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Presented by;
T.SRI PRAVALLIKA;
M.PHARM;
PHARMACOLOGY;
Chalapathi institute of pharmaceutical
sciences, lam,guntur.
Contents:-
 Definition
 From fertilization to implantation
 Oral contraceptives
 How birth control medication works
 How to choose the drug
 Types of oc’s
 Available drugs
 Emergency hormonal contraception
 Drug interactions
 Side effects
 Warning
 Over dose
 Missed dose
 Storage.
DEFINITION:-
 Oral contraceptives are medicines
 taken by mouth to help
 prevent pregnancy.
 They are also known as “birth
 control pills”.
FROM FERTILIZATION TO
IMPLANTATION
ORAL
CONTRACEPTIVES:-
 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.
HOW BIRTH CONTROL MEDICATION
WORK:-
 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
 By altering the fallopian tubes (the tubes through which eggs
move
from the ovaries to the uterus) so that they cannot effectively
move eggs toward the uterus
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
HOW TO CHOOSE THE DRUG?
 Choosing which estrogen and progesterone dose, type, and
administration method is
 Highly patient specific, meaning that the choice greatly
depends on factors unique to an individual.
 General goals are to choose a product that provides good
menstrual cycle control with the fewest adverse (side)
effects and to use the lowest hormone dose possible.
 After beginning birth control medications, it may be
necessary to adjust the dose or to choose a different
product.
TYPES OF ORAL CONTRACEPTIVES:-
 THE COMBINED PILL
 THE PROGESTOGEN ONLY PILL
 Formulations may be :
 1. Monophasic (each tablet contains a fixed
amount of estrogen and progestin);
 2. Biphasic (each tablet contains a fixed
amount of estrogen, while the amount of progestin
increases in the second half of
the cycle); or
 3. Triphasic (the amount of estrogen may be
fixed or variable, while the amount of progestin
increases in 3 equal phases).
The combined pill
(combinations of an oestrogen with a
progestogen)
The combined pill
(combinations of an oestrogen with a
progestogen)
 The oestrogen in most combined preparations(second-
generation pills) is ethinylestradiol,although a few
preparations contain mestranol instead.
 The progestogen may be norethisterone,levonorgestrel,
ethynodiol, or-in 'thirdgeneration‘ pills-desogestrel or
gestodene,which are more potent, have less androgenic
action and cause less change in lipoprotein metabolism,
but which probably cause a greater risk of
thromboembolism than do secondgeneration preparations.
The combined pill:-
 The oestrogen content is generally 20-50μg of
ethinylestradiol or its equivalent, and a preparation is
chosen with the lowest oestrogen and progestogen
content that is well tolerated and gives good cycle
control in the individual woman.
 This combined pill is taken for 21 consecutive days
followed by 7 pill-free days, which causes a withdrawal
bleed. Normal cycles of menstruation usually
commence fairly soon after discontinuing treatment.
MODE OF ACTION:-
 oestrogen inhibits secretion of FSH via negative feedback
on the anterior pituitary, and thus suppresses development
of the ovarian follicle progestogen inhibits secretion of LH
and thus prevents ovulation; it also makes the cervical
mucus less suitable for the passage of sperm.
 oestrogen and progestogen act in concert to alter the
endometrium in such a way as to discourage implantation.
 They may also interfere with the coordinated contractions
of cervix, uterus and fallopian tubes that facilitate
fertilisation and implantation.
The progestogen-only pill:-
 The drugs used in progestogen only pills include
 norethisterone, levonorgestrel or ethynodiol.
 The pill is taken daily without interruption.
MODE OF ACTION:-
 The mode of action is primarily on the cervical mucus,
which is made inhospitable to sperm. The progestogen
probably also hinders implantation through its effect
on the endometrium and on the motility and
secretions of the fallopian tubes
AVAILABLE DRUGS:-
 Estrogens
 Ethinyl estradiol
 Mestranol
 Progesterones
 Norethynodrel
 Norethindrone
 Norethindrone acetate
 Norgestimate
 Desogestrel
 Ethynodiol diacetate
 Norgestrel
 Levonorgestrel
 Drospirenone
HORMONE CONTAINING
CONTRACEPTIVES:-
 Combination contraceptives, that is,contraceptive
medications containing both estrogen and
progesterone, are the most effective means for
contraception with the exception of surgical
sterilization.
 Several types of combination birth control pills exist,
including monophasic pills, biphasic pills,triphasic
pills, and 91-day-cycle pills.
MONOPHASIC PILLS:-
 Monophasic pills have a constant dose of both
estrogen and progestin in each of the hormonally
active pills throughout the entire cycle (21 days of
ingesting active pills).
 Several of the brands listed above may be available in
several strengths of estrogen or progesterone, from
which doctors choose according to a woman’s
individual needs.
BI-PHASIC PILLS:-
 Biphasic pills typically contain 2 different progesterone
doses. The progesterone dose is increased about
halfway through the cycle.
 TRIPHASIC PILLS:-
 Triphasic pills gradually increase the dose of
estrogen during the cycle (some pills also increase
the progesterone dose).
 Three different increasing pill doses are contained
in each cycle.
EMERGENCY HORMONAL
CONTRACEPTION:-
 Levonelle 1500 (one step)
 Contains high dose progesterone (levonorgesterel)
 One 1500mcg tablet taken as soon as possible after
unprotected intercourse (up to 72 hours after)
 Preferably within 12 hours, no later than 72 hours.
HOW DOES EHC WORKS:-
 Dependent on point in the menstrual cycle
 Either prevents or delays ovulation, prevents
fertilisation or prevents implantation of the fertilised
egg into the uterus.
 Clinical opinion is that EHC is not an abortifacient
NINETY ONE DAY BIRTH CONTROL PILLS:-
 These pills are monophasic birth control pills that have
been approved for use on a daily basis for 84 days
without interruption.
 Users have fewer scheduled menstrual cycles (only 1
period every 3 months).
 Data from clinical trials show that many women,
especially in the first few cycles of use, have more
unplanned bleeding and spotting between the
expected menstrual periods than women taking
conventional combination birth control pills.
LONG ACTING, INJECTABLE, PROGESTERONE ONLY
CONTRACEPTIVES:-
 Medroxyprogesterone acetate (Depo-Provera)
 Use:
 The first injection is given within 5 days following the onset of
menstruation.
 After that, an injection is needed every 11-13 weeks.
 Side effects:
 Since progesterone is the only hormonal ingredient, estrogen-
related side effects are avoided.
 A side effect unique to this method of birth control is that most
women eventually stop having their periods.
 Depo-Provera may last in the body for several months in women
who have used it on a long-term basis and can actually delay the
return to fertility after stopping the drug.
 Approximately 70% of former users desiring pregnancy conceive
within 12 months, and 90% of former users conceive within 24
months. Other side effects include weight gain and depression.
TOPICAL CONTRACEPTIVE PATCH:-
 Norelgestromin/ethinyl estradiol (Ortho Evra)
 The topical patch may be applied to clean, dry skin on the shoulders, upper arms,
buttocks, or abdomen.
 It should not be applied to red or inflamed areas of the skin or in areas where tight
clothing may rub.
 The patch may be less effective in women weighing more than 198 pounds(90 kg).
 Use:
 A new patch is applied on the same day of the week, each week for 3 weeks in a row.
 The first patch is applied either on the first day of the menstrual period or on the Sunday
following menses.
 On the fourth week, no patch is applied.
 Menstruation should begin during this time.
 This 4-week period is considered 1 cycle.
 Another 4-week cycle is started by applying a new patch following the 7-day
 patch-free period.
SIDE EFFECTS:-
 Side effects are similar to other birth control agents
containing both estrogen and progesterone.
 Effects include menstrual irregularities,weight gain,
and mood changes.
Other specific side effects include a skin reaction at the
site of application and problems with contact use
WHY SHOULD NOT USE THESE MEDICATIONS:-
 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
 Heart valve disease with complications
 Severe hypertension
 Diabetes that causes blood vessel problems
 Poorly controlled diabetes
 Unexplained abnormal bleeding from the uterus
 Jaundice during pregnancy or jaundice with prior hormonal
 contraceptive use
DRUG INTERACTIONS:-
 Certain drugs can decrease the effectiveness of
combination-type birth control pills by decreasing the drug
concentration in your system (impaired enterohepatic
recirculation or hepatic induction). This can result in
pregnancy.
 Drugs that may cause this effect include: many
antibiotics(e.g., cephalosporins, chloramphenicol,
macrolides, penicillins, tetracyclines, sulfas), aprepitant,
bexarotene, bosentan, dapsone, griseofulvin, certain HIV
protease inhibitors (e.g., amprenavir, nelfinavir, ritonavir),
modafinil, nevirapine, rifamycins (e.g., rifampin), many
seizure medications (e.g., barbiturates, carbamazepine,
phenytoin, primidone, topiramate), St. John's wort.
DRUG INTERACTIONS:-
 Before using this medication, tell your doctor or pharmacist of
all prescription and non-prescription/herbal medications you
may use, especially of: thyroid hormone drugs, certain
benzodiazepines (e.g.,diazepam, chlordiazepoxide), prednisone-
like drugs, certain antidepressants (e.g., tricyclics), beta-blockers
(e.g., metoprolol), "blood thinners" (anticoagulants such as
warfarin), insulin.
 This product can affect the results of certain lab tests (e.g.,
thyroid).Inform all laboratory personnel that you use this drug.
Birth control pills may significantly intensify the effects of
alcohol.
 Consult your doctor or pharmacist about this. Do not start or
stop any medicine without doctor or pharmacist approval.
SIDE EFFECTS:-
 Nausea, breast tenderness, fluid retention,
 weight gain, acne, breakthrough bleeding,
 missed periods, headaches, depression, anxiety,
 change in vision, other mood changes, and
 lower sexual desire.
 Additionally, the following more serious side
 effects may occur:
 Thromboembolism (blood clots)
 Breast cancer
 Cervical cancer
 Benign liver tumors
Diabetes
WARNING:-
 Smoking cigarettes while using this medication
increases your chance of having heart problems.
 Do not smoke while using this medication.
 The risk of heart problems increases with
age(especially in women greater than 35 years of age)
and with frequent smoking (15 cigarettes per day or
greater).
OVER DOSE:-
 If overdose is suspected, contact your local poison
control center or emergency room immediately.
Symptoms of overdose may include nausea and
vomiting.
 Females may experience vaginal bleeding.
MISSED DOSE:-
 Missed dose advice differs and depends on the brand
used, and the number of doses missed.
 Refer to the product package information for advice on
missed doses. Ask your doctor or pharmacist if you
have any questions.
STORAGE:-
 Store at room temperature between 59 and 86 degrees
F (between 15 and 30 degrees C) away from moisture
and sunlight.
 Do not store in the bathroom.
REFFERENCE:-
 From the slideshare app.,
 And from the google.
Oral contraceptives

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Oral contraceptives

  • 1. Presented by; T.SRI PRAVALLIKA; M.PHARM; PHARMACOLOGY; Chalapathi institute of pharmaceutical sciences, lam,guntur.
  • 2. Contents:-  Definition  From fertilization to implantation  Oral contraceptives  How birth control medication works  How to choose the drug  Types of oc’s  Available drugs  Emergency hormonal contraception  Drug interactions  Side effects  Warning  Over dose  Missed dose  Storage.
  • 3. DEFINITION:-  Oral contraceptives are medicines  taken by mouth to help  prevent pregnancy.  They are also known as “birth  control pills”.
  • 5. ORAL CONTRACEPTIVES:-  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.
  • 6. HOW BIRTH CONTROL MEDICATION WORK:-  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  By altering the fallopian tubes (the tubes through which eggs move from the ovaries to the uterus) so that they cannot effectively move eggs toward the uterus
  • 7.
  • 8. 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
  • 9. HOW TO CHOOSE THE DRUG?  Choosing which estrogen and progesterone dose, type, and administration method is  Highly patient specific, meaning that the choice greatly depends on factors unique to an individual.  General goals are to choose a product that provides good menstrual cycle control with the fewest adverse (side) effects and to use the lowest hormone dose possible.  After beginning birth control medications, it may be necessary to adjust the dose or to choose a different product.
  • 10. TYPES OF ORAL CONTRACEPTIVES:-  THE COMBINED PILL  THE PROGESTOGEN ONLY PILL
  • 11.  Formulations may be :  1. Monophasic (each tablet contains a fixed amount of estrogen and progestin);  2. Biphasic (each tablet contains a fixed amount of estrogen, while the amount of progestin increases in the second half of the cycle); or  3. Triphasic (the amount of estrogen may be fixed or variable, while the amount of progestin increases in 3 equal phases). The combined pill (combinations of an oestrogen with a progestogen)
  • 12. The combined pill (combinations of an oestrogen with a progestogen)  The oestrogen in most combined preparations(second- generation pills) is ethinylestradiol,although a few preparations contain mestranol instead.  The progestogen may be norethisterone,levonorgestrel, ethynodiol, or-in 'thirdgeneration‘ pills-desogestrel or gestodene,which are more potent, have less androgenic action and cause less change in lipoprotein metabolism, but which probably cause a greater risk of thromboembolism than do secondgeneration preparations.
  • 13. The combined pill:-  The oestrogen content is generally 20-50μg of ethinylestradiol or its equivalent, and a preparation is chosen with the lowest oestrogen and progestogen content that is well tolerated and gives good cycle control in the individual woman.  This combined pill is taken for 21 consecutive days followed by 7 pill-free days, which causes a withdrawal bleed. Normal cycles of menstruation usually commence fairly soon after discontinuing treatment.
  • 14. MODE OF ACTION:-  oestrogen inhibits secretion of FSH via negative feedback on the anterior pituitary, and thus suppresses development of the ovarian follicle progestogen inhibits secretion of LH and thus prevents ovulation; it also makes the cervical mucus less suitable for the passage of sperm.  oestrogen and progestogen act in concert to alter the endometrium in such a way as to discourage implantation.  They may also interfere with the coordinated contractions of cervix, uterus and fallopian tubes that facilitate fertilisation and implantation.
  • 15.
  • 16. The progestogen-only pill:-  The drugs used in progestogen only pills include  norethisterone, levonorgestrel or ethynodiol.  The pill is taken daily without interruption.
  • 17. MODE OF ACTION:-  The mode of action is primarily on the cervical mucus, which is made inhospitable to sperm. The progestogen probably also hinders implantation through its effect on the endometrium and on the motility and secretions of the fallopian tubes
  • 18. AVAILABLE DRUGS:-  Estrogens  Ethinyl estradiol  Mestranol  Progesterones  Norethynodrel  Norethindrone  Norethindrone acetate  Norgestimate  Desogestrel  Ethynodiol diacetate  Norgestrel  Levonorgestrel  Drospirenone
  • 19. HORMONE CONTAINING CONTRACEPTIVES:-  Combination contraceptives, that is,contraceptive medications containing both estrogen and progesterone, are the most effective means for contraception with the exception of surgical sterilization.  Several types of combination birth control pills exist, including monophasic pills, biphasic pills,triphasic pills, and 91-day-cycle pills.
  • 20. MONOPHASIC PILLS:-  Monophasic pills have a constant dose of both estrogen and progestin in each of the hormonally active pills throughout the entire cycle (21 days of ingesting active pills).  Several of the brands listed above may be available in several strengths of estrogen or progesterone, from which doctors choose according to a woman’s individual needs.
  • 21. BI-PHASIC PILLS:-  Biphasic pills typically contain 2 different progesterone doses. The progesterone dose is increased about halfway through the cycle.  TRIPHASIC PILLS:-  Triphasic pills gradually increase the dose of estrogen during the cycle (some pills also increase the progesterone dose).  Three different increasing pill doses are contained in each cycle.
  • 22. EMERGENCY HORMONAL CONTRACEPTION:-  Levonelle 1500 (one step)  Contains high dose progesterone (levonorgesterel)  One 1500mcg tablet taken as soon as possible after unprotected intercourse (up to 72 hours after)  Preferably within 12 hours, no later than 72 hours.
  • 23. HOW DOES EHC WORKS:-  Dependent on point in the menstrual cycle  Either prevents or delays ovulation, prevents fertilisation or prevents implantation of the fertilised egg into the uterus.  Clinical opinion is that EHC is not an abortifacient
  • 24. NINETY ONE DAY BIRTH CONTROL PILLS:-  These pills are monophasic birth control pills that have been approved for use on a daily basis for 84 days without interruption.  Users have fewer scheduled menstrual cycles (only 1 period every 3 months).  Data from clinical trials show that many women, especially in the first few cycles of use, have more unplanned bleeding and spotting between the expected menstrual periods than women taking conventional combination birth control pills.
  • 25. LONG ACTING, INJECTABLE, PROGESTERONE ONLY CONTRACEPTIVES:-  Medroxyprogesterone acetate (Depo-Provera)  Use:  The first injection is given within 5 days following the onset of menstruation.  After that, an injection is needed every 11-13 weeks.  Side effects:  Since progesterone is the only hormonal ingredient, estrogen- related side effects are avoided.  A side effect unique to this method of birth control is that most women eventually stop having their periods.  Depo-Provera may last in the body for several months in women who have used it on a long-term basis and can actually delay the return to fertility after stopping the drug.  Approximately 70% of former users desiring pregnancy conceive within 12 months, and 90% of former users conceive within 24 months. Other side effects include weight gain and depression.
  • 26. TOPICAL CONTRACEPTIVE PATCH:-  Norelgestromin/ethinyl estradiol (Ortho Evra)  The topical patch may be applied to clean, dry skin on the shoulders, upper arms, buttocks, or abdomen.  It should not be applied to red or inflamed areas of the skin or in areas where tight clothing may rub.  The patch may be less effective in women weighing more than 198 pounds(90 kg).  Use:  A new patch is applied on the same day of the week, each week for 3 weeks in a row.  The first patch is applied either on the first day of the menstrual period or on the Sunday following menses.  On the fourth week, no patch is applied.  Menstruation should begin during this time.  This 4-week period is considered 1 cycle.  Another 4-week cycle is started by applying a new patch following the 7-day  patch-free period.
  • 27. SIDE EFFECTS:-  Side effects are similar to other birth control agents containing both estrogen and progesterone.  Effects include menstrual irregularities,weight gain, and mood changes. Other specific side effects include a skin reaction at the site of application and problems with contact use
  • 28. WHY SHOULD NOT USE THESE MEDICATIONS:-  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  Heart valve disease with complications  Severe hypertension  Diabetes that causes blood vessel problems  Poorly controlled diabetes  Unexplained abnormal bleeding from the uterus  Jaundice during pregnancy or jaundice with prior hormonal  contraceptive use
  • 29. DRUG INTERACTIONS:-  Certain drugs can decrease the effectiveness of combination-type birth control pills by decreasing the drug concentration in your system (impaired enterohepatic recirculation or hepatic induction). This can result in pregnancy.  Drugs that may cause this effect include: many antibiotics(e.g., cephalosporins, chloramphenicol, macrolides, penicillins, tetracyclines, sulfas), aprepitant, bexarotene, bosentan, dapsone, griseofulvin, certain HIV protease inhibitors (e.g., amprenavir, nelfinavir, ritonavir), modafinil, nevirapine, rifamycins (e.g., rifampin), many seizure medications (e.g., barbiturates, carbamazepine, phenytoin, primidone, topiramate), St. John's wort.
  • 30. DRUG INTERACTIONS:-  Before using this medication, tell your doctor or pharmacist of all prescription and non-prescription/herbal medications you may use, especially of: thyroid hormone drugs, certain benzodiazepines (e.g.,diazepam, chlordiazepoxide), prednisone- like drugs, certain antidepressants (e.g., tricyclics), beta-blockers (e.g., metoprolol), "blood thinners" (anticoagulants such as warfarin), insulin.  This product can affect the results of certain lab tests (e.g., thyroid).Inform all laboratory personnel that you use this drug. Birth control pills may significantly intensify the effects of alcohol.  Consult your doctor or pharmacist about this. Do not start or stop any medicine without doctor or pharmacist approval.
  • 31. SIDE EFFECTS:-  Nausea, breast tenderness, fluid retention,  weight gain, acne, breakthrough bleeding,  missed periods, headaches, depression, anxiety,  change in vision, other mood changes, and  lower sexual desire.  Additionally, the following more serious side  effects may occur:  Thromboembolism (blood clots)  Breast cancer  Cervical cancer  Benign liver tumors Diabetes
  • 32. WARNING:-  Smoking cigarettes while using this medication increases your chance of having heart problems.  Do not smoke while using this medication.  The risk of heart problems increases with age(especially in women greater than 35 years of age) and with frequent smoking (15 cigarettes per day or greater).
  • 33. OVER DOSE:-  If overdose is suspected, contact your local poison control center or emergency room immediately. Symptoms of overdose may include nausea and vomiting.  Females may experience vaginal bleeding.
  • 34. MISSED DOSE:-  Missed dose advice differs and depends on the brand used, and the number of doses missed.  Refer to the product package information for advice on missed doses. Ask your doctor or pharmacist if you have any questions.
  • 35. STORAGE:-  Store at room temperature between 59 and 86 degrees F (between 15 and 30 degrees C) away from moisture and sunlight.  Do not store in the bathroom.
  • 36. REFFERENCE:-  From the slideshare app.,  And from the google.