ORAL CONTRACEPTIVES

Presented by:
Pauline Teo
Pharmacy Department, Hospital Miri

8th July, 2009

 OUTLINE
 Contraceptive methods
 Menstrual cycle
 Mechanisms of action
 Type of OCPs
 Non-contraception benefits of OCPs
 Adverse effects
 Contraindications
 Drug interactions
 Counseling 2
 CONTRACEPTION METHODS
 Hormonal methods Oral contraceptives
 Mechanical/Barrier methods
 Natural methods
 Sterilization
 Emergency contraception
Oral contraceptives

Combined oral Progestin-only pills Emergency

contraceptives (COC) (mini-pill) contraception 3
THE MENSTRUAL CYCLE

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 THE ESTROGENS

Estrogens

Natural
• estradiol Semi-synthetic Synthetic
• estrone • ethinyl estradiol • mestranol
• estriol

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 THE PROGESTOGENS
 Progesterone – most important natural
progestogens
 Examples of Progestogen:
 Medroxyprogesterone,
Dyhydrogesterone, Gestodene,
Levonorgestrel, Cyproterone acetate,
Desogestrel, Drospirenone,
Norethisterone, Norgestimate
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 ORAL CONTRACEPTIVES:
Mechanisms of action
 Estrogen
 inhibit secretion of FSH & thus preventing the
development of a dominant follicle
 Progestogen
 suppress LH & thus prevent ovulation
 cause atrophy of endometrium
 alter fallopian tube secretion
 thicken cervical mucus which interferes with
sperm transport
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MECHANISMS OF ACTION

Suppress ovulation

Reduce sperm transport in

upper genital tract
(fallopian tubes)

Change endometrium making

implantation less likely

Thicken cervical mucus

(preventing sperm
penetration)

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 COMBINED ORAL CONTRACEPTIVES
(COC)
 Estrogen + Progestogen
 Estrogen content: 20-40 ug
 21 days of active (hormone-containing)
pills followed by either 7 days of placebo
pills or instructions of not to take pills for
7 days
 Menstrual bleeding usually begins 1 to 4
days after cessation of a 21-day cycle of
COCs or during placebo tablets of 28-day
pack
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 COC (con’t)

COC

Monophasic Biphasic Triphasic

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 COC (con’t)
 Monophasic: contain a fixed ratio of estrogen &
progestin given daily for 21 days
 Eg:
 Marvelon®, Regulon® (Desogestrel 150ug, EE 30ug)
 Microgynon 30®, Nordette®, Rigevidon®
(Levonogestrel 150ug, EE 30ug)
 Diane 35®, Estelle-35® (Cryproterone acetate 2mg,
EE 35ug)
 Meliane® (Gestodene 75ug, EE 20ug)
 Mercilon®, Novynette® (Desogestrel 150ug, EE 20ug)
 Loette® (Levonogestrel 100ug, EE 20ug)
 Gynera®, Minulet® (Gestodene 75ug, EE 30ug)
 Yasmin® (Drospirenone 3mg, EE 30ug)
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 COC (con’t)
 Biphasic: contain a fixed dose of estrogen
(days 1-21) with a lower progestin dose on
days 1 to 10 than on days 11 to 21
 1st half: the progestin/estrogen ratio is lower
to allow the endometrium to thicken as it
normally does.
 2nd half: the progestin/estrogen ratio is
higher to allow normal shedding of the lining of
the uterus to occur
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 COC (con’t)
 Triphasic: have constant or changing
estrogen concentrations and varying
progestin concentrations throughout the
cycle
 Eg:
 Trinordiol®
 6 brown tabs (EE 30ug, Levonogestrel
50ug) + 5 white tabs (EE 40ug,
Levonogestrel 75ug) + 10 yellow tabs
(EE 30ug, Levonogestrel 125ug) 13
 PROGESTIN-ONLY PILLS
 Contain no estrogen
 Given for 28 days continuously
 A good choice in lactating women
 efficacy is increased as a result of the combined
effect of prolactin-induced suppression of ovulation
 does not adversely affect milk volume & infant
growth
 Alternative for those who are unable to take
estrogens
 Less effective than COC
 Eg: Noriday® (norethisterone 0.35mg)
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 EMERGENCY CONTRACEPTION
 Used only when there is an episode of
unprotected sex or there is potential
contraceptive failure
 Synonyms: “morning-after pill”, “post-coital
contraception”
 Should be taken within 72 hours
 If vomiting occurs within 2 hours after drug
intake, dose should be repeated
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 EMERGENCY CONTRACEPTION
(con’t)
 Progestogen only emergency
contraception (POEC)
 0.75mg levonorgestrel (Madonna®,
Postinor-2®)
 2nd dose: 12 hours later (not >16 hours)
 1.5mg levonorgestrel (Escapelle®)
 s/e: nausea (20%), vomiting (5%)

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 NON-CONTRACEPTION BENEFITS
OF OCPs
 Improves menstrual disorders
 ↓ in dysmenorrhea
 prevent ectopic pregnancy
 ↓ risk of pelvic infection
 ↓ in functional ovarian cysts
 ↓ risk of loss of bone density
 ↓ incidence of ovarian cancer
 ↓ incidence of endometrial cancer
 Improvement in acne & hirsutism 17
 ADVERSE EFFECTS
 Breakthrough bleeding/ spotting
 Amenorrhea
 Nausea, vomiting, anorexia
 Breast tenderness
 Headache
 Depression
 Weight gain
 Change in BP
 Acne
 Chloasma 18
 CONTRAINDICATIONS
 Smokers aged ≥ 35 years
 Hypertension
 Myocardial infarct
 Stroke
 Thrombosis
 Severe migraine
 Poorly controlled diabetes
 Severe obesity
 Gall bladder disease or liver tumours
 Known or suspected pregnancy
 Unexplained vaginal bleeding 19
 DRUG INTERACTIONS
 ↓ effectiveness of OCP
 Rifampicin
 Antifungal
 Barbiturates
 Phenytoin
 Certain antibiotics
 Activated charcoal
 Laxatives
 St John’s wort
 Requirement for oral antidiabetics & insulin can
change
 The actions of TCAs, theophylline, diazepam are
potentiated by OCP
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 COUNSELING
 Daily, same time each day
 Take with food or immediately after food
 If you vomit within 4 hours of taking pill, repeat the dose
 Start 1st day of menstrual cycle  protection starts from
the very 1st pill
 Start on other time in menstrual cycle  must use a
different form of contraception for 7 days (COC) or 48
hours (POP)
 Do not protect against STDs (eg: HIV/AIDS)
 If you miss 2 or more menstrual periods, should check
for pregnancy
 If you become sick and have severe diarrhea or
vomiting for several days, you should use another
method of contraception until you next period 21
 IF COCs ARE MISSED
 A pill is regarded as missed if it is >12hours late
 If you forget to take 1 pill, take it as soon as you
remember, even if it means taking 2 pills on 1
day.
 Missed 2 or more pills
Take a pill at once:
- If 7 or more pills left, take the rest of the pills
as usual
- If < 7 pills left, take the rest of the pills as
usual and omit the pill-free interval
Additional contraceptive for the next 7 days
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 IF POPs ARE MISSED
 A pill is regarded as missed if it is >3 hours
late
 The missed pill should be taken as soon as
one remembers
 The next pill should be taken at the usual
time
 Avoid sexual activity
 If sexual activity cannot be avoided, use
additional contraception for 48 hours.
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 REFERENCES
 Milton SW Lum 2003. Contraception. Malaysia: Kuala Lumpur
 Blackburn RD, Cunkelman JA & Zlidar VM 2000. Oral
Contraceptives-An Update. Population Reports: Series A, Number
9
 Zlidar VM 2000. Helping Women Use the Pill. Population Reports:
Series A, Number 10
 MyHEALTH for life. Reproductive Health: Family Planning.
Adapted from http://www.myhealth.gov.my
 British National Formulary (BNF), Issue 54, September 2007. RPS
Publishing
 MedlinePlus Drug Information: Estrogen and Progestin (Oral
Contraceptives). American Society of Health-System Pharmacists,
Inc. Adapted from http://www.nlm.nih.gov/medlineplus/druginfo/
meds/a601050.html [27 April 2009]
 Roberts H 2008. Combined oral contraceptives: Issues for current
users. BPJ:12:21-29.
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