Levonorgestrel-Ethinyl Estradiol

Generic Name: Levonorgestrel-Ethinyl Estradiol

Brand Names: Seasonale, Seasonique, LoSeasonique, Amethia

Levonorgestrel-ethinyl estradiol is a combined hormonal contraceptive containing a progestin and estrogen. Extended-cycle formulations reduce menstrual frequency.

Women's HealthContraceptionHormones

Drug Class

Combined Oral Contraceptive (Estrogen-Progestin)

Pregnancy

Contraindicated in pregnancy. Not indicated for use during pregnancy. If pregnancy occurs while taking the medication, discontinue immediately. Combined oral contraceptives are not associated with teratogenic effects when inadvertently taken during early pregnancy.

Available Forms

Oral tablet (various formulations): 0.1 mg/20 mcg, 0.15 mg/30 mcg, 0.25 mg/50 mcg, Oral tablet (triphasic regimens): varying levonorgestrel doses with 30–40 mcg ethinyl estradiol, Extended-cycle oral tablet (91-day regimen): 0.15 mg/30 mcg (84 active tablets + 7 inert or low-dose EE tablets)

What It's Used For

Dosage Quick Reference

These are general dosage guidelines. Your doctor will determine the appropriate dose for your specific situation.

Condition	Starting Dose	Maintenance Dose
Contraception (monophasic 28-day)	1 tablet daily starting on Day 1 of menses or first Sunday	1 tablet daily at the same time each day; 21 active + 7 placebo
Contraception (extended cycle, 91-day)	1 tablet daily starting Day 1 of menses	1 tablet daily for 84 days active, then 7 low-dose EE or placebo tablets
Acne vulgaris (select formulations)	1 tablet daily as directed	Continue for at least 6 months to assess benefit

Side Effects

Common Side Effects:

Nausea
Breast tenderness
Headache
Breakthrough bleeding/spotting
Weight changes
Mood changes
Decreased libido
Acne (may improve or worsen)

Serious Side Effects:

Venous thromboembolism (DVT, PE)
Arterial thromboembolism (MI, stroke)
Hypertension
Hepatic tumors
Gallbladder disease
Melasma
Cervical cancer (increased risk with long-term use)

Drug Interactions

Enzyme-inducing antiepileptics (carbamazepine, phenytoin, phenobarbital, topiramate at high doses): Reduce contraceptive efficacy through CYP3A4 induction. Use backup contraception or alternative contraceptive method.
Rifampin: Potent CYP3A4 inducer that significantly decreases ethinyl estradiol and progestin levels. Do not rely on oral contraceptives for pregnancy prevention during rifampin therapy.
HIV protease inhibitors and NNRTIs: Complex bidirectional interactions. Some increase and some decrease hormonal contraceptive levels. Consult a specialist for specific antiretroviral combinations.
Lamotrigine: Ethinyl estradiol increases lamotrigine clearance, potentially reducing seizure control. Lamotrigine dose adjustments may be needed when starting or stopping oral contraceptives.
St. John's wort: Induces CYP3A4 and may reduce contraceptive efficacy. Breakthrough bleeding or pregnancy may result.

Additional Information

Levonorgestrel/ethinyl estradiol is a combination oral contraceptive containing a progestin and an estrogen, used for the prevention of pregnancy. This widely prescribed contraceptive is available in various formulations and provides reliable birth control when taken correctly.

Mechanism of Action

The combination of levonorgestrel and ethinyl estradiol prevents pregnancy through multiple mechanisms. The primary mechanism is suppression of gonadotropins (FSH and LH), which inhibits ovulation. Levonorgestrel, the progestin component, primarily suppresses the LH surge necessary for ovulation. Additionally, the hormones cause changes to the cervical mucus, making it hostile to sperm penetration, and alterations to the endometrium that may reduce the likelihood of implantation. The estrogen component (ethinyl estradiol) contributes to ovulation suppression and helps stabilize the endometrium, preventing breakthrough bleeding.

Available Formulations

Levonorgestrel/ethinyl estradiol is available in numerous brand and generic formulations with varying doses and regimens: monophasic (same dose throughout cycle), biphasic, and triphasic (varying doses). Common formulations include 21/7 regimens (21 active pills, 7 placebo) and extended-cycle regimens (84 active pills). Doses of ethinyl estradiol range from 20-35 mcg; levonorgestrel doses vary from 0.05-0.15 mg.

Medical Uses

Levonorgestrel/ethinyl estradiol is FDA-approved for prevention of pregnancy. Some formulations are also approved for treatment of acne vulgaris in females at least 15 years of age who desire contraception. Off-label uses include management of dysmenorrhea, menorrhagia, endometriosis, and premenstrual syndrome. Extended-cycle formulations are used to reduce menstrual frequency.

Dosing Guidelines

Take one tablet daily at the same time each day, as directed for the specific product. Most formulations are taken for 21 days followed by 7 days of placebo (or hormone-free interval). Extended-cycle products have different schedules. Start timing varies: Sunday start, Day 1 start, or quick start methods may be used. If a pill is missed, follow product-specific instructions; backup contraception may be needed.

Important Safety Information

Combination oral contraceptives carry a boxed warning that cigarette smoking increases the risk of serious cardiovascular side effects (MI, stroke, thromboembolism), especially in women over 35 who smoke heavily; women who smoke should not use combination oral contraceptives. Other serious risks include VTE, stroke, MI, hepatic tumors, gallbladder disease, hypertension, and carbohydrate/lipid metabolic effects. Contraindications include thrombophlebitis or thromboembolic disorders, history of DVT/PE, cerebrovascular disease, coronary artery disease, breast cancer, hepatic tumors, and undiagnosed abnormal uterine bleeding.

Drug Interactions

CYP3A4 inducers (rifampin, phenytoin, carbamazepine, St. John's Wort, some HIV medications) may decrease contraceptive efficacy; backup contraception may be needed. Ethinyl estradiol may increase levels of CYP3A4 substrates (cyclosporine). The contraceptive may decrease lamotrigine levels. Antibiotics (other than rifampin) generally do not significantly affect contraceptive efficacy, though some product labeling recommends backup contraception.

Special Populations

Combination oral contraceptives are contraindicated during pregnancy. They are not recommended during breastfeeding in the first 4-6 weeks postpartum (may decrease milk production); progestin-only methods are preferred. Safety and efficacy have been established in reproductive-age females. Women over 35 who smoke should not use combination oral contraceptives. No dose adjustment is needed for renal impairment. The medication should not be used in women with significant hepatic impairment.

Frequently Asked Questions

With perfect use (taking the pill at the same time every day without missing any), the failure rate is about 0.3 percent per year. With typical use, the failure rate is about 7 percent per year, mainly due to missed pills.

If you miss one pill, take it as soon as you remember and take the next pill at your regular time (you may take two pills in one day). If you miss two or more pills in a row, take the most recent missed pill, skip any other missed pills, use backup contraception for 7 days, and consult the specific instructions for your pill pack.

Combined oral contraceptives slightly increase the risk of venous thromboembolism (blood clots) from about 1–5 per 10,000 women per year (without hormones) to about 3–9 per 10,000 women per year. Risk is highest in the first year of use and in women with additional risk factors such as smoking, obesity, or a family history of clotting disorders.

Yes, many women safely skip placebo pills and start a new pack immediately to postpone or skip their withdrawal bleed. Extended-cycle regimens are specifically designed for fewer periods per year. Discuss this approach with your provider.

No. Fertility typically returns within one to three months after stopping combined oral contraceptives, though it may take slightly longer for some women. Long-term use does not impair future fertility.

The risk of cardiovascular complications increases with age, especially after 35, and particularly in women who smoke. Most guidelines recommend against combined hormonal contraceptives for women over 35 who smoke. Your provider can help determine when to transition to an alternative method.

Questions to Ask Your Doctor

Consider discussing these topics at your next appointment:

✓Do I have any risk factors for blood clots that make combined oral contraceptives unsafe?
✓Are any of my current medications likely to reduce the effectiveness of this birth control?
✓Should I consider an extended-cycle regimen to reduce the frequency of my periods?
✓Are there non-contraceptive benefits of this pill that are relevant to my health?

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Related Health Conditions

This medication is commonly used to treat or manage the following conditions:

Acne

Acne vulgaris, a chronic inflammatory skin condition, arises from clogged hair follicles due to excess sebum, dead skin cells, bacteria, hormones, genetics, diet, stress, or medications.

Learn More

Migraine

Migraine is a debilitating neurological condition causing recurrent headaches with throbbing pain, nausea, and light/sound sensitivity, likely stemming from complex brain, nerve, and blood vessel interactions.

Learn More

Stroke

A stroke, caused by interrupted brain blood supply from blockage (ischemic) or bleeding (hemorrhagic), is a medical emergency requiring prompt treatment to minimize brain damage.

Learn More

Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.