HAILEY FE 1/20
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HAILEY FE 1/20 (HAILEY FE 1/20).
Combination oral contraceptive containing ethinyl estradiol and norethindrone. Suppresses gonadotropin (FSH and LH) release via negative feedback on the hypothalamic-pituitary-ovarian axis, inhibiting ovulation. Also alters cervical mucus and endometrial lining to impair sperm penetration and implantation.
| Metabolism | Ethinyl estradiol is primarily metabolized via CYP3A4 hydroxylation and conjugation (glucuronidation/sulfation). Norethindrone is metabolized by reduction, hydroxylation, and conjugation, primarily via CYP3A4. |
| Excretion | Renal (approximately 50-60% as metabolites, including glucuronide conjugates of ethinyl estradiol and norethindrone, and about 20% as unchanged norethindrone); Fecal (approximately 30-40% as metabolites); Biliary (minor, with enterohepatic circulation of ethinyl estradiol conjugates). |
| Half-life | Ethinyl estradiol: approximately 17 ± 5 hours (terminal); Norethindrone: approximately 8 ± 2 hours (terminal). Clinical context: Steady-state reached within 7-10 days; once-daily dosing maintains effective concentrations for contraceptive efficacy. |
| Protein binding | Ethinyl estradiol: approximately 97-98% bound to albumin (primarily) and sex hormone-binding globulin (SHBG); Norethindrone: approximately 93-95% bound to albumin and SHBG. |
| Volume of Distribution | Ethinyl estradiol: approximately 2-4 L/kg; Norethindrone: approximately 4-6 L/kg. Clinical meaning: Extensive tissue distribution, with accumulation in adipose tissue and reproductive organs. |
| Bioavailability | Oral: Ethinyl estradiol ~40-45% (first-pass metabolism); Norethindrone ~60-65% (first-pass metabolism). |
| Onset of Action | Oral: Contraceptive effect begins after 7 consecutive daily doses; peak serum concentrations of ethinyl estradiol and norethindrone occur at 1-2 hours post-dose. |
| Duration of Action | Oral: 24-hour dosing interval; contraceptive protection maintained with consistent daily dosing; missed doses increase pregnancy risk. |
One tablet orally once daily for 21 consecutive days followed by 7 days of placebo tablets.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Contraindicated in severe renal impairment or acute renal failure due to risk of hyperkalemia. |
| Liver impairment | Contraindicated in patients with active liver disease or Child-Pugh class B or C cirrhosis. For Child-Pugh class A, use with caution and monitor liver function. |
| Pediatric use | Not indicated for use before menarche. For post-menarchal adolescents, same dosing as adults: one tablet orally once daily for 21 days, then 7 days of placebo. |
| Geriatric use | Not indicated for use in postmenopausal women. No specific geriatric dosing adjustments; consider increased risk of thromboembolic events and cardiovascular disease. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HAILEY FE 1/20 (HAILEY FE 1/20).
| Breastfeeding | Excreted in breast milk in small amounts. Estrogen and progestin levels may affect milk composition and reduce milk production. M/P ratio not reported; use caution, especially in the immediate postpartum period. Avoid use in breastfeeding women if possible. |
| Teratogenic Risk | First trimester: No increased risk of major birth defects in large epidemiological studies. Second and third trimesters: Use is not recommended due to potential adverse effects on fetal development, including possible estrogenic effects and association with congenital anomalies in animal studies. Fetal risk cannot be ruled out. |
■ FDA Black Box Warning
Cigarette smoking increases risk of serious cardiovascular events (e.g., stroke, myocardial infarction, thromboembolism) from combination oral contraceptives. Risk increases with age (>35 years) and heavy smoking (≥15 cigarettes/day). Women who are >35 years old and smoke should not use this product.
| Serious Effects |
["Thrombophlebitis or thromboembolic disorders (current or history).","Cerebrovascular or coronary artery disease (current or history).","Known or suspected breast carcinoma or estrogen-dependent neoplasia.","Undiagnosed abnormal genital bleeding.","Pregnancy (known or suspected).","Benign or malignant liver tumor (active or history).","Active liver disease with abnormal liver function.","Hypersensitivity to any component.","Age >35 years with cigarette smoking."]
| Precautions | ["Increased risk of thrombotic disorders including venous thromboembolism, stroke, and myocardial infarction.","Discontinue if sudden partial or complete loss of vision or onset of proptosis, diplopia, migraine.","Elevated blood pressure; use caution in hypertension.","Gallbladder disease; increased risk of gallstones.","Carbohydrate and lipid metabolism effects; use caution in diabetes and hyperlipidemia.","Hepatic neoplasia; discontinue if jaundice or liver dysfunction.","Chloasma; avoid sun or UV exposure.","Bleeding irregularities; may cause breakthrough bleeding and spotting.","Possible decreased efficacy with concomitant enzyme-inducing drugs."] |
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| Fetal Monitoring | Monitor blood pressure, glucose tolerance, and liver function. Assess for symptoms of depression, jaundice, and thromboembolic events. No specific fetal monitoring required, but discuss risks with pregnant women. |
| Fertility Effects | No known permanent effects on fertility. Return to fertility may be delayed after discontinuation; normal menstrual cycles typically resume within 1-3 months. |