Oral Oral ContraceptivesContraceptivesEstrogen and Progestin

2

Desired Outcome of Desired Outcome of contraception:contraception:

• prevent pregnancy

• improvements in certain health conditions (OCs)

• management of perimenopause.

• improvements in menstrual cycle regularity (hormonal)

CompositionsCompositions

• Hormonal contraceptives contain either a combination of synthetic estrogen and synthetic progestin or a progestin alone.

How they work?• Progestins thicken cervical mucus, delay

sperm transport, and induce endometrial atrophy. They also block the LH surge and thus inhibit ovulation.

• Estrogens suppress FSH release, which may contribute to blocking the LH surge (an acute rise of LH ), and also stabilizes the endometrial lining and provides cycle control.

3

4

components of hormonal contraceptives components of hormonal contraceptives

Estrogens:

• ethinyl estradiol (EE) and mestranol

• Mestranol → liver → EE to be active.

• 50% less potent than EE.

• doses of 20 to 50 mcg of EE.

Progestins:• They are different in their:• progestational activity• Their inherent estrogenic , antiestrogenic , androgenic effects.• Their estrogenic and antiestrogenic properties occur because

progestins are metabolized to estrogenic substances. • Androgenic properties occur because of the structural

similarity of the progestin to testosterone.

• The recommendation of the American College of Obstetricians and Gynecologists is to allow provision of hormonal contraception after a simple medical history and blood pressure measurement

5

6

noncontraceptive benefits of oral noncontraceptive benefits of oral

contraceptivescontraceptives::• decreased menstrual blood loss.• improvement of menstrual irregularity.• Decrease ovulatory pain• Decrease the risk ovarian & endometrial

cancer.• Decreased the occurrence of ectopic

pregnancy.• decreased menstrual cramps .• Decreased iron deficiency anemia from

period.• Decreased risk endometriosis, uterine

fibroids, benign breast disease.

7

8

9

10

11

13

Women Older Than 35 Years:Women Older Than 35 Years:

• Recommended: use (less than 50 mcg of estrogen) in healthy nonsmoking women.

• Women over 35 years who smoke and take OCs have an increased risk of MI; therefore, clinicians should prescribe CHCs with caution, if at all, in these patients.

• The WHO states that smoking 15 or more cigarettes per day by women over 35 years is a contraindication to the use of CHCs, and that the risks generally outweigh the benefits even in those who smoke fewer than 15 cigarettes per day.

• Progestin-only contraceptive methods should be considered for women in this group.

• Women older 35 yrs with migraine, HTN, DM(1&2),dyslipidemia and current smoker should not take CHCs.

• CHC may increase or decrease the frequency of migraine.

• However CHCs may be considered for healthy, non-smoker women, with migraine that is only without aura.

• BUT not with aura.• OCs can be used women with stable SLE

and without antiphospholipid antibodies.• CHCs should be avoided women with

SLE ,antiphospholipid antibodies and or vascular complication. Progestin-only contraceptives can be used with those patient.

14

Breast cancer Breast cancer

• CHCs choice should not be affected by the presence of benign breast disease or a family history of breast cancer with either mutation.

• women with recent personal history of breast cancer should not use CHCs, but that CHCs can be considered in women without evidence of disease for 5 years.

15

ThromboembolismThromboembolism

• Estrogens have a dose-related effect in the development VTE and PE.

• This is especially true inwomen with underlying hypercoagulable states or who have acquired conditions(e.g., obesity, pregnancy, immobility, trauma, surgery, and certainmalignancies.)

16

Obesity Obesity

17

• OCs have lower efficacy in obese women, and low dose of OC may be specially problematic.

General considerations General considerations for Ocs.for Ocs.

• >99% of efficacy with perfect use.

• Up to 8% of unintended pregnancy with typical use.

• Monophasic OCs contain the same amounts of estrogen and progestin for 21 days, followed by 7 days of placebo.

• Biphasic and triphasic pills contain variable amounts of estrogen and progestin for 21 days and are followed by a 7-day placebo phase.

18

General considerations General considerations for Ocs.for Ocs.extended-cycle OC:

• ↑ hormone-containing pills from 21 to 84 days 7-day placebo phase,only 4 menstrual cycles/ year.

• One product provides hormone-containing pills daily throughout the year.

Continuous combination regimens:• OCs for 21 days, then very-low-dose estrogen and

progestin for an additional 4 to

7 days(at usual placebo time).

19

third-generation OCs:

OCs containing newer progestins:

• Desogestrel

• Drospirenone

• Gestodene

• Norgestimate

• These progestins:• potent progestational agents• have no estrogenic effects• less androgenic compared with levonorgestrel

on a weight basis

• improved side-effect profiles, as improving mild to moderate acne.

Drospirenone:

• antimineralocorticoid and antialdosterone activities• result in less weight gain compared to use of OCs

containing levonorgestrel.

20

Progestin-only Progestin-only minipills minipills

• 28 days of active hormone per cycle

• less effective than combination OCs

• irregular and unpredictable menstrual bleeding

• must be taken every day of the menstrual cycle at approximately the same time.

• If taken more than 3 hours late backup method of contraception for 48 hours.

• ectopic pregnancy is high because it does not block ovulation.

21

Initiating an Oral Contraceptive:Initiating an Oral Contraceptive:

different methods:

• on the first day of bleeding during the menstrual cycle.

• on the first Sunday after the menstrual cycle begins.

• on the fifth day after the menstrual cycle begins.

22

quick start" method:quick start" method:

• patient takes the first tablet on the first day of her office visit.

• use a second method of contraception for at least 7 days

• the menstrual period will be delayed until completion of the active tablets in the current OC pack.

23

Choice of OCs Choice of OCs • choice is based on:

• the hormonal content and dose

• preferred formulation

• coexisting medical conditions

• In women without coexisting medical conditions, an OC containing 35mcg or less of EE and less than 0.5 mg of norethindrone is recommended.

24

20 to25mcg 20 to25mcg • Adolescents, underweight

women<50kg. women >35years, and those who are perimenopausal may have fewer S/E with this dose.

• However, they are associated with more breakthrough bleeding and an increased risk of contraceptive failure if doses are missed.

Overweight and obese women:

• higher contraceptive failure rates with low dose OCs

• benefit from pills containing at least 35 mcg of EE.

25

Who uses progestin only Ocs?Who uses progestin only Ocs?• cerebrovascular disease• SLE with vascular disease• history of estrogen dependent cancer• smokers over the age of 35• postpartum and/or breastfeeding• migraine headaches• history of VTE• cardiovascular disease

26

Managing Side Managing Side EffectsEffects

Many symptoms occurring in the first cycle of OC use (e.g., breakthrough bleeding, nausea, bloating), improve by the second or third cycle of use.Warning signs•Women should be instructed to immediately discontinue CHCs if they experience warning signs often called ACHES (abdominal pain, chest pain, headaches, eye problems, and severe leg pain).

27

28

Managing Oral Contraceptive Drug Managing Oral Contraceptive Drug Interactions:Interactions:• Use additional method

Rifampin:

• risk of OC failure

• additional nonhormonal contraceptive agent during rifampin therapy.

if breakthrough bleeding during concomitant use of antibiotics and OCs:

• use an alternate method of contraception during the period of concomitantuse.

anticonvulsants: reduce efficacyphenobarbital,cabamezapine,and phenytoin.

• another form of contraception such as:• IUDs• injectable medroxyprogesterone• Implants.• nonhormonal options.

29

d/cd/c

• The average delay in ovulation after d/c OCs is 1 to 2 weeks.

• allow 2 to 3 normal menstrual periods before becoming pregnant

30

31

Thank youThank youABDIWAHID ADAMABDIWAHID ADAM

ABDIRAHMAN AL-NOAMIABDIRAHMAN AL-NOAMIPHARM DPHARM D