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Presented by:
Pauline Teo
Pharmacy Department, Hospital Miri
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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
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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
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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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