Pharcomology of Oral Contraception

PHARCOMOLOGY
ORAL CONTRACEPTION
PRESENTED BY Dr Muna Muse Mohamed
DEPARTEMENT :- OBG/GYN
Reg No:- 2022-04-09784
Supervisor :- Prof.Dr. SAIDI ODOMA
Definition
 Oral contraceptions are medicines that are taken by mouth to
prevent pregnancy,they are also called Birth control pills
 They include:
Combined oral contraceptive pills.
Progestin only pills
Emergency contraception pills.
1. COMBINED ORAL CONTRACEPTIVE
PILLS (COCs).
 Combination contraceptives containing both estrogen and
progesterone
 They are the most effective means for contraception.

COMPOSITION OF COCs
COCs are composed of estrogen and progestins.
 The commonly used progestins are :
 Levonorgestrel
 Norethisterone
 Desogestrel.
 The commonly used estrogen are

Ethinyl-estradiol
Menstranol.
Mechanism of action of COCs
 Suppression of hypothalamic gonadotropin-releasing hormone by negative
feedback. This in turn blocks pituitary secretion of follicle-stimulating
hormone (FSH) and luteinizing hormone (LH) and thereby inhibits ovulation.
 Estrogen component in COCs blocks ovulation by suppressing FSH release.
 The progestin component prevent pregnancy by:
 Preventing ovulation by suppressing LH( Main effect).
 Thickens cervical mucus
 Renders the endometrium unfavorable for implantation.(by causing
atrophy).
PRESCRIPTION OF COCs
 A simple regime of “3 weeks on and 1 week off ”:Packet of 21 tablets.

 One tablet is to be taken daily at bed time for consecutive 21 days.
 Then have a 7 days break.
 Next pack should be started on the eighth day.
 Packing of 28 tablets
 No break between packs.
 The last 7 pills are dummies(placebo) and contain only either iron or
vitamin preparations.
Different formulations of COCs.
 Monophasic pills:
They 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).
 Biphasic pills :
The Contain 2 different progesterone doses. The progesterone dose is
increases in the second half of the cycle.
 Triphasic :
 In these preparations, the hormonal doses of both estrogen and
progestin vary over the course of the cycle.
 First 6 tablets contain 0.05 mg levonorgestrel and 30 mg of ethinyl
estradiol
 Next 5 tablets contain 0.075 mg levonorgestrel and 40 mg ethinyl
estradiol.
 The last 10 tablets contain 0.125mg levonorgestrel and 30 mg
ethinyl estradiol.
ADVERSE EFFECTES OF COCs
 Nausea, vomiting, headache (Estrogen)
 Leg cramps (Progestin)
 Weioght gain( Progestin): Not common finding in COCs users.
 Mastalgia (estrogen and progestin) .
 Chloasma (estrogen)
 Acne (Progestin)
Metabolic Changes associated with COCs.
 Estrogen lowers LDL cholesterol concentrations.
 Estrogens boost hepatic production of fibrinogen and many of the
clotting factor.
 Estrogen also augment Angiotensinogen production and its conversion by
renin to angiotensin I may be associated with “pill-induced hypertension,”
 COCs elevate sex hormone-binding globulin (SHBG) levels, which in turn
lower concentrations of bioavailable testosterone and thus, lessen
androgenic side effects.
Cardiovascular Effects of COCs.
 Hypertension:
 Due to increased production of angiotensinogen.
 Rarely induce HTN, because low dose of COCs is used.
 Deep-vein thrombosis and pulmonary embolism

 Increased risk
 Due to production of fibrinogen and other clotting factors.
Contraindications of COCs
 DVT or History of DVT.
 Patient with Hypertension.
 History of Myocardial infarction.
 History of stroke.
 Smokers above 35 years old.
 Breast cancer.
 Lactating mother below 6 months. Etc.
DRUG INTERACTIONS WITH COCs.
 COCs are metabolized in the liver

 Anticonvulsants: The metabolism of COCs is accelerated by any drug that
increases liver microsomal enzyme activity such as
 Phenobarbital
 Phenytoin
 griseofulvin
As a result, the contraceptive efficacy of a COC is likely to be decreased in

women taking these drugs.
DRUG INTERACTIONS WITH COCs.
 Antibiotics
 Rifampin is the only antibiotic proven to decrease serum ethinyl
estradiol and progestin levels in women taking COCs
 It has similar to liver enzyme-inducing anticonvulsants

2. PROGESTIN ONLY PILLS( POP).
 It contains very low dose of a progestin in any one of the
following form:-
Levonorgestrel 75 μg
 norethisterone 350 μg
desogestrel 75 μg
lynestrenol 500 μg
 norgestrel 30 μg.
Mechanism of action of POP.
 works mainly by making cervical mucus thick and viscous,
thereby prevents sperm penetration.
 Prevent implantation by causing atrophic endometrium
 Rarely prevent ovulation ( in 2 percent of cases)

Prescription of POPs
 The first pill has to be taken on the first day of the cycle and then
continuously.
 It has to be taken regularly and at the same time of the day.
 There must be no break between the packs.
 If a progestin-only pill is taken even 4 hours late, a supplemental
form of contraception must be used for the next 48 hours.
Advantages of POPs
 Side effects attributed to estrogen in the combined pill are
totally eliminated.
 No adverse effect on lactation
 It may be prescribed in patient having (medical disorders)
hypertension, fibroid, diabetes, epilepsy, smoking and history
of thromboembolism
 Reduces the risk of endometrial cancer.
Adverse effects of POP
 Acne, mastalgia, headache.
 Breakthrough bleeding
 Amenorrhea in about 20–30 percent
 Failure rate is about 0.5–2 per 100 women years of use
 Weight gain
3. Emergency contraception pills
( Morning after pill)
 May contain: Progestin , Estrogen or both.
 Prevent or delay ovulation.
 Should be given Preferably within 12 hours, no later than 72 hours after
unprotected sexual intercourse.
Example :-
 Levonorgestrel : Given as single dose at 1.5mg. ( Pregn. Rate:0–1% )
 Ethinyl estradiol 2.5 mg BD × 5 days ( 0–0.6%)
 Ethinyl estradiol 50 μg + Norgestrel 0.25 mg 2 tab stat and 2 after 12 hours.( 0–2%)
REFERENCES
 William obstetrics 25th Edition

 UpTodate. Online.
 Dutta’s text book of obstetrics.

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What are the different types of oral contraceptives discussed?

How do combined oral contraceptive pills work?

PHARCOMOLOGY

 They are the most effective means for contraception.

 The commonly used estrogen are

 A simple regime of “3 weeks on and 1 week off ”:Packet of 21 tablets.

 Deep-vein thrombosis and pulmonary embolism

 COCs are metabolized in the liver

As a result, the contraceptive efficacy of a COC is likely to be decreased in

 Rifampin is the only antibiotic proven to decrease serum ethinyl

estradiol and progestin levels in women taking COCs

 It has similar to liver enzyme-inducing anticonvulsants

 Prevent implantation by causing atrophic endometrium

 Rarely prevent ovulation ( in 2 percent of cases)

 William obstetrics 25th Edition

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