% effective during the first 63 days of pregnancy. It is also effective in the second trimester of pregnancy. Effectiveness should be verified two weeks after use. It is taken by mouth.
  • 17.  Mifepristone acts directly by antagonizing the effects of progesterone at PRs, as well as indirectly by causing a decrease in progesterone secretion from the corpus luteum. These combined effects lead to an increase in the level of prostaglandins, which stimulates uterine contractions.  Mifepristone also causes a softening of the cervix, which aids in expulsion of the fertilized ovum. Mifepristone treatment is followed by the use of misoprostol, a prostaglandin E2 analog, to ensure a complete abortion.
  • 18.  Common side effects include abdominal pain, feeling tired, and vaginal bleeding. Serious side effects may include heavy vaginal bleeding, bacterial infection, and birth defects if the pregnancy does not end.
  • 19. Norgestril  Norgestrel (a form of progestin) is a hormone that prevents pregnancy by making vaginal fluid thicker to help prevent sperm from reaching an egg (fertilization), and changing the lining of the uterus (womb) to prevent attachment of a fertilized egg. If a fertilized egg does not attach to the uterus, it passes out of the body. This medication also stops the release of an egg (ovulation) in about half of a woman's menstrual cycles.  This medication is used to prevent pregnancy. It is often referred to as the "mini-pill" because it does not contain any estrogen.
  • 20.  Side effects  Nausea, vomiting, stomach cramping/bloating, dizziness, headache, tiredness, breast tenderness, decrease in breast size, acne, oily scalp, hair loss, weight gain, and vaginal infections may occur.
  • 21. Levonorgestrol  Levonorgestrol is a hormonal medication which is used in a number of birth control methods. It is combined with an estrogen to make combination birth control pills. As an emergency birth control, sold under the brand name Plan B among others, it is useful within 120 hours of unprotected sex. The more time that has passed since sex, the less effective the medication becomes, and it does not work after pregnancy (implantation) has occurred. It decreases the chances of pregnancy by 57 to
  • 22. Side Effects:  Nausea/vomiting, abdominal pain, tiredness, dizziness, changes in vaginal bleeding, breast tenderness, or headache may occur.  https://www.youtube.com/watch?v=kMY- v0F6bX0