Oral contraceptives (OCs) are a popular method
of contraception and combined oral contraceptives
(COCs) containing estrogen and progestin are the
most prescribed form of OCs. The estrogen used
in most COCs is ethinyl estradiol and most women
should not be prescribed more than 35 mcg of
ethinyl estradiol. The progestins used in COCs
vary in progestin potency as well as estrogenic and
androgenic activities. Selection of a COC should be
based on the biologic activity of the estrogen and
progestin components and the desired hormonal
effect that is appropriate for each patient.1
Contraindications of Oral Contraceptive Use2
• History of stroke, ischemic heart disease, or venous thromboembolism
• History of an estrogen-dependent tumor
• Pregnancy
• Undiagnosed abnormal uterine bleeding
• Hypercholesterolemia
• Women over age 35 years who smoke
POINT OF REFERENCE
Oral Contraceptives and Women’s Health Screenings
Table 1. Side Effects and Management 3, 4
Hormone content
Related side effects
Hormone content
Related side effects
Estrogen excess
• Breast cystic changes/tenderness
• Dysmenorrhea
• Chloasma (discoloration of skin)
Estrogen deficiency
•
•
•
•
Spotting (days 1-9)
Continuous bleeding/spotting
Hypomenorrhea
Atrophic vaginitis
Progestin excess
•
•
•
•
•
•
Progestin deficiency
•
•
•
•
BTB (days 10-21)
Delayed withdrawal bleeding
Dysmenorrhea
Hypermenorrhea
Androgen excess
Side effect
Increase in appetite
Depression
Fatigue
Libido decrease
Weight gain (non-cyclic)
Hypertension
• Acne, increase in libido, hirsutism oily skin/scalp, edema
Management
Side effect
Management
Acne
• ↑ estrogen or,
• ↓ androgen/ progestin
Androgenic effect
• Select 3rd generation progestin, low
dose norethindrone or ethynodiol
diacetate
Amenorrhea
• ↑ estrogen
Irregular, heavy, painful
menses
• ↑ progestin or,
• ↓ estrogen
Breast tenderness/
swelling
• ↓ estrogen
Hirsutism
• ↑ estrogen or,
• ↓ androgen
BTB, spotting
(days 1-9)
• ↑ estrogen
BTB, spotting
(days 10-28)
• ↑ progestin
Nausea
• Take with food at night
• ↓ estrogen or ↑ progestin
High risk of thrombosis
• ↓ estrogen
BTB= breakthrough bleeding
Table 2. Pharmacological Effects of Progestins Used in Oral Contraceptives3
Estrogen effect
Progestin effect
Androgen effect
Most
Ethynodiol
Desogestrel, Levonorgestrel
Levonorgestrel
Intermediate
Norethindrone
Norgestrel, Norgestimate
Norgestrel, Desogestrel
Least
Desogestrel, Levonorgestrel,
Norgestrel, Norgestimate
Norethindrone
Ethynodiol, Norgestimate,
Norethindrone
Available Combination Oral Contraceptive Products3, 4
Black bold = Generic Products → Tier 1, Lowest Copay
Gray italics = Brand Products → Tier 2 or above, Higher Copay
Product Name
Estrogen
(mcg)
Progestin
(mg)
Estrogen
activity
Progestin
activity
Androgenic
activity
Necon 1/50®, Norinyl 1+50®, Ortho-Novum 1/50®
50 Mestranol
1 NE
I
I
I
Ovcon-50®
50 EE
1 NE
H
I
I
1 ED
H
H
I/H
Monophasic Products
Zovia 1/50E
®
Ogestrel 0.5/50
0.5 NT
H
H
H
1 NE
I
I/H
I
Necon 0.5/35®, Nortrel 0.5/35®, Brevicon®, Modicon®
0.5 NE
I
L
L
Balziva™, Zenchent™, Ovcon-35®, Femcon® Fe Chw
0.4 NE
I
L
L
MonoNessa , Previfem™, Sprintec™, Ortho-Cyclen
0.25 NG
I
L
L
1 ED
I
H
L
3
L
drospirenone
No Data
None
Junel 1.5/30®, Junel Fe 1.5/30®, Microgestin™ Fe 1.5/30,
Microgestin® 1.5/30, Gildess™ Fe 1.5/30, Loestrin 21
1.5/30®, Loestrin Fe 1.5/30®
1.5 NE
L
H
H
Cryselle®, Low-Ogestrel®, Lo/Ovral®
0.3 NT
L
I
I/H
Apri , Reclipsen , Solia , Desogen ,
Ortho-Cept®
0.15 DE
L
H
L
Jolessa-91d®, Portia®, Quasense®, Levora®, Nordette-28®,
Seasonale-91d®
0.15 LV
L
I
I/H
3
L
drospirenone
H
None
0.09 LV
No Data
No Data
No Data
0.1 LV
L
L
L
1 NE
L
H
I
®
Necon 1/35®, Norinyl 1+35®, Nortrel 1/35®,
Ortho-Novum 1/35®
35 EE
®
®
Kelnor 1/35®, Zovia 1/35E®
Ocella , Yasmin
®
30 EE
®
®
®
®
®
Gianvi™, Yaz®
20 EE
Lybrel-90d™
Aviane™, Lessina , Lutera , Sronyx , Alesse
®
®
®
®
Junel® 21 1/20, Junel® Fe 1/20, Microgestin™ Fe 1/20,
Gildess™ Fe 1/20, Loestrin 24 Fe®, Loestrin 21 1/20®
Product Name
Phase 1
Phase 2
Estrogen
activity
Progestin
activity
Androgenic
activity
Kariva®, Azurette®, Mircette®
20 EE x 21d
0.15 DE
10 EE x 5d
L
H
L
LoSeasonique™
20 EE x 84d
0.1 LV
10 EE x 7d
No Data
No Data
No Data
Seasonique™
30 EE x 84d
0.15 LV
10 EE x 7d
No Data
No Data
No Data
Necon 10/11®, Ortho-Novum®
35 EE x 10d
0.5 NE
35 EE x 11d
1 NE
H
I
L/I
Biphasic Products
Product Name
Phase 1
Phase 2
Phase 3
Estrogen
activity
Progestin
activity
Androgenic
activity
Aranelle®, Leena®, Tri-Norinyl®
35 EE x 21d
0.5 NE x 7d
35 EE
1 NE x 9d
35 EE
0.5 NE x5d
I
I
L/I
Necon 7/7/7®, Ortho-Novum 7/7/7®
35 EE x 21d
0.5 NE x 7d
35 EE
0.75 NE x 7d
35 EE
1 NE x 7d
I
I
L/I
Enpresse®, Trivora®, Triphasil®
30 EE x 6d
0.05 LV
40 EE x 5d
0.075 LV
30 EE x10d
0.125 LV
I
H
L
Cesia®, Velivet®, Caziant®, Cyclessa® 25 EE x 21d
0.1 DE x 7d
25 EE
0.125 DE x 7d
25 EE
0.15 DE x 7d
L
H
L
Tri-Previfem™, TriNessa™,
Tri-Sprintec™, Ortho Tri-Cyclen®
35 EE x 21d
0.18 NG x 7d
35 EE
0.215 NG x 7d
35 EE
0.25 NG x 7d
I
L
L
Ortho Tri-Cyclen Lo®
25 EE x 21d
0.18 NG x 7d
25 EE
0.215 NG x 7d
25 EE
0.25 NG x 7d
L
L
L
Tilia Fe®, Tri-Legest™, Tri-Legest
Fe™, Estrostep® Fe
20 EE x 5d
1 NE x 21d
30 EE x7d
1 NE
35 EE x 9d
1 NE
L
H
I
Triphasic Products
Product Name
Phase 1
Phase 2
Phase 3
Phase 4
Estrogen
activity
Progestin
activity
Androgenic
activity
3mg EV x 2d
2mg EV
2mg DN x 5d
2mg EV
3mg DN x17d
1mg EV x2d
No Data
No Data
No Data
4-Phasic Products
Natazia™
DE= desogestrel, EE= ethinyl estradiol, ED= ethynodiol diacetate, LV= levonorgestrel, NE= norethindrone,
NT= norgestrel, NG= norgestimate, EV= estradiol valerate, DN= dienogest, L=Low, I=Intermediate, H=High Activity
Newer Oral Contraceptives5
Newer oral contraceptives contain lower doses of
ethinyl estradiol and new progestins such as desogestrel,
norgestimate and drospirenone. Lower doses of estrogen
reduce the risk of thromboembolism; however, no studies
have shown that products containing less than 30 mcg
of ethinyl estradiol actually offer a safety advantage.
Newer progestins provide greater progestational activity and
less androgenic activity and seem to have better side effect
profiles; lower incidence of lipid disorders, mood changes,
acne, weight gain and myocardial infarction. Unfortunately,
these newer progestins have reported an increase in risk of
deep venous thrombosis in several epidemiological studies.
Unique Formulation Products4
Shortened Hormone Free Interval (HFI)
Extended Cycle
Definition
• L
ow dose oral contraceptives with more
than 21 days of hormones but maintains
a 28 day cycle
• Longer active pills duration so less number
of menses per year • Can use any monophasic
Benefit
• Shorter menses
• Less break through bleeding
• Theoretically may minimize hormone
withdrawal symptoms
• Theoretically beneficial for patients who have
menstrual symptoms or estrogen withdraw
symptoms during HFI
Products
•
•
•
•
• Seasonale - 4 menses per year
• Seasonique - 4 menses per year
• Lybrel – no menses per year
Mircette
Yaz
Yasmin
Loestrin-24
Additional FDA Indications for Oral Contraceptives4
• Acne: Ortho Tri-Cyclen, Estrostep, Yaz
• Premenstrual dysphoric disorder (PMDD): Yaz
Chlamydia Information and Screening6, 7
Chlamydia is a common sexually transmitted disease (STD)
caused by Chlamydia trachomatis. When it is not treated,
it can spread into the uterus or fallopian tubes and cause
pelvic inflammatory disease (PID). Chlamydia then can
increase the risk of infertility, ectopic pregnancy and chronic
pelvic pain. Pregnant women infected with chlamydia can
pass the infection to their infants during delivery, potentially
resulting in neonatal conjunctivitis and pneumonia.
Cervical Cancer Information and Screening8,9
Cervical cancer affects all women and it occurs more
commonly in women who are 30 years of age or older.
Fortunately, cervical cancer is the easiest female cancer
to prevent because of screenings and vaccines for human
papillomavirus (HPV) infections. With early detection,
cervical cancer is highly treatable.
Therefore, it is important to encourage patients to obtain
routine chlamydia screenings as recommended below.
• Less than 25 years old – if sexually active, screen annually
• Older than 25 years old and having sex with more than one
partner – screen annually
• Older than 25 years old and has a new sex partner –
screen annually
• Pregnant women – screen annually
Therefore, it is important to encourage patients to obtain
routine cervical cancer screenings as recommended below.
• Papilloma test (or Pap smear)
• Less than 30 years old – screen annually
• Age 30 or older – if a patient had 3 normal pap tests for 3
years in a row, screen every 2 or 3 years
• 65 to 75 years old – stop after at least 3 normal pap tests
and no abnormal results in the last 10 years
• HPV test to look for the virus that can cause cell changes
References:
1.
Martin KA, Douglas PS. Risks and side effects associated with estrogen-progestin contraceptives. In:UpToDate, Barbiery RL, Crowley WF (Ed), UpToDate, Waltham, MA, 2009.
2.
Martin KA, Barbiery RL. Overview of the use of estrogen-progestin contraceptives. In: UpToDate, Snyder PJ, Crowley WF (Ed), UpToDate, Waltham, MA, 2009.
3.
Facts and Comparisons Online Database. Available at: http://factsandcomparisons.com. Accessed on September 7, 2010.
4.Pharmacist’s letter. Hormonal contraception. Available at: http://www.pharmacistsletter.com/(S(glqsfdiuzjottc55mw32lgjc))/pl/detaildocuments/220809.pdf?rn=1&cs=STUDENT&s=PL. Accessed on September
7, 2010.
5.Pharmacist’s letter. Concerns about the newer oral contraceptives. Available at: http://www.pharmacistsletter.com/(S(glqsfdiuzjottc55mw32lgjc))/pl/detaildocuments/230303.pdf?rn=1&cs=STUDENT&s=PL.
Accessed on September 7, 2010.
6.
Centers for Disease Control and Prevention. Chlamydia-CDC fact sheet. Available at: http://www.cdc.gov/std/Chlamydia/STDFact-Chlamydia.htm#WhatIs. Accessed on September 7, 2010.
7.
Centers for Disease Control and Prevention. Sexually Transmitted Diseases Surveillance, 2008. Available at: http://www.cdc.gov/std/stats08/chlamydia.htm. Accessed on September 7, 2010.
8.
Centers for Disease Control and Prevention. Gynecologic Cancers. Available at: http://www.cdc.gov/cancer/cervical/index.htm. Accessed on September 7, 2010.
9.
The national women’s health information center. Pap Test: frequently asked questions. Available at: http://www.womenshealth.gov/faq/pap-test.pdf. Accessed on September 7, 2010.
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