Usage
- Ethinyl Estradiol + Levonorgestrel is prescribed for oral contraception (prevention of pregnancy). Some formulations are also indicated for the treatment of abnormal uterine bleeding, particularly functional uterine bleeding unrelated to pregnancy.
- Pharmacological Classification: Combined hormonal contraceptive (estrogen-progestogen).
- Mechanism of Action: This combination primarily prevents pregnancy by inhibiting ovulation. The estrogen component suppresses the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland, thus preventing the development and release of a mature egg. The progestin component thickens cervical mucus, making it difficult for sperm to enter the uterus, and alters the uterine lining, making it less receptive to implantation.
Alternate Names
- Combined oral contraceptive pill (COCP), birth control pill, the pill.
- Brand Names: Alesse, Altavera, Amethyst, Aviane, Balcoltra, Camrese Lo, Chateal, Daysee, Dolishale, Falessa, Falmina, Jaimiess, Jolessa, Kurvelo, Lessina, Levlen, LoSeasonique, Lutera, Marlissa, Portia, Preven (discontinued in the US), Seasonale, Seasonique, Setlakin, Simpesse, Sronyx, Trivora, Tyblume, Vienva.
How It Works
- Pharmacodynamics: Ethinyl estradiol, a synthetic estrogen, and levonorgestrel, a synthetic progestogen, work synergistically to achieve contraception. Estrogen primarily suppresses the hypothalamic-pituitary-ovarian axis, inhibiting ovulation. Progestogen thickens cervical mucus, hinders sperm transport, and induces endometrial changes unfavorable for implantation.
- Pharmacokinetics:
- Absorption: Both drugs are rapidly absorbed from the gastrointestinal tract. Levonorgestrel has near 100% bioavailability, whereas ethinyl estradiol’s bioavailability is lower (38-48%) due to first-pass metabolism.
- Metabolism: Both are extensively metabolized in the liver, primarily by CYP3A4 enzymes.
- Elimination: Metabolites are excreted in urine and feces.
- Mode of Action: Ethinyl estradiol binds to estrogen receptors, while levonorgestrel binds to progesterone receptors. These actions lead to the described pharmacodynamic effects.
- Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: The primary mechanism involves receptor binding (estrogen and progesterone receptors).
Dosage
Standard Dosage
Children: Use and dose must be determined by a doctor. Not recommended before menarche.
Special Cases:
- Elderly Patients: Generally not indicated for postmenopausal women.
- Patients with Renal Impairment: Dose adjustment may be necessary.
- Patients with Hepatic Dysfunction: Use with caution; dose adjustment may be required. Contraindicated in severe liver disease.
- Patients with Comorbid Conditions: Caution in patients with diabetes, cardiovascular disease, hypertension, hyperlipidemia, history of thromboembolism, migraines, or liver disease.
Clinical Use Cases
Ethinyl Estradiol + Levonorgestrel’s primary indication is contraception. It does not have specific dosage recommendations for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dose adjustments are necessary for patients with hepatic or renal impairment and those taking interacting medications. Genetic polymorphisms affecting drug metabolism may also require dose adjustments.
Side Effects
Common Side Effects:
Nausea, vomiting, headache, breast tenderness, breakthrough bleeding, weight changes, mood changes, acne, fluid retention, changes in libido.
Rare but Serious Side Effects:
Blood clots (deep vein thrombosis, pulmonary embolism, stroke, heart attack), liver problems (jaundice, hepatitis), gallbladder disease, hypertension, increased risk of breast and cervical cancer.
Long-Term Effects:
Potential for increased risk of certain cancers with prolonged use.
Adverse Drug Reactions (ADR):
Severe allergic reactions, thromboembolic events, hepatic dysfunction, significant blood pressure elevation.
Contraindications
Pregnancy, history of thromboembolic disorders, breast cancer or other estrogen/progestin-sensitive cancers, liver disease (tumors, hepatitis, cirrhosis), undiagnosed abnormal uterine bleeding, smoking (especially in women over 35), uncontrolled hypertension, diabetes with vascular complications, migraines with aura.
Drug Interactions
Several drugs can interact with Ethinyl Estradiol + Levonorgestrel, including:
- Enzyme inducers (e.g., rifampin, phenytoin, carbamazepine): Reduce contraceptive effectiveness.
- Enzyme inhibitors (e.g., some antifungals, some antibiotics): May increase hormone levels and risk of side effects.
- St. John’s Wort, certain antivirals, lamotrigine.
- Food and lifestyle factors: Alcohol, grapefruit juice, smoking can potentially affect metabolism.
Pregnancy and Breastfeeding
- Pregnancy Safety Category: X (contraindicated).
- Fetal risks: Although inadvertent exposure during early pregnancy has not been linked to birth defects, it’s crucial to discontinue use if pregnancy occurs.
- Breastfeeding: Small amounts of hormones are excreted in breast milk. May decrease milk production. Alternative contraception is recommended while breastfeeding.
Drug Profile Summary
- Mechanism of Action: Inhibits ovulation, thickens cervical mucus, alters endometrium.
- Side Effects: Nausea, headache, bleeding irregularities, thromboembolic events (rare).
- Contraindications: Pregnancy, thromboembolic history, estrogen/progestogen-sensitive cancers, liver disease.
- Drug Interactions: Enzyme inducers/inhibitors, certain antibiotics, St. John’s Wort.
- Pregnancy & Breastfeeding: Contraindicated in pregnancy; not recommended during breastfeeding.
- Dosage: One tablet daily, typically 21 active/7 inactive pill cycle.
- Monitoring Parameters: Blood pressure, BMI, lipid profile (if at risk), signs of thromboembolism, depression.
Popular Combinations
Ethinyl Estradiol + Levonorgestrel is itself a combination product and is generally not combined with other medications for contraception. However, folate supplementation is often recommended alongside COCPs.
Precautions
- Pre-screening for cardiovascular risk factors, liver function, and family history of thromboembolic disorders.
- Pregnant Women: Contraindicated.
- Breastfeeding Mothers: Not recommended.
- Children & Elderly: Use with caution in adolescents and generally avoid in older women.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ethinyl Estradiol + Levonorgestrel?
A: One tablet daily, containing a specific combination of ethinyl estradiol and levonorgestrel (dosages vary depending on the specific product), usually taken for 21 days followed by 7 days of placebo or a lower dose of estrogen. Extended-cycle regimens are also available.
Q2: What are the common side effects?
A: Nausea, vomiting, headache, breast tenderness, breakthrough bleeding, weight changes, mood changes, and acne.
Q3: When should a patient start taking the pill?
A: Either on the first day of their period (Day 1 start) or the first Sunday after their period starts (Sunday start).
Q4: What if a patient misses a pill?
A: If one or two active pills are missed, take the missed pill as soon as possible and continue as usual. If three or more active pills are missed, consider emergency contraception and use a backup method for 7 days.
Q5: Can Ethinyl Estradiol + Levonorgestrel be used while breastfeeding?
A: It’s generally not recommended due to potential effects on milk production and infant exposure to hormones. Alternative contraceptive methods are preferred.
Q6: Who should not take this medication?
A: Women who are pregnant or have a history of blood clots, stroke, heart attack, liver disease, certain cancers (breast, cervical), or uncontrolled high blood pressure. Smokers, especially those over 35, should not take it.
Q7: Does this pill protect against sexually transmitted infections (STIs)?
A: No, it does not offer any protection against STIs. Barrier methods like condoms are essential for STI prevention.
Q8: What should be monitored while a patient is taking this medication?
A: Blood pressure, body mass index (BMI), and signs of potential complications such as blood clots (leg pain, chest pain, shortness of breath) or liver problems (jaundice, abdominal pain).
Q9: How does smoking affect the use of this pill?
A: Smoking significantly increases the risk of serious cardiovascular side effects, such as blood clots, heart attack, and stroke, particularly in women over 35. Smoking is a strong contraindication for this medication.
